General Information of the Protein
Protein ID
PT02663
Protein Name
Nuclear receptor ROR-gamma
Secondarily
Protein Name
Nuclear receptor RZR-gamma
Nuclear receptor subfamily 1 group F member 3
RAR-related orphan receptor C
Retinoid-related orphan receptor-gamma
Gene Name
RORC
Secondarily
Gene Name
NR1F3
RORG
RZRG
Sequence
MDRAPQRQHRASRELLAAKKTHTSQIEVIPCKICGDKSSGIHYGVITCEGCKGFFRRSQRCNAAYSCTRQQNCPIDRTSRNRCQHCRLQKCLALGMSRDAVKFGRMSKKQRDSLHAEVQKQLQQRQQQQQEPVVKTPPAGAQGADTLTYTLGLPDGQLPLGSSPDLPEASACPPGLLKASGSGPSYSNNLAKAGLNGASCHLEYSPERGKAEGRESFYSTGSQLTPDRCGLRFEEHRHPGLGELGQGPDSYGSPSFRSTPEAPYASLTEIEHLVQSVCKSYRETCQLRLEDLLRQRSNIFSREEVTGYQRKSMWEMWERCAHHLTEAIQYVVEFAKRLSGFMELCQNDQIVLLKAGAMEVVLVRMCRAYNADNRTVFFEGKYGGMELFRALGCSELISSIFDFSHSLSALHFSEDEIALYTALVLINAHRPGLQEKRKVEQLQYNLELAFHHHLCKTHRQSILAKLPPKGKLRSLCSQHVERLQIFQHLHPIVVQAAFPPLYKELFSTETESPVGLSK
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Organism
Homo sapiens, Human
Protein Classification
Transcription factor
>
Nuclear receptor
>
Nuclear hormone receptor subfamily 1
>
Nuclear hormone receptor subfamily 1 group F
>
Nuclear hormone receptor subfamily 1 group F member 3
Function
Nuclear receptor that binds DNA as a monomer to ROR response elements (RORE) containing a single core motif half-site 5'-AGGTCA-3' preceded by a short A-T-rich sequence. Key regulator of cellular differentiation, immunity, peripheral circadian rhythm as well as lipid, steroid, xenobiotics and glucose metabolism (PubMed:19381306, PubMed:19965867, PubMed:22789990, PubMed:26160376, PubMed:20203100). Considered to have intrinsic transcriptional activity, have some natural ligands like oxysterols that act as agonists (25-hydroxycholesterol) or inverse agonists (7-oxygenated sterols), enhancing or repressing the transcriptional activity, respectively (PubMed:19965867, PubMed:22789990). Recruits distinct combinations of cofactors to target gene regulatory regions to modulate their transcriptional expression, depending on the tissue, time and promoter contexts. Regulates the circadian expression of clock genes such as CRY1, BMAL1 and NR1D1 in peripheral tissues and in a tissue-selective manner. Competes with NR1D1 for binding to their shared DNA response element on some clock genes such as BMAL1, CRY1 and NR1D1 itself, resulting in NR1D1-mediated repression or RORC-mediated activation of the expression, leading to the circadian pattern of clock genes expression. Therefore influences the period length and stability of the clock. Involved in the regulation of the rhythmic expression of genes involved in glucose and lipid metabolism, including PLIN2 and AVPR1A (PubMed:19965867). Negative regulator of adipocyte differentiation through the regulation of early phase genes expression, such as MMP3. Controls adipogenesis as well as adipocyte size and modulates insulin sensitivity in obesity. In liver, has specific and redundant functions with RORA as positive or negative modulator of expression of genes encoding phase I and Phase II proteins involved in the metabolism of lipids, steroids and xenobiotics, such as SULT1E1. Also plays a role in the regulation of hepatocyte glucose metabolism through the regulation of G6PC1 and PCK1 (PubMed:19965867). Regulates the rhythmic expression of PROX1 and promotes its nuclear localization (PubMed:19381306, PubMed:19965867, PubMed:22789990, PubMed:26160376, PubMed:20203100). Plays an indispensable role in the induction of IFN-gamma dependent anti-mycobacterial systemic immunity (PubMed:26160376).
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Uniprot ID
Primary ID:
P51449

Secondarily ID:
Q5SZR9
Q8N5V7
Q8NCY8
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HGNC ID
HGNC:10260
Subcellular Location
Nucleus
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
Compound ID Compound Name Compound Formula
CP0536538
sodium;(4S)-6-(2-chloro-4-fluoroanilino)-4-[4-cyclopropyl-5-[5-(1,1-difluoro-2,2-dimethylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H26ClF3N3NaO5
 1
1
EC50 = 6 nM
   TI
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CP0546922
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(1,1-difluoro-2,2-dimethylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C27H29ClF2N3NaO5
 1
1
EC50 = 6 nM
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   LI
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CP0536537
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2,2-dimethylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C27H31ClN3NaO5
 1
1
EC50 = 7 nM
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CP0542756
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(1,1-difluoro-2-methylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H27ClF2N3NaO5
 1
1
EC50 = 7 nM
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CP0546923
sodium;(4S)-6-(4-chloro-2-fluoroanilino)-4-[4-cyclopropyl-5-[5-(1,1-difluoro-2,2-dimethylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H26ClF3N3NaO5
 1
1
EC50 = 7 nM
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CP0528301
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(1,1-difluoro-3-methylbutyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C27H29ClF2N3NaO5
 1
1
EC50 = 8 nM
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CP0559600
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(3-methylbutyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C27H31ClN3NaO5
 1
1
EC50 = 8 nM
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CP0189687
sodium;(4S)-4-[4-cyclopropyl-5-[5-(2,2-dimethylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-(2,4-dichloroanilino)-6-oxohexanoate
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C26H28Cl2N3NaO5
 1
1
EC50 = 9 nM
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CP0482671
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[3-(2-methylpropyl)-1,2-oxazol-5-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO5
 1
1
EC50 = 12 nM
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CP0556867
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,2-oxazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO5
 1
1
EC50 = 14 nM
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CP0482672
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[2-(2-methylpropyl)-1,3-thiazol-5-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO4S
 1
1
EC50 = 17 nM
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CP0058361
CHEMBL3774855
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C28H39N5O2
 1
1
EC50 = 34 nM
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CP0571262
(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[4-(2-methylpropyl)phenyl]-1,2-oxazol-3-yl]-6-oxohexanoic acid
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C29H33ClN2O4
 1
1
EC50 = 44 nM
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CP0528300
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,3,4-thiadiazol-2-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C25H28ClN4NaO4S
 1
1
EC50 = 56 nM
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CP0556868
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,2,4-oxadiazol-3-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C25H28ClN4NaO5
 1
1
EC50 = 62 nM
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CP0459830
(1S,2S,4S)-2-[4-cyclopropyl-5-[3-(2-methylpropyl)cyclobutyl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)-4-hydroxycyclopentane-1-carboxamide
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C27H38N4O2
 1
1
EC50 = 98 nM
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CP0536535
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,3-thiazol-2-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO4S
 1
1
EC50 = 120 nM
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CP0414833
3-[4-cyclopropyl-5-[3-(2-methylpropyl)cyclobutyl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C24H34N4O
 1
1
EC50 = 140 nM
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CP0546924
N-ethyl-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-4-nitrobenzenesulfonamide
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C17H14F6N2O5S
 1
1
EC50 = 190 nM
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CP0559971
(3R,4S)-4-[4-cyclopropyl-5-[3-(2-methylpropyl)cyclobutyl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)-1-methylpiperidine-3-carboxamide
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C28H41N5O
 1
1
EC50 = 230 nM
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CP0458491
3-[4-cyclopropyl-5-[3-(2-methylpropyl)cyclobutyl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C24H34N4O
 1
1
EC50 = 400 nM
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CP0556866
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)-5-hydroxypentanamide
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C24H36N4O2
 1
1
EC50 = 440 nM
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CP0551795
3-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,2-oxazol-3-yl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C23H29N5O2
 1
1
EC50 = 450 nM
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CP0571263
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[5-(2-methylpropyl)-1,3-oxazol-2-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO5
 1
1
EC50 = 660 nM
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CP0555703
3-[5-(2-cyclohexylethyl)-4-ethyl-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C25H32N4O
 1
1
EC50 = 820 nM
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CP0181318
3-[5-(2-cyclohexylethyl)-4-ethyl-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C23H34N4O
 1
1
EC50 = 900 nM
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CP0397886
3-[5-(2-cyclohexylethyl)-4-(2,2-difluorocyclopropyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C24H32F2N4O
 1
1
EC50 = 920 nM
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CP0381787
N-(3-chloro-2-methylphenyl)-3-[5-(2-cyclohexylethyl)-4-ethyl-1,2,4-triazol-3-yl]propanamide
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C22H31ClN4O
 1
1
EC50 = 960 nM
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CP0551794
3-[5-(2-cyclohexylethyl)-4-cyclopropyl-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C24H34N4O
 1
1
EC50 = 980 nM
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CP0414830
3-[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C26H26N4O
 1
1
EC50 = 1000 nM
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CP0455009
3-[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]-2-methyl-N-naphthalen-1-ylpropanamide
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C27H28N4O
 1
1
EC50 = 1300 nM
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CP0360184
2-[[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]sulfanyl]-N-naphthalen-1-ylacetamide
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C25H24N4OS
 1
1
EC50 = 1700 nM
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CP0542045
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C22H32N4O
 1
1
EC50 = 1700 nM
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CP0555702
3-[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]-N-naphthalen-1-ylbutanamide
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C27H28N4O
 1
1
EC50 = 1700 nM
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CP0414832
3-[4-cyclopropyl-5-[4-(2-methylpropyl)phenyl]-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C26H32N4O
 1
1
EC50 = 1800 nM
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CP0414834
3-[4-ethyl-5-(2-phenylethyl)-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C25H26N4O
 1
1
EC50 = 2500 nM
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CP0536518
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)-N',N'-dimethylhexanediamide
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C27H41N5O2
 1
1
EC50 = 2700 nM
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CP0414831
3-[4-cyclopropyl-5-(4,4-dimethylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C23H34N4O
 1
1
EC50 = 2800 nM
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CP0381794
3-[5-(2-cyclohexylethyl)-4-ethyl-1,2,4-triazol-3-yl]-N-(3,5-dimethylphenyl)propanamide
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C23H34N4O
 1
1
EC50 = 2900 nM
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CP0536536
sodium;(4S)-6-(2-chloro-4-methylanilino)-4-[4-cyclopropyl-5-[2-(2-methylpropyl)-1,3-thiazol-4-yl]-1,2-oxazol-3-yl]-6-oxohexanoate
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C26H29ClN3NaO4S
 1
1
EC50 = 3800 nM
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CP0375786
3-[4-cyclopropyl-5-(3-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C22H32N4O
 1
1
EC50 = 3900 nM
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CP0451204
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)-N'-methylhexanediamide
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C26H39N5O2
 1
1
EC50 = 6400 nM
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CP0555704
3-[5-(3,3-dimethylbutyl)-4-ethyl-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C23H30N4O
 1
1
EC50 = 6700 nM
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CP0375787
3-[4-cyclobutyl-5-(2-cyclohexylethyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)propanamide
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C25H36N4O
 1
1
EC50 = 9500 nM
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CP0488163
5-acetamido-3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)pentanamide
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C26H39N5O2
 1
1
EC50 = 11000 nM
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CP0375785
3-[4-ethyl-5-(3-methylbutyl)-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C22H28N4O
 1
1
EC50 = 13000 nM
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CP0397884
3-[5-(cyclohexylmethyl)-4-ethyl-1,2,4-triazol-3-yl]-N-naphthalen-1-ylpropanamide
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C24H30N4O
 1
1
EC50 = 14000 nM
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CP0536517
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)hexanediamide
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C25H37N5O2
 1
1
EC50 = 16000 nM
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CP0550671
3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-5-(dimethylamino)-N-(2,4-dimethylphenyl)pentanamide
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C26H41N5O
 1
1
EC50 = 19000 nM
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CP0414829
2-[[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]oxy]-N-naphthalen-1-ylacetamide
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C25H24N4O2
 1
1
EC50 > 20000 nM
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CP0474191
3-[5-(2,3-dihydro-1H-inden-2-yl)-4-ethyl-1,2,4-triazol-3-yl]-3-hydroxy-N-naphthalen-1-ylpropanamide
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C26H26N4O2
 1
1
EC50 > 20000 nM
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CP0561097
3-(5-cyclohexyl-4-ethyl-1,2,4-triazol-3-yl)-N-naphthalen-1-ylpropanamide
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C23H28N4O
 1
1
EC50 > 20000 nM
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CP0528299
4-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-6-(2,4-dimethylanilino)-6-oxohexanoic acid
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C25H36N4O3
 1
1
EC50 > 20000 nM
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CP0537901
5-amino-3-[4-cyclopropyl-5-(4-methylpentyl)-1,2,4-triazol-3-yl]-N-(2,4-dimethylphenyl)pentanamide
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C24H37N5O
 1
1
EC50 > 20000 nM
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Biochemical Assays
Compound ID Compound Name Compound Formula
CP0543989
2-[[4-chloro-2-(trifluoromethyl)phenyl]methyl]-N-[(4-ethylsulfonylphenyl)methyl]-1-(2-fluoroethyl)indole-5-carboxamide
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C28H25ClF4N2O3S
 1
1 EC50 = 2 nM
CP0238145
5-[(5R)-5-[[1-[(2-ethoxyphenyl)methyl]-2,3-dihydroindol-5-yl]carbamoyl]-2-methoxy-7,8-dihydro-5H-1,6-naphthyridin-6-yl]-5-oxopentanoic acid
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C32H36N4O6
 2
1 EC50 = 2.1 nM
2 IC50 = 6 nM
CP0228649
1-[4-[3-fluoro-4-[[(3S,7S)-7-methyl-4,4-dioxo-3-phenyl-1,4,5-oxathiazepan-5-yl]methyl]phenyl]piperazin-1-yl]ethanone
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C24H30FN3O4S
 1
1 EC50 = 3 nM
CP0455535
(5R)-6-acetyl-N-[1-[(2-ethoxyphenyl)methyl]-2,3-dihydroindol-5-yl]-2-methoxy-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C29H32N4O4
 2
1 EC50 = 4.1 nM
2 IC50 = 7.2 nM
CP0558424
N-[(5-ethylsulfonylpyridin-2-yl)methyl]-4-[2-(6-propan-2-yloxy-2,3-dihydro-1,4-benzoxazin-4-yl)ethyl]benzamide
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C28H33N3O5S
 1
1 EC50 = 4.6 nM
CP0129308
4-[1-[2-chloro-6-(trifluoromethyl)benzoyl]indazol-3-yl]benzoic acid
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C22H12ClF3N2O3
 2
1 EC50 = 4.7 nM
2 EC50 = 16 nM
CP0228650
1-[4-[4-[[(7R)-1,1-dioxo-7-phenylthiazepan-2-yl]methyl]-3-fluorophenyl]piperazin-1-yl]ethanone
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C24H30FN3O3S
 1
1 EC50 = 6 nM
CP0451260
N-[(5-methylsulfonylpyridin-2-yl)methyl]-4-[2-(6-propan-2-yloxy-2,3-dihydro-1,4-benzoxazin-4-yl)ethyl]benzamide
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C27H31N3O5S
 1
1 EC50 = 7.5 nM
CP0482000
N-[4-[[benzyl(propyl)amino]methyl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C27H32N2O3S
 2
1 EC50 = 7.8 nM
2 EC50 = 98.8 nM
CP0252881
1-[4-[3-fluoro-4-[[(3S,6S)-6-methyl-4,4-dioxo-3-phenyl-1,4,5-oxathiazepan-5-yl]methyl]phenyl]piperazin-1-yl]ethanone
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C24H30FN3O4S
 1
1 EC50 = 8 nM
CP0189740
N-[(5-ethylsulfonylpyridin-2-yl)methyl]-4-[2-[7-(2-methylpropyl)-3,4-dihydro-2H-quinolin-1-yl]ethyl]benzamide
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C30H37N3O3S
 1
1 EC50 = 8.9 nM
CP0180479
6-acetyl-2-methoxy-N-[1-[(2-methoxyphenyl)methyl]-2,3-dihydroindol-5-yl]-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C28H30N4O4
 2
1 EC50 = 9.5 nM
2 IC50 = 14 nM
CP0551553
N-[(4-ethylsulfonylphenyl)methyl]-1-propan-2-yl-2-[[3-(trifluoromethyl)phenyl]methyl]indole-5-carboxamide
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C29H29F3N2O3S
 1
1 EC50 = 10 nM
CP0385839
4-[3-[2-chloro-6-(trifluoromethyl)benzoyl]imidazo[1,5-a]pyridin-1-yl]benzoic acid
   Show/Hide
C22H12ClF3N2O3
 1
1 EC50 = 10 nM
CP0361253
6-acetyl-2-methoxy-N-[1-[[2-(trifluoromethoxy)phenyl]methyl]-2,3-dihydroindol-5-yl]-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C28H27F3N4O4
 2
1 EC50 = 11 nM
2 IC50 = 20 nM
CP0576937
2-[[4-chloro-2-(trifluoromethyl)phenyl]methyl]-N-[(4-ethylsulfonylphenyl)methyl]-1-propan-2-ylindole-5-carboxamide
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C29H28ClF3N2O3S
 1
1 EC50 = 11 nM
CP0543990
N-[(4-ethylsulfonylphenyl)methyl]-2-[[4-fluoro-2-(trifluoromethyl)phenyl]methyl]-1-propan-2-ylindole-5-carboxamide
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C29H28F4N2O3S
 1
1 EC50 = 14 nM
CP0574891
2-[[4-chloro-2-(trifluoromethyl)phenyl]methyl]-1-cyclopropyl-N-[(4-ethylsulfonylphenyl)methyl]indole-5-carboxamide
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C29H26ClF3N2O3S
 1
1 EC50 = 14 nM
CP0311598
(3R,5S)-5-[(3aR,9bR)-9b-(4-fluorophenyl)sulfonyl-7-(1,1,1,2,3,3,3-heptafluoropropan-2-yl)-2,3a,4,5-tetrahydro-1H-benzo[e]indole-3-carbonyl]-3-fluoro-1-(2-hydroxy-2-methylpropyl)pyrrolidin-2-one
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C30H29F9N2O5S
 1
1 EC50 = 16 nM
CP0364216
2-[(2S)-6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]acetic acid
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C24H17F6NO5S
 1
1 EC50 = 16.1 nM
CP0060417
2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]acetic acid
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C24H17F6NO5S
 1
1 EC50 = 20.8 nM
CP0257822
N-(2-methylpropyl)-N-[[4-(4-methylsulfonylphenyl)phenyl]methyl]-1-phenylmethanesulfonamide
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C25H29NO4S2
 3
1 EC50 = 21 nM
2 EC50 = 25 nM
3 IC50 = 32 nM
CP0511831
6-(4-acetylpiperazin-1-yl)-N-[(2-chloro-6-fluorophenyl)methyl]-N-methyl-3,4-dihydro-1H-isoquinoline-2-sulfonamide
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C23H28ClFN4O3S
 1
1 EC50 = 21 nM
CP0551554
2-[(2-ethylphenyl)methyl]-N-[(4-ethylsulfonylphenyl)methyl]-1-propan-2-ylindole-5-carboxamide
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C30H34N2O3S
 1
1 EC50 = 25 nM
CP0354660
4-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]butanoic acid
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C26H21F6NO5S
 1
1 EC50 = 25.2 nM
CP0354665
3-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonylindol-2-yl]propanoic acid
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C25H17F6NO5S
 1
1 EC50 = 25.5 nM
CP0546846
N-[(4-ethylsulfonylphenyl)methyl]-1-propan-2-yl-2-[[2-(trifluoromethyl)phenyl]methyl]indole-5-carboxamide
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C29H29F3N2O3S
 1
1 EC50 = 29 nM
CP0060756
3-[(2S)-6-[3-(difluoromethoxy)-5-fluorophenyl]-4-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydro-1,4-benzoxazin-2-yl]-2,2-dimethylpropanoic acid
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C27H23F6NO6S
 2
1 EC50 = 30 nM
2 EC50 = 30.1 nM
CP0052231
N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-N-cyclobutyl-1-phenylmethanesulfonamide
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C24H31N3O3S
 3
1 EC50 = 30 nM
2 IC50 = 29 nM
3 IC50 = 46 nM
CP0361259
5-[(5R)-5-[(7-fluoro-1,1-dimethyl-2,3-dihydroinden-5-yl)carbamoyl]-2-methoxy-7,8-dihydro-5H-1,6-naphthyridin-6-yl]-5-oxopentanoic acid
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C26H30FN3O5
 2
1 EC50 = 31 nM
2 IC50 = 3.3 nM
CP0364067
3-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]propanoic acid
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C25H19F6NO5S
 1
1 EC50 = 31.3 nM
CP0059785
N-[[4-[4-(methanesulfonamido)phenyl]phenyl]methyl]-N-(2-methylpropyl)-1-phenylmethanesulfonamide
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C25H30N2O4S2
 2
1 EC50 = 32 nM
2 IC50 = 46 nM
CP0111022
US10301272, Example 15/6
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C26H33Cl2N3O5S3
 1
1 EC50 = 35 nM
CP0199799
US10301272, Example 15
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C28H35N3O5S3
 1
1 EC50 = 37 nM
CP0168528
4-[4-[[benzylsulfonyl(2-methylpropyl)amino]methyl]phenyl]benzamide
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C25H28N2O3S
 3
1 EC50 = 40 nM
2 IC50 = 31 nM
3 IC50 = 33 nM
CP0060757
2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]-1-(1,1-dioxo-1,4-thiazinan-4-yl)ethanone
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C28H24F6N2O6S2
 1
1 EC50 = 43.4 nM
CP0567797
2-(4-ethylsulfonylphenyl)-N-[4-[2-[7-(2-methylpropyl)-3,4-dihydro-2H-quinolin-1-yl]ethyl]phenyl]acetamide
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C31H38N2O3S
 1
1 EC50 = 46.4 nM
CP0364061
2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]-1-(2-oxa-6-azaspiro[3.3]heptan-6-yl)ethanone
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C29H24F6N2O5S
 1
1 EC50 = 47.9 nM
CP0366515
1-[2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]acetyl]azetidine-3-carboxylic acid
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C28H22F6N2O6S
 1
1 EC50 = 49.3 nM
CP0238128
(5R)-6-acetyl-2-methoxy-N-[4-[(2-methoxyphenyl)methoxy]phenyl]-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C26H27N3O5
 2
1 EC50 = 53 nM
2 IC50 = 44 nM
CP0477503
1-[2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]acetyl]piperidine-4-carboxylic acid
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C30H26F6N2O6S
 1
1 EC50 = 57.1 nM
CP0073479
4-(cyclopropylmethyl)-N-(1,1-dioxothian-4-yl)-5-[4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]naphthalen-1-yl]-1,3-thiazole-2-carboxamide
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C26H28F3N3O5S3
 1
1 EC50 = 58 nM
CP0218446
4-[(3,3-difluorocyclobutyl)methyl]-N-(2-hydroxy-2-methylpropyl)-5-[4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]naphthalen-1-yl]-1,3-thiazole-2-carboxamide
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C26H28F5N3O4S2
 1
1 EC50 = 60 nM
CP0073466
US10301272, Example 7/8
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C30H41N3O5S2
 1
1 EC50 = 68 nM
CP0074613
CHEMBL3314002
   Show/Hide
C28H38ClN3O5S2
 1
1 EC50 = 77 nM
CP0073529
US10301272, Example 7/9
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C30H37N3O5S2
 2
1 EC50 = 82 nM
2 Kd = 0.12 nM
CP0317638
6-(4-acetylpiperazin-1-yl)-N-methyl-N-[[2-(trifluoromethyl)phenyl]methyl]-3,4-dihydro-1H-isoquinoline-2-sulfonamide
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C24H29F3N4O3S
 1
1 EC50 = 97 nM
CP0073467
US10301272, Example 7/7
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C26H33Cl2N3O5S2
 1
1 EC50 = 98 nM
CP0354663
2-[6-[3-(difluoromethoxy)-5-fluorophenyl]-1-[3-(trifluoromethyl)phenyl]sulfonyl-2,3-dihydroindol-2-yl]-1-(4-hydroxypiperidin-1-yl)ethanone
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C29H26F6N2O5S
 1
1 EC50 = 106 nM
CP0249036
US10301272, Example 6/64
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C30H40N4O4S2
 1
1 EC50 = 113 nM
CP0369897
US10301272, Example 6/46
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C30H37N3O5S3
 1
1 EC50 = 120 nM
CP0249037
US10301272, Example 6/11
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C30H39N3O4S2
 1
1 EC50 = 132 nM
CP0576650
N-[(4-ethylsulfonylphenyl)methyl]-1-propan-2-yl-2-[[4-(trifluoromethyl)phenyl]methyl]indole-5-carboxamide
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C29H29F3N2O3S
 1
1 EC50 = 150 nM
CP0074608
US10301272, Example 7/13
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C28H37F2N3O6S2
 1
1 EC50 = 202 nM
CP0074611
CHEMBL4128687
   Show/Hide
C26H32ClF2N3O5S2
 1
1 EC50 = 230 nM
CP0335291
2,3-dichloro-4-[4-(cyclobutylmethyl)-2-(2,2-dioxo-2lambda6-thia-6-azaspiro[3.3]heptane-6-carbonyl)-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C23H24Cl2F3N3O5S3
 1
1 EC50 = 284 nM
CP0180350
US10301272, Example 6/28
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C29H36N4O5S2
 1
1 EC50 = 300 nM
CP0249286
CHEMBL4129634
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C27H28F3N3O5S2
 1
1 EC50 = 317 nM
CP0059780
N-(2-methylpropyl)-N-[[5-(3-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 2
1 EC50 = 360 nM
2 IC50 = 370 nM
CP0451566
US10301272, Example 6/17
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C31H37N3O5S2
 1
1 EC50 = 404 nM
CP0123414
CHEMBL4126040
   Show/Hide
C26H34ClN3O5S2
 1
1 EC50 = 440 nM
CP0234135
N-(2-methylpropyl)-N-[[5-(4-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 2
1 EC50 = 460 nM
2 IC50 = 130 nM
CP0073551
US10301272, Example 8/7
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C30H36F3N3O4S
 1
1 EC50 = 505 nM
CP0218448
5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-N-(2-hydroxy-2-methylpropyl)-4-[(2-methylpropan-2-yl)oxymethyl]-1,3-thiazole-2-carboxamide
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C22H28Cl2F3N3O5S2
 1
1 EC50 = 692 nM
CP0074081
CHEMBL4128665
   Show/Hide
C27H34F3N3O5S2
 1
1 EC50 = 840 nM
CP0086254
N-tert-butyl-4-[4-(cyclohexylmethyl)-2-(7,7-dioxo-7lambda6-thia-2-azaspiro[3.5]nonane-2-carbonyl)-1,3-thiazol-5-yl]naphthalene-1-sulfonamide
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C32H41N3O5S3
 1
1 EC50 = 906 nM
CP0317606
6-(4-acetylpiperazin-1-yl)-N-[(2-chlorophenyl)methyl]-N-methyl-3,4-dihydro-1H-isoquinoline-2-sulfonamide
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C23H29ClN4O3S
 1
1 EC50 = 982 nM
CP0389716
CHEMBL4128427
   Show/Hide
C29H38F3N3O5S2
 1
1 EC50 = 1040 nM
CP0216551
CHEMBL4127926
   Show/Hide
C30H38F3N3O4S
 1
1 EC50 = 1400 nM
CP0218445
US10301272, Example 21/22
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C23H28F5N3O4S2
 1
1 EC50 = 1630 nM
CP0389754
US10301272, Example 9/6
   Show/Hide
C31H41N3O4S
 1
1 EC50 = 2400 nM
CP0353858
US10301272, Example 6/49
   Show/Hide
C31H39N3O5S2
 1
1 EC50 = 4400 nM
CP0073546
US10301272, Example 7/3
   Show/Hide
C30H40N2O3S
 1
1 EC50 = 10000 nM
CP0248636
6-acetyl-2-methoxy-N-(4-phenylmethoxyphenyl)-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C25H25N3O4
 2
1 EC50 > 10000 nM
2 IC50 = 1200 nM
CP0253241
6-acetyl-N-[4-[(2-chlorophenyl)methoxy]phenyl]-2-methoxy-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C25H24ClN3O4
 2
1 EC50 > 10000 nM
2 IC50 = 290 nM
CP0361254
(5S)-6-acetyl-2-methoxy-N-[4-[(2-methoxyphenyl)methoxy]phenyl]-7,8-dihydro-5H-1,6-naphthyridine-5-carboxamide
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C26H27N3O5
 2
1 EC50 > 10000 nM
2 IC50 > 10000 nM
CP0068743
N-[5-chloro-6-[(1S)-1-phenylethoxy]pyridin-3-yl]-2-(4-ethylsulfonylphenyl)acetamide
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C23H23ClN2O4S
 4
1 IC50 = 0.6 nM
2 IC50 = 255 nM
3 Kd = 8 nM
4 Kd = 35.5 nM
CP0326785
4-[3-(2,6-dichlorobenzoyl)-7-fluoro-1H-indol-1-yl]benzoic acid
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C22H12Cl2FNO3
 1
1 IC50 = 1 nM
CP0571707
N-[5-chloro-3-[[(3S)-4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl]methyl]-2-methylphenyl]-2-methylpyrimidine-5-carboxamide
   Show/Hide
C25H32ClN5O2
 1
1 IC50 = 1 nM
CP0242453
4-[3-(2,6-dichlorobenzoyl)indol-1-yl]-3-fluorobenzoic acid
   Show/Hide
C22H12Cl2FNO3
 1
1 IC50 = 1.1 nM
CP0363398
4-[3-(2,6-dichlorobenzoyl)indol-1-yl]benzoic acid
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C22H13Cl2NO3
 1
1 IC50 = 1.6 nM
CP0134715
N-[5-(2-chlorobenzoyl)-4-(3-chlorophenyl)thiophen-2-yl]-2-(4-ethylsulfonylphenyl)acetamide
   Show/Hide
C27H21Cl2NO4S2
 4
1 IC50 = 2 nM
2 IC50 = 10 nM
3 IC50 = 23 nM
4 Ki = 25.12 nM
CP0326256
1-[2,4-dichloro-3-[2-(5-chlorofuran-2-yl)-5-methyl-4-(trifluoromethyl)imidazol-1-yl]phenyl]azetidine-3-carboxamide
   Show/Hide
C19H14Cl3F3N4O2
 1
1 IC50 = 2 nM
CP0326782
4-[1-(2,6-dichlorobenzoyl)indazol-3-yl]benzoic acid
   Show/Hide
C21H12Cl2N2O3
 1
1 IC50 = 2 nM
CP0359931
4-[3-[2-chloro-6-(trifluoromethyl)benzoyl]-7-fluoroindol-1-yl]benzoic acid
   Show/Hide
C23H12ClF4NO3
 1
1 IC50 = 2 nM
CP0341565
N-(3-chloro-4-cyanophenyl)-N'-[3-(cyclopropylmethyl)-1-ethyl-2,4-dioxoquinazolin-6-yl]-3-methylpentanediamide
   Show/Hide
C27H28ClN5O4
 1
1 IC50 = 2.5 nM
CP0144907
(5R)-N-(3,5-difluoro-4-trimethylsilylphenyl)-8-methoxy-4-(3-oxo-1,2-oxazole-5-carbonyl)-3,5-dihydro-2H-1,4-benzoxazepine-5-carboxamide
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C24H25F2N3O6Si
 1
1 IC50 = 2.8 nM
CP0674649
N-(4-(3-acetamido-1-isopropyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N-[2H]-methylbenzamide
   Show/Hide
C27H29ClFN5O2
 1
1 IC50 = 3 nM
CP0145639
N-[4-(5-carbamoyl-2-chlorophenyl)-2-(diethylamino)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
   Show/Hide
C25H24Cl2FN3O2
 1
1 IC50 = 3 nM
CP0563763
N-[4-(5-carbamoyl-2-chlorophenyl)-2-piperidin-1-ylphenyl]-2-chloro-6-fluoro-N-methylbenzamide
   Show/Hide
C26H24Cl2FN3O2
 1
1 IC50 = 3 nM
CP0271206
5-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-5-oxopentanoic acid
   Show/Hide
C25H30F2N2O5Si
 1
1 IC50 = 3 nM
CP0144906
(1R)-2-(5-amino-5-oxopentanoyl)-N-(3,5-difluoro-4-trimethylsilylphenyl)-6-methoxy-3,4-dihydro-1H-isoquinoline-1-carboxamide
   Show/Hide
C25H31F2N3O4Si
 1
1 IC50 = 3.1 nM
CP0112450
N-[3,5-dichloro-4-[2-(difluoromethoxy)phenyl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
   Show/Hide
C23H19Cl2F2NO4S
 1
1 IC50 = 3.162 nM
CP0369645
N-[3-chloro-4-[2-(trifluoromethoxy)phenyl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
   Show/Hide
C23H19ClF3NO4S
 1
1 IC50 = 3.162 nM
CP0281543
N-[5-(2-acetamido-4-propan-2-yl-1,3-thiazol-5-yl)-3-piperidin-1-ylpyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
   Show/Hide
C26H29ClFN5O2S
 1
1 IC50 = 3.2 nM
CP0806353
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-(2-hydroxyacetamido)-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N-[2H]-methylbenzamide
   Show/Hide
C27H29ClFN5O3
 1
1 IC50 = 3.3 nM
CP0770850
N-(4-(3-acetamido-1-isopropyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2,6-dichloro-N-[2H]-methylbenzamide
   Show/Hide
C27H29Cl2N5O2
 1
1 IC50 = 3.4 nM
CP0394521
2-[2-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-2-oxoethoxy]acetic acid
   Show/Hide
C24H28F2N2O6Si
 1
1 IC50 = 3.5 nM
CP0341566
N-(3-chloro-4-cyanophenyl)-N'-(1,3-diethyl-2,4-dioxoquinazolin-6-yl)-3-methylpentanediamide
   Show/Hide
C25H26ClN5O4
 1
1 IC50 = 3.6 nM
CP0060047
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-piperidin-1-ylphenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
   Show/Hide
C27H31ClFN5O2
 1
1 IC50 = 3.8 nM
CP0127326
5-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-3-methyl-5-oxopentanoic acid
   Show/Hide
C26H32F2N2O5Si
 1
1 IC50 = 3.8 nM
CP0478855
4-[3-(2,6-dichlorobenzoyl)indazol-1-yl]benzoic acid
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C21H12Cl2N2O3
 1
1 IC50 = 3.8 nM
CP0364454
4-[1-[2-chloro-6-(trifluoromethyl)benzoyl]-4-fluoroindazol-3-yl]-3-fluorobenzoic acid
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C22H10ClF5N2O3
 2
1 IC50 = 3.8 nM
2 IC50 = 9.4 nM
CP0416508
N-(3-chloro-4-cyanophenyl)-N'-[1-(cyclopropylmethyl)-3-ethyl-2,4-dioxoquinazolin-6-yl]-3-methylpentanediamide
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C27H28ClN5O4
 1
1 IC50 = 3.9 nM
CP0141520
N-[3,5-dichloro-4-[2-(trifluoromethoxy)phenyl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C23H18Cl2F3NO4S
 3
1 IC50 = 3.981 nM
2 IC50 = 34 nM
3 IC50 = 35.2 nM
CP0353090
1-[2,4-dichloro-3-[2-(5-chlorofuran-2-yl)-5-methyl-4-(2-methylpropyl)imidazol-1-yl]phenyl]azetidine-3-carboxylic acid
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C22H22Cl3N3O3
 1
1 IC50 = 4 nM
CP0353091
2-(5-chlorofuran-2-yl)-1-(2,6-dichlorophenyl)-5-methyl-4-(trifluoromethyl)imidazole
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C15H8Cl3F3N2O
 1
1 IC50 = 4 nM
CP0402070
1-(2,6-dichlorophenyl)-2-(furan-2-yl)-5-methyl-4-(2-methylpropyl)imidazole
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C18H18Cl2N2O
 1
1 IC50 = 4 nM
CP0520433
4-[3-[2-chloro-6-(trifluoromethyl)benzoyl]-1 H-indol-1-yl]benzoic 4-[3-(2,6-dichlorobenzoyl)-7-fluoro-1H-indol-1-yl]-3-fluoro-benzoic acid
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C22H11Cl2F2NO3
 1
1 IC50 = 4 nM
CP0111082
(E)-4-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-4-oxobut-2-enoic acid
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C24H26F2N2O5Si
 1
1 IC50 = 4.1 nM
CP0127328
4-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-4-oxobutanoic acid
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C24H28F2N2O5Si
 1
1 IC50 = 4.2 nM
CP0252170
N-[(1R)-2-(3,5-difluoro-4-trimethylsilylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-3-oxo-1,2-oxazole-5-carboxamide
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C23H25F2N3O5Si
 2
1 IC50 = 4.3 nM
2 IC50 = 18 nM
CP0396454
5-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-3-hydroxy-3-methyl-5-oxopentanoic acid
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C26H32F2N2O6Si
 1
1 IC50 = 4.5 nM
CP0660102
N-(4-(3-acetamido-1-isopropyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-fluoro-N[2H],6-dimethylbenzamide
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C28H32FN5O2
 1
1 IC50 = 4.8 nM
CP0526724
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)pentanediamide
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C26H24N4O2
 1
1 IC50 = 4.8 nM
CP0199396
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C27H29ClFN5O2
 1
1 IC50 = 4.9 nM
CP0717530
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(1-isopropyl-3-propionamido-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C28H31ClFN5O2
 1
1 IC50 = 4.9 nM
CP0788336
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-formamido-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C26H27ClFN5O2
 1
1 IC50 = 4.9 nM
CP0560136
N-[1,3-bis(cyclopropylmethyl)-2,4-dioxoquinazolin-6-yl]-N'-(3-chloro-4-cyanophenyl)-3-methylpentanediamide
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C29H30ClN5O4
 1
1 IC50 = 4.9 nM
CP0694116
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-(cyclopropanecarboxamido)-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C29H31ClFN5O2
 1
1 IC50 = 5 nM
CP0402071
2-[2,4-dichloro-3-[2-cyclopropyl-5-methyl-4-[1-(trifluoromethyl)cyclopropyl]imidazol-1-yl]phenyl]-2-azaspiro[3.3]heptane-6-carboxylic acid
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C24H24Cl2F3N3O2
 1
1 IC50 = 5 nM
CP0402072
3-[2,4-dichloro-3-[2-(5-chlorofuran-2-yl)-5-methyl-4-[1-(trifluoromethyl)cyclopropyl]imidazol-1-yl]anilino]-2,2-dimethylpropanoic acid
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C23H21Cl3F3N3O3
 1
1 IC50 = 5 nM
CP0574588
4-benzyl-1-(2,6-dichlorophenyl)-2-(furan-2-yl)-5-methylimidazole
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C21H16Cl2N2O
 1
1 IC50 = 5 nM
CP0078472
N-[3,5-dichloro-4-[2-(trifluoromethoxy)phenyl]phenyl]-2-(4-methylsulfonylphenyl)acetamide
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C22H16Cl2F3NO4S
 1
1 IC50 = 5.012 nM
CP0731677
N-(4-(3-acetamido-1-cyclopentyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C29H31ClFN5O2
 1
1 IC50 = 5.1 nM
CP0659888
N-(4-(3-acetamido-1-cyclobutyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C28H29ClFN5O2
 1
1 IC50 = 5.2 nM
CP0144908
(1R)-N-(3,5-difluoro-4-trimethylsilylphenyl)-6-methoxy-2-(3-oxo-1,2-oxazole-5-carbonyl)-3,4-dihydro-1H-isoquinoline-1-carboxamide
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C24H25F2N3O5Si
 1
1 IC50 = 5.3 nM
CP0111081
5-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-3,3-dimethyl-5-oxopentanoic acid
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C27H34F2N2O5Si
 1
1 IC50 = 5.6 nM
CP0412818
N-(4-cyanophenyl)-N'-(9-ethyl-5,6,7,8-tetrahydrocarbazol-3-yl)-3-methylpentanediamide
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C27H30N4O2
 1
1 IC50 = 5.9 nM
CP0770851
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(1-isopropyl-3-(3-methylureido)-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C27H30ClFN6O2
 1
1 IC50 = 6 nM
CP0072489
N-[5-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-3-piperidin-1-ylpyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
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C26H30ClFN6O2
 1
1 IC50 = 6.2 nM
CP0674427
N-(4-(3-acetamido-1-(cyclopropylmethyl)-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C28H29ClFN5O2
 1
1 IC50 = 6.4 nM
CP0549025
6-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-6-oxohexanoic acid
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C26H32F2N2O5Si
 1
1 IC50 = 6.6 nM
CP0060563
2-[1-[2,4-dichloro-3-[2-(5-chlorofuran-2-yl)-5-methyl-4-(trifluoromethyl)imidazol-1-yl]phenyl]azetidin-3-yl]acetic acid
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C20H15Cl3F3N3O3
 1
1 IC50 = 7 nM
CP0350381
2-[2-[(S)-(3,5-dimethyl-1,2-oxazol-4-yl)-hydroxymethyl]-1-benzofuran-5-yl]-N-[(S)-(2,4-dimethylphenyl)-phenylmethyl]acetamide
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C31H30N2O4
 1
1 IC50 = 7 nM
CP0082875
4-[[(1R)-2-(3,5-difluoro-4-trimethylsilylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-methylamino]-4-oxobutanoic acid
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C23H28F2N2O5Si
 1
1 IC50 = 7.5 nM
CP0118634
N-(3-chloro-4-cyanophenyl)-N'-(2,4-diethyl-3-oxo-1,4-benzoxazin-7-yl)-3-methylpentanediamide
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C25H27ClN4O4
 1
1 IC50 = 7.5 nM
CP0477736
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)-3-methylpentanediamide
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C27H26N4O2
 1
1 IC50 = 7.5 nM
CP0408940
(1R)-N-(3,5-difluoro-4-trimethylsilylphenyl)-2-[2-(2,4-dioxo-1,3-thiazolidin-5-yl)acetyl]-6-methoxy-3,4-dihydro-1H-isoquinoline-1-carboxamide
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C25H27F2N3O5SSi
 1
1 IC50 = 7.6 nM
CP0248827
2-[[2-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-2-oxoethyl]-methylamino]acetic acid
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C25H31F2N3O5Si
 1
1 IC50 = 7.8 nM
CP0053566
N-[5-(2-chlorobenzoyl)-4-(3-chlorophenyl)-1,3-thiazol-2-yl]-2-(4-ethylsulfonylphenyl)acetamide
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C26H20Cl2N2O4S2
 5
1 IC50 = 7.943 nM
2 IC50 = 9 nM
3 IC50 = 15.85 nM
4 IC50 = 22 nM
5 Ki = 39.81 nM
CP0579634
N-(2-methyl-6-morpholin-4-ylpyridin-3-yl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C28H37N3O6S
 1
1 IC50 = 8 nM
CP0189867
4-[3-(2-chlorobenzoyl)-7-methylindol-1-yl]-3-fluorobenzoic acid
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C23H15ClFNO3
 1
1 IC50 = 8.1 nM
CP0660103
N-(4-(3-acetamido-1-(1-cyclopropylethyl)-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C29H31ClFN5O2
 1
1 IC50 = 8.4 nM
CP0281549
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-pyrrolidin-1-ylphenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C26H29ClFN5O2
 1
1 IC50 = 8.6 nM
CP0652292
N-(5-(3-acetamido-1-isopropyl-1H-pyrazol-5-yl)-3-(3-azabicyclo[3.1.0]hexan-3-yl)pyridin-2-yl)-2-chloro-6-fluoro-N-[2H]-methylbenzamide
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C26H28ClFN6O2
 1
1 IC50 = 9.2 nM
CP0717531
N-(5-(3-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(2-chloro-6-fluoro-N[2H]-methylbenzamido)phenyl)-1-isopropyl-1H-pyrazol-3-yl)-3-hydroxyazetidine-1-carboxamide
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C29H32ClFN6O3
 1
1 IC50 = 9.4 nM
CP0528744
N-[5-(5-carbamoyl-2-chlorophenyl)-3-(cyclobutylmethoxy)pyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
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C25H22Cl2FN3O3
 1
1 IC50 = 10 nM
CP0946875
[2H]-N-(5-(5-carbamoyl-2-chlorophenyl)-3-(cyclobutylmethoxy)pyridin-2-yl)-2-chloro-6-fluoro-N-methylbenzamide
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C25H22Cl2FN3O3
 1
1 IC50 = 10 nM
CP0066901
N-[5-[4-chloro-2-(trifluoromethyl)phenoxy]-4-(3-cyanophenyl)-1,3-thiazol-2-yl]-2-(4-ethylsulfonylphenyl)acetamide
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C27H19ClF3N3O4S2
 2
1 IC50 = 10 nM
2 IC50 = 19.95 nM
CP0187559
N-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenyl]methyl]-N-cyclobutyl-1-(2-fluorophenyl)methanesulfonamide
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C24H29F2N3O3S
 1
1 IC50 = 10 nM
CP0098044
N-(5-benzoyl-4-phenyl-1,3-thiazol-2-yl)-2-(4-ethylsulfonylphenyl)acetamide
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C26H22N2O4S2
 4
1 IC50 = 10 nM
2 IC50 = 15.85 nM
3 IC50 = 31.62 nM
4 IC50 = 39.81 nM
CP0520885
N-(4-ethylphenyl)-3-(hydroxymethyl)-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)benzenesulfonamide
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C25H35NO5S
 2
1 IC50 = 10 nM
2 IC50 = 17 nM
CP0577877
N-(cyclopropylmethyl)-N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H31NO5S
 1
1 IC50 = 10 nM
CP0224309
N-[4-(5-carbamoyl-2-chlorophenyl)-2-propoxyphenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C24H21Cl2FN2O3
 1
1 IC50 = 11 nM
CP0718057
6-chloro-4'-(2-chloro-6-fluoro-N-methylbenzamido)-3'-(2,2,2-trifluoroethoxy)biphenyl-3-carboxamide
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C23H16Cl2F4N2O3
 1
1 IC50 = 11 nM
CP0830825
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-((1r,3r)-3-hydroxycyclobutanecarboxamido)-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C30H33ClFN5O3
 1
1 IC50 = 12 nM
CP0488542
N-cyclobutyl-N-(2,4-dimethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H31NO5S
 1
1 IC50 = 12 nM
CP0215047
N-(3-chloro-4-cyanophenyl)-N'-(4-ethyl-2-methyl-3-oxo-1,4-benzoxazin-7-yl)-3-methylpentanediamide
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C24H25ClN4O4
 1
1 IC50 = 13 nM
CP0045843
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-phenylphenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C28H26ClFN4O2
 1
1 IC50 = 15 nM
CP0660138
N-(4-(3-acetamido-1-neopentyl-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C29H33ClFN5O2
 1
1 IC50 = 15 nM
CP0560135
N-[4-cyano-3-(trifluoromethyl)phenyl]-N'-(9-ethylcarbazol-3-yl)-3-methylpentanediamide
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C28H25F3N4O2
 1
1 IC50 = 15 nM
CP0577875
N-(2,4-dimethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H33NO5S
 1
1 IC50 = 15 nM
CP0731675
N-(5-(3-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(2-chloro-6-fluoro-N[2H]-methylbenzamido)phenyl)-1-isopropyl-1H-pyrazol-3-yl)-2-oxa-6-azaspiro[3.3]heptane-6-carboxamide
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C31H34ClFN6O3
 1
1 IC50 = 16 nM
CP0427356
(Z)-4-[(1R)-1-[(3,5-difluoro-4-trimethylsilylphenyl)carbamoyl]-6-methoxy-3,4-dihydro-1H-isoquinolin-2-yl]-4-oxobut-2-enoic acid
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C24H26F2N2O5Si
 1
1 IC50 = 17 nM
CP0059556
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-(cyclobutylmethoxy)phenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C27H30ClFN4O3
 1
1 IC50 = 18 nM
CP0660137
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-(3-(2-hydroxyethyl)ureido)-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C28H32ClFN6O3
 1
1 IC50 = 18 nM
CP0175229
N-[5-(5-carbamoyl-2-chlorophenyl)-3-(2,2,2-trifluoroethoxy)pyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
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C22H15Cl2F4N3O3
 1
1 IC50 = 20 nM
CP0075606
4-[3-(2,6-dichlorobenzoyl)pyrrolo[2,3-b]pyridin-1-yl]benzoic acid
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C21H12Cl2N2O3
 1
1 IC50 = 20 nM
CP0359929
4-[3-(2-chloro-6-fluorobenzoyl)indol-1-yl]benzoic acid
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C22H13ClFNO3
 1
1 IC50 = 20 nM
CP0544566
(2S)-N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H33NO5S
 1
1 IC50 = 20 nM
CP0571812
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H33NO5S
 1
1 IC50 = 20 nM
CP0576571
(2R)-N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H33NO5S
 1
1 IC50 = 20 nM
CP0830828
isopropyl 5-(3-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(2-chloro-6-fluoro-N[2H]-methylbenzamido)phenyl)-1-isopropyl-1H-pyrazol-3-ylcarbamate
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C29H33ClFN5O3
 1
1 IC50 = 21 nM
CP0096332
1-[2,4-dichloro-3-[2-(5-chlorofuran-2-yl)-5-methyl-4-(trifluoromethyl)imidazol-1-yl]phenyl]azetidine-3-carboxylic acid
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C19H13Cl3F3N3O3
 1
1 IC50 = 21 nM
CP0247153
N-[2-butoxy-4-(5-carbamoyl-2-chlorophenyl)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C25H23Cl2FN2O3
 1
1 IC50 = 22 nM
CP0356460
4-[3-(2,6-dichlorobenzoyl)-4-fluoroindol-1-yl]benzoic acid
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C22H12Cl2FNO3
 1
1 IC50 = 25 nM
CP0088476
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-(2,2,2-trifluoroethoxy)phenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C24H23ClF4N4O3
 1
1 IC50 = 26 nM
CP0045935
N-[4-(5-carbamoyl-2-chlorophenyl)-2-(2,2,2-trifluoroethoxy)phenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C23H16Cl2F4N2O3
 1
1 IC50 = 29 nM
CP0532485
propan-2-yl (2S)-2-[2,6-dichloro-N-(furan-2-carbonyl)anilino]propanoate
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C17H17Cl2NO4
 1
1 IC50 = 29 nM
CP0266018
N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-1-phenyl-N-(2,2,2-trifluoroethyl)methanesulfonamide
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C22H26F3N3O3S
 1
1 IC50 = 30 nM
CP0116134
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-N-(4-fluorophenyl)-2-methylpropanamide
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C26H27FN2O4S
 1
1 IC50 < 30 nM
CP0116135
N-(4-cyanopyridin-2-yl)-2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-2-methylpropanamide
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C26H25FN4O4S
 1
1 IC50 < 30 nM
CP0116165
N-(2,4-difluorophenyl)-2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-2-methylpropanamide
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C26H25F3N2O4S
 1
1 IC50 < 30 nM
CP0168881
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-2-methyl-N-phenylpropanamide
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C26H28N2O4S
 1
1 IC50 < 30 nM
CP0243406
N-[4-[1-(azetidin-1-yl)-2-methyl-1-oxopropan-2-yl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C23H28N2O4S
 1
1 IC50 < 30 nM
CP0262111
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-N,2-dimethyl-N-phenylpropanamide
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C27H30N2O4S
 1
1 IC50 < 30 nM
CP0262112
N-[4-[1-(2,3-dihydroindol-1-yl)-2-methyl-1-oxopropan-2-yl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C28H30N2O4S
 1
1 IC50 < 30 nM
CP0262113
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]-2-fluorophenyl]-N-(4-fluorophenyl)-2-methylpropanamide
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C26H26F2N2O4S
 1
1 IC50 < 30 nM
CP0361258
N-[4-[1-(1,3-dihydroisoindol-2-yl)-2-methyl-1-oxopropan-2-yl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C28H30N2O4S
 1
1 IC50 < 30 nM
CP0407763
2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-N,N,2-trimethylpropanamide
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C22H28N2O4S
 1
1 IC50 = 30 nM
CP0551961
2-(4-ethylsulfonylphenyl)-N-[4-[2-[7-(2-methylpropyl)-3,4-dihydro-2H-quinolin-1-yl]-2-oxoethyl]phenyl]acetamide
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C31H36N2O4S
 1
1 IC50 = 31.5 nM
CP0361257
N-[4-[1-(2-azaspiro[3.3]heptan-2-yl)-2-methyl-1-oxopropan-2-yl]phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C26H32N2O4S
 1
1 IC50 = 33 nM
CP0260504
N-cyclobutyl-N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H31NO5S
 1
1 IC50 = 33 nM
CP0237544
4-fluoro-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
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C17H11F10NO3S
 1
1 IC50 = 34 nM
CP0085610
2-(4-ethylsulfonylphenyl)-N-[4-(2-methyl-1-oxo-1-piperidin-1-ylpropan-2-yl)phenyl]acetamide
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C25H32N2O4S
 1
1 IC50 = 36 nM
CP0146700
2-chloro-6-fluoro-N-[4-(1-methyl-5-propan-2-ylpyrazol-4-yl)-2-(2,2,2-trifluoroethoxy)phenyl]-N-(trideuteriomethyl)benzamide
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C23H22ClF4N3O2
 1
1 IC50 = 38 nM
CP0677744
N-(4-(3-acetamido-1-(oxetan-3-yl)-1H-pyrazol-5-yl)-2-(3-azabicyclo[3.1.0]hexan-3-yl)phenyl)-2-chloro-6-fluoro-N[2H]-methylbenzamide
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C27H27ClFN5O3
 1
1 IC50 = 40 nM
CP0552825
N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-N-[[2-(trifluoromethyl)phenyl]methyl]-2,3-dihydrochromene-6-sulfonamide
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C26H30F3NO5S
 1
1 IC50 = 40 nM
CP0253451
N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-N-(2-methylpropyl)-1-phenylmethanesulfonamide
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C24H33N3O3S
 1
1 IC50 = 47 nM
CP0484672
N-[4-(5-carbamoyl-2-chlorophenyl)-2-ethoxyphenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C23H19Cl2FN2O3
 1
1 IC50 = 50 nM
CP0773205
N-(4-(3-acetamido-1-isopropyl-1H-pyrazol-5-yl)-2-(bicyclo[3.1.0]hexan-3-yloxy)phenyl)-2-chloro-6-fluoro-N-[2H]-methylbenzamide
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C28H30ClFN4O3
 1
1 IC50 = 54 nM
CP0365042
N-[4-(5-carbamoyl-2-chlorophenyl)-2-propan-2-yloxyphenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C24H21Cl2FN2O3
 1
1 IC50 = 54 nM
CP0202748
US9458171, 95
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C27H25F8NO5S
 1
1 IC50 = 55 nM
CP0120332
3-(1,3-benzodioxol-5-yl)-1-(3,5-dimethylpiperidin-1-yl)-3-(2-hydroxy-4,6-dimethoxyphenyl)propan-1-one
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C25H31NO6
 1
1 IC50 = 57 nM
CP0252169
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-3-oxo-1,2-oxazole-5-carboxamide
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C24H27N3O5
 1
1 IC50 = 57 nM
CP0445966
N-[2-(3,5-difluoro-4-trimethylsilylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-3-oxo-1,2-oxazole-5-carboxamide
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C23H25F2N3O5Si
 1
1 IC50 = 57 nM
CP0335252
N-(4-cyanophenyl)-2-[[2-[(9-ethylcarbazol-3-yl)amino]-2-oxoethyl]-methylamino]acetamide
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C26H25N5O2
 1
1 IC50 = 57 nM
CP0367481
(6aR,7R,10aS)-4-(4-fluorophenyl)-7,10a-dimethyl-2-(2-methylpyridin-4-yl)-8-oxo-5,6,6a,7-tetrahydrobenzo[h]quinazoline-9-carbonitrile
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C27H23FN4O
 1
1 IC50 = 58 nM
CP0387093
N-[3-[[(3S)-4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl]methyl]-5-fluoro-2-methylphenyl]-6-methylpyridine-3-carboxamide
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C26H33FN4O2
 1
1 IC50 = 59 nM
CP0003740
N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
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C17H12F9NO3S
 6
1 IC50 = 60 nM
2 IC50 = 204 nM
3 IC50 = 501.19 nM
4 IC50 = 1700 nM
5 IC50 = 2010 nM
6 Ki = 51 nM
CP0408147
N-[1-(4-methoxyphenyl)-2-oxo-2-(4-trimethylsilylanilino)ethyl]-N-methyl-3-oxo-1,2-oxazole-5-carboxamide
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C23H27N3O5Si
 1
1 IC50 = 60 nM
CP0488538
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-ylmethyl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C27H35NO5S
 1
1 IC50 = 60 nM
CP0353045
US10647665, Example 1-15
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C23H17Cl2F3N2O4
 1
1 IC50 = 63.8 nM
CP0116164
ethyl 2-[4-[[2-(4-ethylsulfonylphenyl)acetyl]amino]phenyl]-2-methylpropanoate
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C22H27NO5S
 1
1 IC50 = 64 nM
CP0552054
N-[3-[[(3S)-4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl]methyl]-5-fluoro-2-methylphenyl]-3-phenylpropanamide
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C28H36FN3O2
 1
1 IC50 = 67 nM
CP0830827
N-(2-(3-azabicyclo[3.1.0]hexan-3-yl)-4-(3-(2-(dimethylamino)acetamido)-1-isopropyl-1H-pyrazol-5-yl)phenyl)-2-chloro-6-fluoro-N-[2H]-methylbenzamide
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C29H34ClFN6O2
 1
1 IC50 = 70 nM
CP0124889
N-[2-(4-tert-butyl-3-chloroanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C26H28ClN3O4
 1
1 IC50 = 75 nM
CP0199395
N-[4-(5-acetamido-2-propan-2-ylpyrazol-3-yl)-2-(2-methylpropoxy)phenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C26H30ClFN4O3
 1
1 IC50 = 76 nM
CP0549844
N-(4-cyanophenyl)-2-[2-[(9-ethylcarbazol-3-yl)amino]-2-oxoethoxy]acetamide
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C25H22N4O3
 1
1 IC50 = 81 nM
CP0339295
(6aR,7R,10aS)-2-(2-cyclopropylpyridin-4-yl)-4-(2-fluorophenyl)-10a-methyl-8-oxo-7-propyl-5,6,6a,7-tetrahydrobenzo[h]quinazoline-9-carbonitrile
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C31H29FN4O
 1
1 IC50 = 82 nM
CP0550142
N-[2-[(1,1-dimethyl-2,3-dihydroinden-5-yl)amino]-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H29N3O4
 1
1 IC50 = 84 nM
CP0702332
[2H]-N-(5-(5-carbamoyl-2-chlorophenyl)-3-(2,2,2-trifluoroethoxy)pyridin-2-yl)-2-chloro-6-fluoro-N-methylbenzamide
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C22H15Cl2F4N3O3
 1
1 IC50 = 89 nM
CP0488539
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-[1-(oxan-4-yl)ethyl]-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C28H37NO5S
 1
1 IC50 = 93 nM
CP0546328
N-(4-tert-butylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C28H37NO5S
 1
1 IC50 = 93 nM
CP0325717
N-[[4-(4-acetylpiperazin-1-yl)phenyl]methyl]-1-phenyl-N-propan-2-ylmethanesulfonamide
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C23H31N3O3S
 1
1 IC50 = 95 nM
CP0120333
1-(3,5-dimethylpiperidin-1-yl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)propan-1-one
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C25H33NO5
 1
1 IC50 = 96 nM
CP0580078
2-(oxan-4-yl)-6-[2-[2-(trifluoromethyl)phenyl]pyrrolidin-1-yl]sulfonyl-2,3-dihydrochromen-4-one
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C25H26F3NO5S
 1
1 IC50 = 96 nM
CP0576570
N-(4-ethylphenyl)-4-fluoro-N-(2-methylpropyl)-2-(oxan-4-yl)-3,4-dihydro-2H-chromene-6-sulfonamide
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C26H34FNO4S
 1
1 IC50 = 97 nM
CP0219108
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-6-oxo-1H-pyridine-3-carboxamide
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C25H27N3O4
 1
1 IC50 = 99 nM
CP0563762
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-N-methylbenzamide
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C24H19Cl2FN2O2
 1
1 IC50 = 100 nM
CP0219107
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C26H29N3O4
 1
1 IC50 = 100 nM
CP0396048
N-[1-(4-methoxyphenyl)-2-oxo-2-(4-trimethylsilylanilino)ethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C25H29N3O4Si
 1
1 IC50 = 100 nM
CP0579898
N-(4-fluorophenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C24H28FNO5S
 1
1 IC50 = 100 nM
CP0552822
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-3-oxo-1H-isoindole-5-sulfonamide
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C25H32N2O4S
 1
1 IC50 = 105 nM
CP0156196
1-(3,5-dimethylpiperidin-1-yl)-3-(2-hydroxy-4,6-dimethoxyphenyl)-3-(2-methoxyphenyl)propan-1-one
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C25H33NO5
 1
1 IC50 = 106 nM
CP0566951
N-[1-(4-methoxyphenyl)-2-oxo-2-(4-trimethylsilylanilino)ethyl]-N-methyl-1,2-oxazole-5-carboxamide
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C23H27N3O4Si
 1
1 IC50 = 110 nM
CP0118610
N-(3-chloro-4-cyanophenyl)-N'-(4-ethyl-3-oxo-1,4-benzoxazin-7-yl)-3-methylpentanediamide
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C23H23ClN4O4
 1
1 IC50 = 110 nM
CP0551495
N-(cyclobutylmethyl)-N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C27H33NO5S
 1
1 IC50 = 111 nM
CP0580007
N-(4-ethylphenyl)-2-(4-methyloxan-4-yl)-N-(2-methylpropyl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C27H35NO5S
 1
1 IC50 = 115 nM
CP0580017
N-(4-ethylphenyl)-7-(hydroxymethyl)-N-(2-methylpropyl)-6-(oxan-4-ylmethoxy)naphthalene-2-sulfonamide
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C29H37NO5S
 1
1 IC50 = 139 nM
CP0526723
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)hexanediamide
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C27H26N4O2
 1
1 IC50 = 140 nM
CP0579899
N-[4-(dimethylamino)phenyl]-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H34N2O5S
 1
1 IC50 = 144 nM
CP0361647
US9458171, 16
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C27H26F7NO6S
 1
1 IC50 = 146 nM
CP0180490
4-[3-(2,6-dichlorobenzoyl)-2-methylindol-1-yl]benzoic acid
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C23H15Cl2NO3
 1
1 IC50 = 156 nM
CP0579635
N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-N-(2,2,2-trifluoroethyl)-2,3-dihydrochromene-6-sulfonamide
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C24H26F3NO5S
 1
1 IC50 = 157 nM
CP0566953
N-[1-(4-methoxyphenyl)-2-oxo-2-(4-trimethylsilylanilino)ethyl]-N-methylfuran-2-carboxamide
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C24H28N2O4Si
 1
1 IC50 = 160 nM
CP0564978
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-1,2-oxazole-5-carboxamide
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C24H27N3O4
 1
1 IC50 = 170 nM
CP0118636
N-(3-chloro-4-cyanophenyl)-N'-(1-ethylindol-5-yl)-3-methylpentanediamide
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C23H23ClN4O2
 1
1 IC50 = 170 nM
CP0260503
N-(3-fluorophenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C24H28FNO5S
 1
1 IC50 = 189 nM
CP0078421
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-N-(2-hydroxyethyl)benzamide
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C25H21Cl2FN2O3
 1
1 IC50 = 190 nM
CP0341568
N-(3-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)-3-methylpentanediamide
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C27H26N4O2
 1
1 IC50 = 190 nM
CP0484671
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-4,4-dimethyl-2,3-dihydroquinolin-6-yl]benzamide
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C25H21Cl2FN2O2
 1
1 IC50 = 200 nM
CP0189181
N-[1-(4-methoxyphenyl)-2-oxo-2-(4-propan-2-ylanilino)ethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C25H27N3O4
 1
1 IC50 = 200 nM
CP0046607
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]benzamide
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C23H17Cl2FN2O2
 1
1 IC50 = 220 nM
CP0224311
N-[4-(5-carbamoyl-2-chlorophenyl)-2-(trifluoromethyl)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C22H14Cl2F4N2O2
 1
1 IC50 = 230 nM
CP0189183
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-6-oxo-N-propyl-1H-pyridine-3-carboxamide
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C28H33N3O4
 1
1 IC50 = 230 nM
CP0199394
5-[4-[(2-chloro-6-fluorobenzoyl)-(trideuteriomethyl)amino]-3-(2,2,2-trifluoroethoxy)phenyl]-1-propan-2-ylpyrazole-3-carboxamide
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C23H21ClF4N4O3
 1
1 IC50 = 240 nM
CP0544567
N-(6-fluoro-2,3-dihydro-1H-inden-1-yl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C27H32FNO5S
 1
1 IC50 = 245 nM
CP0101389
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-4-methyl-2,3-dihydroquinoxalin-6-yl]benzamide
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C23H18Cl2FN3O2
 1
1 IC50 = 250 nM
CP0580019
N-benzyl-N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C29H31NO5S
 1
1 IC50 = 252 nM
CP0341567
N-(3-chloro-4-cyanophenyl)-N'-(3-ethyl-2-oxo-1,3-benzoxazol-6-yl)-3-methylpentanediamide
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C22H21ClN4O4
 1
1 IC50 = 260 nM
CP0542965
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxochromene-6-sulfonamide
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C26H31NO5S
 1
1 IC50 = 271 nM
CP0549915
N-(4-ethylphenyl)-N-(2-methylpropyl)-2-(1-methylsulfonylpiperidin-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C27H36N2O6S2
 1
1 IC50 = 281 nM
CP0198871
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)-3,3-dimethylpentanediamide
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C28H28N4O2
 1
1 IC50 = 290 nM
CP0552826
N-(2,4-difluorophenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C24H27F2NO5S
 1
1 IC50 = 295 nM
CP0188108
3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-4-methylbenzamide
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C24H20ClFN2O2
 1
1 IC50 = 300 nM
CP0408677
N-[2-(4-tert-butylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methylfuran-2-carboxamide
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C25H28N2O4
 1
1 IC50 = 300 nM
CP0404168
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-N-ethylbenzamide
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C25H21Cl2FN2O2
 1
1 IC50 = 330 nM
CP0565873
6-[3-[[(3S)-4-(cyclopentanecarbonyl)-3-methylpiperazin-1-yl]methyl]-5-fluoro-2-methylanilino]-6-oxohexanoic acid
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C25H36FN3O4
 1
1 IC50 = 330 nM
CP0189866
4-[3-(2,6-dichlorobenzoyl)-7-methoxyindol-1-yl]benzoic acid
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C23H15Cl2NO4
 1
1 IC50 = 350 nM
CP0348513
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-2,3,4,5-tetrahydro-1-benzazepin-7-yl]benzamide
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C24H19Cl2FN2O2
 1
1 IC50 = 360 nM
CP0141347
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-N-cyclopentylbenzamide
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C28H25Cl2FN2O2
 1
1 IC50 = 370 nM
CP0365048
N-[4-(5-carbamoyl-2-chlorophenyl)-2-methoxyphenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C22H17Cl2FN2O3
 1
1 IC50 = 370 nM
CP0412821
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)butanediamide
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C25H22N4O2
 1
1 IC50 = 410 nM
CP0552824
N-(4-cyanophenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C25H28N2O5S
 1
1 IC50 = 425 nM
CP0488541
N-(1-benzothiophen-2-yl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H29NO5S2
 1
1 IC50 = 432 nM
CP0141496
1-[3-[[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]methyl]piperidin-1-yl]propan-1-one
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C25H27F6N3O4S
 2
1 IC50 = 440 nM
2 Kd = 450 nM
CP0260501
N-(4-ethylphenyl)-N-(2-methylpropyl)-7-(oxan-4-ylmethoxy)-1-oxo-2,3-dihydroindene-4-sulfonamide
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C27H35NO5S
 1
1 IC50 = 451 nM
CP0260502
2-(3,5-dimethyl-1,2-oxazol-4-yl)-N-(4-ethylphenyl)-N-(2-methylpropyl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C26H30N2O5S
 1
1 IC50 = 458 nM
CP0253044
N-[4-(5-carbamoyl-2-chlorophenyl)-2-(ethylamino)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C23H20Cl2FN3O2
 1
1 IC50 = 500 nM
CP0252385
2-chloro-6-fluoro-N-[4-(1-methyl-3-propan-2-ylpyrazol-4-yl)-2-(2,2,2-trifluoroethoxy)phenyl]-N-(trideuteriomethyl)benzamide
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C23H22ClF4N3O2
 1
1 IC50 = 530 nM
CP0365040
4-chloro-5-[1-(2-chloro-6-fluorobenzoyl)-3,4-dihydro-2H-quinolin-6-yl]-2-fluorobenzamide
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C23H16Cl2F2N2O2
 1
1 IC50 = 550 nM
CP0248164
1-[4-[[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]methyl]piperidin-1-yl]-2-methylpropan-1-one
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C26H29F6N3O4S
 2
1 IC50 = 590 nM
2 Kd = 1600 nM
CP0343454
N-[4-[5-(2-amino-2-oxoethyl)-2-propan-2-ylpyrazol-3-yl]-2-(2,2,2-trifluoroethoxy)phenyl]-2-chloro-6-fluoro-N-(trideuteriomethyl)benzamide
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C24H23ClF4N4O3
 1
1 IC50 = 610 nM
CP0188270
N-[3-(2,5-dichlorophenyl)phenyl]-2-(4-ethylsulfonylphenyl)acetamide
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C22H19Cl2NO3S
 1
1 IC50 = 630.96 nM
CP0175226
4-chloro-3-[1-(2-chloro-6-fluorobenzoyl)-3,3-dimethyl-2,4-dihydroquinolin-6-yl]benzamide
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C25H21Cl2FN2O2
 1
1 IC50 = 640 nM
CP0040077
(3beta)-3-hydroxyurs-12-en-28-oic acid
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C30H48O3
 2
1 IC50 = 680 nM
2 IC50 = 9410 nM
CP0365046
N-[4-(5-carbamoyl-2-chlorophenyl)-2-ethylphenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C23H19Cl2FN2O2
 1
1 IC50 = 730 nM
CP0577874
N-(4-ethylphenyl)-N-(2-methylpropyl)-4-oxo-2-piperidin-4-yl-2,3-dihydrochromene-6-sulfonamide
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C26H34N2O4S
 1
1 IC50 = 755 nM
CP0553082
1-butan-2-yl-7-[cyclohexyl(methyl)amino]-3-(4-methylpiperazin-1-yl)pyrido[3,4-b]pyrazin-2-one
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C23H36N6O
 1
1 IC50 = 780 nM
CP0549921
N-(4-ethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C22H25NO5S
 1
1 IC50 = 782 nM
CP0365045
N-[2-bromo-4-(5-carbamoyl-2-chlorophenyl)phenyl]-2-chloro-6-fluoro-N-methylbenzamide
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C21H14BrCl2FN2O2
 1
1 IC50 = 820 nM
CP0412819
N-(9-ethylcarbazol-3-yl)-N'-(4-fluorophenyl)-3-methylpentanediamide
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C26H26FN3O2
 1
1 IC50 = 840 nM
CP0552823
2-(1-cyclopentylsulfonylpiperidin-4-yl)-N-(4-ethylphenyl)-N-(2-methylpropyl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C31H42N2O6S2
 1
1 IC50 = 861 nM
CP0095817
1-[4-[[4-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]phenyl]methyl]piperazin-1-yl]ethanone
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C22H22F6N2O2
 2
1 IC50 = 1000 nM
2 Ki = 1000 nM
CP0260030
4-[2,2-dioxo-3-[(4-pentan-3-ylphenyl)methyl]-2lambda6,1,3-benzothiadiazol-1-yl]-1-pyrrolidin-1-ylbutan-1-one
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C26H35N3O3S
 2
1 IC50 = 1000 nM
2 Kd = 1500 nM
CP0577876
N-(2,4-dimethylphenyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C22H25NO5S
 1
1 IC50 = 1104 nM
CP0552821
oxan-4-ylmethyl 7-[(4-ethylphenyl)-(2-methylpropyl)sulfamoyl]-3-(oxan-4-ylmethoxy)naphthalene-2-carboxylate
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C35H45NO7S
 1
1 IC50 = 1465 nM
CP0260500
N-(4-ethylphenyl)-N-(2-methylpropyl)-4-(oxan-4-ylmethoxy)-5-oxo-7,8-dihydro-6H-naphthalene-1-sulfonamide
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C28H37NO5S
 1
1 IC50 = 1863 nM
CP0054979
DIGOXIN
   Show/Hide
C41H64O14
 2
1 IC50 = 1980 nM
2 IC50 = 4100 nM
CP0580018
2-[1-(cyclopentanecarbonyl)piperidin-4-yl]-N-(4-ethylphenyl)-N-(2-methylpropyl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C32H42N2O5S
 1
1 IC50 = 2217 nM
CP0208514
2-oxo-N-(4-phenoxyphenyl)-1H-benzo[cd]indole-6-sulfonamide
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C23H16N2O4S
 1
1 IC50 = 3090 nM
CP0542963
methyl 7-[(4-ethylphenyl)-(2-methylpropyl)sulfamoyl]-3-(oxan-4-ylmethoxy)naphthalene-2-carboxylate
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C30H37NO6S
 1
1 IC50 = 3274 nM
CP0564992
N-[(1S)-2-(3,5-difluoro-4-trimethylsilylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-3-oxo-1,2-oxazole-5-carboxamide
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C23H25F2N3O5Si
 1
1 IC50 = 3400 nM
CP0334820
4-[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]-N-[(3-methoxyphenyl)methyl]-N-methylbutanamide
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C29H29F6N3O5S
 2
1 IC50 = 3500 nM
2 Kd = 480 nM
CP0095581
1,1,1,3,3,3-hexafluoro-2-[3-fluoro-4-[4-[[4-(pyridin-4-ylmethyl)piperazin-1-yl]methyl]phenyl]phenyl]propan-2-ol
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C26H24F7N3O
 2
1 IC50 = 3540 nM
2 Ki = 105 nM
CP0488540
N-(2-fluorophenyl)-N-(2-methylpropyl)-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C24H28FNO5S
 1
1 IC50 = 4217 nM
CP0252387
N-[5-(4-acetamido-1-propan-2-ylimidazol-2-yl)-3-piperidin-1-ylpyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
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C26H30ClFN6O2
 1
1 IC50 = 4800 nM
CP0129839
4-[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]-N-(4-hydroxybutan-2-yl)-N-methylbutanamide
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C25H29F6N3O5S
 2
1 IC50 = 5400 nM
2 Kd = 1600 nM
CP0557981
N-(4-cyanophenyl)-3-methyl-N'-(6,7,8,9-tetrahydro-5H-carbazol-3-yl)pentanediamide
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C25H26N4O2
 1
1 IC50 = 5500 nM
CP0331274
N-[2-(4-tert-butylanilino)-1-(4-methoxy-2-methylphenyl)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H31N3O4
 1
1 IC50 = 5700 nM
CP0209305
N-(1-ethyl-2-oxobenzo[cd]indol-6-yl)sulfonyl-N-(4-methoxyphenyl)pyridine-4-carboxamide
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C26H21N3O5S
 1
1 IC50 = 5880 nM
CP0218473
1-ethyl-2-oxo-N-(4-phenyldiazenylphenyl)benzo[cd]indole-6-sulfonamide
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C25H20N4O3S
 1
1 IC50 = 6050 nM
CP0365210
N'-(9-ethylcarbazol-3-yl)-3-methyl-N-phenylpentanediamide
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C26H27N3O2
 1
1 IC50 = 6300 nM
CP0482021
N-[1-(4-methoxyphenyl)-2-(4-methylanilino)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C23H23N3O4
 1
1 IC50 = 6600 nM
CP0412820
N-(4-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)-N,N',3-trimethylpentanediamide
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C29H30N4O2
 1
1 IC50 = 6700 nM
CP0245521
N-(6-ethoxy-1,3-benzothiazol-2-yl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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C22H19N3O4S2
 1
1 IC50 = 6720 nM
CP0341216
tert-butyl N-[3-[(1-ethyl-2-oxobenzo[cd]indol-6-yl)sulfonylamino]phenyl]carbamate
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C24H25N3O5S
 1
1 IC50 = 7040 nM
CP0564993
N-[3-(4-tert-butylanilino)-2-(4-methoxyphenyl)-3-oxopropyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H31N3O4
 1
1 IC50 = 7200 nM
CP0218474
N-(4-methoxyphenyl)-4-[(2-oxo-1H-benzo[cd]indol-6-yl)sulfonylamino]benzamide
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C25H19N3O5S
 1
1 IC50 = 8350 nM
CP0316507
1-ethyl-N-(4-morpholin-4-ylphenyl)-2-oxobenzo[cd]indole-6-sulfonamide
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C23H23N3O4S
 1
1 IC50 = 12150 nM
CP0341215
1-ethyl-N-isoquinolin-8-yl-2-oxobenzo[cd]indole-6-sulfonamide
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C22H17N3O3S
 1
1 IC50 = 17520 nM
CP0434664
N-(2-tert-butylphenyl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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C23H24N2O3S
 1
1 IC50 = 18980 nM
CP0124348
N-(3,4-dimethoxyphenyl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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C21H20N2O5S
 1
1 IC50 = 20100 nM
CP0411808
N-(7,7-dimethyl-9-oxo-6,8-dihydrodibenzofuran-3-yl)-2-oxo-1H-benzo[cd]indole-6-sulfonamide
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C25H20N2O5S
 1
1 IC50 = 20270 nM
CP0316509
N-[(2,5-dichlorophenyl)methyl]-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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C20H16Cl2N2O3S
 1
1 IC50 = 31610 nM
CP0159378
N-(4-morpholin-4-ylphenyl)-2-oxo-1H-benzo[cd]indole-6-sulfonamide
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C21H19N3O4S
 1
1 IC50 = 48420 nM
CP0316508
N-(4-acetylphenyl)-1-ethyl-2-oxobenzo[cd]indole-6-sulfonamide
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C21H18N2O4S
 1
1 IC50 = 70140 nM
CP0124347
N-[4-[(1-ethyl-2-oxobenzo[cd]indol-6-yl)sulfonylamino]phenyl]acetamide
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C21H19N3O4S
 1
1 IC50 = 89760 nM
CP0089090
N-[5-(5-acetamido-2-propan-2-yl-1,2,4-triazol-3-yl)-3-piperidin-1-ylpyridin-2-yl]-2-chloro-6-fluoro-N-methylbenzamide
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C25H29ClFN7O2
 1
1 IC50 > 5000 nM
CP0109734
N-[3-(4-tert-butylanilino)-1-(4-methoxyphenyl)-3-oxopropyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H31N3O4
 1
1 IC50 > 10000 nM
CP0189182
N-[1-(4-tert-butylanilino)-3-(4-methoxyphenyl)-1-oxopropan-2-yl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H31N3O4
 1
1 IC50 > 10000 nM
CP0564974
N-[2-(4-tert-butyl-N-methylanilino)-1-(4-methoxyphenyl)-2-oxoethyl]-N-methyl-6-oxo-1H-pyridine-3-carboxamide
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C27H31N3O4
 1
1 IC50 > 10000 nM
CP0365211
N-(2-cyanophenyl)-N'-(9-ethylcarbazol-3-yl)-3-methylpentanediamide
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C27H26N4O2
 1
1 IC50 > 10000 nM
CP0260505
N-[(5-ethylsulfonylpyridin-2-yl)methyl]-2-(oxan-4-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C22H26N2O7S2
 1
1 IC50 > 10000 nM
CP0551496
N-(4-ethylphenyl)-2-(oxan-4-yl)-N-(oxetan-3-yl)-4-oxo-2,3-dihydrochromene-6-sulfonamide
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C25H29NO6S
 1
1 IC50 > 10000 nM
CP0576569
7-[(4-ethylphenyl)-(2-methylpropyl)sulfamoyl]-3-(oxan-4-ylmethoxy)naphthalene-2-carboxylic acid
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C29H35NO6S
 1
1 IC50 > 10000 nM
CP0576572
6-[(6-ethyl-3-methyl-3,4-dihydro-2H-quinolin-1-yl)sulfonyl]-2-(oxan-4-yl)-2,3-dihydrochromen-4-one
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C26H31NO5S
 1
1 IC50 > 10000 nM
CP0577873
tert-butyl 4-[6-[(4-ethylphenyl)-(2-methylpropyl)sulfamoyl]-4-oxo-2,3-dihydrochromen-2-yl]piperidine-1-carboxylate
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C31H42N2O6S
 1
1 IC50 > 10000 nM
CP0557510
US10080744, Example 3/26
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C28H32F6N4O5S2
 1
1 Kd = 0.03 nM
CP0339640
US10080744, Example 3/38
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C27H30F6N4O5S2
 1
1 Kd = 0.04 nM
CP0339634
3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluorobutan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C23H27Cl2F3N2O4S2
 1
1 Kd = 0.05 nM
CP0516618
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-[(4-fluorophenyl)methyl]-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C27H23F7N4O5S2
 1
1 Kd = 0.07 nM
CP0341592
3-[4-(cyclobutylmethyl)-5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluorobutan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C24H28F6N2O4S2
 1
1 Kd = 0.27 nM
CP0341598
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-[(3,3-difluoropiperidin-1-yl)methyl]-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C26H27F8N5O5S2
 1
1 Kd = 0.3 nM
CP0577120
US10080744, Example 3/3
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C28H29F3N4O5S2
 1
1 Kd = 0.35 nM
CP0526829
3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C22H25Cl2F3N2O4S2
 1
1 Kd = 0.36 nM
CP0557575
3-[3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-1,2,4-oxadiazol-5-yl]-2,2-dimethylpropanoic acid
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C24H25Cl2F3N4O5S2
 1
1 Kd = 0.39 nM
CP0525796
US10080744, Example 18
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C25H26Cl2F3N3O4S3
 1
1 Kd = 0.5 nM
CP0330312
2,3-dichloro-4-[4-(4,4-difluoropiperidine-1-carbonyl)-2-[5-(2-hydroxypropan-2-yl)-1,3,4-oxadiazol-2-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C23H22Cl2F5N5O5S2
 1
1 Kd = 0.7 nM
CP0341758
US10080744, Example 1/1
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C29H36N4O4S2
 1
1 Kd = 0.82 nM
CP0268256
US10301272, Example 6/4
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C29H39N3O4S2
 1
1 Kd = 1.1 nM
CP0341602
2,3-dichloro-4-[4-(4,4-difluoropiperidine-1-carbonyl)-2-[5-(2-hydroxypropan-2-yl)-4-methyl-1,2,4-triazol-3-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C24H25Cl2F5N6O4S2
 1
1 Kd = 1.5 nM
CP0564300
3-[6-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]pyrimidin-4-yl]-2,2-dimethylpropanoic acid
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C26H27Cl2F3N4O4S2
 1
1 Kd = 1.5 nM
CP0321517
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-(2-methylpropyl)-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
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C24H26F6N4O5S2
 1
1 Kd = 2 nM
CP0330311
3-[5-[5-[2-(difluoromethyl)-3-fluoro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-4-(2-methoxy-2-methylpropyl)-1,3-thiazol-2-yl]-1,3,4-oxadiazol-2-yl]-2,2-dimethylpropanoic acid
   Show/Hide
C25H28F6N4O6S2
 1
1 Kd = 2.3 nM
CP0553969
3-[3-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-1,2-oxazol-5-yl]-2,2-dimethylpropanoic acid
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C25H26Cl2F3N3O5S2
 1
1 Kd = 2.7 nM
CP0341601
2,3-dichloro-4-[4-(4-fluoropiperidine-1-carbonyl)-2-[5-(2-hydroxy-2-methylpropyl)-1,3,4-oxadiazol-2-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluorobutan-2-yl]benzenesulfonamide
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C25H27Cl2F4N5O5S2
 1
1 Kd = 3.2 nM
CP0321519
2,3-dichloro-4-[4-(4-fluoropiperidine-1-carbonyl)-2-[5-(2-hydroxypropan-2-yl)-1,2,4-oxadiazol-3-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C23H23Cl2F4N5O5S2
 1
1 Kd = 3.9 nM
CP0538061
CHEMBL4634072
   Show/Hide
C24H23Cl2F3N4O5S2
 1
1 Kd = 4.3 nM
CP0521151
5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-N,N-diethyl-2-[5-(2-hydroxypropan-2-yl)-1,3,4-oxadiazol-2-yl]-1,3-thiazole-4-carboxamide
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C22H24Cl2F3N5O5S2
 1
1 Kd = 5 nM
CP0133587
3-[5-[2-chloro-4-[[(2S)-1,1,1-trifluorobutan-2-yl]sulfamoyl]phenyl]-4-(cyclobutylmethyl)-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C23H28ClF3N2O4S2
 1
1 Kd = 6.5 nM
CP0133588
3-[4-(cyclobutylmethyl)-5-[2-(trifluoromethyl)-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-2,2-dimethylpropanoic acid
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C23H26F6N2O4S2
 1
1 Kd = 8.7 nM
CP0516619
2,3-dichloro-4-[4-(4-fluoropiperidine-1-carbonyl)-2-[5-(2-hydroxypropan-2-yl)-1,3,4-oxadiazol-2-yl]-1,3-thiazol-5-yl]-N-[(2S)-1,1,1-trifluoropropan-2-yl]benzenesulfonamide
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C23H23Cl2F4N5O5S2
 1
1 Kd = 11 nM
CP0247502
4-[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]-N-methyl-N-[(2-methylphenyl)methyl]butanamide
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C29H29F6N3O4S
 1
1 Kd = 2400 nM
CP0152535
4-(3-benzyl-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl)-1-pyrrolidin-1-ylbutan-1-one
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C21H25N3O3S
 1
1 Kd = 2700 nM
CP0089428
4-[2,2-dioxo-3-[(4-propan-2-ylphenyl)methyl]-2lambda6,1,3-benzothiadiazol-1-yl]-1-pyrrolidin-1-ylbutan-1-one
   Show/Hide
C24H31N3O3S
 1
1 Kd = 4600 nM
CP0516617
3-[5-[4-(cyclobutylmethyl)-5-[2,3-dichloro-4-[[(2S)-1,1,1-trifluoropropan-2-yl]sulfamoyl]phenyl]-1,3-thiazol-2-yl]-1,3,4-thiadiazol-2-yl]-2,2-dimethylpropanoic acid
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C24H25Cl2F3N4O4S3
 1
1 Kd = 14169 nM
CP0334821
4-[2,2-dioxo-3-[[4-(2,2,2-trifluoro-1-hydroxyethyl)phenyl]methyl]-2lambda6,1,3-benzothiadiazol-1-yl]-1-pyrrolidin-1-ylbutan-1-one
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C23H26F3N3O4S
 1
1 Kd > 10000 nM
CP0335474
4-[3-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]methyl]-2,2-dioxo-2lambda6,1,3-benzothiadiazol-1-yl]-1-pyrrolidin-1-ylbutan-1-one
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C24H25F6N3O4S
 1
1 Kd > 10000 nM
CP0205289
N-[5-[[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]sulfamoyl]-4-methyl-1,3-thiazol-2-yl]acetamide
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C15H13F6N3O4S2
 1
1 Ki = 111 nM
Clinical Information about the Protein
Target 1 ( Nuclear receptor ROR-gamma (RORG) )
Target Type Clinical trial Target
Disease 6 Target-related Diseases  6
1 Plaque psoriasis [ICD-11: EA90.0]
2 Solid tumour/cancer [ICD-11: 2A00-2F9Z]
3 Autoimmune disease [ICD-11: 4A40-4A45]
4 Atherosclerosis [ICD-11: BD40]
5 Liver cancer [ICD-11: 2C12]
6 Rheumatoid arthritis [ICD-11: FA20]
Clinical Trial Drug(s) 2 Clinical Trial Drugs  2
1 GSK2981278 Phase 2
Plaque psoriasis
2 LYC-55716 Phase 2
Solid tumour/cancer
Preclinical Drug(s) 5 Preclinical Drugs  5
1 ML209 Preclinical
Autoimmune disease
2 Nobiletin Preclinical
Atherosclerosis
3 SR1078 Preclinical
Liver cancer
4 SR1555 Preclinical
Rheumatoid arthritis
5 SR2211 Preclinical
Autoimmune disease