General Information of the Protein
Protein ID
PT01887
Protein Name
Oxysterols receptor LXR-beta
Secondarily
Protein Name
Liver X receptor beta
Nuclear receptor NER
Nuclear receptor subfamily 1 group H member 2
Ubiquitously-expressed nuclear receptor
Gene Name
NR1H2
Secondarily
Gene Name
LXRB
NER
UNR
Sequence
MSSPTTSSLDTPLPGNGPPQPGAPSSSPTVKEEGPEPWPGGPDPDVPGTDEASSACSTDWVIPDPEEEPERKRKKGPAPKMLGHELCRVCGDKASGFHYNVLSCEGCKGFFRRSVVRGGARRYACRGGGTCQMDAFMRRKCQQCRLRKCKEAGMREQCVLSEEQIRKKKIRKQQQESQSQSQSPVGPQGSSSSASGPGASPGGSEAGSQGSGEGEGVQLTAAQELMIQQLVAAQLQCNKRSFSDQPKVTPWPLGADPQSRDARQQRFAHFTELAIISVQEIVDFAKQVPGFLQLGREDQIALLKASTIEIMLLETARRYNHETECITFLKDFTYSKDDFHRAGLQVEFINPIFEFSRAMRRLGLDDAEYALLIAINIFSADRPNVQEPGRVEALQQPYVEALLSYTRIKRPQDQLRFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
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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 H
>
Nuclear hormone receptor subfamily 1 group H member 3
Function
Nuclear receptor that exhibits a ligand-dependent transcriptional activation activity (PubMed:25661920). Binds preferentially to double-stranded oligonucleotide direct repeats having the consensus half-site sequence 5'-AGGTCA-3' and 4-nt spacing (DR-4). Regulates cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8; DLDLR and LRP8. Interplays functionally with RORA for the regulation of genes involved in liver metabolism (By similarity). Induces LPCAT3-dependent phospholipid remodeling in endoplasmic reticulum (ER) membranes of hepatocytes, driving SREBF1 processing and lipogenesis (By similarity). Via LPCAT3, triggers the incorporation of arachidonate into phosphatidylcholines of ER membranes, increasing membrane dynamics and enabling triacylglycerols transfer to nascent very low-density lipoprotein (VLDL) particles (By similarity). Via LPCAT3 also counteracts lipid-induced ER stress response and inflammation, likely by modulating SRC kinase membrane compartmentalization and limiting the synthesis of lipid inflammatory mediators (By similarity). Plays an anti-inflammatory role during the hepatic acute phase response by acting as a corepressor: inhibits the hepatic acute phase response by preventing dissociation of the N-Cor corepressor complex (PubMed:20159957).
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Uniprot ID
Primary ID:
P55055

Secondarily ID:
A8K490
B4DNM6
E7EWA6
Q12970
Q5I0Y1
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Ensembl ID
ENSG00000131408
HGNC ID
HGNC:7965
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: CL000011 , CHO
Compound ID Compound Name Compound Formula
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
 1
1
EC50 = 16 nM
   TI
   LI
   LO
   TS
CP0394759
2-[4-({[3-(3-benzyl-8-chloroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
   Show/Hide
C31H25ClN2O2
 2
1
EC50 = 23 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0510893
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
   Show/Hide
C32H23F3N2O3
 2
1
EC50 = 29 nM
   TI
   LI
   LO
   TS
2
IC50 = 2.4 nM
   TI
   LI
   LO
   TS
CP0244920
biarylether alcohol quinoline, 5b
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C32H26F3NO2
 1
1
EC50 = 31 nM
   TI
   LI
   LO
   TS
CP0221684
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
   Show/Hide
C32H25F3N2O2
 2
1
EC50 = 33 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.9 nM
   TI
   LI
   LO
   TS
CP0394755
2-[4-({[3-(3-benzoyl-8-chloroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C31H23ClN2O3
 2
1
EC50 = 39 nM
   TI
   LI
   LO
   TS
2
IC50 = 2.7 nM
   TI
   LI
   LO
   TS
CP0394761
2-{4-[({3-[3-phenyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C31H23F3N2O2
 2
1
EC50 = 44 nM
   TI
   LI
   LO
   TS
2
IC50 = 3.7 nM
   TI
   LI
   LO
   TS
CP0434065
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}propanoic acid
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C33H25F3N2O3
 2
1
EC50 = 58 nM
   TI
   LI
   LO
   TS
2
IC50 = 2.6 nM
   TI
   LI
   LO
   TS
CP0437270
2-[4-({[3-(3-benzoyl-8-methylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C32H26N2O3
 2
1
EC50 = 61 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.5 nM
   TI
   LI
   LO
   TS
CP0203734
2-(4-{3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid
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C32H24F3NO3
 1
1
EC50 = 71 nM
   TI
   LI
   LO
   TS
CP0431994
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2-methylpropanoic acid
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C34H27F3N2O3
 2
1
EC50 = 78 nM
   TI
   LI
   LO
   TS
2
IC50 = 3.8 nM
   TI
   LI
   LO
   TS
CP0431991
2-[4-({[3-(3-benzyl-8-methylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C32H28N2O2
 2
1
EC50 = 90 nM
   TI
   LI
   LO
   TS
2
IC50 = 5 nM
   TI
   LI
   LO
   TS
CP0530681
2-{4-[({3-[3-methyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C26H21F3N2O2
 2
1
EC50 = 100 nM
   TI
   LI
   LO
   TS
2
IC50 = 4.3 nM
   TI
   LI
   LO
   TS
CP0180321
biarylether alcohol quinoline, 5i
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C25H22ClNO2
 1
1
EC50 = 108 nM
   TI
   LI
   LO
   TS
CP0051600
2-(2-chloro-4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
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C23H24ClF3N2O4
 1
1
EC50 = 124 nM
   TI
   LI
   LO
   TS
CP0099162
2-(2-oxo-1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)indolin-5-yl)acetic acid
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C24H23F3N2O5
 1
1
EC50 = 140 nM
   TI
   LI
   LO
   TS
CP0434066
2-{3-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C32H23F3N2O3
 2
1
EC50 = 141 nM
   TI
   LI
   LO
   TS
2
IC50 = 6 nM
   TI
   LI
   LO
   TS
CP0221685
2-(4-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid
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C32H22F3NO4
 1
1
EC50 = 143 nM
   TI
   LI
   LO
   TS
CP0154694
2-(5-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrazin-2-yl)acetic acid
   Show/Hide
C21H23F3N4O4
 1
1
EC50 = 150 nM
   TI
   LI
   LO
   TS
CP0221704
4-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
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C31H20F3NO4
 1
1
EC50 = 186 nM
   TI
   LI
   LO
   TS
CP0106854
biarylether alcohol quinoline, 5c
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C29H20F3NO2
 1
1
EC50 = 210 nM
   TI
   LI
   LO
   TS
CP0353477
biarylether alcohol quinoline, 5f
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C24H18F3NO2
 1
1
EC50 = 233 nM
   TI
   LI
   LO
   TS
CP0855521
5-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl] benzylidene}-2-thioxo-1,3-thiazolidin-4-one
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C34H22F3N3O2S2
 2
1
EC50 = 286 nM
   TI
   LI
   LO
   TS
2
IC50 = 310 nM
   TI
   LI
   LO
   TS
CP0283095
Quinoline 11
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C32H22F3NO4
 1
1
EC50 = 296 nM
   TI
   LI
   LO
   TS
CP0200289
2-(2-methyl-4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
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C24H27F3N2O4
 1
1
EC50 = 303 nM
   TI
   LI
   LO
   TS
CP0425193
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetamide
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C32H24F3N3O2
 2
1
EC50 = 316 nM
   TI
   LI
   LO
   TS
2
IC50 = 1.4 nM
   TI
   LI
   LO
   TS
CP0099161
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
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C23H25F3N2O4
 1
1
EC50 = 360 nM
   TI
   LI
   LO
   TS
CP0425194
4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]benzoic acid
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C31H21F3N2O3
 2
1
EC50 = 365 nM
   TI
   LI
   LO
   TS
2
IC50 = 138 nM
   TI
   LI
   LO
   TS
CP0436384
(5Z)-5-({4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}methylidene)-1,3-thiazolidine-2,4-dione
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C34H22F3N3O3S
 2
1
EC50 = 369 nM
   TI
   LI
   LO
   TS
2
IC50 = 276 nM
   TI
   LI
   LO
   TS
CP0166835
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}(methyl)amino)methyl]phenyl}acetic acid
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C33H27F3N2O2
 1
1
EC50 = 374 nM
   TI
   LI
   LO
   TS
CP0277299
biarylether alcohol quinoline, 9b
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C29H20F3NO2
 1
1
EC50 = 406 nM
   TI
   LI
   LO
   TS
CP0006936
2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-[2,2-di(phenyl)ethyl]amino]propoxy]phenyl]acetic acid
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C33H31ClF3NO3
 1
1
EC50 = 410 nM
   TI
   LI
   LO
   TS
CP0434059
2-{4-[({3-[3-cyano-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
   Show/Hide
C26H18F3N3O2
 2
1
EC50 = 450 nM
   TI
   LI
   LO
   TS
2
IC50 = 33.8 nM
   TI
   LI
   LO
   TS
CP0179493
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)acetic acid
   Show/Hide
C24H23F3N2O4
 1
1
EC50 = 450 nM
   TI
   LI
   LO
   TS
CP0051604
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrimidin-5-yl)acetic acid
   Show/Hide
C21H23F3N4O4
 1
1
EC50 = 470 nM
   TI
   LI
   LO
   TS
CP0171368
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indazol-5-yl)acetic acid
   Show/Hide
C23H22F3N3O4
 1
1
EC50 = 580 nM
   TI
   LI
   LO
   TS
CP0069744
biarylether methoxy quinoline, 9a
   Show/Hide
C30H22F3NO2
 1
1
EC50 = 612 nM
   TI
   LI
   LO
   TS
CP0341708
biarylether alcohol quinoline, 5d
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C29H20F3NO2
 1
1
EC50 = 646 nM
   TI
   LI
   LO
   TS
CP0051591
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)thiazol-5-yl)acetic acid
   Show/Hide
C20H22F3N3O4S
 1
1
EC50 = 650 nM
   TI
   LI
   LO
   TS
CP0434062
2-[4-({[3-(3-benzoyl-8-fluoroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
   Show/Hide
C31H23FN2O3
 2
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
2
IC50 = 17 nM
   TI
   LI
   LO
   TS
CP0328071
3-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)propanoic acid
   Show/Hide
C25H25F3N2O4
 1
1
EC50 = 700 nM
   TI
   LI
   LO
   TS
CP0525916
3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]-N-benzylaniline
   Show/Hide
C30H21F3N2O
 2
1
EC50 = 770 nM
   TI
   LI
   LO
   TS
2
IC50 = 45 nM
   TI
   LI
   LO
   TS
CP0439549
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}ethan-1-ol
   Show/Hide
C32H25F3N2O2
 2
1
EC50 = 795 nM
   TI
   LI
   LO
   TS
2
IC50 = 5.4 nM
   TI
   LI
   LO
   TS
CP0394758
2-(4-{[(3-{3-[hydroxy(phenyl)methyl]-8-(trifluoromethyl)quinolin-4-yl}phenyl)amino]methyl}phenyl)acetic acid
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C32H25F3N2O3
 2
1
EC50 = 812 nM
   TI
   LI
   LO
   TS
2
IC50 = 56.4 nM
   TI
   LI
   LO
   TS
CP0281088
BMC171663 Compound 4a
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C31H22F3NO3
 1
1
EC50 = 895 nM
   TI
   LI
   LO
   TS
CP0106853
biarylether alcohol quinoline, 5h
   Show/Hide
C23H18ClNO2
 1
1
EC50 = 938 nM
   TI
   LI
   LO
   TS
CP0225856
biarylether alcohol quinoline, 5e
   Show/Hide
C28H20ClNO2
 1
1
EC50 = 1010 nM
   TI
   LI
   LO
   TS
CP0069743
biarylether alcohol quinoline, 5a
   Show/Hide
C30H22F3NO2
 1
1
EC50 = 1030 nM
   TI
   LI
   LO
   TS
CP0394791
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenoxy}acetic acid
   Show/Hide
C32H23F3N2O4
 2
1
EC50 = 1271 nM
   TI
   LI
   LO
   TS
2
IC50 = 12 nM
   TI
   LI
   LO
   TS
CP0200285
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)-2-(trifluoromethyl)phenyl)acetic acid
   Show/Hide
C24H24F6N2O4
 1
1
EC50 = 1300 nM
   TI
   LI
   LO
   TS
CP0225855
biarylether alcohol quinoline, 5g
   Show/Hide
C24H18F3NO2
 1
1
EC50 = 1370 nM
   TI
   LI
   LO
   TS
CP0203736
3-benzoyl-4-phenyl-8-(trifluoromethyl)quinoline
   Show/Hide
C23H14F3NO
 1
1
EC50 = 1400 nM
   TI
   LI
   LO
   TS
CP0283093
4-{4-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
   Show/Hide
C31H20F3NO4
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0283094
3-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
   Show/Hide
C31H20F3NO4
 1
1
EC50 = 1500 nM
   TI
   LI
   LO
   TS
CP0394756
2-[4-({[3-(3-benzoylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
   Show/Hide
C31H24N2O3
 2
1
EC50 = 1650 nM
   TI
   LI
   LO
   TS
2
IC50 = 154 nM
   TI
   LI
   LO
   TS
CP0216283
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-benzo[d][1,2,3]triazol-5-yl)acetic acid
   Show/Hide
C22H21F3N4O4
 1
1
EC50 = 1700 nM
   TI
   LI
   LO
   TS
CP0240364
3-methyl quinoline, 8d
   Show/Hide
C24H18ClNO3
 1
1
EC50 = 1810 nM
   TI
   LI
   LO
   TS
CP0510891
methyl alcohol analogue,39
   Show/Hide
C31H23F3N2O2
 2
1
EC50 = 2304 nM
   TI
   LI
   LO
   TS
2
IC50 = 12.8 nM
   TI
   LI
   LO
   TS
CP0436387
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2,2-difluoroacetic acid
   Show/Hide
C32H21F5N2O3
 2
1
EC50 = 2395 nM
   TI
   LI
   LO
   TS
2
IC50 = 7.8 nM
   TI
   LI
   LO
   TS
CP0099133
1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indole-5-carboxylic acid
   Show/Hide
C23H21F3N2O4
 1
1
EC50 = 2800 nM
   TI
   LI
   LO
   TS
CP0069745
3-methyl quinoline, 8b
   Show/Hide
C25H18F3NO3
 1
1
EC50 = 3400 nM
   TI
   LI
   LO
   TS
CP0156187
2-(3-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
   Show/Hide
C23H25F3N2O4
 1
1
EC50 = 3500 nM
   TI
   LI
   LO
   TS
CP0394792
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2-hydroxyacetic acid
   Show/Hide
C32H23F3N2O4
 2
1
EC50 = 4003 nM
   TI
   LI
   LO
   TS
2
IC50 = 8.5 nM
   TI
   LI
   LO
   TS
CP0051589
2-oxo-1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)indoline-5-carboxylic acid
   Show/Hide
C23H21F3N2O5
 1
1
EC50 = 4400 nM
   TI
   LI
   LO
   TS
CP0190669
4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)benzoic acid
   Show/Hide
C22H23F3N2O4
 1
1
EC50 = 5100 nM
   TI
   LI
   LO
   TS
CP0079923
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid
   Show/Hide
C22H21ClF3NO4S
 1
1
EC50 = 7300 nM
   TI
   LI
   LO
   TS
CP0051606
2-(4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylamino)phenyl)acetic acid
   Show/Hide
C22H23F3N2O4
 1
1
EC50 = 7700 nM
   TI
   LI
   LO
   TS
CP0099163
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-benzo[d]imidazol-5-yl)acetic acid
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C23H22F3N3O4
 1
1
EC50 = 8600 nM
   TI
   LI
   LO
   TS
CP0156189
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propoxy)phenyl)acetic acid
   Show/Hide
C22H21ClF3NO5
 1
1
EC50 = 9700 nM
   TI
   LI
   LO
   TS
CP0437268
2-{4-[({3-[3-carbamoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
   Show/Hide
C26H20F3N3O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
CP0522252
(2E)-3-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}prop-2-enoic acid
   Show/Hide
C33H23F3N2O3
 1
1
IC50 > 10000 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0173378
(4aR,9S)-6-Hydroxy-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carboxylic acid ((1S,4aS,10aR)-6-hydroxy-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carbonyl)-amide
   Show/Hide
C34H43NO4
 2
1 EC50 = 1 nM
2 IC50 = 1 nM
CP0132783
N-benzyl-N-[[5-[4-(hydroxymethyl)-3-methylsulfonylphenyl]thiophen-2-yl]methyl]-2-(trifluoromethyl)benzenesulfonamide
   Show/Hide
C27H24F3NO5S3
 3
1 EC50 = 1 nM
2 IC50 = 0.6 nM
3 Ki = 1.3 nM
CP0109649
2,6-dimethyl-13-methylcarbonyloxy-(2S)-tricyclo[8.4.0.02,7]tetradeca-1(10),11,13-triene-6-carboxylic 2,6-dimethyl-13-methylcarbonyloxy-(2S,6S,7R)-tricyclo[8.4.0.02,7]tetradeca-1(14),10,12-triene-6-carboxylic anhydride
   Show/Hide
C38H46O7
 2
1 EC50 = 2 nM
2 IC50 = 2 nM
CP0006936
2-[3-[3-[[2-chloro-3-(trifluoromethyl)phenyl]methyl-[2,2-di(phenyl)ethyl]amino]propoxy]phenyl]acetic acid
   Show/Hide
C33H31ClF3NO3
 10
1 EC50 = 4 nM
2 EC50 = 5 nM
3 EC50 = 20 nM
4 EC50 = 40 nM
5 EC50 = 78 nM
6 EC50 = 390 nM
7 EC50 = 400 nM
8 IC50 = 7.943 nM
9 IC50 = 12 nM
10 IC50 = 30 nM
CP0003740
N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-(2,2,2-trifluoroethyl)benzenesulfonamide
   Show/Hide
C17H12F9NO3S
 16
1 EC50 = 8 nM
2 EC50 = 10 nM
3 EC50 = 30 nM
4 EC50 = 50 nM
5 EC50 = 60 nM
6 EC50 = 102.6 nM
7 EC50 = 400 nM
8 IC50 = 9 nM
9 IC50 = 10 nM
10 IC50 = 13 nM
11 IC50 = 19.95 nM
12 IC50 = 30 nM
13 IC50 = 70 nM
14 IC50 = 100 nM
15 Kd = 103 nM
16 Ki = 17 nM
CP0186266
N-ethyl-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]benzenesulfonamide
   Show/Hide
C17H15F6NO3S
 1
1 EC50 = 10 nM
CP0051425
(2R)-5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[(2,4,6-trifluorophenyl)carbonyl]-2,3-dihydro-1,3,4-thiadiazole
   Show/Hide
C23H16ClF3N2O3S
 1
1 EC50 = 63 nM
CP0195485
5-(4-chlorophenyl)-2-(2,3-dimethoxyphenyl)-3-[(2,4,6-trifluorophenyl)carbonyl]-2,3-dihydro-1,3,4-thiadiazole
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C23H16ClF3N2O3S
 1
1 EC50 = 98 nM
CP0285585
(1S,2R,5S,10S,11S,14R,15R)-14-[(2R)-4-[(2S)-3,3-dimethyloxiran-2-yl]butan-2-yl]-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-7-en-5-ol
   Show/Hide
C27H44O2
 2
1 EC50 = 286 nM
2 EC50 > 20000 nM
CP0214923
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-prop-2-enylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C19H17Cl2F3N2O4S
 1
1 EC50 = 580 nM
CP0198576
(S)-N-(2-chloro-4-(2-chloro-N-methylphenylsulfonamido)phenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C17H15Cl2F3N2O4S
 1
1 EC50 = 626 nM
CP0259297
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-ethylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C18H17Cl2F3N2O4S
 1
1 EC50 = 790 nM
CP0344790
N-[4-[benzyl-(2-chlorophenyl)sulfonylamino]-2-chlorophenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C23H19Cl2F3N2O4S
 1
1 EC50 = 880 nM
CP0285586
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-(cyclopropylmethyl)amino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C20H19Cl2F3N2O4S
 1
1 EC50 = 940 nM
CP0435156
(S)-N-(2-chloro-4-(N,4-dimethylphenylsulfonamido)phenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C18H18ClF3N2O4S
 1
1 EC50 = 1500 nM
CP0259296
(S)-N-(2-chloro-4-(N-methylphenylsulfonamido)phenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C17H16ClF3N2O4S
 1
1 EC50 = 1900 nM
CP0259299
methyl 4-[[3-chloro-4-[(3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl)amino]phenyl]-methylsulfamoyl]benzoate
   Show/Hide
C19H18ClF3N2O6S
 1
1 EC50 = 2320 nM
CP0371199
N-[2-chloro-4-[(4-cyanophenyl)sulfonyl-methylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
   Show/Hide
C18H15ClF3N3O4S
 1
1 EC50 = 2600 nM
CP0198578
methyl 3-[4-[[3-chloro-4-[(3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl)amino]phenyl]-methylsulfamoyl]phenyl]propanoate
   Show/Hide
C21H22ClF3N2O6S
 1
1 EC50 = 3500 nM
CP0059382
(4S,4aR)-6-Hydroxy-4a-methyl-1-(S)-methyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carboxylic acid adamantan-2-ylamide
   Show/Hide
C27H37NO2
 2
1 EC50 > 50000 nM
2 IC50 = 100 nM
CP0214925
4-(N-(3-chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenyl)-N-methylsulfamoyl)benzoic acid
   Show/Hide
C18H16ClF3N2O6S
 1
1 EC50 > 100000 nM
CP0262779
3-(4-(N-(3-chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenyl)-N-methylsulfamoyl)phenyl)propanoic acid
   Show/Hide
C20H20ClF3N2O6S
 1
1 EC50 > 100000 nM
CP0224486
3-benzyl-4-(3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C30H22F3NO2S
 1
1 IC50 = 1.5 nM
CP0107209
4-(4'-fluoro-3'-(methylsulfonyl)biphenyl-3-yl)-3-methyl-8-(trifluoromethyl)quinoline
   Show/Hide
C24H17F4NO2S
 1
1 IC50 = 1.7 nM
CP0294748
3-methyl-4-(3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C24H18F3NO2S
 1
1 IC50 = 1.8 nM
CP0221684
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
   Show/Hide
C32H25F3N2O2
 1
1 IC50 = 1.9 nM
CP0203734
2-(4-{3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid
   Show/Hide
C32H24F3NO3
 1
1 IC50 = 2.1 nM
CP0353477
biarylether alcohol quinoline, 5f
   Show/Hide
C24H18F3NO2
 2
1 IC50 = 2.1 nM
2 IC50 = 12 nM
CP0128474
3-methyl-4-(3-(3-(methylsulfonyl)phenoxy)phenyl)-8-(trifluoromethyl)quinoline
   Show/Hide
C24H18F3NO3S
 1
1 IC50 = 2.4 nM
CP0274549
3-ethyl-4-(3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C25H20F3NO2S
 1
1 IC50 = 2.4 nM
CP0180321
biarylether alcohol quinoline, 5i
   Show/Hide
C25H22ClNO2
 1
1 IC50 = 2.5 nM
CP0038715
4-(4'-fluoro-3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C23H15F4NO2S
 1
1 IC50 = 2.6 nM
CP0290643
3-methyl-4-(4'-methyl-3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C25H20F3NO2S
 1
1 IC50 = 3.2 nM
CP0244920
biarylether alcohol quinoline, 5b
   Show/Hide
C32H26F3NO2
 1
1 IC50 = 3.3 nM
CP0308202
4-(2',4'-difluoro-5'-(methylsulfonyl)biphenyl-3-yl)-3-methyl-8-(trifluoromethyl)quinoline
   Show/Hide
C24H16F5NO2S
 1
1 IC50 = 3.3 nM
CP0308201
4-(3'-(methylsulfonyl)biphenyl-3-yl)-3-propyl-8-(trifluoromethyl)quinoline
   Show/Hide
C26H22F3NO2S
 1
1 IC50 = 3.8 nM
CP0294514
N-[(2-chloro-4-fluorophenyl)methyl]-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
   Show/Hide
C27H23ClFNO4S2
 1
1 IC50 = 3.981 nM
CP0158348
3-isopropyl-4-(3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C26H22F3NO2S
 1
1 IC50 = 4.1 nM
CP0158347
4-(3'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C23H16F3NO2S
 1
1 IC50 = 4.4 nM
CP0107210
4-(2',4'-difluoro-5'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C23H14F5NO2S
 1
1 IC50 = 4.9 nM
CP0221685
2-(4-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid
   Show/Hide
C32H22F3NO4
 1
1 IC50 = 5 nM
CP0287908
2-(5-(3-(3-benzyl-8-(trifluoromethyl)quinolin-4-yl)benzylamino)naphthalen-1-yl)acetic acid
   Show/Hide
C36H27F3N2O2
 1
1 IC50 = 5 nM
CP0191162
N-[(2-chloro-6-fluorophenyl)methyl]-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
   Show/Hide
C27H23ClFNO4S2
 1
1 IC50 = 5.012 nM
CP0107208
4-(3'-(ethylsulfonyl)biphenyl-3-yl)-3-methyl-8-(trifluoromethyl)quinoline
   Show/Hide
C25H20F3NO2S
 1
1 IC50 = 5.2 nM
CP0234158
2-benzyl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
   Show/Hide
C28H21F3N2O3S
 1
1 IC50 = 5.9 nM
CP0328071
3-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)propanoic acid
   Show/Hide
C25H25F3N2O4
 1
1 IC50 = 6 nM
CP0294099
N-[(2-chloro-6-fluorophenyl)methyl]-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]cyclopropanesulfonamide
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C24H23ClFNO4S2
 1
1 IC50 = 6.31 nM
CP0225856
biarylether alcohol quinoline, 5e
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C28H20ClNO2
 1
1 IC50 = 8.3 nM
CP0239960
3-[[3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl]methyl]-1,3-thiazolidine
   Show/Hide
C25H22F3N3O3S2
 1
1 IC50 = 9 nM
CP0256824
2-(5-((3-(3-methyl-8-(trifluoromethyl)quinolin-4-yl)phenyl)methylamino)naphthalen-1-yl)acetic acid
   Show/Hide
C30H23F3N2O2
 1
1 IC50 = 10 nM
CP0051600
2-(2-chloro-4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
   Show/Hide
C23H24ClF3N2O4
 1
1 IC50 = 10 nM
CP0341708
biarylether alcohol quinoline, 5d
   Show/Hide
C29H20F3NO2
 1
1 IC50 = 10 nM
CP0191161
N-[(2-chloro-6-fluorophenyl)methyl]-1-methyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]imidazole-4-sulfonamide
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C25H23ClFN3O4S2
 1
1 IC50 = 10 nM
CP0069743
biarylether alcohol quinoline, 5a
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C30H22F3NO2
 1
1 IC50 = 11.7 nM
CP0106853
biarylether alcohol quinoline, 5h
   Show/Hide
C23H18ClNO2
 1
1 IC50 = 12 nM
CP0301423
N-[(2-chloro-6-fluorophenyl)methyl]-2-methyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
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C28H25ClFNO4S2
 1
1 IC50 = 12.59 nM
CP0099162
2-(2-oxo-1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)indolin-5-yl)acetic acid
   Show/Hide
C24H23F3N2O5
 1
1 IC50 = 13 nM
CP0106854
biarylether alcohol quinoline, 5c
   Show/Hide
C29H20F3NO2
 1
1 IC50 = 14 nM
CP0345734
2-(5-((3-(8-(trifluoromethyl)quinolin-4-yl)phenyl)methylamino)naphthalen-1-yl)acetic acid
   Show/Hide
C29H21F3N2O2
 1
1 IC50 = 15 nM
CP0244943
N-[(2-chloro-6-fluorophenyl)methyl]-2,4,6-trimethyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
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C30H29ClFNO4S2
 1
1 IC50 = 15.85 nM
CP0179493
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)acetic acid
   Show/Hide
C24H23F3N2O4
 1
1 IC50 = 16 nM
CP0200285
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)-2-(trifluoromethyl)phenyl)acetic acid
   Show/Hide
C24H24F6N2O4
 1
1 IC50 = 18 nM
CP0240192
3-Ethyl-2-[3'-(methylsulfonyl)biphenyl-4-yl]-5-(trifluoromethyl)-quinoxaline
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C24H19F3N2O2S
 1
1 IC50 = 18 nM
CP0110590
N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]-N-methylbenzenesulfonamide
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C16H13F6NO3S
 1
1 IC50 = 20 nM
CP0099161
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
   Show/Hide
C23H25F3N2O4
 1
1 IC50 = 25 nM
CP0200289
2-(2-methyl-4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
   Show/Hide
C24H27F3N2O4
 1
1 IC50 = 26 nM
CP0079923
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid
   Show/Hide
C22H21ClF3NO4S
 1
1 IC50 = 28 nM
CP0277299
biarylether alcohol quinoline, 9b
   Show/Hide
C29H20F3NO2
 1
1 IC50 = 28 nM
CP0225855
biarylether alcohol quinoline, 5g
   Show/Hide
C24H18F3NO2
 1
1 IC50 = 31 nM
CP0115565
4-(3'-(ethylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C24H18F3NO2S
 1
1 IC50 = 33 nM
CP0096814
5-Chloro-3-methyl-2-[3'-(methylsulfonyl)biphenyl-4-yl]quinoxaline
   Show/Hide
C22H17ClN2O2S
 1
1 IC50 = 34 nM
CP0154694
2-(5-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrazin-2-yl)acetic acid
   Show/Hide
C21H23F3N4O4
 1
1 IC50 = 40 nM
CP0281088
BMC171663 Compound 4a
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C31H22F3NO3
 1
1 IC50 = 53 nM
CP0128009
3-Methyl-2-[3'-(methylsulfonyl)biphenyl-4-yl]-5-(trifluoromethyl)-quinoxaline
   Show/Hide
C23H17F3N2O2S
 1
1 IC50 = 53 nM
CP0051604
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrimidin-5-yl)acetic acid
   Show/Hide
C21H23F3N4O4
 1
1 IC50 = 55 nM
CP0128007
4-(3-(3-chloro-5-(methylsulfonyl)phenoxy)phenyl)-8-(trifluoromethyl)quinoline-3-carboxamide
   Show/Hide
C24H16ClF3N2O4S
 1
1 IC50 = 61 nM
CP0156189
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propoxy)phenyl)acetic acid
   Show/Hide
C22H21ClF3NO5
 1
1 IC50 = 65 nM
CP0221704
4-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
   Show/Hide
C31H20F3NO4
 1
1 IC50 = 67 nM
CP0268795
3-(3-(8-chloro-2-isopropylimidazo[1,2-a]pyridin-3-yl)phenoxy)-N-(4-methoxybenzyl)-N-methylbenzenesulfonamide
   Show/Hide
C31H30ClN3O4S
 1
1 IC50 = 71 nM
CP0308975
N-[(2-chloro-4-fluorophenyl)methyl]-2,4,6-trimethyl-N-[[4-(3-methylsulfonylphenyl)phenyl]methyl]benzenesulfonamide
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C30H29ClFNO4S2
 1
1 IC50 = 79.43 nM
CP0171368
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indazol-5-yl)acetic acid
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C23H22F3N3O4
 1
1 IC50 = 87 nM
CP0051606
2-(4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylamino)phenyl)acetic acid
   Show/Hide
C22H23F3N2O4
 1
1 IC50 = 89 nM
CP0268792
3-[3-(3-methylsulfonylphenoxy)phenyl]-2-phenyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C27H19F3N2O3S
 1
1 IC50 = 91 nM
CP0156187
2-(3-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
   Show/Hide
C23H25F3N2O4
 1
1 IC50 = 98 nM
CP0051591
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)thiazol-5-yl)acetic acid
   Show/Hide
C20H22F3N3O4S
 1
1 IC50 = 100 nM
CP0203736
3-benzoyl-4-phenyl-8-(trifluoromethyl)quinoline
   Show/Hide
C23H14F3NO
 1
1 IC50 = 107 nM
CP0224483
3-benzyl-4-(4'-(methylsulfonyl)biphenyl-3-yl)-8-(trifluoromethyl)quinoline
   Show/Hide
C30H22F3NO2S
 1
1 IC50 = 109 nM
CP0095700
2-methyl-1-(3-(3-(methylsulfonyl)phenoxy)phenyl)-4-(trifluoromethyl)-1H-benzo[d]imidazole
   Show/Hide
C22H17F3N2O3S
 2
1 IC50 = 111 nM
2 IC50 = 128 nM
CP0166835
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}(methyl)amino)methyl]phenyl}acetic acid
   Show/Hide
C33H27F3N2O2
 1
1 IC50 = 115 nM
CP0353476
biarylether amide quinoline, 4i
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C24H19ClN2O2
 1
1 IC50 = 125 nM
CP0255636
3-[3-(3-methylsulfonylphenoxy)phenyl]-2-propan-2-yl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
   Show/Hide
C24H21F3N2O3S
 1
1 IC50 = 137 nM
CP0061172
N-(cyclopentylmethyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C29H28F3NO5S2
 1
1 IC50 = 150 nM
CP0190669
4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)benzoic acid
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C22H23F3N2O4
 1
1 IC50 = 190 nM
CP0099133
1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indole-5-carboxylic acid
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C23H21F3N2O4
 1
1 IC50 = 199 nM
CP0226706
2-ethyl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C23H19F3N2O3S
 1
1 IC50 = 217 nM
CP0268793
2-tert-butyl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C25H23F3N2O3S
 1
1 IC50 = 222 nM
CP0240364
3-methyl quinoline, 8d
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C24H18ClNO3
 1
1 IC50 = 231 nM
CP0144261
3-(3-(8-chloro-2-isopropylimidazo[1,2-a]pyridin-3-yl)phenoxy)-N-methylbenzenesulfonamide
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C23H22ClN3O3S
 1
1 IC50 = 239 nM
CP0069744
biarylether methoxy quinoline, 9a
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C30H22F3NO2
 1
1 IC50 = 287 nM
CP0127474
3-cyano-N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-4-phenylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C27H23F3N2O3S
 1
1 IC50 = 300 nM
CP0314144
N-(cyclobutylmethyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C28H26F3NO5S2
 1
1 IC50 = 300 nM
CP0144282
8-chloro-2-isopropyl-3-(3-(3-(methylsulfonyl)phenoxy)phenyl)imidazo[1,2-a]pyridine
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C23H21ClN2O3S
 1
1 IC50 = 304 nM
CP0216283
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-benzo[d][1,2,3]triazol-5-yl)acetic acid
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C22H21F3N4O4
 1
1 IC50 = 350 nM
CP0144260
2-imidazol-1-yl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C24H17F3N4O3S
 1
1 IC50 = 365 nM
CP0147563
3-cyano-N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(3-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C28H25F3N2O5S2
 1
1 IC50 = 400 nM
CP0314138
N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-4-pyridin-3-ylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C25H23F3N2O3S
 1
1 IC50 = 400 nM
CP0099163
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-benzo[d]imidazol-5-yl)acetic acid
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C23H22F3N3O4
 1
1 IC50 = 410 nM
CP0069745
3-methyl quinoline, 8b
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C25H18F3NO3
 1
1 IC50 = 435 nM
CP0059780
N-(2-methylpropyl)-N-[[5-(3-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 1
1 IC50 = 450 nM
CP0192413
N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]-N-(3,3,3-trifluoropropyl)benzenesulfonamide
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C26H21F6NO5S2
 1
1 IC50 = 500 nM
CP0236919
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-[3-(trifluoromethyl)phenyl]but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H23F6NO3S
 1
1 IC50 = 500 nM
CP0272623
4-[3-[4-[(3-cyanophenyl)sulfonyl-(2-methylpropyl)amino]phenyl]-4,4,4-trifluoro-3-hydroxybut-1-ynyl]benzoic acid
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C28H23F3N2O5S
 1
1 IC50 = 500 nM
CP0314143
N-(cyclopropylmethyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H24F3NO5S2
 1
1 IC50 = 500 nM
CP0144257
3-(3-(3-(ethylsulfonyl)phenoxy)phenyl)-2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C23H19F3N2O3S
 1
1 IC50 = 561 nM
CP0127413
3-cyano-N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C28H25F3N2O5S2
 1
1 IC50 = 600 nM
CP0147562
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(3-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H26F3NO5S2
 1
1 IC50 = 600 nM
CP0192410
N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-4-phenylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C26H24F3NO3S
 1
1 IC50 = 600 nM
CP0192411
N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-5-phenylpent-3-yn-2-yl)phenyl]benzenesulfonamide
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C27H26F3NO3S
 1
1 IC50 = 600 nM
CP0236921
3-cyano-N-[4-[4-(4-cyanophenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C28H22F3N3O3S
 1
1 IC50 = 600 nM
CP0272622
N-[4-[4-(4-chlorophenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-3-cyano-N-(2-methylpropyl)benzenesulfonamide
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C27H22ClF3N2O3S
 1
1 IC50 = 600 nM
CP0314140
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H26F3NO3S
 1
1 IC50 = 600 nM
CP0314141
N-[4-[4-(3-cyanophenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C27H23F3N2O3S
 1
1 IC50 = 600 nM
CP0314142
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H26F3NO5S2
 1
1 IC50 = 600 nM
CP0051589
2-oxo-1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)indoline-5-carboxylic acid
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C23H21F3N2O5
 1
1 IC50 = 700 nM
CP0147559
N-[4-[4-(4-ethoxyphenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C28H28F3NO4S
 1
1 IC50 = 700 nM
CP0314139
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methoxyphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H26F3NO4S
 1
1 IC50 = 700 nM
CP0191445
2-methyl-3-(3-(3-(methylsulfonyl)phenoxy)phenyl)-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C22H17F3N2O3S
 1
1 IC50 = 799 nM
CP0147315
N-[4-[4-(2,4-difluorophenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C26H22F5NO3S
 1
1 IC50 = 800 nM
CP0144311
3-(3-(3-(isopropylsulfonyl)phenoxy)phenyl)-2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C24H21F3N2O3S
 1
1 IC50 = 960 nM
CP0127414
N-(2,2,2-trifluoroethyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C25H19F6NO5S2
 1
1 IC50 = 1000 nM
CP0236920
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(3-methoxyphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H26F3NO4S
 1
1 IC50 = 1000 nM
CP0283094
3-{3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
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C31H20F3NO4
 1
1 IC50 = 1033 nM
CP0314135
N-(2,2,2-trifluoroethyl)-N-[4-[1,1,1-trifluoro-4-(4-fluorophenyl)-2-hydroxybut-3-yn-2-yl]phenyl]benzenesulfonamide
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C24H16F7NO3S
 1
1 IC50 = 1100 nM
CP0314136
N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-5,5-dimethylhex-3-yn-2-yl)phenyl]benzenesulfonamide
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C24H28F3NO3S
 1
1 IC50 = 1100 nM
CP0314137
N-[4-[4-(cyclohexen-1-yl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C26H28F3NO3S
 1
1 IC50 = 1100 nM
CP0157000
N-(2,2-dimethylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(4-methylsulfonylphenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C28H28F3NO5S2
 1
1 IC50 = 1200 nM
CP0281897
N-methyl-N-[4-(1,1,1-trifluoro-2-hydroxy-4-phenylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C23H18F3NO3S
 1
1 IC50 = 1400 nM
CP0281900
2,5-dichloro-N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-4-phenylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C26H22Cl2F3NO3S
 1
1 IC50 = 1400 nM
CP0165937
N-[4-[4-(1-ethylpyrazol-4-yl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C25H26F3N3O3S
 1
1 IC50 = 1700 nM
CP0061574
3-[3-[4-[benzenesulfonyl(2-methylpropyl)amino]phenyl]-4,4,4-trifluoro-3-hydroxybut-1-ynyl]benzoic acid
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C27H24F3NO5S
 1
1 IC50 = 1800 nM
CP0054652
2-[2-[(E)-2-(3,4-dimethoxyphenyl)ethenyl]phenyl]isoindole-1,3-dione
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C24H19NO4
 1
1 IC50 = 1800 nM
CP0156998
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-[4-(trifluoromethyl)phenyl]but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H23F6NO3S
 1
1 IC50 = 2500 nM
CP0283093
4-{4-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}benzoic acid
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C31H20F3NO4
 1
1 IC50 = 2738 nM
CP0156999
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(2-methyl-4-nitrophenyl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C27H25F3N2O5S
 1
1 IC50 = 2800 nM
CP0272621
N-[4-[4-(3,5-dimethyl-1,2-oxazol-4-yl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C25H25F3N2O4S
 1
1 IC50 = 3200 nM
CP0192412
N-[4-[4-(4-butylphenyl)-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-N-(2-methylpropyl)benzenesulfonamide
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C30H32F3NO3S
 1
1 IC50 = 3500 nM
CP0127512
N-(2-methylpropyl)-N-[4-(1,1,1-trifluoro-2-hydroxy-4-pyridin-2-ylbut-3-yn-2-yl)phenyl]benzenesulfonamide
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C25H23F3N2O3S
 1
1 IC50 = 3800 nM
CP0147557
N-[4-(1,1,1,5,5,5-hexafluoro-2-hydroxypent-3-yn-2-yl)phenyl]-N-methylbenzenesulfonamide
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C18H13F6NO3S
 1
1 IC50 = 4100 nM
CP0259528
3-cyano-N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-[4-(trifluoromethylsulfonyl)phenyl]but-3-yn-2-yl]phenyl]benzenesulfonamide
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C28H22F6N2O5S2
 1
1 IC50 = 4300 nM
CP0165936
N-(2-methylpropyl)-N-[4-[1,1,1-trifluoro-2-hydroxy-4-(3-methylimidazol-4-yl)but-3-yn-2-yl]phenyl]benzenesulfonamide
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C24H24F3N3O3S
 1
1 IC50 = 5100 nM
CP0283095
Quinoline 11
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C32H22F3NO4
 1
1 IC50 > 1000 nM
CP0144258
3-(3-(3-(2-methyl-8-(trifluoromethyl)imidazo[1,2-a]pyridin-3-yl)phenoxy)phenylsulfonyl)propan-1-ol
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C24H21F3N2O4S
 1
1 IC50 > 1000 nM
CP0144283
2-isopropyl-3-(3-(3-(methylsulfonyl)benzyloxy)phenyl)-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C25H23F3N2O3S
 1
1 IC50 > 1000 nM
CP0166339
2-ethyl-3-(3-(3-(methylsulfonyl)benzyl)phenyl)-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C24H21F3N2O2S
 1
1 IC50 > 1000 nM
CP0234122
3-[3-(3-methylsulfonylphenoxy)phenyl]-2-(piperidin-1-ylmethyl)-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C27H26F3N3O3S
 1
1 IC50 > 1000 nM
CP0271955
2-isopropyl-3-(3-(3-(methylsulfonyl)phenoxy)phenyl)imidazo[1,2-a]pyridine-8-carbonitrile
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C24H21N3O3S
 1
1 IC50 > 1000 nM
CP0236922
N-[4-[4-[4-(benzenesulfonyl)phenyl]-1,1,1-trifluoro-2-hydroxybut-3-yn-2-yl]phenyl]-3-cyano-N-(2-methylpropyl)benzenesulfonamide
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C33H27F3N2O5S2
 1
1 IC50 > 10000 nM
CP0132850
5-chloro-2-[(2R)-4-(4-fluoro-3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidine
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C19H21ClF4N4O2S
 1
1 Ki = 1 nM
CP0305129
2-[(2R)-4-(4-fluoro-3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidine
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C19H22F4N4O2S
 1
1 Ki = 1 nM
CP0055767
(6R)-5-(5-fluoro-6-methoxypyrimidin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C20H22FN5O3S
 1
1 Ki = 1 nM
CP0054911
[4-[(3R)-4-[5-(hydroxymethyl)-4-(trifluoromethyl)pyrimidin-2-yl]-3-propan-2-ylpiperazin-1-yl]-2-methylsulfonylphenyl]methanol
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C21H27F3N4O4S
 1
1 Ki = 3 nM
CP0399531
(6R)-2-(3-methylsulfonylphenyl)-5-[2-methyl-6-(trifluoromethyl)pyrimidin-4-yl]-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C21H22F3N5O2S
 1
1 Ki = 3 nM
CP0055084
2-[(2R)-4-(3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidine
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C19H23F3N4O2S
 1
1 Ki = 4 nM
CP0059897
(6R)-5-(6-methoxy-2-methylpyrimidin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C21H25N5O3S
 1
1 Ki = 4 nM
CP0091584
(6R)-6-tert-butyl-5-(2-methoxypyridin-4-yl)-2-(3-methylsulfonylphenyl)-4,6-dihydropyrrolo[3,4-c]pyrazole
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C22H26N4O3S
 1
1 Ki = 5 nM
CP0055573
(6R)-5-(2-methoxy-6-methylpyridin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C22H26N4O3S
 1
1 Ki = 6 nM
CP0055575
[4-[(6R)-5-[5-(hydroxymethyl)-4-(trifluoromethyl)pyrimidin-2-yl]-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazol-2-yl]-2-methylsulfonylphenyl]methanol
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C22H24F3N5O4S
 1
1 Ki = 6 nM
CP0134107
[2-[(6R)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl]-4-(trifluoromethyl)pyrimidin-5-yl]methanol
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C21H22F3N5O3S
 1
1 Ki = 6 nM
CP0046458
(6R)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-5-[4-(trifluoromethyl)pyrimidin-2-yl]-4,6-dihydropyrrolo[3,4-c]pyrazole
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C20H20F3N5O2S
 1
1 Ki = 7 nM
CP0211513
(6R)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-5-[6-(trifluoromethyl)pyrimidin-4-yl]-4,6-dihydropyrrolo[3,4-c]pyrazole
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C20H20F3N5O2S
 1
1 Ki = 7 nM
CP0132852
2-[2-[(2R)-4-(4-fluoro-3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidin-5-yl]propan-2-ol
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C22H28F4N4O3S
 1
1 Ki = 8 nM
CP0091127
[2-[(2R)-4-(4-fluoro-3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidin-5-yl]methanol
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C20H24F4N4O3S
 1
1 Ki = 9 nM
CP0059895
(6R)-5-(5-fluoro-2-methoxypyrimidin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C20H22FN5O3S
 1
1 Ki = 13 nM
CP0059896
(6R)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-5-[2-(trifluoromethyl)pyrimidin-4-yl]-4,6-dihydropyrrolo[3,4-c]pyrazole
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C20H20F3N5O2S
 1
1 Ki = 13 nM
CP0134055
(6R)-5-(2-methoxypyridin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C21H24N4O3S
 1
1 Ki = 13 nM
CP0134054
(6R)-5-(2-methoxy-6-methylpyrimidin-4-yl)-2-(3-methylsulfonylphenyl)-6-propan-2-yl-4,6-dihydropyrrolo[3,4-c]pyrazole
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C21H25N5O3S
 1
1 Ki = 17 nM
CP0132853
[4-[(3S)-4-[5-(hydroxymethyl)-4-(trifluoromethyl)pyrimidin-2-yl]-3-propan-2-ylpiperazin-1-yl]-2-methylsulfonylphenyl]methanol
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C21H27F3N4O4S
 1
1 Ki = 160 nM
CP0272352
tert-butyl (2'R,3R)-1-[3-[4-(hydroxymethyl)-3-methylsulfonylphenyl]phenyl]-2-oxo-2'-propan-2-ylspiro[indole-3,3'-pyrrolidine]-1'-carboxylate
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C33H38N2O6S
 1
1 Ki = 2300 nM
Clinical Information about the Protein
Target 1 ( Oxysterols receptor LXR-beta (NR1H2) )
Target Type Clinical trial Target
Disease 1 Target-related Disease  1
1 Major depressive disorder [ICD-11: 6A70.3]
Investigative Drug(s) 1 Investigative Drug  1
1 GW-3965 Investigative
Major depressive disorder