General Information of the Protein
Protein ID
PT01555
Protein Name
Oxysterols receptor LXR-alpha
Secondarily
Protein Name
Liver X receptor alpha
Nuclear receptor subfamily 1 group H member 3
Gene Name
NR1H3
Secondarily
Gene Name
LXRA
Sequence
MSLWLGAPVPDIPPDSAVELWKPGAQDASSQAQGGSSCILREEARMPHSAGGTAGVGLEAAEPTALLTRAEPPSEPTEIRPQKRKKGPAPKMLGNELCSVCGDKASGFHYNVLSCEGCKGFFRRSVIKGAHYICHSGGHCPMDTYMRRKCQECRLRKCRQAGMREECVLSEEQIRLKKLKRQEEEQAHATSLPPRASSPPQILPQLSPEQLGMIEKLVAAQQQCNRRSFSDRLRVTPWPMAPDPHSREARQQRFAHFTELAIVSVQEIVDFAKQLPGFLQLSREDQIALLKTSAIEVMLLETSRRYNPGSESITFLKDFSYNREDFAKAGLQVEFINPIFEFSRAMNELQLNDAEFALLIAISIFSADRPNVQDQLQVERLQHTYVEALHAYVSIHHPHDRLMFPRMLMKLVSLRTLSSVHSEQVFALRLQDKKLPPLLSEIWDVHE
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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:19481530, PubMed:25661920). Interaction with retinoic acid receptor (RXR) shifts RXR from its role as a silent DNA-binding partner to an active ligand-binding subunit in mediating retinoid responses through target genes defined by LXRES (By similarity). LXRES are DR4-type response elements characterized by direct repeats of two similar hexanuclotide half-sites spaced by four nucleotides (By similarity). Plays an important role in the regulation of cholesterol homeostasis, regulating cholesterol uptake through MYLIP-dependent ubiquitination of LDLR, VLDLR and LRP8 (PubMed:19481530). 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. 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).
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Uniprot ID
Primary ID:
Q13133

Secondarily ID:
A8K3J9
D3DQR1
Q8IW13
Q96H87
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Ensembl ID
ENSG00000025434
HGNC ID
HGNC:7966
Subcellular Location
Nucleus
Cytoplasm
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
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 = 170 nM
   TI
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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 = 180 nM
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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 = 450 nM
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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
EC50 = 480 nM
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CP0154694
2-(5-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrazin-2-yl)acetic acid
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C21H23F3N4O4
 1
1
EC50 = 540 nM
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CP0179493
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)acetic acid
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C24H23F3N2O4
 1
1
EC50 = 590 nM
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CP0051604
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrimidin-5-yl)acetic acid
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C21H23F3N4O4
 1
1
EC50 = 620 nM
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CP0328071
3-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)propanoic acid
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C25H25F3N2O4
 1
1
EC50 = 820 nM
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CP0051591
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)thiazol-5-yl)acetic acid
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C20H22F3N3O4S
 1
1
EC50 = 1100 nM
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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 = 1300 nM
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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
EC50 = 1900 nM
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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
EC50 = 2300 nM
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CP0156187
2-(3-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
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C23H25F3N2O4
 1
1
EC50 = 2600 nM
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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
EC50 = 3000 nM
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CP0200285
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)-2-(trifluoromethyl)phenyl)acetic acid
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C24H24F6N2O4
 1
1
EC50 = 3600 nM
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CP0099132
2-(6-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyridin-3-yl)acetic acid
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C22H24F3N3O4
 1
1
EC50 = 5000 nM
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CP0079923
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid
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C22H21ClF3NO4S
 1
1
EC50 = 5900 nM
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CP0190669
4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)benzoic acid
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C22H23F3N2O4
 1
1
EC50 = 6000 nM
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CP0051606
2-(4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylamino)phenyl)acetic acid
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C22H23F3N2O4
 1
1
EC50 = 8000 nM
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CP0394759
2-[4-({[3-(3-benzyl-8-chloroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C31H25ClN2O2
 1
1
IC50 = 5 nM
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CP0510893
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C32H23F3N2O3
 1
1
IC50 = 7 nM
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CP0221684
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C32H25F3N2O2
 1
1
IC50 = 7.6 nM
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CP0394761
2-{4-[({3-[3-phenyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C31H23F3N2O2
 1
1
IC50 = 8 nM
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CP0394755
2-[4-({[3-(3-benzoyl-8-chloroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C31H23ClN2O3
 1
1
IC50 = 9 nM
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CP0425193
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetamide
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C32H24F3N3O2
 1
1
IC50 = 11 nM
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CP0434065
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}propanoic acid
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C33H25F3N2O3
 1
1
IC50 = 15.2 nM
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CP0530681
2-{4-[({3-[3-methyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C26H21F3N2O2
 1
1
IC50 = 16 nM
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CP0431994
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2-methylpropanoic acid
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C34H27F3N2O3
 1
1
IC50 = 17.2 nM
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CP0437270
2-[4-({[3-(3-benzoyl-8-methylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C32H26N2O3
 1
1
IC50 = 18 nM
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CP0431991
2-[4-({[3-(3-benzyl-8-methylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C32H28N2O2
 1
1
IC50 = 21 nM
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CP0436387
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2,2-difluoroacetic acid
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C32H21F5N2O3
 1
1
IC50 = 30.2 nM
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CP0394792
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}-2-hydroxyacetic acid
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C32H23F3N2O4
 1
1
IC50 = 33.6 nM
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CP0434066
2-{3-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C32H23F3N2O3
 1
1
IC50 = 33.6 nM
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CP0439549
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}ethan-1-ol
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C32H25F3N2O2
 1
1
IC50 = 34 nM
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CP0394791
2-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenoxy}acetic acid
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C32H23F3N2O4
 1
1
IC50 = 63.9 nM
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CP0510891
methyl alcohol analogue,39
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C31H23F3N2O2
 1
1
IC50 = 90.5 nM
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CP0434062
2-[4-({[3-(3-benzoyl-8-fluoroquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C31H23FN2O3
 1
1
IC50 = 104 nM
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CP0434059
2-{4-[({3-[3-cyano-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C26H18F3N3O2
 1
1
IC50 = 150 nM
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CP0525916
3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]-N-benzylaniline
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C30H21F3N2O
 1
1
IC50 = 241 nM
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CP0394758
2-(4-{[(3-{3-[hydroxy(phenyl)methyl]-8-(trifluoromethyl)quinolin-4-yl}phenyl)amino]methyl}phenyl)acetic acid
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C32H25F3N2O3
 1
1
IC50 = 384 nM
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CP0425194
4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]benzoic acid
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C31H21F3N2O3
 1
1
IC50 = 420 nM
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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
 1
1
IC50 = 456 nM
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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
 1
1
IC50 = 479 nM
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CP0394756
2-[4-({[3-(3-benzoylquinolin-4-yl)phenyl]amino}methyl)phenyl]acetic acid
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C31H24N2O3
 1
1
IC50 = 650 nM
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CP0437268
2-{4-[({3-[3-carbamoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C26H20F3N3O3
 1
1
IC50 > 10000 nM
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CP0522252
(2E)-3-{4-[({3-[3-benzoyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}prop-2-enoic acid
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C33H23F3N2O3
 1
1
IC50 > 10000 nM
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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
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C34H43NO4
 2
1 EC50 = 1 nM
2 IC50 = 1 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
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C38H46O7
 2
1 EC50 = 2 nM
2 IC50 = 2 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
 16
1 EC50 = 10 nM
2 EC50 = 50 nM
3 EC50 = 55 nM
4 EC50 = 60 nM
5 EC50 = 85 nM
6 EC50 = 91.1 nM
7 EC50 = 120 nM
8 EC50 = 500 nM
9 IC50 = 9 nM
10 IC50 = 10 nM
11 IC50 = 13 nM
12 IC50 = 30 nM
13 IC50 = 75 nM
14 IC50 = 100 nM
15 Kd = 92.4 nM
16 Ki = 24 nM
CP0132783
N-benzyl-N-[[5-[4-(hydroxymethyl)-3-methylsulfonylphenyl]thiophen-2-yl]methyl]-2-(trifluoromethyl)benzenesulfonamide
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C27H24F3NO5S3
 3
1 EC50 = 19 nM
2 IC50 = 34 nM
3 Ki = 20 nM
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
 12
1 EC50 = 22 nM
2 EC50 = 66 nM
3 EC50 = 80 nM
4 EC50 = 125 nM
5 EC50 = 190 nM
6 EC50 = 200 nM
7 EC50 = 280 nM
8 EC50 = 1128 nM
9 EC50 = 1300 nM
10 IC50 = 100 nM
11 IC50 = 235 nM
12 Kd = 6970 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
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C27H44O2
 4
1 EC50 = 95 nM
2 EC50 = 280 nM
3 EC50 = 3000 nM
4 EC50 > 20000 nM
CP0080875
(1S,4aS,10aR)-6-Hydroxy-1,4a-dimethyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carboxylic acid (adamantan-1-ylmethyl)-amide
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C28H39NO2
 2
1 EC50 = 230 nM
2 IC50 = 100 nM
CP0173384
(4S,4aR)-6-Hydroxy-4a-methyl-1-(S)-methyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carboxylic acid ((1R,2R,3R,5S)-2,6,6-trimethyl-bicyclo[3.1.1]hept-3-yl)-amide
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C27H39NO2
 2
1 EC50 = 280 nM
2 IC50 = 270 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
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C27H37NO2
 2
1 EC50 = 320 nM
2 IC50 = 130 nM
CP0186266
N-ethyl-N-[4-(1,1,1,3,3,3-hexafluoro-2-hydroxypropan-2-yl)phenyl]benzenesulfonamide
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C17H15F6NO3S
 1
1 EC50 = 320 nM
CP0051425
(2R)-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 = 346 nM
CP0214923
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-prop-2-enylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C19H17Cl2F3N2O4S
 1
1 EC50 = 470 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 = 608 nM
CP0210744
3-[((4S,4aR)-6-Hydroxy-4a-methyl-1-(S)-methyl-1,2,3,4,4a,9,10,10a-octahydro-phenanthrene-1-carbonyl)-amino]-adamantane-1-carboxylic acid ethyl ester
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C30H41NO4
 2
1 EC50 = 760 nM
2 IC50 = 30 nM
CP0259297
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-ethylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C18H17Cl2F3N2O4S
 1
1 EC50 = 1000 nM
CP0240312
(1S,2R,5S,10S,11S,14R,15S)-14-[(2S,3R)-3-hydroxy-6-methylheptan-2-yl]-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-7-en-5-ol
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C27H46O2
 1
1 EC50 = 1000 nM
CP0285586
N-[2-chloro-4-[(2-chlorophenyl)sulfonyl-(cyclopropylmethyl)amino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C20H19Cl2F3N2O4S
 1
1 EC50 = 1080 nM
CP0435156
(S)-N-(2-chloro-4-(N,4-dimethylphenylsulfonamido)phenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C18H18ClF3N2O4S
 1
1 EC50 = 1970 nM
CP0259299
methyl 4-[[3-chloro-4-[(3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl)amino]phenyl]-methylsulfamoyl]benzoate
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C19H18ClF3N2O6S
 1
1 EC50 = 3100 nM
CP0259296
(S)-N-(2-chloro-4-(N-methylphenylsulfonamido)phenyl)-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C17H16ClF3N2O4S
 1
1 EC50 = 3300 nM
CP0371199
N-[2-chloro-4-[(4-cyanophenyl)sulfonyl-methylamino]phenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C18H15ClF3N3O4S
 1
1 EC50 = 3400 nM
CP0198578
methyl 3-[4-[[3-chloro-4-[(3,3,3-trifluoro-2-hydroxy-2-methylpropanoyl)amino]phenyl]-methylsulfamoyl]phenyl]propanoate
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C21H22ClF3N2O6S
 1
1 EC50 = 3500 nM
CP0214925
4-(N-(3-chloro-4-(3,3,3-trifluoro-2-hydroxy-2-methylpropanamido)phenyl)-N-methylsulfamoyl)benzoic acid
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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
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C20H20ClF3N2O6S
 1
1 EC50 > 100000 nM
CP0344790
N-[4-[benzyl-(2-chlorophenyl)sulfonylamino]-2-chlorophenyl]-3,3,3-trifluoro-2-hydroxy-2-methylpropanamide
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C23H19Cl2F3N2O4S
 1
1 EC50 > 100000 nM
CP0234158
2-benzyl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C28H21F3N2O3S
 1
1 IC50 = 0.81 nM
CP0128474
3-methyl-4-(3-(3-(methylsulfonyl)phenoxy)phenyl)-8-(trifluoromethyl)quinoline
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C24H18F3NO3S
 1
1 IC50 = 1 nM
CP0239960
3-[[3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridin-2-yl]methyl]-1,3-thiazolidine
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C25H22F3N3O3S2
 1
1 IC50 = 2 nM
CP0255636
3-[3-(3-methylsulfonylphenoxy)phenyl]-2-propan-2-yl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C24H21F3N2O3S
 1
1 IC50 = 3.5 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 = 6.5 nM
CP0095700
2-methyl-1-(3-(3-(methylsulfonyl)phenoxy)phenyl)-4-(trifluoromethyl)-1H-benzo[d]imidazole
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C22H17F3N2O3S
 1
1 IC50 = 7 nM
CP0268792
3-[3-(3-methylsulfonylphenoxy)phenyl]-2-phenyl-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C27H19F3N2O3S
 1
1 IC50 = 7.2 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 = 7.5 nM
CP0221684
2-{4-[({3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenyl}amino)methyl]phenyl}acetic acid
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C32H25F3N2O2
 1
1 IC50 = 7.6 nM
CP0353476
biarylether amide quinoline, 4i
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C24H19ClN2O2
 1
1 IC50 = 9 nM
CP0203734
2-(4-{3-[3-benzyl-8-(trifluoromethyl)quinolin-4-yl]phenoxymethyl}phenyl)acetic acid
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C32H24F3NO3
 1
1 IC50 = 9.5 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 = 10 nM
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 IC50 = 12 nM
CP0226706
2-ethyl-3-[3-(3-methylsulfonylphenoxy)phenyl]-8-(trifluoromethyl)imidazo[1,2-a]pyridine
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C23H19F3N2O3S
 1
1 IC50 = 14 nM
CP0179493
2-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)acetic acid
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C24H23F3N2O4
 1
1 IC50 = 16 nM
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 IC50 = 18 nM
CP0328071
3-(1-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)-1H-indol-5-yl)propanoic acid
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C25H25F3N2O4
 1
1 IC50 = 18 nM
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 IC50 = 19 nM
CP0268795
3-(3-(8-chloro-2-isopropylimidazo[1,2-a]pyridin-3-yl)phenoxy)-N-(4-methoxybenzyl)-N-methylbenzenesulfonamide
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C31H30ClN3O4S
 1
1 IC50 = 24 nM
CP0051604
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrimidin-5-yl)acetic acid
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C21H23F3N4O4
 1
1 IC50 = 26 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 = 30 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 = 30 nM
CP0079923
2-(3-chloro-4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylthio)phenyl)acetic acid
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C22H21ClF3NO4S
 1
1 IC50 = 32 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 = 33 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 = 40 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 = 43 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 = 49 nM
CP0200285
2-(4-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)-2-(trifluoromethyl)phenyl)acetic acid
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C24H24F6N2O4
 1
1 IC50 = 60 nM
CP0051591
2-(2-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)thiazol-5-yl)acetic acid
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C20H22F3N3O4S
 1
1 IC50 = 67 nM
CP0051606
2-(4-(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propylamino)phenyl)acetic acid
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C22H23F3N2O4
 1
1 IC50 = 68 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 = 69 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 = 72 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 = 73 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 = 79 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 = 79 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 = 89 nM
CP0154694
2-(5-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyrazin-2-yl)acetic acid
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C21H23F3N4O4
 1
1 IC50 = 90 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 = 97 nM
CP0156187
2-(3-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)phenyl)acetic acid
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C23H25F3N2O4
 1
1 IC50 = 102 nM
CP0099132
2-(6-(methyl(3-(7-propyl-3-(trifluoromethyl)benzo[d]isoxazol-6-yloxy)propyl)amino)pyridin-3-yl)acetic acid
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C22H24F3N3O4
 1
1 IC50 = 105 nM
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 IC50 = 117 nM
CP0287908
2-(5-(3-(3-benzyl-8-(trifluoromethyl)quinolin-4-yl)benzylamino)naphthalen-1-yl)acetic acid
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C36H27F3N2O2
 1
1 IC50 = 123 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 = 188 nM
CP0256824
2-(5-((3-(3-methyl-8-(trifluoromethyl)quinolin-4-yl)phenyl)methylamino)naphthalen-1-yl)acetic acid
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C30H23F3N2O2
 1
1 IC50 = 211 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 = 410 nM
CP0345734
2-(5-((3-(8-(trifluoromethyl)quinolin-4-yl)phenyl)methylamino)naphthalen-1-yl)acetic acid
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C29H21F3N2O2
 1
1 IC50 = 745 nM
CP0059780
N-(2-methylpropyl)-N-[[5-(3-methylsulfonylphenyl)thiophen-2-yl]methyl]-1-phenylmethanesulfonamide
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C23H27NO4S3
 1
1 IC50 = 29000 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 = 3 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 = 7 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 = 20 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 = 22 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 = 25 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 = 32 nM
CP0055084
2-[(2R)-4-(3-methylsulfonylphenyl)-2-propan-2-ylpiperazin-1-yl]-4-(trifluoromethyl)pyrimidine
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C19H23F3N4O2S
 1
1 Ki = 43 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 = 48 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 = 51 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 = 63 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 = 71 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 = 81 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 = 86 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 = 136 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 = 146 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 = 157 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 = 186 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 = 204 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 = 218 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 = 1072 nM
Clinical Information about the Protein
Target 1 ( Oxysterols receptor LXR-alpha (NR1H3) )
Target Type Patented-recorded 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
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06394 Oxysterols receptor LXR-beta Mus musculus, Mouse
PT06830 Oxysterols receptor LXR-beta Rattus norvegicus, Rat