ChEMBL ligand: CHEMBL2137199
Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] There should be some charts here, you may need to enable JavaScript!
Liver X receptor-α/LXR-alpha in Human [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] There should be some charts here, you may need to enable JavaScript!
RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398] There should be some charts here, you may need to enable JavaScript!
RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753] There should be some charts here, you may need to enable JavaScript!
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
ChEMBL	Inverse agonist activity at human GAL4-fused FXR LBD transfected in 293T cell measured after 24 hrs by dual luciferase assay	B	4.7	pIC50	>20000	nM	IC50	J Med Chem (2021) 64: 8775-8797 [PMID:34121397]
Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133]
ChEMBL	Inverse agonist activity at human GAL4-fused LXRalpha LBD transfected in 293T cell measured after 24 hrs by dual luciferase assay	B	4.7	pIC50	>20000	nM	IC50	J Med Chem (2021) 64: 8775-8797 [PMID:34121397]
RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
ChEMBL	Inverse agonist activity at human GAL4-fused RORalpha LBD transfected in 293T cell measured after 24 hrs by dual luciferase assay	B	4.7	pIC50	>20000	nM	IC50	J Med Chem (2021) 64: 8775-8797 [PMID:34121397]
RAR-related orphan receptor-β/Nuclear receptor ROR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3091268] [GtoPdb: 599] [UniProtKB: Q92753]
ChEMBL	Inverse agonist activity at human GAL4-fused RORbeta LBD transfected in 293T cell measured after 24 hrs by dual luciferase assay	B	4.7	pIC50	>20000	nM	IC50	J Med Chem (2021) 64: 8775-8797 [PMID:34121397]
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL	Displacement of [3H]T0901317 from GST-tagged ROR gamma ligand binding domain (unknown origin) after 20 hrs by scintillation proximity assay	B	6.98	pKi	105	nM	Ki	Medchemcomm (2013) 4: 764-776
ChEMBL	Binding affinity to RORc (unknown origin) by radioligand binding assay	B	6.98	pKi	105	nM	Ki	J Med Chem (2014) 57: 5871-5892 [PMID:24502334]
GtoPdb	Displacement of radioligand [3H]T1317 in a competition-based SPA assay.	-	6.98	pKi	105	nM	Ki	ACS Chem Biol (2012) 7: 672-7 [PMID:22292739]
ChEMBL	Antagonist activity at human His6-tagged RORgamma ligand binding domain (262 to 507 aa) assessed as inhibition of SRC1-4 co-activator peptide recruitment by luminescence-based AlphaScreen assay	B	5.45	pIC50	3540	nM	IC50	Eur J Med Chem (2014) 78: 431-441 [PMID:24704616]
ChEMBL	Displacement of N-terminal biotinylated SRC1-4 coactivator peptide from N-terminal His6-fused human RORgamma-LBD (262 to 507 residues) expressed in Escherichia coli BL21 (DE3) by luminescence-based Alphascreen assay	B	6.04	pIC50	910	nM	IC50	Eur J Med Chem (2016) 116: 13-26 [PMID:27043267]
ChEMBL	Antagonist activity at Gal4-fused RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay	B	6.37	pIC50	430	nM	IC50	Eur J Med Chem (2014) 78: 431-441 [PMID:24704616]
ChEMBL	Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay	B	6.38	pIC50	420	nM	IC50	Eur J Med Chem (2014) 78: 431-441 [PMID:24704616]
ChEMBL	Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs	B	6.49	pIC50	320	nM	IC50	Medchemcomm (2013) 4: 764-776
ChEMBL	Inhibition of human GAL4-fused RORgamma transfected in HEK293 cells co-transfected with G6Pase by luciferase reporter assay	B	6.49	pIC50	320	nM	IC50	J Med Chem (2018) 61: 10976-10995 [PMID:30010338]
ChEMBL	Displacement of [3H]T0901317 from human RoRc expressed in HepG2 cells by scintillation proximity binding assay	B	6.82	pIC50	150	nM	IC50	J Med Chem (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL	Inhibition of Gal4-RORgamma-LBD (180 to 507 residues) (unknown origin) expressed in HEK293T cells after 24 hrs by dual-luciferase reporter assay	B	6.96	pIC50	110	nM	IC50	Eur J Med Chem (2016) 116: 13-26 [PMID:27043267]
ChEMBL	Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay	B	6.49	pEC50	320	nM	EC50	J Med Chem (2014) 57: 5871-5892 [PMID:24502334]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]