ChEMBL ligand: CHEMBL2137199
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
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	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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]