ChEMBL ligand: CHEMBL3094388
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-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-α/Nuclear receptor ROR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
GtoPdb	Competitive radioligand binding assay using [3H]25-hydroxycholesterol as tracer.	-	6.76	pKi	172	nM	Ki	Nature (2011) 472: 491-4 [PMID:21499262]
ChEMBL	Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR alpha ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay	B	6.76	pKi	172	nM	Ki	MedChemComm (2013) 4: 764-776
ChEMBL	Binding affinity to RORa-LBD (unknown origin) by radioligand binding assay	B	6.76	pKi	172	nM	Ki	J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL	Inverse agonist activity at GAL4-fused ROR alpha (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay	B	5.4	pEC50	4000	nM	EC50	MedChemComm (2013) 4: 764-776
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
GtoPdb	Competitive radioligand binding assay using [3H]25-hydroxycholesterol as tracer.	-	6.95	pKi	111	nM	Ki	Nature (2011) 472: 491-4 [PMID:21499262]
ChEMBL	Displacement of 25-[3H]hydroxycholesterol from GST-tagged ROR gamma ligand binding domain (unknown origin) expressed in Escherichia coli BL21 gold (DE3) cells by radioligand competition assay	B	6.95	pKi	111	nM	Ki	MedChemComm (2013) 4: 764-776
ChEMBL	Binding affinity to RORc-LBD (unknown origin) by radioligand binding assay	B	6.95	pKi	111	nM	Ki	J. Med. Chem. (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL	Displacement of [3H2]-25-hydroxycholesterol from N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system after 3 hrs by scintillation counting analysis	B	5.7	pIC50	2000	nM	IC50	Bioorg. Med. Chem. Lett. (2013) 23: 6604-6609 [PMID:24239186]
ChEMBL	Inverse agonist activity at GAL4-fused ROR gamma (unknown origin) expressed in HEK293 cells assessed as inhibition of transcriptional activity after 24 hrs by luciferase reporter gene assay	B	5.4	pEC50	4000	nM	EC50	MedChemComm (2013) 4: 764-776
ChEMBL	Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis	B	6.04	pEC50	911	nM	EC50	Bioorg. Med. Chem. Lett. (2013) 23: 6604-6609 [PMID:24239186]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]