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 35:

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]