SR1001 [Ligand Id: 10143] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3094388
  • RAR-related orphan receptor-α/Nuclear receptor ROR-alpha in Human [ChEMBL: CHEMBL5868] [GtoPdb: 598] [UniProtKB: P35398]
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  • RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]