SR1555 [Ligand Id: 10145] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3218917
  • 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-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 pKi 1000 nM Ki Medchemcomm (2013) 4: 764-776
ChEMBL Inhibition of GAL4-fused ROR gamma (unknown origin) expressed in HEK293T cells assessed as suppression of transcriptional activity after 20 hrs B 5.82 pIC50 1500 nM IC50 Medchemcomm (2013) 4: 764-776
GtoPdb In a competitive radioligand binding assay using [3H]T0901317 as tracer and measuring displacement from the ligand binding domain fragment of RORγ. - 6 pIC50 1000 nM IC50 ACS Chem Biol (2012) 7: 1515-9 [PMID:22769242]
ChEMBL Binding affinity to RORc-LBD (unknown origin) by radioligand binding assay B 6 pIC50 1000 nM IC50 J Med Chem (2014) 57: 5871-5892 [PMID:24502334]
ChEMBL Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay B 5.82 pEC50 1500 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]