SR1555 [Ligand Id: 10145] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3218917 |
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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 34:
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]
