giredestrant [Ligand Id: 12715] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4650316 (Gdc-9545, GDC-9545, Giredestrant, RO-7197597, RO7197597) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] | ||||||||
| GtoPdb | Antagonist potency in T47D wild-type cells | - | 10.3 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2021) 64: 11841-11856 [PMID:34251202] |
| ChEMBL | Antagonist activity at estrogen receptor in human T47D cells incubated for 18 hrs by ultra high sensitivity luminescence reporter gene assay | B | 10.3 | pIC50 | 0.05 | nM | IC50 | J Med Chem (2021) 64: 11841-11856 [PMID:34251202] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG expressed in HEK293 cells incubated for 5 mins by patch clamp assay | B | 5.21 | pIC50 | 6100 | nM | IC50 | J Med Chem (2021) 64: 11841-11856 [PMID:34251202] |
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]
