exemestane [Ligand Id: 7073] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1200374 (Aromasin, Exemestane, FCE-24304, FCE24304, NSC-758907, PNU-155971) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
| ChEMBL | Irreversible inhibition of human aromatase extracted from placental microsomes | B | 7.59 | pKi | 26 | nM | Ki | Eur J Med Chem (2015) 105: 1-38 [PMID:26469743] |
| ChEMBL | Competitive inhibition of human placental microsome aromatase using varying levels of [1beta2beta3H]-androstenedione as substrate | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (2019) 62: 3636-3657 [PMID:30852901] |
| ChEMBL | Inhibition of human placental microsome aromatase using [3H]androstenedione as substrate preincubated for 32 mins in presence of NADPH followed by substrate addition and measured after 10 mins | B | 7.59 | pKi | 26 | nM | Ki | J Med Chem (2020) 63: 4824-4836 [PMID:32302132] |
| GtoPdb | - | - | 7.6 | pKi | - | - | - | J Steroid Biochem (1988) 30: 391-4 [PMID:3386266] |
| ChEMBL | Competitive inhibition of human aromatase extracted from placental microsomes | B | 7.99 | pKi | 10.2 | nM | Ki | Eur J Med Chem (2015) 105: 1-38 [PMID:26469743] |
| ChEMBL | Inhibition of human placental microsome aromatase expressed in human MCF7 cells using [1beta-3H] androstenedione as substrate after 1 hr by liquid scintillation counting | B | 6.05 | pIC50 | 900 | nM | IC50 | Eur J Med Chem (2014) 87: 336-345 [PMID:25277066] |
| ChEMBL | Inhibition of aromatase (unknown origin) | B | 6.64 | pIC50 | 230 | nM | IC50 | Eur J Med Chem (2015) 105: 1-38 [PMID:26469743] |
| ChEMBL | Inhibition of human placental aromatase using [3H]-1beta-androstenedione as substrate after 16 hrs by [3H]-water method | B | 7.3 | pIC50 | 50.1 | nM | IC50 | J Med Chem (2012) 55: 8464-8476 [PMID:22951074] |
| ChEMBL | Inhibition of human placental microsome aromatase using [1beta-3H] androstenedione as substrate after 15 mins by liquid scintillation counting | B | 7.3 | pIC50 | 50 | nM | IC50 | Eur J Med Chem (2014) 87: 336-345 [PMID:25277066] |
| ChEMBL | Inhibition of CYP19 in human placental microsome using [1beta-3H]-androstenedione as substrate after 15 mins in presence of NADPH by liquid scintillation counter method | B | 7.37 | pIC50 | 42.5 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2645-2649 [PMID:28512028] |
| GtoPdb | - | - | 7.4 | pIC50 | 50.1 | nM | IC50 | J Steroid Biochem (1988) 30: 391-4 [PMID:3386266] |
| ChEMBL | Inhibition of aromatase (unknown origin) | B | 7.64 | pIC50 | 23 | nM | IC50 | J Nat Prod (2021) 84: 1738-1747 [PMID:34110821] |
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]
