anastrozole [Ligand Id: 5137] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1399 (Anastrozole, Arimidex, ICI D1033, ICI-D1033, Nastrosa, NSC-719344, NSC-759855, Rvg-106400, ZD-1033, ZD1033) |
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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 | Competitive inhibition of human aromatase using dibenzylfluorescein substrate after 10 mins preincubation measured every 10 sec for 5 mins by Michaelis-Menten and Dixon plot analysis | B | 9.89 | pKi | 0.13 | nM | Ki | Bioorg Med Chem (2012) 20: 2427-2434 [PMID:22386564] |
| ChEMBL | Displacement of [1,2,6,7-3H]-androstenedione from human placental CYP19 | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2006) 49: 1016-1022 [PMID:16451067] |
| ChEMBL | Inhibition of human placental microsome CYP19 | B | 7.82 | pIC50 | 15.14 | nM | IC50 | J Med Chem (2005) 48: 7282-7289 [PMID:16279787] |
| GtoPdb | - | - | 7.82 | pIC50 | 15 | nM | IC50 | J Steroid Biochem Mol Biol (1996) 58: 439-45 [PMID:8903429] |
| ChEMBL | Inhibition of human placental microsome CYP19 | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3050-3064 [PMID:20413308] |
| ChEMBL | Inhibition of aromatase | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem (2012) 20: 2603-2613 [PMID:22444875] |
| ChEMBL | Inhibition of aromatase in human placental microsomes | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4713-4715 [PMID:18640836] |
| ChEMBL | Inhibition of human aromatase using dibenzylfluorescein substrate preincubated for 30 mins measured after 30 mins by fluorescence assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Bioorg Med Chem (2012) 20: 2427-2434 [PMID:22386564] |
| ChEMBL | Inhibition of aromatase (unknown origin) transfected in human MCF7 cells | B | 8.44 | pIC50 | 3.6 | nM | IC50 | J Med Chem (2016) 59: 5131-5148 [PMID:26689671] |
| ChEMBL | Inhibition of aromatase in human JEG3 cells by scintillation spectrometry | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2010) 53: 2155-2170 [PMID:20148564] |
| ChEMBL | Inhibition of aromatase (unknown origin) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2015) 58: 7634-7658 [PMID:25992880] |
| ChEMBL | Inhibition of aromatase (unknown origin) | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Bioorg Med Chem (2018) 26: 1986-1995 [PMID:29525337] |
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]
