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 aromatase in human breast tumor | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2022) 241: 114658-114658 [PMID:35964426] |
| 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 (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 | 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 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]
