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, ZD1033, ZD-1033)
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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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]