ChEMBL ligand: CHEMBL1093458 (4-hydroxy-n-desmethyltamoxifen, Endoxifen, N-desmethyl-4-hydroxytamoxifen, NSC-749798, Z-endoxifen)
CYP19A1/Cytochrome P450 19A1 in Human [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] There should be some charts here, you may need to enable JavaScript!
Estrogen receptor-α/Estrogen receptor alpha in Human [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372] There should be some charts here, you may need to enable JavaScript!

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]
GtoPdb	-	-	5.4	pKi	4000	nM	Ki	Breast Cancer Res Treat (2012) 131: 473-81 [PMID:21390495]
ChEMBL	Inhibition of human aromatase assessed as reduction in fluorescence intensity preincubated with NADPH regenerating system for 10 mins followed by substrate addition incubated for 60 mins by fluorescence based microplate reader analysis	B	5	pIC50	>10000	nM	IC50	Eur J Med Chem (2021) 224: 113733-113733 [PMID:34364162]
ChEMBL	Inhibition of recombinant human aromatase preincubated for 10 mins followed by substrate and beta-NADP+ addition and measured for 60 mins by fluorescence method	B	5.21	pIC50	6100	nM	IC50	Eur J Med Chem (2019) 168: 253-262 [PMID:30822713]
GtoPdb	-	-	5.22	pIC50	6000	nM	IC50	Breast Cancer Res Treat (2012) 133: 99-109 [PMID:21814747]
ChEMBL	Inhibition of human recombinant placental aromatase	B	5.22	pIC50	6000	nM	IC50	J Med Chem (2013) 56: 4611-4618 [PMID:23731360]
ChEMBL	Inhibition of human placental microsomal aromatase using testosterone as substrate assessed as formation of estradiol after 10 mins	B	5.22	pIC50	6000	nM	IC50	J Med Chem (2016) 59: 5131-5148 [PMID:26689671]
Estrogen receptor-α/Estrogen receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL206] [GtoPdb: 620] [UniProtKB: P03372]
ChEMBL	Binding affinity to human ERalpha measured after 2 hrs by fluorescence polarization plate reader	B	7.52	pIC50	30	nM	IC50	Eur J Med Chem (2021) 224: 113733-113733 [PMID:34364162]

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]