ChEMBL ligand: CHEMBL2386284
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!
Estrogen receptor-β/Estrogen receptor beta in Human [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731] 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	-	-	6.35	pKi	442	nM	Ki	J Med Chem (2013) 56: 4611-8 [PMID:23731360]
ChEMBL	Inhibition of human recombinant microsomal aromatase using 7-methoxy-4-trifluoromethylcoumarin as substrate by Lineweaver-Burk plot analysis	B	6.35	pKi	442	nM	Ki	J Med Chem (2013) 56: 4611-4618 [PMID:23731360]
ChEMBL	Inhibition of human recombinant microsomal aromatase-mediated 7-methoxy-4-trifluoromethylcoumarin conversion to 7-hydroxytrifluoromethylcoumarin preincubated for 10 mins measured after 30 mins by fluorescence assay	B	5.99	pIC50	1029	nM	IC50	J Med Chem (2013) 56: 4611-4618 [PMID:23731360]
ChEMBL	Inhibition of recombinant human microsomal CYP19 using MFC as substrate measured after 30 mins by fluorometric analysis	B	5.99	pIC50	1029	nM	IC50	Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367]
ChEMBL	Inhibition of human placental microsomal aromatase using testosterone as substrate assessed as formation of estradiol after 10 mins	B	7.52	pIC50	30	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	Displacement of fluorescent ES2 from human recombinant ERalpha after 2 hrs by fluorimetric analysis	B	7.77	pEC50	17	nM	EC50	J Med Chem (2013) 56: 4611-4618 [PMID:23731360]
ChEMBL	Displacement of fluorescent ES2 from recombinant human ERalpha after 2 hrs in absence of light by fluorometric analysis	B	7.77	pEC50	17	nM	EC50	Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367]
GtoPdb	-	-	7.77	pEC50	17	nM	EC50	J Med Chem (2013) 56: 4611-8 [PMID:23731360]
Estrogen receptor-β/Estrogen receptor beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL242] [GtoPdb: 621] [UniProtKB: Q92731]
GtoPdb	-	-	7.56	pEC50	27.5	nM	EC50	J Med Chem (2013) 56: 4611-8 [PMID:23731360]
ChEMBL	Displacement of fluorescent ES2 from human recombinant ERbeta after 2 hrs by fluorimetric analysis	B	7.56	pEC50	27.5	nM	EC50	J Med Chem (2013) 56: 4611-4618 [PMID:23731360]
ChEMBL	Displacement of fluorescent ES2 from recombinant human ERbeta after 2 hrs in absence of light by fluorometric analysis	B	7.56	pEC50	27.5	nM	EC50	Bioorg Med Chem (2016) 24: 5400-5409 [PMID:27647367]

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]