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Assay Detail

CHEMBL3101167

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of human CYP19 preincubated for 10 mins followed by protein addition measured after 90 mins by fluorimetric analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and in Vivo Evaluation of Potent Dual CYP11B2 (Aldosterone Synthase) and CYP11B1 Inhibitors.
Meredith EL, Ksander G, Monovich LG, Papillon JP, Liu Q, Miranda K, Morris P, Rao C, Burgis R, Capparelli M, Hu QY, Singh A, Rigel DF, Jeng AY, Beil M, Fu F, Hu CW, LaSala D.
ACS Med Chem Lett (2013) 4 : 1203 -1207
PubMed 24900631 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.93 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3099686 1 7.30
CHEMBL3099683 1 5.96
CHEMBL3099695 OSILODROSTAT 4.0 1 5.22
CHEMBL287677 DEXFADROSTAT 2.0 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3099686 IC50 = 50.0 nM 7.30
CHEMBL3099683 IC50 = 1100.0 nM 5.96
CHEMBL3099695 OSILODROSTAT IC50 = 6000.0 nM 5.22
CHEMBL287677 DEXFADROSTAT IC50 = 6000.0 nM 5.22