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Assay Detail

CHEMBL666801

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

Binding
Inhibition of 1 uM [1-beta-3H]-androstenedione binding to human placental microsome Cytochrome P450 19A1
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biochemical studies of 16- or 19-substituted androst-4-enes as aromatase inhibitors.
Numazawa M, Mutsumi A, Hoshi K, Oshibe M, Ishikawa E, Kigawa H.
J Med Chem (1991) 34 : 2496 -2504
PubMed 1875347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.25 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1629805 1 6.57
CHEMBL132530 FORMESTANE 2.0 1 6.39
CHEMBL1629804 1 6.28
CHEMBL83835 1 5.92
CHEMBL440691 1 5.64
CHEMBL309656 1 5.40
CHEMBL83422 1 5.39
CHEMBL81134 1 5.23
CHEMBL439950 1 5.14
CHEMBL2112309 1 4.58
CHEMBL311077 1 4.42
CHEMBL443530 1 4.36
CHEMBL82981 1 4.21
CHEMBL81255 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1629805 IC50 = 270.0 nM 6.57
CHEMBL132530 FORMESTANE IC50 = 410.0 nM 6.39
CHEMBL1629804 IC50 = 530.0 nM 6.28
CHEMBL83835 IC50 = 1200.0 nM 5.92
CHEMBL440691 IC50 = 2300.0 nM 5.64
CHEMBL309656 IC50 = 4000.0 nM 5.40
CHEMBL83422 IC50 = 4100.0 nM 5.39
CHEMBL81134 IC50 = 5900.0 nM 5.23
CHEMBL439950 IC50 = 7300.0 nM 5.14
CHEMBL2112309 IC50 = 26000.0 nM 4.58
CHEMBL311077 IC50 = 38000.0 nM 4.42
CHEMBL443530 IC50 = 44000.0 nM 4.36
CHEMBL82981 IC50 = 62000.0 nM 4.21
CHEMBL81255 IC50 = 100000.0 nM 4.00