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Assay Detail

CHEMBL664889

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

Binding
Binding affinity for human placental microsome cytochrome P450 19A1 with 1 uM [1-beta-3H]-androstenedione
9
Total Activities
9
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
Ki 9 6.57 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1629805 1 7.89
CHEMBL1629804 1 7.43
CHEMBL440691 1 6.77
CHEMBL83422 1 6.64
CHEMBL309656 1 6.54
CHEMBL83835 1 6.35
CHEMBL81134 1 6.34
CHEMBL439950 1 6.08
CHEMBL82981 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1629805 Ki = 13.0 nM 7.89
CHEMBL1629804 Ki = 37.0 nM 7.43
CHEMBL440691 Ki = 170.0 nM 6.77
CHEMBL83422 Ki = 228.0 nM 6.64
CHEMBL309656 Ki = 289.0 nM 6.54
CHEMBL83835 Ki = 443.0 nM 6.35
CHEMBL81134 Ki = 455.0 nM 6.34
CHEMBL439950 Ki = 830.0 nM 6.08
CHEMBL82981 Ki = 7750.0 nM 5.11