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Assay Detail

CHEMBL662245

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

Binding
The binding affinity was determined on Cytochrome P450 19A1 by analysis of Dixon plot
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis of androst-5-en-7-ones and androsta-3,5-dien-7-ones and their related 7-deoxy analogs as conformational and catalytic probes for the active site of aromatase.
Numazawa M, Mutsumi A, Tachibana M, Hoshi K.
J Med Chem (1994) 37 : 2198 -2205
PubMed 8035427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.77 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1629804 1 7.89
CHEMBL71152 1 7.24
CHEMBL2311169 1 6.92
CHEMBL262723 1 6.66
CHEMBL70367 1 6.60
CHEMBL1630911 1 6.00
CHEMBL302305 1 5.75
CHEMBL71117 1 5.70
CHEMBL71082 1 5.62
CHEMBL71612 1 5.52
CHEMBL68674 1 5.52
CHEMBL311400 1 5.28
CHEMBL302249 1 5.26
CHEMBL71363 1 4.96
CHEMBL302741 1 4.96
CHEMBL71169 1 4.89
CHEMBL302530 1 4.82
CHEMBL421491 1 4.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1629804 Ki = 13.0 nM 7.89
CHEMBL71152 Ki = 58.0 nM 7.24
CHEMBL2311169 Ki = 120.0 nM 6.92
CHEMBL262723 Ki = 220.0 nM 6.66
CHEMBL70367 Ki = 250.0 nM 6.60
CHEMBL1630911 Ki = 1000.0 nM 6.00
CHEMBL302305 Ki = 1800.0 nM 5.75
CHEMBL71117 Ki = 2000.0 nM 5.70
CHEMBL71082 Ki = 2400.0 nM 5.62
CHEMBL71612 Ki = 3000.0 nM 5.52
CHEMBL68674 Ki = 3000.0 nM 5.52
CHEMBL311400 Ki = 5300.0 nM 5.28
CHEMBL302249 Ki = 5500.0 nM 5.26
CHEMBL71363 Ki = 11000.0 nM 4.96
CHEMBL302741 Ki = 11000.0 nM 4.96
CHEMBL71169 Ki = 13000.0 nM 4.89
CHEMBL302530 Ki = 15000.0 nM 4.82
CHEMBL421491 Ki = 45000.0 nM 4.35