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Assay Detail

CHEMBL660323

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Binding
Apparent inhibition constant for aromatase inhibition, was obtained by Dixon plot
14
Total Activities
14
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

Role of hydrophilic interaction in binding of hydroxylated 3-deoxy C(19) steroids to the active site of aromatase.
Numazawa M, Yamada K, Nitta S, Sasaki C, Kidokoro K.
J Med Chem (2001) 44 : 4277 -4283
PubMed 11708928 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.32 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630274 1 8.47
CHEMBL1629805 1 8.24
CHEMBL1630261 1 8.22
CHEMBL1629804 1 8.17
CHEMBL1629806 1 7.68
CHEMBL3349864 1 7.60
CHEMBL3349856 1 7.24
CHEMBL2111917 1 7.22
CHEMBL2112739 1 7.05
CHEMBL1630267 1 6.96
CHEMBL2311169 1 6.92
CHEMBL1630266 1 6.60
CHEMBL1630273 1 6.10
CHEMBL1630911 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630274 Ki = 3.4 nM 8.47
CHEMBL1629805 Ki = 5.8 nM 8.24
CHEMBL1630261 Ki = 6.0 nM 8.22
CHEMBL1629804 Ki = 6.8 nM 8.17
CHEMBL1629806 Ki = 21.0 nM 7.68
CHEMBL3349864 Ki = 25.0 nM 7.60
CHEMBL3349856 Ki = 58.0 nM 7.24
CHEMBL2111917 Ki = 60.0 nM 7.22
CHEMBL2112739 Ki = 90.0 nM 7.05
CHEMBL1630267 Ki = 110.0 nM 6.96
CHEMBL2311169 Ki = 120.0 nM 6.92
CHEMBL1630266 Ki = 250.0 nM 6.60
CHEMBL1630273 Ki = 800.0 nM 6.10
CHEMBL1630911 Ki = 1000.0 nM 6.00