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Assay Detail

CHEMBL3755861

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

Binding
Competitive inhibition of human aromatase extracted from placental microsomes by Dixon plot analysis in presence of [1beta-3H]androstenedione
13
Total Activities
13
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

Developing steroidal aromatase inhibitors-an effective armament to win the battle against breast cancer.
Yadav MR, Barmade MA, Tamboli RS, Murumkar PR.
Eur J Med Chem (2015) 105 : 1 -38
PubMed 26469743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 6.84 8.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3753810 1 8.33
CHEMBL3752065 1 8.30
CHEMBL3754719 1 8.09
CHEMBL3752973 1 8.09
CHEMBL3753667 1 8.09
CHEMBL3752460 1 8.09
CHEMBL3752149 1 6.84
CHEMBL3752280 1 6.21
CHEMBL3752699 1 5.96
CHEMBL3753297 1 5.96
CHEMBL3752351 1 5.26
CHEMBL3753191 1 4.96
CHEMBL3754516 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3753810 Ki = 4.7 nM 8.33
CHEMBL3752065 Ki = 5.0 nM 8.30
CHEMBL3754719 Ki = 8.2 nM 8.09
CHEMBL3752973 Ki = 8.2 nM 8.09
CHEMBL3753667 Ki = 8.2 nM 8.09
CHEMBL3752460 Ki = 8.2 nM 8.09
CHEMBL3752149 Ki = 143.0 nM 6.84
CHEMBL3752280 Ki = 610.0 nM 6.21
CHEMBL3752699 Ki = 1100.0 nM 5.96
CHEMBL3753297 Ki = 1100.0 nM 5.96
CHEMBL3752351 Ki = 5500.0 nM 5.26
CHEMBL3753191 Ki = 11100.0 nM 4.96
CHEMBL3754516 Ki = 16000.0 nM 4.80