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Assay Detail

CHEMBL666790

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

Binding
Inhibition of human placental microsome cytochrome P450 19A1 aromatase
8
Total Activities
8
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

A new class of nonsteroidal aromatase inhibitors: design and synthesis of chromone and xanthone derivatives and inhibition of the P450 enzymes aromatase and 17 alpha-hydroxylase/C17,20-lyase.
Recanatini M, Bisi A, Cavalli A, Belluti F, Gobbi S, Rampa A, Valenti P, Palzer M, Palusczak A, Hartmann RW.
J Med Chem (2001) 44 : 672 -680
PubMed 11262078 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.33 7.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL9298 FADROZOLE 2.0 1 7.28
CHEMBL158984 1 7.00
CHEMBL161230 1 6.62
CHEMBL350922 1 6.41
CHEMBL158635 1 6.26
CHEMBL351167 1 5.96
CHEMBL161530 1 5.68
CHEMBL157925 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL9298 FADROZOLE IC50 = 52.0 nM 7.28
CHEMBL158984 IC50 = 100.0 nM 7.00
CHEMBL161230 IC50 = 240.0 nM 6.62
CHEMBL350922 IC50 = 390.0 nM 6.41
CHEMBL158635 IC50 = 550.0 nM 6.26
CHEMBL351167 IC50 = 1100.0 nM 5.96
CHEMBL161530 IC50 = 2100.0 nM 5.68
CHEMBL157925 IC50 = 3700.0 nM 5.43