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Assay Detail

CHEMBL865872

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

Binding
Displacement of [1,2,6,7-3H]-androstenedione from human placental CYP19
16
Total Activities
16
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

Potent CYP19 (aromatase) 1-[(benzofuran-2-yl)(phenylmethyl)pyridine, -imidazole, and -triazole inhibitors: synthesis and biological evaluation.
Saberi MR, Vinh TK, Yee SW, Griffiths BJ, Evans PJ, Simons C.
J Med Chem (2006) 49 : 1016 -1022
PubMed 16451067 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.93 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197650 1 8.00
CHEMBL202226 1 7.70
CHEMBL382902 1 7.36
CHEMBL372999 1 7.36
CHEMBL198291 1 7.31
CHEMBL202612 1 7.31
CHEMBL202231 1 7.22
CHEMBL201831 1 7.00
CHEMBL202065 1 6.89
CHEMBL379019 1 6.89
CHEMBL382500 1 6.89
CHEMBL202020 1 6.80
CHEMBL1399 ANASTROZOLE 4.0 1 6.22
CHEMBL199334 1 6.22
CHEMBL371663 1 5.91
CHEMBL446706 1 5.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197650 IC50 = 10.0 nM 8.00
CHEMBL202226 IC50 = 20.0 nM 7.70
CHEMBL382902 IC50 = 44.0 nM 7.36
CHEMBL372999 IC50 = 44.0 nM 7.36
CHEMBL198291 IC50 = 49.0 nM 7.31
CHEMBL202612 IC50 = 49.0 nM 7.31
CHEMBL202231 IC50 = 60.0 nM 7.22
CHEMBL201831 IC50 = 100.0 nM 7.00
CHEMBL202065 IC50 = 130.0 nM 6.89
CHEMBL379019 IC50 = 130.0 nM 6.89
CHEMBL382500 IC50 = 130.0 nM 6.89
CHEMBL202020 IC50 = 160.0 nM 6.80
CHEMBL1399 ANASTROZOLE IC50 = 600.0 nM 6.22
CHEMBL199334 IC50 = 600.0 nM 6.22
CHEMBL371663 IC50 = 1230.0 nM 5.91
CHEMBL446706 IC50 = 1460.0 nM 5.84