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Assay Detail

CHEMBL2166348

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

Binding
Inhibition of CYP19 in human placental microsomes using [1beta-3H]-androstendione as a substrate
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Tissue Placenta
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Selective dual inhibitors of CYP19 and CYP11B2: targeting cardiovascular diseases hiding in the shadow of breast cancer.
Hu Q, Yin L, Hartmann RW.
J Med Chem (2012) 55 : 7080 -7089
PubMed 22861193 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 6.80 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2165321 1 7.96
CHEMBL1083653 1 7.92
CHEMBL2165319 1 7.66
CHEMBL2165320 1 7.46
CHEMBL2165317 1 7.32
CHEMBL2165315 1 7.31
CHEMBL9298 FADROZOLE 2.0 1 7.28
CHEMBL2165318 1 6.79
CHEMBL2165325 1 6.56
CHEMBL2165323 1 6.41
CHEMBL446083 1 6.37
CHEMBL2165314 1 6.35
CHEMBL2165316 1 6.31
CHEMBL2165324 1 6.02
CHEMBL2165322 1 5.54
CHEMBL2165313 1 5.51
CHEMBL62811 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2165321 IC50 = 11.0 nM 7.96
CHEMBL1083653 IC50 = 12.0 nM 7.92
CHEMBL2165319 IC50 = 22.0 nM 7.66
CHEMBL2165320 IC50 = 35.0 nM 7.46
CHEMBL2165317 IC50 = 48.0 nM 7.32
CHEMBL2165315 IC50 = 49.0 nM 7.31
CHEMBL9298 FADROZOLE IC50 = 52.0 nM 7.28
CHEMBL2165318 IC50 = 162.0 nM 6.79
CHEMBL2165325 IC50 = 275.0 nM 6.56
CHEMBL2165323 IC50 = 394.0 nM 6.41
CHEMBL446083 IC50 = 426.0 nM 6.37
CHEMBL2165314 IC50 = 447.0 nM 6.35
CHEMBL2165316 IC50 = 488.0 nM 6.31
CHEMBL2165324 IC50 = 954.0 nM 6.02
CHEMBL2165322 IC50 = 2901.0 nM 5.54
CHEMBL2165313 IC50 = 3073.0 nM 5.51
CHEMBL62811 IC50 > 5000.0 nM -