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Assay Detail

CHEMBL661696

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

Binding
In vitro inhibition of cytochrome P450 19A1 in human placental microsomes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Placenta
Subcellular Microsomes
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and structure-activity relationships of 6-substituted androst-4-ene analogs as aromatase inhibitors.
Numazawa M, Kamiyama T, Tachibana M, Oshibe M.
J Med Chem (1996) 39 : 2245 -2252
PubMed 8667367 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 28 9.27 10.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310735 1 10.43
CHEMBL305205 1 10.31
CHEMBL73993 1 10.30
CHEMBL1629804 1 10.22
CHEMBL70436 1 9.96
CHEMBL307581 1 9.92
CHEMBL308537 1 9.89
CHEMBL72228 1 9.80
CHEMBL307643 1 9.72
CHEMBL304305 1 9.64
CHEMBL304770 1 9.59
CHEMBL307690 1 9.49
CHEMBL73279 1 9.44
CHEMBL70317 1 9.36
CHEMBL74339 1 8.89
CHEMBL73367 1 8.80
CHEMBL306022 1 8.48
CHEMBL70959 1 8.43
CHEMBL305630 1 8.05
CHEMBL72415 1 7.92
CHEMBL69891 1 7.85
CHEMBL73071 1 7.37
CHEMBL74295 1 -
CHEMBL72538 1 -
CHEMBL73368 1 -
CHEMBL72056 1 -
CHEMBL73219 1 -
CHEMBL307006 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310735 IC50 = 0.037 nM 10.43
CHEMBL305205 IC50 = 0.049 nM 10.31
CHEMBL73993 IC50 = 0.05 nM 10.30
CHEMBL1629804 IC50 = 0.06 nM 10.22
CHEMBL70436 IC50 = 0.11 nM 9.96
CHEMBL307581 IC50 = 0.12 nM 9.92
CHEMBL308537 IC50 = 0.13 nM 9.89
CHEMBL72228 IC50 = 0.16 nM 9.80
CHEMBL307643 IC50 = 0.19 nM 9.72
CHEMBL304305 IC50 = 0.23 nM 9.64
CHEMBL304770 IC50 = 0.26 nM 9.59
CHEMBL307690 IC50 = 0.32 nM 9.49
CHEMBL73279 IC50 = 0.36 nM 9.44
CHEMBL70317 IC50 = 0.44 nM 9.36
CHEMBL74339 IC50 = 1.3 nM 8.89
CHEMBL73367 IC50 = 1.6 nM 8.80
CHEMBL306022 IC50 = 3.3 nM 8.48
CHEMBL70959 IC50 = 3.7 nM 8.43
CHEMBL305630 IC50 = 9.0 nM 8.05
CHEMBL72415 IC50 = 12.0 nM 7.92
CHEMBL69891 IC50 = 14.0 nM 7.85
CHEMBL73071 IC50 = 43.0 nM 7.37
CHEMBL74295 IC50 > 50.0 nM -
CHEMBL72538 IC50 > 50.0 nM -
CHEMBL73368 IC50 > 50.0 nM -
CHEMBL72056 IC50 > 50.0 nM -
CHEMBL73219 IC50 > 50.0 nM -
CHEMBL307006 IC50 > 50.0 nM -