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Assay Detail

CHEMBL666403

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

Binding
Apparent inhibition constant (Ki) against Cytochrome P450 19A1
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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
Ki 26 7.88 10.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL73279 1 10.35
CHEMBL73367 1 9.85
CHEMBL74339 1 9.74
CHEMBL306022 1 9.47
CHEMBL70959 1 9.42
CHEMBL69891 1 8.54
CHEMBL310735 1 8.51
CHEMBL305205 1 8.28
CHEMBL73071 1 8.26
CHEMBL73993 1 8.22
CHEMBL1629804 1 8.17
CHEMBL307581 1 7.92
CHEMBL308537 1 7.92
CHEMBL72228 1 7.75
CHEMBL307643 1 7.68
CHEMBL304770 1 7.62
CHEMBL304305 1 7.52
CHEMBL70436 1 7.37
CHEMBL307690 1 7.37
CHEMBL307006 1 7.36
CHEMBL70317 1 7.29
CHEMBL73219 1 7.00
CHEMBL305630 1 6.40
CHEMBL72415 1 5.92
CHEMBL72538 1 5.58
CHEMBL74295 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL73279 Ki = 0.045 nM 10.35
CHEMBL73367 Ki = 0.14 nM 9.85
CHEMBL74339 Ki = 0.18 nM 9.74
CHEMBL306022 Ki = 0.34 nM 9.47
CHEMBL70959 Ki = 0.38 nM 9.42
CHEMBL69891 Ki = 2.9 nM 8.54
CHEMBL310735 Ki = 3.1 nM 8.51
CHEMBL305205 Ki = 5.3 nM 8.28
CHEMBL73071 Ki = 5.5 nM 8.26
CHEMBL73993 Ki = 6.0 nM 8.22
CHEMBL1629804 Ki = 6.8 nM 8.17
CHEMBL307581 Ki = 12.0 nM 7.92
CHEMBL308537 Ki = 12.0 nM 7.92
CHEMBL72228 Ki = 18.0 nM 7.75
CHEMBL307643 Ki = 21.0 nM 7.68
CHEMBL304770 Ki = 24.0 nM 7.62
CHEMBL304305 Ki = 30.0 nM 7.52
CHEMBL70436 Ki = 43.0 nM 7.37
CHEMBL307690 Ki = 43.0 nM 7.37
CHEMBL307006 Ki = 44.0 nM 7.36
CHEMBL70317 Ki = 51.0 nM 7.29
CHEMBL73219 Ki = 100.0 nM 7.00
CHEMBL305630 Ki = 400.0 nM 6.40
CHEMBL72415 Ki = 1200.0 nM 5.92
CHEMBL72538 Ki = 2600.0 nM 5.58
CHEMBL74295 Ki = 4100.0 nM 5.39