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Assay Detail

CHEMBL4398432

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

Binding
Inhibition of aromatase (unknown origin)
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aromatase (CHEMBL1978)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Estrogen signaling: An emanating therapeutic target for breast cancer treatment.
Saha T, Makar S, Swetha R, Gutti G, Singh SK.
Eur J Med Chem (2019) 177 : 116 -143
PubMed 31129450 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 8.29 9.70
Ki 2 6.99 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4465348 1 9.70
CHEMBL3622064 1 9.60
CHEMBL3622055 1 9.59
CHEMBL31760 1 9.15
CHEMBL108483 1 9.09
CHEMBL3622063 1 8.68
CHEMBL322322 1 8.64
CHEMBL4540847 1 7.39
CHEMBL3754505 1 7.21
CHEMBL4583456 1 7.04
CHEMBL3753089 1 6.76
CHEMBL10137 1 6.21
CHEMBL10026 1 6.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4465348 IC50 = 0.2 nM 9.70
CHEMBL3622064 IC50 = 0.25 nM 9.60
CHEMBL3622055 IC50 = 0.26 nM 9.59
CHEMBL31760 IC50 = 0.7 nM 9.15
CHEMBL108483 IC50 = 0.82 nM 9.09
CHEMBL3622063 IC50 = 2.1 nM 8.68
CHEMBL322322 IC50 = 2.3 nM 8.64
CHEMBL4540847 IC50 = 41.0 nM 7.39
CHEMBL3754505 Ki = 61.0 nM 7.21
CHEMBL4583456 IC50 = 91.0 nM 7.04
CHEMBL3753089 Ki = 174.0 nM 6.76
CHEMBL10137 IC50 = 620.0 nM 6.21
CHEMBL10026 IC50 = 800.0 nM 6.10