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Assay Detail

CHEMBL5376029

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

Binding
Inhibition of human aromatase using ASD as substrate pre-incubated for 5 mins followed by substrate addition and measured after 16 hrs by UV/vis-spectrophotometry
ChEMBL ↗
701
Total Activities
701
Compounds Tested
1
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

Combating breast cancer with non-steroidal aromatase inhibitors (NSAIs): Understanding the chemico-biological interactions through comparative SAR/QSAR study.
Adhikari N, Amin SA, Saha A, Jha T.
Eur J Med Chem (2017) 137 : 365 -438
PubMed 28622580 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 701 6.41 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5438093 — — 1 10.70
CHEMBL5425028 — — 1 10.55
CHEMBL5408436 — — 1 10.00
CHEMBL3623231 — — 1 9.92
CHEMBL5401648 — — 1 9.85
CHEMBL5436996 — — 1 9.80
CHEMBL3623232 — — 1 9.70
CHEMBL5406734 — — 1 9.68
CHEMBL5416513 — — 1 9.66
CHEMBL3622064 — — 1 9.60
CHEMBL5404073 — — 1 9.60
CHEMBL3622055 — — 1 9.59
CHEMBL5412416 — — 1 9.55
CHEMBL3622054 — — 1 9.55
CHEMBL5440424 — — 1 9.55
CHEMBL5401315 — — 1 9.51
CHEMBL5417335 — — 1 9.44
CHEMBL5402457 — — 1 9.44
CHEMBL5421435 — — 1 9.43
CHEMBL5410657 — — 1 9.42
CHEMBL5407526 — — 1 9.41
CHEMBL5396464 — — 1 9.39
CHEMBL5440379 — — 1 9.38
CHEMBL3622056 — — 1 9.38
CHEMBL3622057 — — 1 9.35
CHEMBL3622058 — — 1 9.29
CHEMBL5439970 — — 1 9.22
CHEMBL5402413 — — 1 9.22
CHEMBL5402619 — — 1 9.19
CHEMBL31760 — — 1 9.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5438093 — IC50 = 0.02 nM 10.70
CHEMBL5425028 — IC50 = 0.02799 nM 10.55
CHEMBL5408436 — IC50 = 0.1 nM 10.00
CHEMBL3623231 — IC50 = 0.1199 nM 9.92
CHEMBL5401648 — IC50 = 0.14 nM 9.85
CHEMBL5436996 — IC50 = 0.16 nM 9.80
CHEMBL3623232 — IC50 = 0.2 nM 9.70
CHEMBL5406734 — IC50 = 0.2099 nM 9.68
CHEMBL5416513 — IC50 = 0.2198 nM 9.66
CHEMBL5404073 — IC50 = 0.25 nM 9.60
CHEMBL3622064 — IC50 = 0.25 nM 9.60
CHEMBL3622055 — IC50 = 0.26 nM 9.59
CHEMBL5412416 — IC50 = 0.2799 nM 9.55
CHEMBL3622054 — IC50 = 0.2799 nM 9.55
CHEMBL5440424 — IC50 = 0.2799 nM 9.55
CHEMBL5401315 — IC50 = 0.3097 nM 9.51
CHEMBL5417335 — IC50 = 0.3597 nM 9.44
CHEMBL5402457 — IC50 = 0.3597 nM 9.44
CHEMBL5421435 — IC50 = 0.3698 nM 9.43
CHEMBL5410657 — IC50 = 0.3802 nM 9.42
CHEMBL5407526 — IC50 = 0.3899 nM 9.41
CHEMBL5396464 — IC50 = 0.4102 nM 9.39
CHEMBL3622056 — IC50 = 0.4198 nM 9.38
CHEMBL5440379 — IC50 = 0.4198 nM 9.38
CHEMBL3622057 — IC50 = 0.4498 nM 9.35
CHEMBL3622058 — IC50 = 0.5105 nM 9.29
CHEMBL5439970 — IC50 = 0.5998 nM 9.22
CHEMBL5402413 — IC50 = 0.5998 nM 9.22
CHEMBL5402619 — IC50 = 0.6501 nM 9.19
CHEMBL31760 — IC50 = 0.6998 nM 9.15
CHEMBL3622059 — IC50 = 0.7295 nM 9.14
CHEMBL3818343 — IC50 = 0.871 nM 9.06
CHEMBL5431850 — IC50 = 0.8892 nM 9.05
CHEMBL5399449 — IC50 = 1.0 nM 9.00
CHEMBL5417041 — IC50 = 1.0 nM 9.00
CHEMBL5397670 — IC50 = 1.099 nM 8.96
CHEMBL5412669 — IC50 = 1.099 nM 8.96
CHEMBL5395326 — IC50 = 1.3 nM 8.89
CHEMBL5402090 — IC50 = 1.3 nM 8.89
CHEMBL5404820 — IC50 = 1.3 nM 8.89
CHEMBL5413153 — IC50 = 1.4 nM 8.85
CHEMBL5412425 — IC50 = 1.5 nM 8.82
CHEMBL5413848 — IC50 = 1.5 nM 8.82
CHEMBL5424630 — IC50 = 1.5 nM 8.82
CHEMBL5423824 — IC50 = 1.5 nM 8.82
CHEMBL5400488 — IC50 = 1.5 nM 8.82
CHEMBL5413770 — IC50 = 1.6 nM 8.80
CHEMBL5418345 — IC50 = 1.698 nM 8.77
CHEMBL5435238 — IC50 = 1.698 nM 8.77
CHEMBL5412353 — IC50 = 1.698 nM 8.77