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Assay Detail

CHEMBL3745190

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

ADMET
Inhibition of human microsomal CYP2A6
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 2A6 (CHEMBL5282)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological activity evaluation and molecular docking studies of novel coumarin substituted thiazolyl-3-aryl-pyrazole-4-carbaldehydes.
Vaarla K, Kesharwani RK, Santosh K, Vedula RR, Kotamraju S, Toopurani MK.
Bioorg Med Chem Lett (2015) 25 : 5797 -5803
PubMed 26542964 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.50 10.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3740883 1 10.24
CHEMBL3740902 1 8.81
CHEMBL3741757 1 8.76
CHEMBL3739596 1 8.71
CHEMBL3742383 1 8.59
CHEMBL3742224 1 8.59
CHEMBL3741819 1 8.57
CHEMBL3740871 1 8.51
CHEMBL3740860 1 8.48
CHEMBL3740335 1 8.47
CHEMBL3742302 1 8.22
CHEMBL3740529 1 7.96
CHEMBL3739579 1 7.89
CHEMBL3739672 1 7.88
CHEMBL3740695 1 7.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3740883 Ki = 0.057 nM 10.24
CHEMBL3740902 Ki = 1.54 nM 8.81
CHEMBL3741757 Ki = 1.73 nM 8.76
CHEMBL3739596 Ki = 1.93 nM 8.71
CHEMBL3742383 Ki = 2.58 nM 8.59
CHEMBL3742224 Ki = 2.57 nM 8.59
CHEMBL3741819 Ki = 2.7 nM 8.57
CHEMBL3740871 Ki = 3.07 nM 8.51
CHEMBL3740860 Ki = 3.27 nM 8.48
CHEMBL3740335 Ki = 3.41 nM 8.47
CHEMBL3742302 Ki = 6.02 nM 8.22
CHEMBL3740529 Ki = 10.97 nM 7.96
CHEMBL3739579 Ki = 12.96 nM 7.89
CHEMBL3739672 Ki = 13.2 nM 7.88
CHEMBL3740695 Ki = 16.62 nM 7.78