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Assay Detail

CHEMBL5716556

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

ADMET
Inhibition of CYP3A4 in human liver microsomes assessed as reduction in midazolam metabolism
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of potent and selective azaindole-based Rho kinase (ROCK) inhibitors.
Schirok H, Kast R, Figueroa-Pérez S, Bennabi S, Gnoth MJ, Feurer A, Heckroth H, Thutewohl M, Paulsen H, Knorr A, Hütter J, Lobell M, Münter K, Geiss V, Ehmke H, Lang D, Radtke M, Mittendorf J, Stasch JP.
ChemMedChem (2008) 3 : 1893 -1904
PubMed 18973168 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 4.92 5.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5274003 1 5.64
CHEMBL5723015 1 5.57
CHEMBL5723002 1 4.52
CHEMBL5428272 1 4.47
CHEMBL1971943 BAY-549 1 4.39
CHEMBL5722974 1 -
CHEMBL5722966 1 -
CHEMBL5722984 1 -
CHEMBL5270382 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5274003 IC50 = 2300.0 nM 5.64
CHEMBL5723015 IC50 = 2700.0 nM 5.57
CHEMBL5723002 IC50 = 30000.0 nM 4.52
CHEMBL5428272 IC50 = 34000.0 nM 4.47
CHEMBL1971943 BAY-549 IC50 = 41000.0 nM 4.39
CHEMBL5722974 IC50 - -
CHEMBL5722966 IC50 - -
CHEMBL5722984 IC50 - -
CHEMBL5270382 IC50 - -