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Assay Detail

CHEMBL663578

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

ADMET
Inhibition of recombinant human Cytochrome P450 3A4
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of a N'-hydroxyphenylformamidine derivative HET0016 as a potent and selective 20-HETE synthase inhibitor.
Sato M, Ishii T, Kobayashi-Matsunaga Y, Amada H, Taniguchi K, Miyata N, Kameo K.
Bioorg Med Chem Lett (2001) 11 : 2993 -2995
PubMed 11714595 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.55 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL101168 1 6.35
CHEMBL321051 1 4.30
CHEMBL100917 1 4.29
CHEMBL103313 1 4.19
CHEMBL267865 1 4.15
CHEMBL319862 1 4.03
CHEMBL101180 1 -
CHEMBL103651 1 -
CHEMBL103320 1 -
CHEMBL100899 1 -
CHEMBL103163 1 -
CHEMBL101296 1 -
CHEMBL445120 1 -
CHEMBL317798 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL101168 IC50 = 450.0 nM 6.35
CHEMBL321051 IC50 = 50000.0 nM 4.30
CHEMBL100917 IC50 = 51000.0 nM 4.29
CHEMBL103313 IC50 = 65000.0 nM 4.19
CHEMBL267865 IC50 = 71000.0 nM 4.15
CHEMBL319862 IC50 = 94000.0 nM 4.03
CHEMBL101180 IC50 > 100000.0 nM -
CHEMBL103651 IC50 > 100000.0 nM -
CHEMBL103320 IC50 > 100000.0 nM -
CHEMBL100899 IC50 > 100000.0 nM -
CHEMBL103163 IC50 > 100000.0 nM -
CHEMBL101296 IC50 > 100000.0 nM -
CHEMBL445120 IC50 > 100000.0 nM -
CHEMBL317798 IC50 > 100000.0 nM -