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Assay Detail

CHEMBL1111995

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

ADMET
Inhibition of human recombinant CYP3A4
7
Total Activities
7
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 3A4 (CHEMBL340)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Second generation analogues of the cancer drug clinical candidate tipifarnib for anti-Chagas disease drug discovery.
Kraus JM, Tatipaka HB, McGuffin SA, Chennamaneni NK, Karimi M, Arif J, Verlinde CL, Buckner FS, Gelb MH.
J Med Chem (2010) 53 : 3887 -3898
PubMed 20429511 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.35 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157101 KETOCONAZOLE 4.0 1 7.96
CHEMBL1397 POSACONAZOLE 4.0 1 7.09
CHEMBL1097187 1 6.56
CHEMBL1097078 1 6.04
CHEMBL1097079 1 5.79
CHEMBL1097772 1 5.63
CHEMBL289228 TIPIFARNIB 3.0 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157101 KETOCONAZOLE IC50 = 11.0 nM 7.96
CHEMBL1397 POSACONAZOLE IC50 = 82.0 nM 7.09
CHEMBL1097187 IC50 = 275.0 nM 6.56
CHEMBL1097078 IC50 = 923.0 nM 6.04
CHEMBL1097079 IC50 = 1628.0 nM 5.79
CHEMBL1097772 IC50 = 2345.0 nM 5.63
CHEMBL289228 TIPIFARNIB IC50 = 4060.0 nM 5.39