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Assay Detail

CHEMBL932840

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

ADMET
Inhibition of CYP3A4
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Naphthamides as novel and potent vascular endothelial growth factor receptor tyrosine kinase inhibitors: design, synthesis, and evaluation.
Harmange JC, Weiss MM, Germain J, Polverino AJ, Borg G, Bready J, Chen D, Choquette D, Coxon A, DeMelfi T, DiPietro L, Doerr N, Estrada J, Flynn J, Graceffa RF, Harriman SP, Kaufman S, La DS, Long A, Martin MW, Neervannan S, Patel VF, Potashman M, Regal K, Roveto PM, Schrag ML, Starnes C, Tasker A, Teffera Y, Wang L, White RD, Whittington DA, Zanon R.
J Med Chem (2008) 51 : 1649 -1667
PubMed 18324761 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.50 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL272693 1 7.00
CHEMBL406388 1 5.70
CHEMBL269915 1 4.89
CHEMBL270978 1 4.40
CHEMBL429743 1 -
CHEMBL429585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL272693 IC50 = 100.0 nM 7.00
CHEMBL406388 IC50 = 2000.0 nM 5.70
CHEMBL269915 IC50 = 13000.0 nM 4.89
CHEMBL270978 IC50 = 40000.0 nM 4.40
CHEMBL429743 IC50 > 50000.0 nM -
CHEMBL429585 IC50 > 50000.0 nM -