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Assay Detail

CHEMBL910524

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

ADMET
Inhibition of CYP3A4
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Optimization of monocarboxylate transporter 1 blockers through analysis and modulation of atropisomer interconversion properties.
Guile SD, Bantick JR, Cooper ME, Donald DK, Eyssade C, Ingall AH, Lewis RJ, Martin BP, Mohammed RT, Potter TJ, Reynolds RH, St-Gallay SA, Wright AD.
J Med Chem (2007) 50 : 254 -263
PubMed 17228867 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.80 6.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL219483 1 6.00
CHEMBL219098 1 5.14
CHEMBL218573 1 5.08
CHEMBL384536 1 4.82
CHEMBL205742 1 4.80
CHEMBL218628 1 4.66
CHEMBL387125 1 4.36
CHEMBL219861 1 4.34
CHEMBL375166 1 4.00
CHEMBL218468 1 -
CHEMBL219311 1 -
CHEMBL373974 1 -
CHEMBL441550 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL219483 IC50 = 1000.0 nM 6.00
CHEMBL219098 IC50 = 7200.0 nM 5.14
CHEMBL218573 IC50 = 8300.0 nM 5.08
CHEMBL384536 IC50 = 15000.0 nM 4.82
CHEMBL205742 IC50 = 16000.0 nM 4.80
CHEMBL218628 IC50 = 22000.0 nM 4.66
CHEMBL387125 IC50 = 44000.0 nM 4.36
CHEMBL219861 IC50 = 46000.0 nM 4.34
CHEMBL375166 IC50 = 100000.0 nM 4.00
CHEMBL218468 IC50 > 50000.0 nM -
CHEMBL219311 IC50 - -
CHEMBL373974 IC50 - -
CHEMBL441550 IC50 - -