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Assay Detail

CHEMBL921270

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 Autocuration

Target

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

Publication

Novel 2-phenylquinolin-7-yl-derived imidazo[1,5-a]pyrazines as potent insulin-like growth factor-I receptor (IGF-IR) inhibitors.
Mulvihill MJ, Ji QS, Coate HR, Cooke A, Dong H, Feng L, Foreman K, Rosenfeld-Franklin M, Honda A, Mak G, Mulvihill KM, Nigro AI, O'Connor M, Pirrit C, Steinig AG, Siu K, Stolz KM, Sun Y, Tavares PA, Yao Y, Gibson NW.
Bioorg Med Chem (2008) 16 : 1359 -1375
PubMed 17983756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.95 5.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL261805 1 5.47
CHEMBL408712 1 5.12
CHEMBL258951 1 5.11
CHEMBL258648 1 4.92
CHEMBL411062 1 4.82
CHEMBL413828 1 4.82
CHEMBL261146 1 4.77
CHEMBL260298 1 4.77
CHEMBL430051 1 4.72
CHEMBL411082 1 -
CHEMBL261253 1 -
CHEMBL411074 1 -
CHEMBL410659 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL261805 IC50 = 3400.0 nM 5.47
CHEMBL408712 IC50 = 7500.0 nM 5.12
CHEMBL258951 IC50 = 7800.0 nM 5.11
CHEMBL258648 IC50 = 12000.0 nM 4.92
CHEMBL411062 IC50 = 15000.0 nM 4.82
CHEMBL413828 IC50 = 15000.0 nM 4.82
CHEMBL261146 IC50 = 17000.0 nM 4.77
CHEMBL260298 IC50 = 17000.0 nM 4.77
CHEMBL430051 IC50 = 19000.0 nM 4.72
CHEMBL411082 IC50 > 20000.0 nM -
CHEMBL261253 IC50 > 20000.0 nM -
CHEMBL411074 IC50 > 20000.0 nM -
CHEMBL410659 IC50 > 20000.0 nM -