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Assay Detail

CHEMBL5037545

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

ADMET
Inhibition of CYP3A4 in human liver microsomes using ketoconazole as substrate incubated for 5 mins in presence of NADPH by LC-MS/MS analysis
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsomes
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structure-Guided Optimization Provides a Series of TTK Protein Inhibitors with Potent Antitumor Activity.
Elsner J, Cashion D, Robinson D, Bahmanyar S, Tehrani L, Fultz KE, Narla RK, Peng X, Tran T, Apuy J, LeBrun L, Leftheris K, Boylan JF, Zhu D, Riggs JR.
J Med Chem (2021) 64 : 12670 -12679
PubMed 34459599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 5.80 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4062218 1 6.55
CHEMBL5093015 1 5.92
CHEMBL5075313 1 5.72
CHEMBL5081270 1 5.70
CHEMBL5073101 1 5.51
CHEMBL5079606 1 5.41
CHEMBL4569626 1 -
CHEMBL5086435 1 -
CHEMBL5092826 1 -
CHEMBL5091689 1 -
CHEMBL5084062 1 -
CHEMBL5085278 1 -
CHEMBL5086022 1 -
CHEMBL5087340 1 -
CHEMBL5077627 1 -
CHEMBL5081668 1 -
CHEMBL5085182 1 -
CHEMBL5085753 1 -
CHEMBL5077668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4062218 IC50 = 280.0 nM 6.55
CHEMBL5093015 IC50 = 1200.0 nM 5.92
CHEMBL5075313 IC50 = 1900.0 nM 5.72
CHEMBL5081270 IC50 = 2000.0 nM 5.70
CHEMBL5073101 IC50 = 3100.0 nM 5.51
CHEMBL5079606 IC50 = 3900.0 nM 5.41
CHEMBL4569626 IC50 > 5000.0 nM -
CHEMBL5086435 IC50 > 5000.0 nM -
CHEMBL5092826 IC50 - -
CHEMBL5091689 IC50 - -
CHEMBL5084062 IC50 > 5000.0 nM -
CHEMBL5085278 IC50 > 5000.0 nM -
CHEMBL5086022 IC50 > 5000.0 nM -
CHEMBL5087340 IC50 - -
CHEMBL5077627 IC50 > 5000.0 nM -
CHEMBL5081668 IC50 > 5000.0 nM -
CHEMBL5085182 IC50 > 5000.0 nM -
CHEMBL5085753 IC50 > 5000.0 nM -
CHEMBL5077668 IC50 > 5000.0 nM -