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Assay Detail

CHEMBL4371971

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

ADMET
Inhibition of CYP3A4 in human liver microsomes using midazolam as substrate preincubated for 5 mins followed by NADPH cofactor addition and measured after 10 mins by LC-MS/MS analysis
4
Total Activities
4
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

Discovery and evaluation of novel FAAH inhibitors in neuropathic pain model.
Bhuniya D, Kharul RK, Hajare A, Shaikh N, Bhosale S, Balwe S, Begum F, De S, Athavankar S, Joshi D, Madgula V, Joshi K, Raje AA, Meru AV, Magdum A, Mookhtiar KA, Barbhaiya R.
Bioorg Med Chem Lett (2019) 29 : 238 -243
PubMed 30503633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.62 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4593464 1 8.62
CHEMBL4557596 1 -
CHEMBL4474161 1 -
CHEMBL4438972 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4593464 IC50 = 2.4 nM 8.62
CHEMBL4557596 IC50 > 12.5 nM -
CHEMBL4474161 IC50 > 12.5 nM -
CHEMBL4438972 IC50 > 12.5 nM -