Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL2344726

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

ADMET
Inhibition of CYP3A4 (unknown origin) using 7-benzyloxy-4-trifluoromethylcoumarin as substrate
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

The synthesis and SAR of calcitonin gene-related peptide (CGRP) receptor antagonists derived from tyrosine surrogates. Part 2.
Han X, Civiello RL, Conway CM, Cook DA, Davis CD, Degnan AP, Jiang XJ, Macci R, Mathias NR, Moench P, Pin SS, Schartman R, Signor LJ, Thalody G, Tora G, Whiterock V, Xu C, Macor JE, Dubowchik GM.
Bioorg Med Chem Lett (2013) 23 : 1870 -1873
PubMed 23402880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 4.73 5.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2336418 1 5.46
CHEMBL2336422 1 4.89
CHEMBL2336412 1 4.75
CHEMBL2336424 1 4.62
CHEMBL2336421 1 4.60
CHEMBL450668 1 4.58
CHEMBL2336415 1 4.50
CHEMBL454791 1 4.44
CHEMBL2336411 1 -
CHEMBL2336413 1 -
CHEMBL2336416 1 -
CHEMBL2336417 1 -
CHEMBL2336419 1 -
CHEMBL454751 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2336418 IC50 = 3500.0 nM 5.46
CHEMBL2336422 IC50 = 13000.0 nM 4.89
CHEMBL2336412 IC50 = 18000.0 nM 4.75
CHEMBL2336424 IC50 = 24000.0 nM 4.62
CHEMBL2336421 IC50 = 25000.0 nM 4.60
CHEMBL450668 IC50 = 26000.0 nM 4.58
CHEMBL2336415 IC50 = 32000.0 nM 4.50
CHEMBL454791 IC50 = 36000.0 nM 4.44
CHEMBL2336411 IC50 > 40000.0 nM -
CHEMBL2336413 IC50 > 40000.0 nM -
CHEMBL2336416 IC50 > 40000.0 nM -
CHEMBL2336417 IC50 > 40000.0 nM -
CHEMBL2336419 IC50 > 40000.0 nM -
CHEMBL454751 IC50 > 40000.0 nM -