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Assay Detail

CHEMBL4406418

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

Binding
Inhibition of CYP4Z1 (unknown origin) in human HepG2 cell membranes transduced with lentiviral vector using luciferin-benzyl ether as substrate preincubated with NADPH for 30 mins followed by substrate addition and measured after 10 mins by P450-glo luciferase based luminescence assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HepG2
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 4Z1 (CHEMBL4523375)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and Characterization of the First Selective and Potent Mechanism-Based Inhibitor of Cytochrome P450 4Z1.
Kowalski JP, McDonald MG, Pelletier RD, Hanenberg H, Wiek C, Rettie AE.
J Med Chem (2020) 63 : 4824 -4836
PubMed 32302132 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.23 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564920 1 7.00
CHEMBL4557940 1 6.70
CHEMBL4590991 1 6.70
CHEMBL4435658 1 6.52
CHEMBL4447108 1 6.40
CHEMBL4466562 1 6.30
CHEMBL4568702 1 6.16
CHEMBL4554028 1 5.85
CHEMBL4442292 1 5.77
CHEMBL101168 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564920 IC50 = 100.0 nM 7.00
CHEMBL4557940 IC50 = 200.0 nM 6.70
CHEMBL4590991 IC50 = 200.0 nM 6.70
CHEMBL4435658 IC50 = 300.0 nM 6.52
CHEMBL4447108 IC50 = 400.0 nM 6.40
CHEMBL4466562 IC50 = 500.0 nM 6.30
CHEMBL4568702 IC50 = 700.0 nM 6.16
CHEMBL4554028 IC50 = 1400.0 nM 5.85
CHEMBL4442292 IC50 = 1700.0 nM 5.77
CHEMBL101168 IC50 = 12000.0 nM 4.92