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Assay Detail

CHEMBL3385974

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

ADMET
Inhibition of human recombinant CYP3A4 incubated for 5 mins by fluorescence assay
10
Total Activities
10
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

Exploration of 3-Aminoazetidines as Triple Reuptake Inhibitors by Bioisosteric Modification of 3-α-Oxyazetidine.
Han M, Song C, Jeong N, Hahn HG.
ACS Med Chem Lett (2014) 5 : 999 -1004
PubMed 25221656 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.93 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3331508 1 6.92
CHEMBL1175 DULOXETINE 4.0 1 6.36
CHEMBL3331484 1 6.30
CHEMBL3331507 1 6.30
CHEMBL3331504 1 6.09
CHEMBL3331503 1 5.96
CHEMBL3331469 1 5.88
CHEMBL157101 KETOCONAZOLE 4.0 1 5.60
CHEMBL3331506 1 5.44
CHEMBL3331502 1 4.49

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3331508 IC50 = 120.0 nM 6.92
CHEMBL1175 DULOXETINE IC50 = 440.0 nM 6.36
CHEMBL3331484 IC50 = 500.0 nM 6.30
CHEMBL3331507 IC50 = 500.0 nM 6.30
CHEMBL3331504 IC50 = 810.0 nM 6.09
CHEMBL3331503 IC50 = 1100.0 nM 5.96
CHEMBL3331469 IC50 = 1330.0 nM 5.88
CHEMBL157101 KETOCONAZOLE IC50 = 2500.0 nM 5.60
CHEMBL3331506 IC50 = 3640.0 nM 5.44
CHEMBL3331502 IC50 = 32700.0 nM 4.49