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Assay Detail

CHEMBL4394046

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

ADMET
Inhibition of human CYP3A4 measured after 30 mins in presence of NADPH regeneration system by luminescent CYP3A4 P450-Glo assay
2
Total Activities
2
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

Fluorinated indole-imidazole conjugates: Selective orally bioavailable 5-HT7 receptor low-basicity agonists, potential neuropathic painkillers.
Hogendorf AS, Hogendorf A, Popiołek-Barczyk K, Ciechanowska A, Mika J, Satała G, Walczak M, Latacz G, Handzlik J, Kieć-Kononowicz K, Ponimaskin E, Schade S, Zeug A, Bijata M, Kubicki M, Kurczab R, Lenda T, Staroń J, Bugno R, Duszyńska B, Pilarski B, Bojarski AJ.
Eur J Med Chem (2019) 170 : 261 -275
PubMed 30904783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.93 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4452569 1 7.00
CHEMBL157101 KETOCONAZOLE 4.0 1 6.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4452569 IC50 = 100.0 nM 7.00
CHEMBL157101 KETOCONAZOLE IC50 = 140.0 nM 6.85