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Assay Detail

CHEMBL4229933

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

ADMET
Inhibition of human supersome CYP3A4 using testosterone as substrate assessed as testosterone 6beta-hydroxylation after 30 mins by HPLC-UV detection
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

Novel multi-target azinesulfonamides of cyclic amine derivatives as potential antipsychotics with pro-social and pro-cognitive effects.
Zajdel P, Kos T, Marciniec K, Satała G, Canale V, Kamiński K, Hołuj M, Lenda T, Koralewski R, Bednarski M, Nowiński L, Wójcikowski J, Daniel WA, Nikiforuk A, Nalepa I, Chmielarz P, Kuśmierczyk J, Bojarski AJ, Popik P.
Eur J Med Chem (2018) 145 : 790 -804
PubMed 29407591 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.82 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4239823 1 5.00
CHEMBL4246655 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4239823 IC50 = 10000.0 nM 5.00
CHEMBL4246655 IC50 = 23000.0 nM 4.64