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Assay Detail

CHEMBL2215825

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

ADMET
Inhibition of human recombinant CYP3A4 using resorufin benzyl ether after 30 mins by fluorescence spectrophotometric analysis
8
Total Activities
8
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

Discovery of 1-[2-(2,4-dimethylphenylsulfanyl)phenyl]piperazine (Lu AA21004): a novel multimodal compound for the treatment of major depressive disorder.
Bang-Andersen B, Ruhland T, Jørgensen M, Smith G, Frederiksen K, Jensen KG, Zhong H, Nielsen SM, Hogg S, Mørk A, Stensbøl TB.
J Med Chem (2011) 54 : 3206 -3221
PubMed 21486038 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 5.10 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2204359 1 5.36
CHEMBL2204363 1 5.26
CHEMBL2204356 1 5.21
CHEMBL2205043 1 5.17
CHEMBL2204357 1 5.06
CHEMBL2204360 1 5.00
CHEMBL2205054 1 4.96
CHEMBL2205045 1 4.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2204359 IC50 = 4400.0 nM 5.36
CHEMBL2204363 IC50 = 5500.0 nM 5.26
CHEMBL2204356 IC50 = 6100.0 nM 5.21
CHEMBL2205043 IC50 = 6800.0 nM 5.17
CHEMBL2204357 IC50 = 8700.0 nM 5.06
CHEMBL2204360 IC50 = 10000.0 nM 5.00
CHEMBL2205054 IC50 = 11000.0 nM 4.96
CHEMBL2205045 IC50 = 16000.0 nM 4.80