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Assay Detail

CHEMBL644755

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

ADMET
Inhibition of Aminopyrine N-demethylase in Phenobarbitone-treated rats
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 2B1 (CHEMBL3335)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Inhibitors of hepatic mixed-function oxidases. 4. Effects of benzimidazole and related compounds on aryl hydrocarbon hydroxylase activity from phenobarbitone and 3-methylcholanthrene induced rats.
Little PJ, Ryan AJ.
J Med Chem (1982) 25 : 622 -626
PubMed 7097715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.69 5.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL347036 PROADIFEN HYDROCHLORIDE -1.0 1 5.09
CHEMBL158007 1 4.82
CHEMBL345675 1 4.58
CHEMBL156313 1 4.28
CHEMBL306226 BENZIMIDAZOLE -1.0 1 -
CHEMBL348508 1 -
CHEMBL156134 1 -
CHEMBL351569 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL347036 PROADIFEN HYDROCHLORIDE IC50 = 8200.0 nM 5.09
CHEMBL158007 IC50 = 15000.0 nM 4.82
CHEMBL345675 IC50 = 26000.0 nM 4.58
CHEMBL156313 IC50 = 53000.0 nM 4.28
CHEMBL306226 BENZIMIDAZOLE IC50 = 980000.0 nM -
CHEMBL348508 IC50 = 300000.0 nM -
CHEMBL156134 IC50 = 370000.0 nM -
CHEMBL351569 IC50 = 670000.0 nM -