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Assay Detail

CHEMBL1908248

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ADMET
Mechanism based inhibition of rabbit cytochrome P450 CYP2B4 measured by 7-EFC O-deethylation activity
5
Total Activities
2
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Oryctolagus cuniculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 2B4 (CHEMBL1743542)
Type SINGLE PROTEIN
Organism Oryctolagus cuniculus

Publication

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
Fontana E, Dansette PM, Poli SM.
Curr Drug Metab (2005) 6 : 413 -454
PubMed 16248836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 4.28 4.43
kinact 2 - -
mechanism based inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1908229 3 4.43
CHEMBL1908221 2 4.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1908229 Ki = 37000.0 nM 4.43
CHEMBL1908221 Ki = 75000.0 nM 4.12
CHEMBL1908221 kinact = 0.23 min-1 -
CHEMBL1908229 kinact = 3.2 min-1 -
CHEMBL1908229 mechanism based inhibition - -