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Assay Detail

CHEMBL1908255

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ADMET
Mechanism based inhibition of rat cytochrome P450 CYP1A1 measured by 7-ethoxyresorufin O-deethylation (EROD)
19
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1A1 (CHEMBL2922)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 9 6.86 8.00
kinact 9 - -
mechanism based inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL253346 2 8.00
CHEMBL1908231 2 8.00
CHEMBL1908230 2 7.70
CHEMBL1908226 2 7.05
CHEMBL1908225 2 6.60
CHEMBL374163 2 6.57
CHEMBL3215311 2 6.52
CHEMBL1908223 2 6.27
CHEMBL1908220 2 5.07
CHEMBL1908224 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL253346 Ki = 10.0 nM 8.00
CHEMBL1908231 Ki = 10.0 nM 8.00
CHEMBL1908230 Ki = 20.0 nM 7.70
CHEMBL1908226 Ki = 90.0 nM 7.05
CHEMBL1908225 Ki = 250.0 nM 6.60
CHEMBL374163 Ki = 270.0 nM 6.57
CHEMBL3215311 Ki = 300.0 nM 6.52
CHEMBL1908223 Ki = 540.0 nM 6.27
CHEMBL1908220 Ki = 8600.0 nM 5.07
CHEMBL1908220 kinact = 0.09 min-1 -
CHEMBL374163 kinact = 0.06 min-1 -
CHEMBL1908223 kinact = 0.5 min-1 -
CHEMBL1908224 mechanism based inhibition - -
CHEMBL1908225 kinact = 0.8 min-1 -
CHEMBL1908226 kinact = 0.1 min-1 -
CHEMBL253346 kinact = 0.3 min-1 -
CHEMBL1908230 kinact = 0.07 min-1 -
CHEMBL1908231 kinact = 0.07 min-1 -
CHEMBL3215311 kinact = 0.02 min-1 -