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Assay Detail

CHEMBL949431

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

ADMET
Inhibition of human recombinant CYP2C8
5
Total Activities
5
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 2C8 (CHEMBL3721)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century.
O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA.
J Med Chem (2009) 52 : 1408 -1415
PubMed 19222165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.89 5.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1630 1 5.57
CHEMBL147587 ISOQUINE 1 4.89
CHEMBL1235 DESETHYL AMODIAQUINE 1 4.70
CHEMBL147806 GSK-369796 1.0 1 4.64
CHEMBL146826 DESETHYL ISOQUINE 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1630 IC50 = 2700.0 nM 5.57
CHEMBL147587 ISOQUINE IC50 = 13000.0 nM 4.89
CHEMBL1235 DESETHYL AMODIAQUINE IC50 = 20000.0 nM 4.70
CHEMBL147806 GSK-369796 IC50 = 23000.0 nM 4.64
CHEMBL146826 DESETHYL ISOQUINE IC50 = 23000.0 nM 4.64