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Assay Detail

CHEMBL910619

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

ADMET
Inhibition of human CYP2C19
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 2C19 (CHEMBL3622)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization.
Yano JK, Denton TT, Cerny MA, Zhang X, Johnson EF, Cashman JR.
J Med Chem (2006) 49 : 6987 -7001
PubMed 17125252 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 4.94 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL214784 1 6.70
CHEMBL215174 1 6.16
CHEMBL215134 1 6.05
CHEMBL359657 1 6.00
CHEMBL386124 1 5.41
CHEMBL214990 1 5.16
CHEMBL179669 1 5.00
CHEMBL178090 1 4.96
CHEMBL179704 1 4.90
CHEMBL360541 1 4.89
CHEMBL178938 1 4.82
CHEMBL149808 1 4.79
CHEMBL179621 1 4.68
CHEMBL178516 1 4.57
CHEMBL217125 1 4.56
CHEMBL369285 1 4.52
CHEMBL214859 1 4.39
CHEMBL385008 1 4.38
CHEMBL361969 1 4.28
CHEMBL361153 1 4.25
CHEMBL360999 1 4.21
CHEMBL360998 1 4.10
CHEMBL368883 1 -
CHEMBL215183 1 -
CHEMBL386250 1 -
CHEMBL180270 1 -
CHEMBL410355 1 -
CHEMBL218397 1 -
CHEMBL385023 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL214784 Ki = 200.0 nM 6.70
CHEMBL215174 Ki = 700.0 nM 6.16
CHEMBL215134 Ki = 900.0 nM 6.05
CHEMBL359657 Ki = 1000.0 nM 6.00
CHEMBL386124 Ki = 3900.0 nM 5.41
CHEMBL214990 Ki = 7000.0 nM 5.16
CHEMBL179669 Ki = 10100.0 nM 5.00
CHEMBL178090 Ki = 11000.0 nM 4.96
CHEMBL179704 Ki = 12500.0 nM 4.90
CHEMBL360541 Ki = 12900.0 nM 4.89
CHEMBL178938 Ki = 15300.0 nM 4.82
CHEMBL149808 Ki = 16400.0 nM 4.79
CHEMBL179621 Ki = 21000.0 nM 4.68
CHEMBL178516 Ki = 26800.0 nM 4.57
CHEMBL217125 Ki = 27500.0 nM 4.56
CHEMBL369285 Ki = 29900.0 nM 4.52
CHEMBL214859 Ki = 41000.0 nM 4.39
CHEMBL385008 Ki = 41400.0 nM 4.38
CHEMBL361969 Ki = 53000.0 nM 4.28
CHEMBL361153 Ki = 55600.0 nM 4.25
CHEMBL360999 Ki = 61000.0 nM 4.21
CHEMBL360998 Ki = 79000.0 nM 4.10
CHEMBL368883 Ki > 300000.0 nM -
CHEMBL215183 Ki > 400000.0 nM -
CHEMBL386250 Ki = 107000.0 nM -
CHEMBL180270 Ki > 400000.0 nM -
CHEMBL410355 Ki > 400000.0 nM -
CHEMBL218397 Ki = 109000.0 nM -
CHEMBL385023 Ki > 400000.0 nM -