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Assay Detail

CHEMBL2020672

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

ADMET
Inhibition of CYP1A2 in human liver microsomes using phenacetin preincubated for 5 mins by LC-MS/MS analysis
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Tissue Liver
Subcellular Microsome
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.
Foti RS, Rock DA, Han X, Flowers RA, Wienkers LC, Wahlstrom JL.
J Med Chem (2012) 55 : 1205 -1214
PubMed 22239545 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.46 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2018907 1 6.41
CHEMBL2018904 1 6.36
CHEMBL2018925 1 6.20
CHEMBL2018923 1 6.17
CHEMBL2018903 1 6.15
CHEMBL2018924 1 6.14
CHEMBL2018908 1 6.10
CHEMBL2018920 1 6.09
CHEMBL2018905 1 6.03
CHEMBL2018919 1 6.02
CHEMBL2018911 1 6.02
CHEMBL2018909 1 5.99
CHEMBL502335 1 5.87
CHEMBL2018916 1 5.86
CHEMBL2018917 1 5.83
CHEMBL2018921 1 5.74
CHEMBL2018906 1 5.63
CHEMBL2018912 1 5.57
CHEMBL2019024 1 5.48
CHEMBL2018913 1 5.09
CHEMBL2019022 1 5.07
CHEMBL488400 1 4.97
CHEMBL296580 1 4.89
CHEMBL2019026 1 4.30
CHEMBL2019025 1 4.30
CHEMBL2019023 1 4.30
CHEMBL2018910 1 4.30
CHEMBL2018922 1 4.30
CHEMBL2018918 1 4.30
CHEMBL2018914 1 4.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2018907 IC50 = 390.0 nM 6.41
CHEMBL2018904 IC50 = 440.0 nM 6.36
CHEMBL2018925 IC50 = 630.0 nM 6.20
CHEMBL2018923 IC50 = 670.0 nM 6.17
CHEMBL2018903 IC50 = 710.0 nM 6.15
CHEMBL2018924 IC50 = 730.0 nM 6.14
CHEMBL2018908 IC50 = 790.0 nM 6.10
CHEMBL2018920 IC50 = 810.0 nM 6.09
CHEMBL2018905 IC50 = 930.0 nM 6.03
CHEMBL2018919 IC50 = 950.0 nM 6.02
CHEMBL2018911 IC50 = 950.0 nM 6.02
CHEMBL2018909 IC50 = 1020.0 nM 5.99
CHEMBL502335 IC50 = 1340.0 nM 5.87
CHEMBL2018916 IC50 = 1390.0 nM 5.86
CHEMBL2018917 IC50 = 1480.0 nM 5.83
CHEMBL2018921 IC50 = 1810.0 nM 5.74
CHEMBL2018906 IC50 = 2340.0 nM 5.63
CHEMBL2018912 IC50 = 2670.0 nM 5.57
CHEMBL2019024 IC50 = 3290.0 nM 5.48
CHEMBL2018913 IC50 = 8080.0 nM 5.09
CHEMBL2019022 IC50 = 8560.0 nM 5.07
CHEMBL488400 IC50 = 10690.0 nM 4.97
CHEMBL296580 IC50 = 12940.0 nM 4.89
CHEMBL2019026 IC50 = 50000.0 nM 4.30
CHEMBL2019025 IC50 = 50000.0 nM 4.30
CHEMBL2019023 IC50 = 50000.0 nM 4.30
CHEMBL2018910 IC50 = 49900.0 nM 4.30
CHEMBL2018922 IC50 = 50000.0 nM 4.30
CHEMBL2018918 IC50 = 50000.0 nM 4.30
CHEMBL2018914 IC50 = 50000.0 nM 4.30
CHEMBL2018926 IC50 > 50000.0 nM -
CHEMBL2018915 IC50 - -