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Assay Detail

CHEMBL4720197

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

ADMET
Inhibition of human liver microsome CYP1A2 using phenacetin as substrate incubated for 5 mins followed by NADPH addition and further incubated for 10 mins in shaking water bath by LC-MS/MS analysis
1
Total Activities
1
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

Design, synthesis and biological evaluation of 7H-pyrrolo[2,3-d]pyrimidin-4-amine derivatives as selective Btk inhibitors with improved pharmacokinetic properties for the treatment of rheumatoid arthritis.
He L,Pei H,Zhang C,Shao M,Li D,Tang M,Wang T,Chen X,Xiang M,Chen L
Eur J Med Chem (2018) 145 : 96 -112
PubMed 29324347 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 7.22 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4755698 1 7.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4755698 IC50 = 60.0 nM 7.22