Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4670198

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

ADMET
Inhibition of CYP1A2 in human liver microsomes using phenacetin as substrate incubated for 5 to 20 mins in presence of NADPH by LC-MS/MS analysis
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of Potent and Selective PI3Kγ Inhibitors.
Drew SL,Thomas-Tran R,Beatty JW,Fournier J,Lawson KV,Miles DH,Mata G,Sharif EU,Yan X,Mailyan AK,Ginn E,Chen J,Wong K,Soni D,Dhanota P,Chen PY,Shaqfeh SG,Meleza C,Pham AT,Chen A,Zhao X,Banuelos J,Jin L,Schindler U,Walters MJ,Young SW,Walker NP,Leleti MR,Powers JP,Jeffrey JL
J Med Chem (2020) 63 : 11235 -11257
PubMed 32865410 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 5.12 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4782083 1 5.12
CHEMBL4755842 1 -
CHEMBL4785086 1 -
CHEMBL4742062 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4782083 IC50 = 7500.0 nM 5.12
CHEMBL4755842 IC50 > 40000.0 nM -
CHEMBL4785086 IC50 > 40000.0 nM -
CHEMBL4742062 IC50 - -