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Assay Detail

CHEMBL4727432

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

Binding
Inhibition of YES1 (unknown origin)
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase Yes (CHEMBL2073)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Potent, non-covalent reversible BTK inhibitors with 8-amino-imidazo[1,5-a]pyrazine core featuring 3-position bicyclic ring substitutes.
Liu J,Guiadeen D,Krikorian A,Gao X,Wang J,Babu Boga S,Alhassan AB,Yu W,Selyutin O,Yu Y,Anand R,Xu J,Kelly J,Duffy JL,Liu S,Yang C,Wu H,Cai J,Bennett C,Maloney KM,Tyagarajan S,Gao YD,Fischmann TO,Presland J,Mansueto M,Xu Z,Leccese E,Zhang-Hoover J,Knemeyer I,Garlisi CG,Stivers P,Brandish PE,Hicks A,Kim R,Kozlowski JA
Bioorg Med Chem Lett (2020) 30 : 127390 -127390
PubMed 32738973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 7.31 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4106978 1 7.92
CHEMBL4108687 1 7.52
CHEMBL4749037 1 7.46
CHEMBL4114929 1 7.27
CHEMBL4107779 1 6.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4106978 IC50 = 12.0 nM 7.92
CHEMBL4108687 IC50 = 30.0 nM 7.52
CHEMBL4749037 IC50 = 35.0 nM 7.46
CHEMBL4114929 IC50 = 54.0 nM 7.27
CHEMBL4107779 IC50 = 430.0 nM 6.37