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Assay Detail

CHEMBL4720253

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

Binding
Inhibition of recombinant human YES using biotinyl-beta Abeta-Abeta AYQAEENTYDEYEN as substrate incubate for 30 mins by LANCE assay
2
Total Activities
2
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

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 2 7.52 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1873475 IBRUTINIB 4.0 1 8.19
CHEMBL4755698 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1873475 IBRUTINIB IC50 = 6.5 nM 8.19
CHEMBL4755698 IC50 = 145.9 nM 6.84