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Assay Detail

CHEMBL1919046

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

Binding
Inhibition of human full-length BTK expressed in Sf9 cells using FAM-Srctide peptide as substrate preincubated for 60 mins measured after 60 mins by TR-FRET Assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Tyrosine-protein kinase BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis.
Kim KH, Maderna A, Schnute ME, Hegen M, Mohan S, Miyashiro J, Lin L, Li E, Keegan S, Lussier J, Wrocklage C, Nickerson-Nutter CL, Wittwer AJ, Soutter H, Caspers N, Han S, Kurumbail R, Dunussi-Joannopoulos K, Douhan J, Wissner A.
Bioorg Med Chem Lett (2011) 21 : 6258 -6263
PubMed 21958547 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.87 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916891 1 9.15
CHEMBL1916897 1 8.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916891 IC50 = 0.7 nM 9.15
CHEMBL1916897 IC50 = 2.6 nM 8.59