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

CHEMBL1918490

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

Functional
Inhibition of anti-IgM-stimulated human B cell proliferation assessed as [3H]thymidine incorporation preincubated for 30 mins measured after 3 days
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type B cell
Confidence 1 — Organism
Curated By Autocuration

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 30 7.95 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1916889 1 8.99
CHEMBL1916881 1 8.70
CHEMBL1916895 1 8.66
CHEMBL1916898 1 8.62
CHEMBL1916888 1 8.59
CHEMBL1916718 1 8.50
CHEMBL1916882 1 8.50
CHEMBL1916891 1 8.47
CHEMBL1916885 1 8.38
CHEMBL1916896 1 8.36
CHEMBL1916880 1 8.31
CHEMBL1916897 1 8.23
CHEMBL1916892 1 8.17
CHEMBL1916894 1 8.09
CHEMBL1916717 1 7.79
CHEMBL1916899 1 7.76
CHEMBL1916893 1 7.63
CHEMBL1916901 1 7.49
CHEMBL1916716 1 7.37
CHEMBL1916887 1 7.35
CHEMBL1916884 1 7.27
CHEMBL1916900 1 6.84
CHEMBL1916902 1 6.64
CHEMBL1916903 1 6.19
CHEMBL1916715 1 -
CHEMBL1916890 1 -
CHEMBL1916886 1 -
CHEMBL1916883 1 -
CHEMBL1916879 1 -
CHEMBL1916719 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1916889 IC50 = 1.02 nM 8.99
CHEMBL1916881 IC50 = 2.0 nM 8.70
CHEMBL1916895 IC50 = 2.17 nM 8.66
CHEMBL1916898 IC50 = 2.41 nM 8.62
CHEMBL1916888 IC50 = 2.56 nM 8.59
CHEMBL1916718 IC50 = 3.165 nM 8.50
CHEMBL1916882 IC50 = 3.17 nM 8.50
CHEMBL1916891 IC50 = 3.41 nM 8.47
CHEMBL1916885 IC50 = 4.12 nM 8.38
CHEMBL1916896 IC50 = 4.4 nM 8.36
CHEMBL1916880 IC50 = 4.88 nM 8.31
CHEMBL1916897 IC50 = 5.84 nM 8.23
CHEMBL1916892 IC50 = 6.75 nM 8.17
CHEMBL1916894 IC50 = 8.08 nM 8.09
CHEMBL1916717 IC50 = 16.15 nM 7.79
CHEMBL1916899 IC50 = 17.4 nM 7.76
CHEMBL1916893 IC50 = 23.5 nM 7.63
CHEMBL1916901 IC50 = 32.3 nM 7.49
CHEMBL1916716 IC50 = 43.15 nM 7.37
CHEMBL1916887 IC50 = 44.9 nM 7.35
CHEMBL1916884 IC50 = 53.7 nM 7.27
CHEMBL1916900 IC50 = 144.0 nM 6.84
CHEMBL1916902 IC50 = 228.0 nM 6.64
CHEMBL1916903 IC50 = 651.0 nM 6.19
CHEMBL1916715 IC50 - -
CHEMBL1916890 IC50 - -
CHEMBL1916886 IC50 - -
CHEMBL1916883 IC50 - -
CHEMBL1916879 IC50 - -
CHEMBL1916719 IC50 - -