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Assay Detail

CHEMBL3789512

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Functional
Antiproliferative activity against B cells (unknown origin)
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Not specified
Cell Type B-cell
Confidence 1 — Organism
Curated By Autocuration

Publication

Approaching the active conformation of 1,3-diaminopyrimidine based covalent inhibitors of Bruton's tyrosine kinase for treatment of Rheumatoid arthritis.
Huang Z, Zhang Q, Yan L, Zhong G, Zhang L, Tan X, Wang Y.
Bioorg Med Chem Lett (2016) 26 : 1954 -1957
PubMed 26976214 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.70 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3301625 SPEBRUTINIB 2.0 1 8.48
CHEMBL3785165 1 8.45
CHEMBL3786656 1 8.23
CHEMBL3787191 1 8.16
CHEMBL3785329 1 7.86
CHEMBL3786931 1 7.83
CHEMBL3787055 1 7.71
CHEMBL3787531 1 7.51
CHEMBL3787615 1 7.19
CHEMBL3787217 1 7.15
CHEMBL3787671 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3301625 SPEBRUTINIB IC50 = 3.28 nM 8.48
CHEMBL3785165 IC50 = 3.55 nM 8.45
CHEMBL3786656 IC50 = 5.85 nM 8.23
CHEMBL3787191 IC50 = 6.84 nM 8.16
CHEMBL3785329 IC50 = 13.7 nM 7.86
CHEMBL3786931 IC50 = 14.9 nM 7.83
CHEMBL3787055 IC50 = 19.4 nM 7.71
CHEMBL3787531 IC50 = 30.6 nM 7.51
CHEMBL3787615 IC50 = 64.0 nM 7.19
CHEMBL3787217 IC50 = 70.6 nM 7.15
CHEMBL3787671 IC50 = 818.4 nM 6.09