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Assay Detail

CHEMBL4000360

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

Binding
Inhibition of BTK in human Ramos cells assessed as inhibition of anti human IgM-induced calcium influx preincubated for 20 mins in dark followed by anti human IgM induction for 8 mins by FLIPR assay
24
Total Activities
24
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 BTK (CHEMBL5251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Pyrrolo[2,3-b]pyridine derivatives as potent Bruton's tyrosine kinase inhibitors.
Zhao X, Huang W, Wang Y, Xin M, Jin Q, Cai J, Tang F, Zhao Y, Xiang H.
Bioorg Med Chem (2015) 23 : 4344 -4353
PubMed 26169764 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.31 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4101864 1 8.52
CHEMBL4079989 1 8.52
CHEMBL4083867 1 8.02
CHEMBL4087347 1 7.92
CHEMBL4095573 1 7.85
CHEMBL4105206 1 7.80
CHEMBL3402584 1 7.67
CHEMBL4085393 1 7.57
CHEMBL2057918 1 7.56
CHEMBL4073491 1 7.50
CHEMBL4075160 1 7.38
CHEMBL4064893 1 7.28
CHEMBL4093393 1 7.25
CHEMBL4091642 1 7.16
CHEMBL4086354 1 7.16
CHEMBL4094133 1 7.03
CHEMBL4097010 1 7.03
CHEMBL4081221 1 6.96
CHEMBL4063859 1 6.71
CHEMBL4105470 1 6.67
CHEMBL4070603 1 6.46
CHEMBL4103325 1 6.39
CHEMBL4065778 1 5.62
CHEMBL4087870 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4101864 IC50 = 3.0 nM 8.52
CHEMBL4079989 IC50 = 3.0 nM 8.52
CHEMBL4083867 IC50 = 9.5 nM 8.02
CHEMBL4087347 IC50 = 12.0 nM 7.92
CHEMBL4095573 IC50 = 14.0 nM 7.85
CHEMBL4105206 IC50 = 16.0 nM 7.80
CHEMBL3402584 IC50 = 21.6 nM 7.67
CHEMBL4085393 IC50 = 27.0 nM 7.57
CHEMBL2057918 IC50 = 27.3 nM 7.56
CHEMBL4073491 IC50 = 32.0 nM 7.50
CHEMBL4075160 IC50 = 42.0 nM 7.38
CHEMBL4064893 IC50 = 52.0 nM 7.28
CHEMBL4093393 IC50 = 56.3 nM 7.25
CHEMBL4091642 IC50 = 69.0 nM 7.16
CHEMBL4086354 IC50 = 69.0 nM 7.16
CHEMBL4094133 IC50 = 94.2 nM 7.03
CHEMBL4097010 IC50 = 92.7 nM 7.03
CHEMBL4081221 IC50 = 110.0 nM 6.96
CHEMBL4063859 IC50 = 196.0 nM 6.71
CHEMBL4105470 IC50 = 213.0 nM 6.67
CHEMBL4070603 IC50 = 350.0 nM 6.46
CHEMBL4103325 IC50 = 410.0 nM 6.39
CHEMBL4065778 IC50 = 2410.0 nM 5.62
CHEMBL4087870 IC50 > 5000.0 nM -