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Assay Detail

CHEMBL3887135

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Binding
Enzymatic Activity Assay: A Caliper-based kinase assay (Caliper Life Sciences, Hopkinton, Mass.) was used to measure inhibition of Btk kinase activity of a compound of Formula (IA), (I′) or (I). Serial dilutions of test compounds were incubated with human recombinant Btk (2 nM), ATP (40 μM) and a phosphoacceptor peptide substrate FAM-GEEPLYWSFPAKKK-NH2 (1 μM) at room temperature for 3 h. The reaction was then terminated with EDTA, final concentration 20 mM and the phosphorylated reaction product was quantified on a Caliper Desktop Profiler (Caliper LabChip 3000). Percent inhibition was calculated for each compound dilution and the concentration that produced 50% inhibition was calculated.
ChEMBL ↗
104
Total Activities
98
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Tyrosine kinase inhibitors
(2015)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 104 8.14 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4114726 — — 1 9.40
CHEMBL3902317 — — 1 9.40
CHEMBL4114690 — — 1 9.22
CHEMBL4114762 — — 1 9.15
CHEMBL6029336 — — 2 9.15
CHEMBL4114774 — — 1 9.05
CHEMBL4114748 — — 1 9.00
CHEMBL4114799 — — 1 9.00
CHEMBL4114765 — — 2 8.89
CHEMBL4114795 — — 1 8.89
CHEMBL4114695 — — 1 8.85
CHEMBL3894014 — — 1 8.82
CHEMBL4114718 — — 1 8.80
CHEMBL4114702 — — 1 8.77
CHEMBL3972359 — — 2 8.77
CHEMBL4114764 — — 1 8.74
CHEMBL3975610 — — 1 8.74
CHEMBL4109651 — — 1 8.70
CHEMBL4114679 — — 1 8.70
CHEMBL4114753 — — 1 8.70
CHEMBL4114802 — — 1 8.70
CHEMBL4114691 — — 1 8.70
CHEMBL4114766 ATUZABRUTINIB 2.0 1 8.70
CHEMBL4114740 — — 1 8.68
CHEMBL4114723 — — 1 8.66
CHEMBL4114800 — — 1 8.64
CHEMBL4114773 — — 1 8.59
CHEMBL3901377 — — 1 8.55
CHEMBL6015630 — — 1 8.52
CHEMBL3918201 — — 1 8.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3902317 — IC50 = 0.4 nM 9.40
CHEMBL4114726 — IC50 = 0.4 nM 9.40
CHEMBL4114690 — IC50 = 0.6 nM 9.22
CHEMBL6029336 — IC50 = 0.7 nM 9.15
CHEMBL4114762 — IC50 = 0.7 nM 9.15
CHEMBL4114774 — IC50 = 0.9 nM 9.05
CHEMBL4114799 — IC50 = 1.0 nM 9.00
CHEMBL4114748 — IC50 = 1.0 nM 9.00
CHEMBL4114765 — IC50 = 1.3 nM 8.89
CHEMBL4114795 — IC50 = 1.3 nM 8.89
CHEMBL4114695 — IC50 = 1.4 nM 8.85
CHEMBL3894014 — IC50 = 1.5 nM 8.82
CHEMBL4114718 — IC50 = 1.6 nM 8.80
CHEMBL4114702 — IC50 = 1.7 nM 8.77
CHEMBL3972359 — IC50 = 1.7 nM 8.77
CHEMBL4114764 — IC50 = 1.8 nM 8.74
CHEMBL3975610 — IC50 = 1.8 nM 8.74
CHEMBL4114766 ATUZABRUTINIB IC50 = 2.0 nM 8.70
CHEMBL4114691 — IC50 = 2.0 nM 8.70
CHEMBL4114802 — IC50 = 2.0 nM 8.70
CHEMBL4114679 — IC50 = 2.0 nM 8.70
CHEMBL4109651 — IC50 = 2.0 nM 8.70
CHEMBL4114753 — IC50 = 2.0 nM 8.70
CHEMBL4114740 — IC50 = 2.1 nM 8.68
CHEMBL4114723 — IC50 = 2.2 nM 8.66
CHEMBL4114800 — IC50 = 2.3 nM 8.64
CHEMBL4114773 — IC50 = 2.6 nM 8.59
CHEMBL4114765 — IC50 = 2.7 nM 8.57
CHEMBL3901377 — IC50 = 2.8 nM 8.55
CHEMBL3918201 — IC50 = 3.0 nM 8.52
CHEMBL4114772 — IC50 = 3.0 nM 8.52
CHEMBL6015630 — IC50 = 3.0 nM 8.52
CHEMBL4114665 — IC50 = 3.0 nM 8.52
CHEMBL4114703 — IC50 = 3.0 nM 8.52
CHEMBL3972359 — IC50 = 3.1 nM 8.51
CHEMBL6029336 — IC50 = 3.2 nM 8.49
CHEMBL3984974 — IC50 = 3.2 nM 8.49
CHEMBL4109432 — IC50 = 3.3 nM 8.48
CHEMBL4114808 — IC50 = 3.6 nM 8.44
CHEMBL3980841 — IC50 = 3.7 nM 8.43
CHEMBL3957855 — IC50 = 3.7 nM 8.43
CHEMBL3940151 — IC50 = 3.8 nM 8.42
CHEMBL4114678 — IC50 = 4.0 nM 8.40
CHEMBL4115689 — IC50 = 4.0 nM 8.40
CHEMBL4114689 — IC50 = 4.0 nM 8.40
CHEMBL4114704 — IC50 = 4.2 nM 8.38
CHEMBL4114770 — IC50 = 4.3 nM 8.37
CHEMBL4114732 — IC50 = 4.4 nM 8.36
CHEMBL4114699 — IC50 = 4.4 nM 8.36
CHEMBL5874026 — IC50 = 4.8 nM 8.32