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Assay Detail

CHEMBL5735104

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

Binding
Enzyme Assay: To V-bottom 384-well plates were added test compounds, human recombinant Btk (1 nM, Invitrogen Corporation), fluoresceinated peptide (1.5 μM), ATP (20 μM), and assay buffer (20 mM HEPES pH 7.4, 10 mM MgCl2, 0.015% Brij 35 surfactant and 4 mM DTT in 1.6% DMSO), with a final volume of 30 μL. After incubating at room temperature for 60 min., the reaction was terminated by adding 45 μL of 35 mM EDTA to each sample. The reaction mixture was analyzed on the Caliper LABCHIP® 3000 (Caliper, Hopkinton, Mass.) by electrophoretic separation of the fluorescent substrate and phosphorylated product. Inhibition data were calculated by comparison to control reactions with no enzyme (for 100% inhibition) and controls with no inhibitor (for 0% inhibition).
ChEMBL ↗
786
Total Activities
222
Compounds Tested
3
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

Indole carboxamide compounds
(2020)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 262 8.48 10.40
kon 262 - -
k_off 262 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5945342 — — 9 10.40
CHEMBL5826570 — — 6 10.40
CHEMBL5741138 — — 3 10.30
CHEMBL5824452 — — 9 10.28
CHEMBL5993286 — — 3 10.22
CHEMBL5836429 — — 3 10.22
CHEMBL4237999 — — 3 10.15
CHEMBL4242527 — — 3 10.10
CHEMBL5868886 — — 12 10.10
CHEMBL5824706 — — 3 10.05
CHEMBL5886785 — — 6 10.05
CHEMBL6048314 — — 6 10.05
CHEMBL5846574 — — 3 10.03
CHEMBL6029889 — — 3 10.00
CHEMBL4648442 — — 3 10.00
CHEMBL5867898 — — 6 10.00
CHEMBL5788106 — — 9 10.00
CHEMBL4246324 — — 3 9.96
CHEMBL4297674 BRANEBRUTINIB 2.0 3 9.96
CHEMBL5913535 — — 3 9.92
CHEMBL5843716 — — 3 9.92
CHEMBL5929460 — — 9 9.92
CHEMBL5841256 — — 3 9.89
CHEMBL5946541 — — 9 9.89
CHEMBL5837508 — — 3 9.85
CHEMBL4248386 — — 3 9.85
CHEMBL4634162 — — 3 9.85
CHEMBL5804765 — — 3 9.85
CHEMBL5821781 — — 3 9.85
CHEMBL6004994 — — 9 9.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5826570 — IC50 = 0.04 nM 10.40
CHEMBL5945342 — IC50 = 0.04 nM 10.40
CHEMBL5741138 — IC50 = 0.05 nM 10.30
CHEMBL5824452 — IC50 = 0.052 nM 10.28
CHEMBL5993286 — IC50 = 0.06 nM 10.22
CHEMBL5836429 — IC50 = 0.06 nM 10.22
CHEMBL4237999 — IC50 = 0.07 nM 10.15
CHEMBL4242527 — IC50 = 0.08 nM 10.10
CHEMBL5868886 — IC50 = 0.08 nM 10.10
CHEMBL5886785 — IC50 = 0.09 nM 10.05
CHEMBL5824706 — IC50 = 0.09 nM 10.05
CHEMBL6048314 — IC50 = 0.09 nM 10.05
CHEMBL5846574 — IC50 = 0.094 nM 10.03
CHEMBL5886785 — IC50 = 0.1 nM 10.00
CHEMBL5867898 — IC50 = 0.1 nM 10.00
CHEMBL6029889 — IC50 = 0.1 nM 10.00
CHEMBL4648442 — IC50 = 0.1 nM 10.00
CHEMBL5788106 — IC50 = 0.1 nM 10.00
CHEMBL4297674 BRANEBRUTINIB IC50 = 0.11 nM 9.96
CHEMBL4246324 — IC50 = 0.11 nM 9.96
CHEMBL5913535 — IC50 = 0.12 nM 9.92
CHEMBL5929460 — IC50 = 0.12 nM 9.92
CHEMBL5843716 — IC50 = 0.12 nM 9.92
CHEMBL5788106 — IC50 = 0.13 nM 9.89
CHEMBL5841256 — IC50 = 0.13 nM 9.89
CHEMBL5946541 — IC50 = 0.13 nM 9.89
CHEMBL4634162 — IC50 = 0.14 nM 9.85
CHEMBL4248386 — IC50 = 0.14 nM 9.85
CHEMBL5821781 — IC50 = 0.14 nM 9.85
CHEMBL5804765 — IC50 = 0.14 nM 9.85
CHEMBL5837508 — IC50 = 0.14 nM 9.85
CHEMBL6004994 — IC50 = 0.15 nM 9.82
CHEMBL5764705 — IC50 = 0.15 nM 9.82
CHEMBL5946541 — IC50 = 0.16 nM 9.80
CHEMBL5913052 — IC50 = 0.17 nM 9.77
CHEMBL6062429 — IC50 = 0.17 nM 9.77
CHEMBL6004994 — IC50 = 0.17 nM 9.77
CHEMBL5824452 — IC50 = 0.19 nM 9.72
CHEMBL5863112 — IC50 = 0.19 nM 9.72
CHEMBL6010840 — IC50 = 0.2 nM 9.70
CHEMBL5830639 — IC50 = 0.2 nM 9.70
CHEMBL5954771 — IC50 = 0.2 nM 9.70
CHEMBL5881482 — IC50 = 0.2 nM 9.70
CHEMBL5918908 — IC50 = 0.2 nM 9.70
CHEMBL6030977 — IC50 = 0.2 nM 9.70
CHEMBL5846842 — IC50 = 0.2 nM 9.70
CHEMBL6056935 — IC50 = 0.21 nM 9.68
CHEMBL4243995 — IC50 = 0.21 nM 9.68
CHEMBL5929460 — IC50 = 0.23 nM 9.64
CHEMBL4247992 — IC50 = 0.23 nM 9.64