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Assay Detail

CHEMBL3888436

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

Binding
Btk 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.
ChEMBL ↗
76
Total Activities
44
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

Substituted tetrahydrocarbazole and carbazole carboxamide compounds
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 76 9.21 9.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3912426 — — 4 9.74
CHEMBL3891545 — — 2 9.72
CHEMBL3923822 — — 2 9.70
CHEMBL3910427 — — 1 9.60
CHEMBL3944101 — — 3 9.60
CHEMBL3928976 — — 2 9.59
CHEMBL3945408 — — 2 9.59
CHEMBL3894000 — — 3 9.59
CHEMBL3899411 — — 2 9.57
CHEMBL3945518 — — 1 9.52
CHEMBL3917869 — — 2 9.51
CHEMBL3907348 — — 3 9.48
CHEMBL3913962 — — 2 9.48
CHEMBL3943055 — — 2 9.48
CHEMBL3987197 — — 1 9.47
CHEMBL3984475 — — 2 9.47
CHEMBL3960384 — — 1 9.46
CHEMBL3908440 — — 2 9.46
CHEMBL3936249 — — 4 9.40
CHEMBL3932965 — — 1 9.39
CHEMBL3903416 — — 2 9.35
CHEMBL3896019 — — 5 9.35
CHEMBL3955854 — — 1 9.35
CHEMBL3954590 — — 2 9.33
CHEMBL4114536 — — 1 9.31
CHEMBL3965224 — — 1 9.31
CHEMBL3900554 BMS-986142 2.0 1 9.27
CHEMBL3901137 — — 2 9.25
CHEMBL3959154 — — 1 9.23
CHEMBL3946439 — — 1 9.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3912426 — IC50 = 0.18 nM 9.74
CHEMBL3891545 — IC50 = 0.19 nM 9.72
CHEMBL3923822 — IC50 = 0.2 nM 9.70
CHEMBL3891545 — IC50 = 0.22 nM 9.66
CHEMBL3944101 — IC50 = 0.25 nM 9.60
CHEMBL3910427 — IC50 = 0.25 nM 9.60
CHEMBL3894000 — IC50 = 0.26 nM 9.59
CHEMBL3945408 — IC50 = 0.26 nM 9.59
CHEMBL3928976 — IC50 = 0.26 nM 9.59
CHEMBL3899411 — IC50 = 0.27 nM 9.57
CHEMBL3944101 — IC50 = 0.28 nM 9.55
CHEMBL3945518 — IC50 = 0.3 nM 9.52
CHEMBL3917869 — IC50 = 0.31 nM 9.51
CHEMBL3894000 — IC50 = 0.32 nM 9.49
CHEMBL3943055 — IC50 = 0.33 nM 9.48
CHEMBL3907348 — IC50 = 0.33 nM 9.48
CHEMBL3913962 — IC50 = 0.33 nM 9.48
CHEMBL3987197 — IC50 = 0.34 nM 9.47
CHEMBL3917869 — IC50 = 0.34 nM 9.47
CHEMBL3984475 — IC50 = 0.34 nM 9.47
CHEMBL3908440 — IC50 = 0.35 nM 9.46
CHEMBL3960384 — IC50 = 0.35 nM 9.46
CHEMBL3936249 — IC50 = 0.4 nM 9.40
CHEMBL3932965 — IC50 = 0.41 nM 9.39
CHEMBL3912426 — IC50 = 0.41 nM 9.39
CHEMBL3913962 — IC50 = 0.44 nM 9.36
CHEMBL3903416 — IC50 = 0.45 nM 9.35
CHEMBL3955854 — IC50 = 0.45 nM 9.35
CHEMBL3896019 — IC50 = 0.45 nM 9.35
CHEMBL3907348 — IC50 = 0.46 nM 9.34
CHEMBL3923822 — IC50 = 0.46 nM 9.34
CHEMBL3984475 — IC50 = 0.46 nM 9.34
CHEMBL3954590 — IC50 = 0.47 nM 9.33
CHEMBL3907348 — IC50 = 0.48 nM 9.32
CHEMBL3896019 — IC50 = 0.48 nM 9.32
CHEMBL4114536 — IC50 = 0.49 nM 9.31
CHEMBL3965224 — IC50 = 0.49 nM 9.31
CHEMBL3900554 BMS-986142 IC50 = 0.54 nM 9.27
CHEMBL3928976 — IC50 = 0.55 nM 9.26
CHEMBL3901137 — IC50 = 0.56 nM 9.25
CHEMBL3959154 — IC50 = 0.59 nM 9.23
CHEMBL3896019 — IC50 = 0.59 nM 9.23
CHEMBL3945408 — IC50 = 0.62 nM 9.21
CHEMBL3946439 — IC50 = 0.62 nM 9.21
CHEMBL3918568 — IC50 = 0.65 nM 9.19
CHEMBL3896019 — IC50 = 0.65 nM 9.19
CHEMBL3931086 — IC50 = 0.66 nM 9.18
CHEMBL3894000 — IC50 = 0.77 nM 9.11
CHEMBL3896019 — IC50 = 0.79 nM 9.10
CHEMBL3895530 — IC50 = 0.81 nM 9.09