Assay Detail
Binding
CHEMBL5733481
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Human Recombinant 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. Inhibition data were calculated by comparison to no enzyme control reactions for 100% inhibition and no inhibitor controls for 0% inhibition. Dose response curves were generated to determine the concentration required for inhibiting 50% of kinase activity (IC50). Compounds were dissolved at 10 mM in DMSO and evaluated at eleven concentrations.
600
Total Activities
167
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 |
Publication
Carbazole derivatives
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 200 | 9.18 | 10.34 |
| kon | 200 | - | - |
| k_off | 200 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5909954 | — | — | 3 | 10.34 |
| CHEMBL5789446 | — | — | 6 | 10.33 |
| CHEMBL5749648 | — | — | 3 | 10.31 |
| CHEMBL5858594 | — | — | 9 | 10.30 |
| CHEMBL5799170 | — | — | 3 | 10.30 |
| CHEMBL5772754 | — | — | 3 | 10.29 |
| CHEMBL5848923 | — | — | 3 | 10.28 |
| CHEMBL5983201 | — | — | 3 | 10.21 |
| CHEMBL6042416 | — | — | 6 | 10.17 |
| CHEMBL5819531 | — | — | 3 | 10.16 |
| CHEMBL5862023 | — | — | 9 | 10.15 |
| CHEMBL5808322 | — | — | 3 | 10.14 |
| CHEMBL5958946 | — | — | 3 | 10.12 |
| CHEMBL6053298 | — | — | 6 | 10.12 |
| CHEMBL5989288 | — | — | 3 | 10.11 |
| CHEMBL4240879 | — | — | 3 | 10.10 |
| CHEMBL5935683 | — | — | 3 | 10.06 |
| CHEMBL5965184 | — | — | 9 | 10.05 |
| CHEMBL5935718 | — | — | 6 | 10.05 |
| CHEMBL6057626 | — | — | 3 | 10.02 |
| CHEMBL5863409 | — | — | 3 | 10.02 |
| CHEMBL5801580 | — | — | 3 | 10.00 |
| CHEMBL5958902 | — | — | 3 | 10.00 |
| CHEMBL5891936 | — | — | 3 | 10.00 |
| CHEMBL5942743 | — | — | 3 | 10.00 |
| CHEMBL5847252 | — | — | 12 | 10.00 |
| CHEMBL5948678 | — | — | 3 | 10.00 |
| CHEMBL5793001 | — | — | 3 | 10.00 |
| CHEMBL5931695 | — | — | 3 | 10.00 |
| CHEMBL5884381 | — | — | 3 | 10.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5909954 | — | IC50 | = | 0.046 | nM | 10.34 |
| CHEMBL5789446 | — | IC50 | = | 0.047 | nM | 10.33 |
| CHEMBL5749648 | — | IC50 | = | 0.049 | nM | 10.31 |
| CHEMBL5799170 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5858594 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5772754 | — | IC50 | = | 0.051 | nM | 10.29 |
| CHEMBL5848923 | — | IC50 | = | 0.052 | nM | 10.28 |
| CHEMBL5983201 | — | IC50 | = | 0.061 | nM | 10.21 |
| CHEMBL6042416 | — | IC50 | = | 0.067 | nM | 10.17 |
| CHEMBL5819531 | — | IC50 | = | 0.069 | nM | 10.16 |
| CHEMBL5862023 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL6042416 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5808322 | — | IC50 | = | 0.073 | nM | 10.14 |
| CHEMBL5958946 | — | IC50 | = | 0.076 | nM | 10.12 |
| CHEMBL6053298 | — | IC50 | = | 0.075 | nM | 10.12 |
| CHEMBL5989288 | — | IC50 | = | 0.078 | nM | 10.11 |
| CHEMBL4240879 | — | IC50 | = | 0.079 | nM | 10.10 |
| CHEMBL5858594 | — | IC50 | = | 0.087 | nM | 10.06 |
| CHEMBL5935683 | — | IC50 | = | 0.088 | nM | 10.06 |
| CHEMBL5935718 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5965184 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL6057626 | — | IC50 | = | 0.095 | nM | 10.02 |
| CHEMBL5863409 | — | IC50 | = | 0.095 | nM | 10.02 |
| CHEMBL5965184 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5884381 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5891936 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5958902 | — | IC50 | = | 0.099 | nM | 10.00 |
| CHEMBL5931695 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5942743 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5847252 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5793001 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5948678 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5801580 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL6053298 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5755283 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL5968758 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL6054817 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL5944790 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5948732 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5793668 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5988397 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL5808911 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5789446 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL5973174 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL5959900 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL6038830 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4248271 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5920793 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4248271 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL4248719 | — | IC50 | = | 0.17 | nM | 9.77 |