Assay Detail
Binding
CHEMBL3706312
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Glo Assay: Human RSK2 protein, purchased from Invitrogen, is used to measure kinase activity utilizing Kinase Glo Plus (Promega) a homogeneous assay technology, which uses a luciferin-luciferase based ATP detection reagent to quantify residual ATP. The assay is performed using 0.75 nM His-RSK2, 0.75 uM ATP and 1.0 uM S6 Kinase/RSK Substrate Peptide 1 (Upstate, catalog #12-124), in assay buffer consisting of 25 mM HEPES, pH 7.5, 10 mM MgCl2, 5 mM MnCl2, 50 mM KCl, 0.2% BSA, 0.01% CHAPS, 100 uM Na3VO4, 0.5 mM DTT, and 1% DMSO. Solutions of test compounds at various concentrations are prepared by 1:3 fold serial dilution of a 1 mM solution of compound in DMSO. The DMSO solutions are further diluted with assay buffer to a final concentration of DMSO of 5%.The assay is performed in a 384 well, white, non-binding plate (Corning, catalogue #3574). Solutions of test compounds (10 uL) are transferred to a dry assay plate, followed by addition of 20 uL kinase.
105
Total Activities
105
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 |
Publication
Heterocyclic compounds containing a pyrrolopyridine or benzimidazole core
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 105 | 7.39 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3673622 | — | — | 1 | 9.70 |
| CHEMBL3673631 | — | — | 1 | 9.57 |
| CHEMBL3673624 | — | — | 1 | 9.47 |
| CHEMBL3673609 | — | — | 1 | 9.41 |
| CHEMBL3673603 | — | — | 1 | 9.11 |
| CHEMBL3673606 | — | — | 1 | 8.96 |
| CHEMBL3673598 | — | — | 1 | 8.80 |
| CHEMBL3639725 | — | — | 1 | 8.80 |
| CHEMBL3673592 | — | — | 1 | 8.68 |
| CHEMBL3673589 | — | — | 1 | 8.64 |
| CHEMBL3673595 | — | — | 1 | 8.64 |
| CHEMBL3673648 | — | — | 1 | 8.59 |
| CHEMBL3673625 | — | — | 1 | 8.52 |
| CHEMBL3673627 | — | — | 1 | 8.52 |
| CHEMBL3673657 | — | — | 1 | 8.48 |
| CHEMBL3673658 | — | — | 1 | 8.44 |
| CHEMBL3673601 | — | — | 1 | 8.42 |
| CHEMBL3673610 | — | — | 1 | 8.42 |
| CHEMBL3673661 | — | — | 1 | 8.41 |
| CHEMBL3673629 | — | — | 1 | 8.40 |
| CHEMBL3673644 | — | — | 1 | 8.37 |
| CHEMBL3673581 | — | — | 1 | 8.33 |
| CHEMBL3673604 | — | — | 1 | 8.32 |
| CHEMBL3673662 | — | — | 1 | 8.29 |
| CHEMBL3673645 | — | — | 1 | 8.28 |
| CHEMBL3673567 | — | — | 1 | 8.26 |
| CHEMBL3673630 | — | — | 1 | 8.21 |
| CHEMBL3673647 | — | — | 1 | 8.18 |
| CHEMBL3673612 | — | — | 1 | 8.17 |
| CHEMBL3673586 | — | — | 1 | 8.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3673622 | — | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL3673631 | — | IC50 | = | 0.27 | nM | 9.57 |
| CHEMBL3673624 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL3673609 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL3673603 | — | IC50 | = | 0.78 | nM | 9.11 |
| CHEMBL3673606 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3639725 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3673598 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3673592 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3673589 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3673595 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3673648 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3673625 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673627 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3673657 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3673658 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL3673610 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3673601 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3673661 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL3673629 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3673644 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL3673581 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL3673604 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3673662 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3673645 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL3673567 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL3673630 | — | IC50 | = | 6.1 | nM | 8.21 |
| CHEMBL3673647 | — | IC50 | = | 6.6 | nM | 8.18 |
| CHEMBL3673612 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL3673586 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL3673607 | — | IC50 | = | 9.7 | nM | 8.01 |
| CHEMBL3673636 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL3673623 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3673611 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3673659 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3673599 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3673632 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3673667 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3673642 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3673643 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3673588 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3673596 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3673580 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3673600 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3673593 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3673635 | — | IC50 | = | 26.5 | nM | 7.58 |
| CHEMBL3673633 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3673640 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3639724 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL3673628 | — | IC50 | = | 34.0 | nM | 7.47 |