Assay Detail
Binding
CHEMBL3887327
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinase Glo Plus 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 .mu.M 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.
239
Total Activities
237
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 |
Publication
Heterocyclic compounds containing an indole core
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 239 | 7.50 | 9.74 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3956539 | — | — | 1 | 9.74 |
| CHEMBL3945993 | — | — | 1 | 9.60 |
| CHEMBL3903528 | — | — | 1 | 9.42 |
| CHEMBL3900064 | — | — | 1 | 9.38 |
| CHEMBL3959915 | — | — | 1 | 9.23 |
| CHEMBL4109143 | — | — | 1 | 9.22 |
| CHEMBL3955947 | — | — | 1 | 9.22 |
| CHEMBL3908561 | — | — | 1 | 9.21 |
| CHEMBL3972132 | — | — | 1 | 9.20 |
| CHEMBL4108521 | — | — | 1 | 9.19 |
| CHEMBL4113357 | — | — | 1 | 9.15 |
| CHEMBL4111661 | — | — | 1 | 9.15 |
| CHEMBL3951802 | — | — | 1 | 9.11 |
| CHEMBL3985027 | — | — | 1 | 9.05 |
| CHEMBL1933288 | — | — | 1 | 8.96 |
| CHEMBL1933280 | — | — | 1 | 8.96 |
| CHEMBL3939884 | — | — | 1 | 8.89 |
| CHEMBL3942136 | — | — | 1 | 8.89 |
| CHEMBL4112559 | — | — | 1 | 8.85 |
| CHEMBL3918100 | — | — | 1 | 8.80 |
| CHEMBL3904474 | — | — | 1 | 8.74 |
| CHEMBL3963988 | — | — | 1 | 8.74 |
| CHEMBL3900130 | — | — | 1 | 8.74 |
| CHEMBL3980724 | — | — | 1 | 8.72 |
| CHEMBL4113926 | — | — | 2 | 8.72 |
| CHEMBL4109800 | — | — | 1 | 8.72 |
| CHEMBL1933278 | — | — | 1 | 8.72 |
| CHEMBL3965519 | — | — | 1 | 8.70 |
| CHEMBL3910099 | — | — | 1 | 8.70 |
| CHEMBL4111985 | — | — | 2 | 8.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3956539 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL3945993 | — | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL3903528 | — | IC50 | = | 0.38 | nM | 9.42 |
| CHEMBL3900064 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL3959915 | — | IC50 | = | 0.59 | nM | 9.23 |
| CHEMBL4109143 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3955947 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3908561 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL3972132 | — | IC50 | = | 0.63 | nM | 9.20 |
| CHEMBL4108521 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL4113357 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL4111661 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL3951802 | — | IC50 | = | 0.77 | nM | 9.11 |
| CHEMBL3985027 | — | IC50 | = | 0.89 | nM | 9.05 |
| CHEMBL1933288 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1933280 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3942136 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3939884 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4112559 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3918100 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3900130 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3963988 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3904474 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL4113926 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3980724 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL4109800 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL1933278 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3965519 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3910099 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3966733 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL4111985 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3969149 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3946668 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3917125 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3916626 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4107750 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL4110776 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1933142 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL3936149 | — | IC50 | = | 3.8 | nM | 8.42 |
| CHEMBL3916789 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3921354 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4108963 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1938803 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL1933287 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3941501 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3955733 | — | IC50 | = | 4.8 | nM | 8.32 |
| CHEMBL3912033 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL3961025 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3981684 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL3917267 | — | IC50 | = | 5.2 | nM | 8.28 |