Assay Detail
Binding
CHEMBL5731735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
V9103X ADP-Glo Kinase Assay Custom: In a 384-well plate, test compound diluted in assay buffer (1% DMSO final) is mixed with 8His-RIPK2 FL enzyme (final concentration of 8 nM). After 15 minutes of pre-incubation at RT, ATP dissolved in assay buffer is added (final concentration 5 μM). The mixture is incubated for 60 minutes at 37° C. in a humidified incubator. Then, ADP Glo Reagent is added, followed by a 40 minute incubation at rt. Finally, Kinase Detection Reagent is added and the entire mixture is incubated for 40 min at RT. The luminescence signal is measured with an Envision reader to determine the amount of ADP produced. Assay buffer: 25 mM HEPES (4-(2-hydroxyethyl)-1-piperazinethanesulfonic acid), 0.1% BSA (bovine serum albumin), 10 mM MgCl2, 5 mM MnCl2, 50 mM KCl, 0.01% CHAPS (3-[(3-cholamidopropyl)dimethylammonio]-1-propanesulfonate), 10 μM Na3VO4, 1 mM DTT (dithiothreitol), pH 7.5 All plates contain wells with vehicle controls instead of compound (1% DMSO) as reference for the high signal (100% CTL (100% of control), high signal), and wells without enzyme as reference for low signal (0% CTL, low signal). The luminescent signal generated is proportional to the ADP produced and is correlated with enzyme activity. The analysis of the data is performed by the calculation of the percentage of ADP production in the presence of the test compound and RIPK2 as compared to the ADP production in the presence of RIPK2 plus 50 μM Gefitinib.
366
Total Activities
120
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Receptor-interacting serine/threonine-protein kinase 2 (CHEMBL5014) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted benzamides as RIPK2 inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 122 | 8.17 | 9.21 |
| kon | 122 | - | - |
| k_off | 122 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5742848 | — | — | 3 | 9.21 |
| CHEMBL5840021 | — | — | 6 | 9.09 |
| CHEMBL6002258 | — | — | 3 | 9.05 |
| CHEMBL5851050 | — | — | 3 | 9.03 |
| CHEMBL5816850 | — | — | 3 | 9.02 |
| CHEMBL5845929 | — | — | 3 | 9.00 |
| CHEMBL5951662 | — | — | 3 | 9.00 |
| CHEMBL5858920 | — | — | 3 | 9.00 |
| CHEMBL6016366 | — | — | 3 | 8.96 |
| CHEMBL6034661 | — | — | 3 | 8.96 |
| CHEMBL5804402 | — | — | 3 | 8.96 |
| CHEMBL5983278 | — | — | 3 | 8.96 |
| CHEMBL6012062 | — | — | 3 | 8.92 |
| CHEMBL5929812 | — | — | 3 | 8.92 |
| CHEMBL5838688 | — | — | 3 | 8.89 |
| CHEMBL5805040 | — | — | 3 | 8.89 |
| CHEMBL6061078 | — | — | 3 | 8.85 |
| CHEMBL6046757 | — | — | 3 | 8.82 |
| CHEMBL5747138 | — | — | 3 | 8.82 |
| CHEMBL5991605 | — | — | 3 | 8.82 |
| CHEMBL5771148 | — | — | 3 | 8.82 |
| CHEMBL5767751 | — | — | 3 | 8.82 |
| CHEMBL5994917 | — | — | 3 | 8.80 |
| CHEMBL5883163 | — | — | 3 | 8.80 |
| CHEMBL5843149 | — | — | 3 | 8.80 |
| CHEMBL6025639 | — | — | 3 | 8.77 |
| CHEMBL5867405 | — | — | 3 | 8.77 |
| CHEMBL6007423 | — | — | 3 | 8.74 |
| CHEMBL5812031 | — | — | 3 | 8.74 |
| CHEMBL5869358 | — | — | 3 | 8.74 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5742848 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL5840021 | — | IC50 | = | 0.81 | nM | 9.09 |
| CHEMBL6002258 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL5851050 | — | IC50 | = | 0.94 | nM | 9.03 |
| CHEMBL5816850 | — | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL5858920 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5845929 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5951662 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL6016366 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5983278 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5804402 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6034661 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL6012062 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5929812 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL5838688 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5805040 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5840021 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL6061078 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5767751 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5747138 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5771148 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL6046757 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5991605 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5843149 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5883163 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5994917 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL6025639 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5867405 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5774824 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL6007423 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5812031 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5869358 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5779258 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5896310 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5811547 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL5780739 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL6014111 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5764888 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5788448 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5741982 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5851139 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL5828620 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5850124 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5751132 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL6004049 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL6040168 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL5887420 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5944666 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL5780702 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL5865109 | — | IC50 | = | 3.4 | nM | 8.47 |