Assay Detail
Binding
CHEMBL5731508
Review assay metadata, readout intent, target linkage, and publication context from the same page.
CaMKII Cell-Based Activity: CaMKII activity in neonatal rat ventricular myocytes (NRVM) was measured by monitoring the phosphorylation level of phospholamban using high-content imaging. NRVMs were plated in a clear bottom 384-well plate in medium supplemented with 10% fetal bovine serum (FBS) and incubated at 37° C., 5% CO2 overnight. The medium was changed to a serum-free medium and compounds were dosed to the cells. The cells were incubated at 37° C., 5% CO2 for 4 hours and were then treated with 100 nM ATX-II (Alomone Labs) to activate CaMKII. 10 minutes after the addition of ATX-II, the cells were fixed with 4% formaldehyde followed by permeabilization with 0.1% triton X100. The fixed cells were stained with an anti-phospho-phospholamban primary antibody (Santa Cruz Biotechnology) and an Alexa488-labeled anti-rabbit IgG secondary antibody (Life Technologies Corporation) as well as Hoechst 33342 (Life Technologies Corporation). The cells were imaged using an ArrayScan VTI (Cellomics) and analyzed for cells containing a positive fluorescent signal at 485 nm, reported as % responder. The % responders were plotted against the compound concentration to determine the compounds EC50.
1053
Total Activities
348
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Fused heterocyclic compounds as CaM kinase inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 351 | 7.17 | 8.43 |
| kon | 351 | - | - |
| k_off | 351 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5841176 | — | — | 3 | 8.43 |
| CHEMBL5905566 | — | — | 3 | 8.17 |
| CHEMBL6050872 | — | — | 3 | 8.11 |
| CHEMBL5913003 | — | — | 3 | 8.09 |
| CHEMBL5936326 | — | — | 3 | 8.09 |
| CHEMBL5744772 | — | — | 3 | 8.08 |
| CHEMBL6012320 | — | — | 3 | 8.08 |
| CHEMBL5980464 | — | — | 3 | 8.04 |
| CHEMBL6053260 | — | — | 3 | 8.03 |
| CHEMBL5843416 | — | — | 3 | 8.03 |
| CHEMBL5881265 | — | — | 3 | 8.02 |
| CHEMBL5791419 | — | — | 3 | 8.02 |
| CHEMBL6048307 | — | — | 3 | 8.01 |
| CHEMBL6027005 | — | — | 3 | 8.01 |
| CHEMBL5853644 | — | — | 3 | 8.00 |
| CHEMBL5984266 | — | — | 3 | 7.98 |
| CHEMBL5830783 | — | — | 3 | 7.97 |
| CHEMBL6045601 | — | — | 3 | 7.95 |
| CHEMBL5850378 | — | — | 3 | 7.93 |
| CHEMBL6036514 | — | — | 3 | 7.91 |
| CHEMBL5743795 | — | — | 3 | 7.89 |
| CHEMBL6022147 | — | — | 3 | 7.87 |
| CHEMBL5837905 | — | — | 3 | 7.87 |
| CHEMBL5969331 | — | — | 3 | 7.86 |
| CHEMBL5740310 | — | — | 3 | 7.86 |
| CHEMBL4215300 | — | — | 3 | 7.86 |
| CHEMBL5821085 | — | — | 3 | 7.86 |
| CHEMBL6031274 | — | — | 3 | 7.85 |
| CHEMBL5990615 | — | — | 3 | 7.84 |
| CHEMBL5847367 | — | — | 3 | 7.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5841176 | — | EC50 | = | 3.75 | nM | 8.43 |
| CHEMBL5905566 | — | EC50 | = | 6.81 | nM | 8.17 |
| CHEMBL6050872 | — | EC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5936326 | — | EC50 | = | 8.2 | nM | 8.09 |
| CHEMBL5913003 | — | EC50 | = | 8.15 | nM | 8.09 |
| CHEMBL5744772 | — | EC50 | = | 8.28 | nM | 8.08 |
| CHEMBL6012320 | — | EC50 | = | 8.24 | nM | 8.08 |
| CHEMBL5980464 | — | EC50 | = | 9.07 | nM | 8.04 |
| CHEMBL5843416 | — | EC50 | = | 9.37 | nM | 8.03 |
| CHEMBL6053260 | — | EC50 | = | 9.45 | nM | 8.03 |
| CHEMBL5791419 | — | EC50 | = | 9.53 | nM | 8.02 |
| CHEMBL5881265 | — | EC50 | = | 9.6 | nM | 8.02 |
| CHEMBL6048307 | — | EC50 | = | 9.83 | nM | 8.01 |
| CHEMBL6027005 | — | EC50 | = | 9.87 | nM | 8.01 |
| CHEMBL5853644 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5984266 | — | EC50 | = | 10.5 | nM | 7.98 |
| CHEMBL5830783 | — | EC50 | = | 10.7 | nM | 7.97 |
| CHEMBL6045601 | — | EC50 | = | 11.2 | nM | 7.95 |
| CHEMBL5850378 | — | EC50 | = | 11.8 | nM | 7.93 |
| CHEMBL6036514 | — | EC50 | = | 12.3 | nM | 7.91 |
| CHEMBL5743795 | — | EC50 | = | 12.8 | nM | 7.89 |
| CHEMBL6022147 | — | EC50 | = | 13.5 | nM | 7.87 |
| CHEMBL5837905 | — | EC50 | = | 13.6 | nM | 7.87 |
| CHEMBL5969331 | — | EC50 | = | 13.9 | nM | 7.86 |
| CHEMBL4215300 | — | EC50 | = | 13.7 | nM | 7.86 |
| CHEMBL5740310 | — | EC50 | = | 13.8 | nM | 7.86 |
| CHEMBL5821085 | — | EC50 | = | 13.9 | nM | 7.86 |
| CHEMBL6031274 | — | EC50 | = | 14.1 | nM | 7.85 |
| CHEMBL5990615 | — | EC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5847367 | — | EC50 | = | 14.9 | nM | 7.83 |
| CHEMBL5862004 | — | EC50 | = | 15.3 | nM | 7.82 |
| CHEMBL5842806 | — | EC50 | = | 15.1 | nM | 7.82 |
| CHEMBL5984762 | — | EC50 | = | 16.2 | nM | 7.79 |
| CHEMBL5866996 | — | EC50 | = | 16.9 | nM | 7.77 |
| CHEMBL4205708 | — | EC50 | = | 17.1 | nM | 7.77 |
| CHEMBL6027992 | — | EC50 | = | 17.3 | nM | 7.76 |
| CHEMBL4210359 | — | EC50 | = | 17.7 | nM | 7.75 |
| CHEMBL5891209 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5797883 | — | EC50 | = | 18.2 | nM | 7.74 |
| CHEMBL5947937 | — | EC50 | = | 19.5 | nM | 7.71 |
| CHEMBL6043861 | — | EC50 | = | 19.9 | nM | 7.70 |
| CHEMBL5848471 | — | EC50 | = | 20.3 | nM | 7.69 |
| CHEMBL6042389 | — | EC50 | = | 20.5 | nM | 7.69 |
| CHEMBL5906270 | — | EC50 | = | 20.5 | nM | 7.69 |
| CHEMBL4218769 | — | EC50 | = | 21.1 | nM | 7.68 |
| CHEMBL4217261 | — | EC50 | = | 21.4 | nM | 7.67 |
| CHEMBL6040672 | — | EC50 | = | 21.4 | nM | 7.67 |
| CHEMBL5856050 | — | EC50 | = | 21.3 | nM | 7.67 |
| CHEMBL5823025 | — | EC50 | = | 21.6 | nM | 7.67 |
| CHEMBL5913064 | — | EC50 | = | 22.0 | nM | 7.66 |