Assay Detail
Binding
CHEMBL1780645
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MK2 pretreated for 30 mins before fluorescein labeled substrate peptide addition measured after 2 hrs by IMAP assay
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
MAP kinase-activated protein kinase 2 (CHEMBL2208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of selective and orally available spiro-3-piperidyl ATP-competitive MK2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 37 | 7.81 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1779362 | — | — | 1 | 8.96 |
| CHEMBL1779367 | — | — | 1 | 8.77 |
| CHEMBL1779366 | — | — | 1 | 8.68 |
| CHEMBL1779365 | — | — | 1 | 8.44 |
| CHEMBL1738702 | — | — | 1 | 8.37 |
| CHEMBL1779360 | — | — | 1 | 8.35 |
| CHEMBL1779359 | — | — | 1 | 8.29 |
| CHEMBL1779352 | — | — | 1 | 8.23 |
| CHEMBL1779358 | — | — | 1 | 8.21 |
| CHEMBL1779361 | — | — | 1 | 8.20 |
| CHEMBL1779488 | — | — | 1 | 8.19 |
| CHEMBL1779485 | — | — | 1 | 8.16 |
| CHEMBL1779357 | — | — | 1 | 8.16 |
| CHEMBL1779363 | — | — | 1 | 8.16 |
| CHEMBL1779372 | — | — | 1 | 8.13 |
| CHEMBL1779350 | — | — | 1 | 8.08 |
| CHEMBL1779374 | — | — | 1 | 8.03 |
| CHEMBL1779346 | — | — | 1 | 8.01 |
| CHEMBL1779347 | — | — | 1 | 8.00 |
| CHEMBL1779355 | — | — | 1 | 7.96 |
| CHEMBL1779368 | — | — | 1 | 7.96 |
| CHEMBL1779353 | — | — | 1 | 7.89 |
| CHEMBL1779364 | — | — | 1 | 7.82 |
| CHEMBL1779356 | — | — | 1 | 7.82 |
| CHEMBL1779487 | — | — | 1 | 7.75 |
| CHEMBL1779371 | — | — | 1 | 7.68 |
| CHEMBL1779370 | — | — | 1 | 7.62 |
| CHEMBL1779369 | — | — | 1 | 7.55 |
| CHEMBL1779349 | — | — | 1 | 7.54 |
| CHEMBL1779354 | — | — | 1 | 7.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1779362 | — | EC50 | = | 1.1 | nM | 8.96 |
| CHEMBL1779367 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL1779366 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL1779365 | — | EC50 | = | 3.6 | nM | 8.44 |
| CHEMBL1738702 | — | EC50 | = | 4.3 | nM | 8.37 |
| CHEMBL1779360 | — | EC50 | = | 4.5 | nM | 8.35 |
| CHEMBL1779359 | — | EC50 | = | 5.1 | nM | 8.29 |
| CHEMBL1779352 | — | EC50 | = | 5.9 | nM | 8.23 |
| CHEMBL1779358 | — | EC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1779361 | — | EC50 | = | 6.3 | nM | 8.20 |
| CHEMBL1779488 | — | EC50 | = | 6.5 | nM | 8.19 |
| CHEMBL1779485 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1779357 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1779363 | — | EC50 | = | 6.9 | nM | 8.16 |
| CHEMBL1779372 | — | EC50 | = | 7.4 | nM | 8.13 |
| CHEMBL1779350 | — | EC50 | = | 8.3 | nM | 8.08 |
| CHEMBL1779374 | — | EC50 | = | 9.3 | nM | 8.03 |
| CHEMBL1779346 | — | EC50 | = | 9.8 | nM | 8.01 |
| CHEMBL1779347 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1779368 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1779355 | — | EC50 | = | 11.0 | nM | 7.96 |
| CHEMBL1779353 | — | EC50 | = | 13.0 | nM | 7.89 |
| CHEMBL1779364 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1779356 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1779487 | — | EC50 | = | 18.0 | nM | 7.75 |
| CHEMBL1779371 | — | EC50 | = | 21.0 | nM | 7.68 |
| CHEMBL1779370 | — | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL1779369 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL1779349 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL1779354 | — | EC50 | = | 59.0 | nM | 7.23 |
| CHEMBL1779373 | — | EC50 | = | 91.0 | nM | 7.04 |
| CHEMBL1779348 | — | EC50 | = | 112.0 | nM | 6.95 |
| CHEMBL1779375 | — | EC50 | = | 126.0 | nM | 6.90 |
| CHEMBL1779486 | — | EC50 | = | 129.0 | nM | 6.89 |
| CHEMBL1779489 | — | EC50 | = | 288.0 | nM | 6.54 |
| CHEMBL226471 | — | EC50 | = | 372.0 | nM | 6.43 |
| CHEMBL1779351 | — | EC50 | = | 724.0 | nM | 6.14 |