Assay Detail
Binding
CHEMBL1805903
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Inhibition of MK2 in human THP-1 cells assessed as inhibition of anisomycin stimulated ser78-hsp27 phosphorylation after 10 mins by FACS analysis
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | THP-1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
MAP kinase-activated protein kinase 2 (CHEMBL2208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In vivo and in vitro SAR of tetracyclic MAPKAP-K2 (MK2) inhibitors. Part I.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 29 | 5.67 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801386 | — | — | 1 | 6.30 |
| CHEMBL1614995 | — | — | 1 | 6.16 |
| CHEMBL1801316 | — | — | 1 | 6.06 |
| CHEMBL1801387 | — | — | 1 | 5.89 |
| CHEMBL1801380 | — | — | 1 | 5.89 |
| CHEMBL1801382 | — | — | 1 | 5.78 |
| CHEMBL1801388 | — | — | 1 | 5.60 |
| CHEMBL1801378 | — | — | 1 | 5.29 |
| CHEMBL1801389 | — | — | 1 | 5.24 |
| CHEMBL1801090 | — | — | 1 | 5.08 |
| CHEMBL1801381 | — | — | 1 | 5.03 |
| CHEMBL1801314 | — | — | 1 | - |
| CHEMBL1801315 | — | — | 1 | - |
| CHEMBL1801373 | — | — | 1 | - |
| CHEMBL1801374 | — | — | 1 | - |
| CHEMBL1801375 | — | — | 1 | - |
| CHEMBL1801376 | — | — | 1 | - |
| CHEMBL1801377 | — | — | 1 | - |
| CHEMBL1801379 | — | — | 1 | - |
| CHEMBL1801313 | — | — | 1 | - |
| CHEMBL1801384 | — | — | 1 | - |
| CHEMBL1801385 | — | — | 1 | - |
| CHEMBL1801089 | — | — | 1 | - |
| CHEMBL1801088 | — | — | 1 | - |
| CHEMBL1801091 | — | — | 1 | - |
| CHEMBL1801392 | — | — | 1 | - |
| CHEMBL1801391 | — | — | 1 | - |
| CHEMBL1801383 | — | — | 1 | - |
| CHEMBL1801390 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801386 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1614995 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1801316 | — | IC50 | = | 875.0 | nM | 6.06 |
| CHEMBL1801387 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1801380 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL1801382 | — | IC50 | = | 1680.0 | nM | 5.78 |
| CHEMBL1801388 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL1801378 | — | IC50 | = | 5078.0 | nM | 5.29 |
| CHEMBL1801389 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL1801090 | — | IC50 | = | 8300.0 | nM | 5.08 |
| CHEMBL1801381 | — | IC50 | = | 9330.0 | nM | 5.03 |
| CHEMBL1801314 | — | IC50 | - | — | - | |
| CHEMBL1801315 | — | IC50 | - | — | - | |
| CHEMBL1801373 | — | IC50 | - | — | - | |
| CHEMBL1801374 | — | IC50 | - | — | - | |
| CHEMBL1801375 | — | IC50 | - | — | - | |
| CHEMBL1801376 | — | IC50 | - | — | - | |
| CHEMBL1801377 | — | IC50 | - | — | - | |
| CHEMBL1801379 | — | IC50 | - | — | - | |
| CHEMBL1801313 | — | IC50 | - | — | - | |
| CHEMBL1801384 | — | IC50 | - | — | - | |
| CHEMBL1801385 | — | IC50 | - | — | - | |
| CHEMBL1801089 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL1801088 | — | IC50 | - | — | - | |
| CHEMBL1801091 | — | IC50 | - | — | - | |
| CHEMBL1801392 | — | IC50 | - | — | - | |
| CHEMBL1801391 | — | IC50 | - | — | - | |
| CHEMBL1801383 | — | IC50 | - | — | - | |
| CHEMBL1801390 | — | IC50 | - | — | - |