Assay Detail
Binding
CHEMBL1805901
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Inhibition of human MK2 using hsp27 peptide biotinyl-AYSRALSRQLSSGVSEIRCOOH as substrate after 45 mins by FRET assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 | 7.46 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1801384 | — | — | 1 | 9.00 |
| CHEMBL1801385 | — | — | 1 | 8.30 |
| CHEMBL1801382 | — | — | 1 | 8.30 |
| CHEMBL1801381 | — | — | 1 | 8.30 |
| CHEMBL1801374 | — | — | 1 | 8.10 |
| CHEMBL1801373 | — | — | 1 | 8.00 |
| CHEMBL1801375 | — | — | 1 | 8.00 |
| CHEMBL1801388 | — | — | 1 | 8.00 |
| CHEMBL1614995 | — | — | 1 | 7.92 |
| CHEMBL1801313 | — | — | 1 | 7.85 |
| CHEMBL1801386 | — | — | 1 | 7.82 |
| CHEMBL1801387 | — | — | 1 | 7.80 |
| CHEMBL1801316 | — | — | 1 | 7.64 |
| CHEMBL1801315 | — | — | 1 | 7.60 |
| CHEMBL1801377 | — | — | 1 | 7.57 |
| CHEMBL1801380 | — | — | 1 | 7.50 |
| CHEMBL1801314 | — | — | 1 | 7.22 |
| CHEMBL1801376 | — | — | 1 | 7.14 |
| CHEMBL1801091 | — | — | 1 | 7.14 |
| CHEMBL1801089 | — | — | 1 | 7.10 |
| CHEMBL1801378 | — | — | 1 | 7.07 |
| CHEMBL1801090 | — | — | 1 | 7.02 |
| CHEMBL1801390 | — | — | 1 | 6.94 |
| CHEMBL1801389 | — | — | 1 | 6.80 |
| CHEMBL1801088 | — | — | 1 | 6.78 |
| CHEMBL1801392 | — | — | 1 | 6.76 |
| CHEMBL1801391 | — | — | 1 | 6.60 |
| CHEMBL1801379 | — | — | 1 | 6.05 |
| CHEMBL1801383 | — | — | 1 | 5.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1801384 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL1801385 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1801382 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1801381 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL1801374 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL1801373 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1801375 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1801388 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1614995 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL1801313 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL1801386 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL1801387 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL1801316 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL1801315 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL1801377 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL1801380 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL1801314 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1801376 | — | IC50 | = | 73.0 | nM | 7.14 |
| CHEMBL1801091 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL1801089 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL1801378 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL1801090 | — | IC50 | = | 96.0 | nM | 7.02 |
| CHEMBL1801390 | — | IC50 | = | 116.0 | nM | 6.94 |
| CHEMBL1801389 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL1801088 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL1801392 | — | IC50 | = | 172.0 | nM | 6.76 |
| CHEMBL1801391 | — | IC50 | = | 253.0 | nM | 6.60 |
| CHEMBL1801379 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL1801383 | — | IC50 | = | 1189.0 | nM | 5.92 |