Assay Detail
Binding
CHEMBL1937262
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of MK2-mediated HSP27 phosphorylation in LPS-stimulated human THP1 cells pre-incubated for 60 mins prior to LPS-induction measured after 60 mins by multi-spot assay
40
Total Activities
34
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
Novel ATP competitive MK2 inhibitors with potent biochemical and cell-based activity throughout the series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 40 | 6.15 | 6.89 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1933173 | — | — | 1 | 6.89 |
| CHEMBL1933188 | — | — | 1 | 6.62 |
| CHEMBL1933164 | — | — | 1 | 6.55 |
| CHEMBL1933181 | — | — | 3 | 6.50 |
| CHEMBL1933162 | — | — | 1 | 6.46 |
| CHEMBL1933189 | — | — | 1 | 6.41 |
| CHEMBL1933192 | — | — | 1 | 6.40 |
| CHEMBL1933191 | — | — | 1 | 6.32 |
| CHEMBL1933166 | — | — | 1 | 6.28 |
| CHEMBL1933179 | — | — | 3 | 6.28 |
| CHEMBL1933176 | — | — | 1 | 6.26 |
| CHEMBL1933187 | — | — | 1 | 6.23 |
| CHEMBL1933186 | — | — | 1 | 6.23 |
| CHEMBL1933183 | — | — | 1 | 6.21 |
| CHEMBL1738702 | — | — | 1 | 6.21 |
| CHEMBL1933172 | — | — | 1 | 6.19 |
| CHEMBL1933193 | — | — | 1 | 6.18 |
| CHEMBL1933185 | — | — | 1 | 6.18 |
| CHEMBL1933171 | — | — | 1 | 6.17 |
| CHEMBL1933178 | — | — | 3 | 6.16 |
| CHEMBL1933170 | — | — | 1 | 6.14 |
| CHEMBL1933174 | — | — | 1 | 6.08 |
| CHEMBL1933190 | — | — | 1 | 6.08 |
| CHEMBL1933169 | — | — | 1 | 6.04 |
| CHEMBL1933180 | — | — | 1 | 5.96 |
| CHEMBL1933184 | — | — | 1 | 5.92 |
| CHEMBL1933175 | — | — | 1 | 5.89 |
| CHEMBL1933168 | — | — | 1 | 5.43 |
| CHEMBL1933182 | — | — | 1 | - |
| CHEMBL1933161 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1933173 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL1933188 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL1933164 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL1933181 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1933162 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL1933189 | — | EC50 | = | 390.0 | nM | 6.41 |
| CHEMBL1933192 | — | EC50 | = | 400.0 | nM | 6.40 |
| CHEMBL1933191 | — | EC50 | = | 480.0 | nM | 6.32 |
| CHEMBL1933166 | — | EC50 | = | 520.0 | nM | 6.28 |
| CHEMBL1933179 | — | EC50 | = | 530.0 | nM | 6.28 |
| CHEMBL1933176 | — | EC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1933187 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1933186 | — | EC50 | = | 590.0 | nM | 6.23 |
| CHEMBL1738702 | — | EC50 | = | 620.0 | nM | 6.21 |
| CHEMBL1933183 | — | EC50 | = | 610.0 | nM | 6.21 |
| CHEMBL1933172 | — | EC50 | = | 640.0 | nM | 6.19 |
| CHEMBL1933193 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1933185 | — | EC50 | = | 660.0 | nM | 6.18 |
| CHEMBL1933171 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL1933178 | — | EC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1933170 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL1933174 | — | EC50 | = | 830.0 | nM | 6.08 |
| CHEMBL1933190 | — | EC50 | = | 840.0 | nM | 6.08 |
| CHEMBL1933181 | — | EC50 | = | 870.0 | nM | 6.06 |
| CHEMBL1933169 | — | EC50 | = | 920.0 | nM | 6.04 |
| CHEMBL1933180 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1933179 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL1933184 | — | EC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL1933175 | — | EC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL1933168 | — | EC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL1933178 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL1933181 | — | EC50 | = | 7400.0 | nM | 5.13 |
| CHEMBL1933182 | — | EC50 | - | — | - | |
| CHEMBL1933179 | — | EC50 | - | — | - | |
| CHEMBL1933177 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL1933178 | — | EC50 | - | — | - | |
| CHEMBL1933167 | — | EC50 | - | — | - | |
| CHEMBL1933165 | — | EC50 | - | — | - | |
| CHEMBL1933163 | — | EC50 | - | — | - | |
| CHEMBL1933161 | — | EC50 | - | — | - |