Assay Detail
Binding
CHEMBL4380947
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST-tagged MNK2 (unknown origin) (72 to 385 residues) expressed in Escherichia coli BL21 (DE3) cells using 5-FAM-TATKSGSTTKNRFVV-NH2 peptide as substrate preincubated with enzyme for 10 mins followed by substrate addition after 60 mins in presence of ATP by caliper mobility shift assay
53
Total Activities
53
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-interacting serine/threonine-protein kinase 2 (CHEMBL4204) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Stepwise Evolution of Fragment Hits against MAPK Interacting Kinases 1 and 2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 53 | 5.72 | 7.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4442209 | — | — | 1 | 7.85 |
| CHEMBL4569209 | — | — | 1 | 7.80 |
| CHEMBL4588193 | — | — | 1 | 7.38 |
| CHEMBL4443472 | — | — | 1 | 7.36 |
| CHEMBL4462099 | — | — | 1 | 7.27 |
| CHEMBL4587472 | — | — | 1 | 7.10 |
| CHEMBL4587832 | — | — | 1 | 7.05 |
| CHEMBL4440223 | — | — | 1 | 6.92 |
| CHEMBL4457274 | — | — | 1 | 6.80 |
| CHEMBL4456135 | — | — | 1 | 6.52 |
| CHEMBL4558635 | — | — | 1 | 6.51 |
| CHEMBL4450463 | — | — | 1 | 6.47 |
| CHEMBL4457368 | — | — | 1 | 6.46 |
| CHEMBL4465294 | — | — | 1 | 6.41 |
| CHEMBL4453446 | — | — | 1 | 6.39 |
| CHEMBL4537933 | — | — | 1 | 6.34 |
| CHEMBL4441602 | — | — | 1 | 6.30 |
| CHEMBL4586717 | — | — | 1 | 6.20 |
| CHEMBL4473517 | — | — | 1 | 6.14 |
| CHEMBL4590023 | — | — | 1 | 6.10 |
| CHEMBL4574792 | — | — | 1 | 6.01 |
| CHEMBL4563423 | — | — | 1 | 6.00 |
| CHEMBL4518152 | — | — | 1 | 5.92 |
| CHEMBL4474546 | — | — | 1 | 5.85 |
| CHEMBL4457163 | — | — | 1 | 5.82 |
| CHEMBL4583708 | — | — | 1 | 5.75 |
| CHEMBL4570689 | — | — | 1 | 5.72 |
| CHEMBL4449392 | — | — | 1 | 5.54 |
| CHEMBL4529617 | — | — | 1 | 5.52 |
| CHEMBL4530427 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4442209 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4569209 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4588193 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL4443472 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL4462099 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4587472 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL4587832 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4440223 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4457274 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL4456135 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4558635 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL4450463 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4457368 | — | IC50 | = | 350.0 | nM | 6.46 |
| CHEMBL4465294 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL4453446 | — | IC50 | = | 410.0 | nM | 6.39 |
| CHEMBL4537933 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4441602 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4586717 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL4473517 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL4590023 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4574792 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4563423 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4518152 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4474546 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4457163 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4583708 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL4570689 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL4449392 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4529617 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL4530427 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4522631 | — | IC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL275339 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL4474769 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2113964 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4539725 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4551912 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4457016 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL2441619 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL4531667 | — | IC50 | = | 7200.0 | nM | 5.14 |
| CHEMBL4452239 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL4527170 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4593941 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL4446188 | — | IC50 | = | 13000.0 | nM | 4.89 |
| CHEMBL1778131 | — | IC50 | = | 17000.0 | nM | 4.77 |
| CHEMBL1778132 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL118266 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL4570088 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4483063 | — | IC50 | = | 43000.0 | nM | 4.37 |
| CHEMBL4452380 | — | IC50 | = | 45000.0 | nM | 4.35 |
| CHEMBL483790 | — | IC50 | = | 60000.0 | nM | 4.22 |