Assay Detail
Binding
CHEMBL5048663
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of full length N-terminal GST tagged human CDK2(1 to 298 residues)/CyclinA2 (1 to 432 residues) expressed in baculovirus expression system using FL peptide as substrate preincubated for 30 mins followed by substrate addition further incubated for 120 mins by EZ reader method
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery and Optimization of Highly Selective Inhibitors of CDK5.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 6.85 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5077138 | — | — | 1 | 8.55 |
| CHEMBL5081712 | — | — | 1 | 7.75 |
| CHEMBL5075328 | — | — | 1 | 7.64 |
| CHEMBL5086375 | — | — | 1 | 7.48 |
| CHEMBL5078762 | — | — | 1 | 7.46 |
| CHEMBL5091792 | — | — | 1 | 7.37 |
| CHEMBL5088595 | — | — | 1 | 7.33 |
| CHEMBL5077125 | — | — | 1 | 7.32 |
| CHEMBL5074832 | — | — | 1 | 7.26 |
| CHEMBL5080351 | — | — | 1 | 7.23 |
| CHEMBL5092400 | — | — | 1 | 7.19 |
| CHEMBL5090019 | — | — | 1 | 7.18 |
| CHEMBL5083778 | — | — | 1 | 7.01 |
| CHEMBL5094270 | — | — | 1 | 6.98 |
| CHEMBL5078596 | — | — | 1 | 6.98 |
| CHEMBL5093640 | — | — | 1 | 6.88 |
| CHEMBL5080813 | — | — | 1 | 6.87 |
| CHEMBL5080361 | — | — | 1 | 6.81 |
| CHEMBL5077028 | — | — | 1 | 6.78 |
| CHEMBL5080866 | — | — | 1 | 6.71 |
| CHEMBL5084200 | — | — | 1 | 6.68 |
| CHEMBL5084882 | — | — | 1 | 6.68 |
| CHEMBL5087911 | — | — | 1 | 6.67 |
| CHEMBL5082140 | — | — | 1 | 6.60 |
| CHEMBL5088315 | — | — | 1 | 6.58 |
| CHEMBL5079342 | — | — | 1 | 6.52 |
| CHEMBL5078192 | — | — | 1 | 6.52 |
| CHEMBL5070707 | — | — | 1 | 6.48 |
| CHEMBL5080123 | — | — | 1 | 6.47 |
| CHEMBL5080566 | — | — | 1 | 6.41 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5077138 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5081712 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5075328 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5086375 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5078762 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5091792 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL5088595 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5077125 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL5074832 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL5080351 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL5092400 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL5090019 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL5083778 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL5094270 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5078596 | — | IC50 | = | 104.0 | nM | 6.98 |
| CHEMBL5093640 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5080813 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL5080361 | — | IC50 | = | 156.0 | nM | 6.81 |
| CHEMBL5077028 | — | IC50 | = | 166.0 | nM | 6.78 |
| CHEMBL5080866 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL5084882 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL5084200 | — | IC50 | = | 211.0 | nM | 6.68 |
| CHEMBL5087911 | — | IC50 | = | 212.0 | nM | 6.67 |
| CHEMBL5082140 | — | IC50 | = | 252.0 | nM | 6.60 |
| CHEMBL5088315 | — | IC50 | = | 264.0 | nM | 6.58 |
| CHEMBL5079342 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL5078192 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL5070707 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5080123 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL5080566 | — | IC50 | = | 392.0 | nM | 6.41 |
| CHEMBL5093012 | — | IC50 | = | 444.0 | nM | 6.35 |
| CHEMBL5088480 | — | IC50 | = | 472.0 | nM | 6.33 |
| CHEMBL5094131 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL5079772 | — | IC50 | = | 539.0 | nM | 6.27 |
| CHEMBL5076000 | — | IC50 | = | 601.0 | nM | 6.22 |
| CHEMBL5093797 | — | IC50 | = | 1365.0 | nM | 5.87 |
| CHEMBL5094209 | — | IC50 | = | 2437.0 | nM | 5.61 |
| CHEMBL5086711 | — | IC50 | > | 30000.0 | nM | - |