Assay Detail
Binding
CHEMBL5363953
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST/His6-fused human full length CDK5 (1 to 292 residues)/N-terminal His6-fused human p25 (104 to 307 residues) coexpressed in Sf9 cells using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay
228
Total Activities
228
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Target
Cyclin-dependent kinase 5/CDK5 activator 1 (CHEMBL1907600) ↗| Type | PROTEIN COMPLEX |
| Organism | Homo sapiens |
Publication
Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 228 | 5.82 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5422486 | — | — | 1 | 7.60 |
| CHEMBL5438158 | — | — | 1 | 6.84 |
| CHEMBL5404544 | — | — | 1 | 6.69 |
| CHEMBL5091238 | — | — | 1 | 6.61 |
| CHEMBL5438293 | — | — | 1 | 6.55 |
| CHEMBL5417147 | — | — | 1 | 6.52 |
| CHEMBL5405059 | — | — | 1 | 6.48 |
| CHEMBL5396550 | — | — | 1 | 6.22 |
| CHEMBL5422654 | — | — | 1 | 6.21 |
| CHEMBL5420645 | — | — | 1 | 6.19 |
| CHEMBL5438728 | — | — | 1 | 6.03 |
| CHEMBL5418722 | — | — | 1 | 5.84 |
| CHEMBL5409574 | — | — | 1 | 5.81 |
| CHEMBL5439276 | — | — | 1 | 5.70 |
| CHEMBL5428651 | — | — | 1 | 5.64 |
| CHEMBL5406081 | — | — | 1 | 5.63 |
| CHEMBL5411888 | — | — | 1 | 5.62 |
| CHEMBL5441121 | — | — | 1 | 5.60 |
| CHEMBL5405233 | — | — | 1 | 5.60 |
| CHEMBL5283849 | — | — | 1 | 5.51 |
| CHEMBL5400230 | — | — | 1 | 5.49 |
| CHEMBL5417890 | — | — | 1 | 5.48 |
| CHEMBL5424272 | — | — | 1 | 5.41 |
| CHEMBL5412101 | — | — | 1 | 5.33 |
| CHEMBL5422936 | — | — | 1 | 5.30 |
| CHEMBL5412565 | — | — | 1 | 5.30 |
| CHEMBL5427398 | — | — | 1 | 5.26 |
| CHEMBL5413726 | — | — | 1 | 5.23 |
| CHEMBL5394477 | — | — | 1 | 5.21 |
| CHEMBL5405969 | — | — | 1 | 5.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5422486 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5438158 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL5404544 | — | IC50 | = | 204.0 | nM | 6.69 |
| CHEMBL5091238 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL5438293 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL5417147 | — | IC50 | = | 304.0 | nM | 6.52 |
| CHEMBL5405059 | — | IC50 | = | 332.0 | nM | 6.48 |
| CHEMBL5396550 | — | IC50 | = | 602.0 | nM | 6.22 |
| CHEMBL5422654 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5420645 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL5438728 | — | IC50 | = | 943.0 | nM | 6.03 |
| CHEMBL5418722 | — | IC50 | = | 1446.0 | nM | 5.84 |
| CHEMBL5409574 | — | IC50 | = | 1541.0 | nM | 5.81 |
| CHEMBL5439276 | — | IC50 | = | 2007.0 | nM | 5.70 |
| CHEMBL5428651 | — | IC50 | = | 2303.0 | nM | 5.64 |
| CHEMBL5406081 | — | IC50 | = | 2337.0 | nM | 5.63 |
| CHEMBL5411888 | — | IC50 | = | 2385.0 | nM | 5.62 |
| CHEMBL5405233 | — | IC50 | = | 2490.0 | nM | 5.60 |
| CHEMBL5441121 | — | IC50 | = | 2525.0 | nM | 5.60 |
| CHEMBL5283849 | — | IC50 | = | 3105.0 | nM | 5.51 |
| CHEMBL5400230 | — | IC50 | = | 3215.0 | nM | 5.49 |
| CHEMBL5417890 | — | IC50 | = | 3291.0 | nM | 5.48 |
| CHEMBL5424272 | — | IC50 | = | 3891.0 | nM | 5.41 |
| CHEMBL5412101 | — | IC50 | = | 4657.0 | nM | 5.33 |
| CHEMBL5412565 | — | IC50 | = | 5006.0 | nM | 5.30 |
| CHEMBL5422936 | — | IC50 | = | 4952.0 | nM | 5.30 |
| CHEMBL5427398 | — | IC50 | = | 5498.0 | nM | 5.26 |
| CHEMBL5413726 | — | IC50 | = | 5895.0 | nM | 5.23 |
| CHEMBL5394477 | — | IC50 | = | 6148.0 | nM | 5.21 |
| CHEMBL5405969 | — | IC50 | = | 6106.0 | nM | 5.21 |
| CHEMBL5430357 | — | IC50 | = | 6708.0 | nM | 5.17 |
| CHEMBL5423245 | — | IC50 | = | 8698.0 | nM | 5.06 |
| CHEMBL5435495 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5421442 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5437649 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5413503 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5439392 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5401217 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5411626 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406461 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5424074 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5421200 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5416947 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5434955 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5404644 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5438852 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5406568 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5395707 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5438412 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5434728 | — | IC50 | > | 10000.0 | nM | - |