Assay Detail
Binding
CHEMBL5363954
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal GST/His6-fused human full length CLK1 (1 to 484 residues) expressed in Sf9 cells assessed as inhibition of autophosphorylation using [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay
232
Total Activities
232
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Sf9 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Dual specificity protein kinase CLK1 (CHEMBL4224) ↗| Type | SINGLE PROTEIN |
| 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 | 232 | 7.43 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5428651 | — | — | 1 | 8.40 |
| CHEMBL5408531 | — | — | 1 | 8.40 |
| CHEMBL5404416 | — | — | 1 | 8.30 |
| CHEMBL5405572 | — | — | 1 | 8.30 |
| CHEMBL5439392 | — | — | 1 | 8.30 |
| CHEMBL5396550 | — | — | 1 | 8.22 |
| CHEMBL5401116 | — | — | 1 | 8.22 |
| CHEMBL5422654 | — | — | 1 | 8.22 |
| CHEMBL5430415 | — | — | 1 | 8.22 |
| CHEMBL5404544 | — | — | 1 | 8.22 |
| CHEMBL5409574 | — | — | 1 | 8.15 |
| CHEMBL5405233 | — | — | 1 | 8.15 |
| CHEMBL5438158 | — | — | 1 | 8.15 |
| CHEMBL5405059 | — | — | 1 | 8.15 |
| CHEMBL5438412 | — | — | 1 | 8.15 |
| CHEMBL5414514 | — | — | 1 | 8.15 |
| CHEMBL5417147 | — | — | 1 | 8.15 |
| CHEMBL5438293 | — | — | 1 | 8.10 |
| CHEMBL5418722 | — | — | 1 | 8.10 |
| CHEMBL5427398 | — | — | 1 | 8.05 |
| CHEMBL5412565 | — | — | 1 | 8.05 |
| CHEMBL5426735 | — | — | 1 | 8.05 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | 1.0 | 1 | 8.05 |
| CHEMBL5440139 | — | — | 1 | 8.05 |
| CHEMBL5420497 | — | — | 1 | 8.05 |
| CHEMBL5420645 | — | — | 1 | 8.05 |
| CHEMBL5091238 | — | — | 1 | 8.05 |
| CHEMBL5430192 | — | — | 1 | 8.00 |
| CHEMBL5439952 | — | — | 1 | 8.00 |
| CHEMBL5438325 | — | — | 1 | 8.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5408531 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5428651 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5439392 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5405572 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5404416 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5401116 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5396550 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5422654 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5404544 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5430415 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5414514 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5409574 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5438158 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5417147 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5405059 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5438412 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5405233 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5418722 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5438293 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5412565 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5420645 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5091238 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5427398 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5426285 | 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5420497 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5440139 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5426735 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5427842 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5438325 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5439952 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5395707 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5400230 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5430192 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5423063 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5396991 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5397343 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5429404 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5422486 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5434921 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5411157 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5429707 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5283849 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5417207 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5416942 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5436133 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5430262 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5428132 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5409730 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5417527 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5418020 | — | IC50 | = | 13.0 | nM | 7.89 |