Assay Detail
Binding
CHEMBL5236876
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GST-tagged TTBK1 (1 to 421) (unknown origin) using DNA Topoisomerase 2-alpha-Thr1342 as substrate incubated for 15 mins followed by ATP addition and further incubated for 120 mins by TR-FRET assay
32
Total Activities
31
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 |
Publication
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 32 | 7.13 | 8.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5268795 | — | — | 1 | 8.64 |
| CHEMBL5283456 | — | — | 1 | 8.64 |
| CHEMBL5280210 | — | — | 1 | 8.57 |
| CHEMBL5272364 | — | — | 1 | 8.55 |
| CHEMBL5279863 | — | — | 1 | 8.11 |
| CHEMBL5282072 | — | — | 1 | 8.01 |
| CHEMBL5268080 | — | — | 1 | 8.00 |
| CHEMBL5271137 | — | — | 1 | 7.75 |
| CHEMBL5273263 | — | — | 1 | 7.75 |
| CHEMBL5282902 | — | — | 1 | 7.70 |
| CHEMBL5290581 | — | — | 1 | 7.50 |
| CHEMBL5274162 | — | — | 1 | 7.43 |
| CHEMBL5280803 | — | — | 1 | 7.41 |
| CHEMBL5288487 | — | — | 1 | 7.24 |
| CHEMBL5278744 | — | — | 1 | 7.22 |
| CHEMBL5274528 | — | — | 1 | 7.07 |
| CHEMBL5290252 | — | — | 2 | 6.91 |
| CHEMBL5279159 | — | — | 1 | 6.73 |
| CHEMBL2334586 | — | — | 1 | 6.70 |
| CHEMBL5275588 | — | — | 1 | 6.45 |
| CHEMBL5272862 | — | — | 1 | 6.38 |
| CHEMBL5181163 | — | — | 1 | 5.99 |
| CHEMBL5283413 | — | — | 1 | 5.71 |
| CHEMBL5193906 | — | — | 1 | 5.60 |
| CHEMBL127907 | — | — | 1 | 5.34 |
| CHEMBL5286028 | — | — | 1 | 4.77 |
| CHEMBL5281273 | — | — | 1 | - |
| CHEMBL5269486 | — | — | 1 | - |
| CHEMBL5282564 | — | — | 1 | - |
| CHEMBL5287032 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5268795 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5283456 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL5280210 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5272364 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL5279863 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL5282072 | — | IC50 | = | 9.8 | nM | 8.01 |
| CHEMBL5268080 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5273263 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5271137 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5282902 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5290581 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL5274162 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5280803 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5288487 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL5278744 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5274528 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL5290252 | — | IC50 | = | 124.0 | nM | 6.91 |
| CHEMBL5279159 | — | IC50 | = | 185.0 | nM | 6.73 |
| CHEMBL2334586 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL5275588 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL5290252 | — | IC50 | = | 352.0 | nM | 6.45 |
| CHEMBL5272862 | — | IC50 | = | 414.0 | nM | 6.38 |
| CHEMBL5181163 | — | IC50 | = | 1022.0 | nM | 5.99 |
| CHEMBL5283413 | — | IC50 | = | 1942.0 | nM | 5.71 |
| CHEMBL5193906 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL127907 | — | IC50 | = | 4610.0 | nM | 5.34 |
| CHEMBL5286028 | — | IC50 | = | 16850.0 | nM | 4.77 |
| CHEMBL5281273 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5269486 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5282564 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5287032 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5287975 | — | IC50 | > | 100000.0 | nM | - |