Assay Detail
Binding
CHEMBL5501744
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Inhibition of TLK2 (unknown origin)
12
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase tousled-like 2 (CHEMBL5404) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery and optimization of narrow spectrum inhibitors of Tousled like kinase 2 (TLK2) using quantitative structure activity relationships.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 6.19 | 7.21 |
| Kd | 5 | 6.56 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.80 |
| CHEMBL235641 | — | — | 1 | 7.21 |
| CHEMBL5527885 | — | — | 2 | 6.57 |
| CHEMBL535 | SUNITINIB | 4.0 | 2 | 6.48 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.42 |
| CHEMBL216543 | — | — | 1 | 6.36 |
| CHEMBL1802727 | — | — | 1 | 6.36 |
| CHEMBL258805 | SU-9516 | 1.0 | 1 | 6.25 |
| CHEMBL13608 | TOCERANIB | 2.0 | 1 | 5.60 |
| CHEMBL3542344 | — | — | 1 | 5.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL235641 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL5527885 | — | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL535 | SUNITINIB | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL475251 | R-406 | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL216543 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL1802727 | — | IC50 | = | 440.0 | nM | 6.36 |
| CHEMBL258805 | SU-9516 | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL535 | SUNITINIB | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL13608 | TOCERANIB | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5527885 | — | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL3542344 | — | IC50 | = | 3000.0 | nM | 5.52 |