Assay Detail
Binding
CHEMBL2034299
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Competitive inhibition of PDK1 using [gamma-33P]-ATP as substrate after 30 mins by scintillation counting
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
3-phosphoinositide-dependent protein kinase 1 (CHEMBL2534) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Thieno[3,2-d]pyrimidin-4(3H)-one derivatives as PDK1 inhibitors discovered by fragment-based screening.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 3.97 | 5.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2029526 | — | — | 1 | 5.28 |
| CHEMBL2029524 | — | — | 1 | 4.96 |
| CHEMBL2029521 | — | — | 1 | 4.82 |
| CHEMBL2029523 | — | — | 1 | 4.48 |
| CHEMBL2029525 | — | — | 1 | 4.41 |
| CHEMBL2029511 | — | — | 1 | 4.26 |
| CHEMBL2029513 | — | — | 1 | 4.21 |
| CHEMBL1612732 | — | — | 1 | 4.07 |
| CHEMBL271138 | — | — | 1 | 4.04 |
| CHEMBL2029520 | — | — | 1 | 4.02 |
| CHEMBL2029522 | — | — | 1 | 3.98 |
| CHEMBL2029519 | — | — | 1 | 3.96 |
| CHEMBL2029517 | — | — | 1 | 3.91 |
| CHEMBL2029518 | — | — | 1 | 3.81 |
| CHEMBL2029516 | — | — | 1 | 3.56 |
| CHEMBL23507 | 5-FLUOROINDOLE-2-CARBOXYLIC ACID | — | 1 | 3.53 |
| CHEMBL2029514 | — | — | 1 | 3.52 |
| CHEMBL2029515 | — | — | 1 | 3.40 |
| CHEMBL1877245 | — | — | 1 | 3.34 |
| CHEMBL2029512 | — | — | 1 | 3.33 |
| CHEMBL1891423 | — | — | 1 | 3.31 |
| CHEMBL2029510 | — | — | 1 | 3.08 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2029526 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2029524 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2029521 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL2029523 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL2029525 | — | IC50 | = | 39000.0 | nM | 4.41 |
| CHEMBL2029511 | — | IC50 | = | 55000.0 | nM | 4.26 |
| CHEMBL2029513 | — | IC50 | = | 61000.0 | nM | 4.21 |
| CHEMBL1612732 | — | IC50 | = | 86000.0 | nM | 4.07 |
| CHEMBL271138 | — | IC50 | = | 92000.0 | nM | 4.04 |
| CHEMBL2029520 | — | IC50 | = | 95000.0 | nM | 4.02 |
| CHEMBL2029522 | — | IC50 | = | 106000.0 | nM | 3.98 |
| CHEMBL2029519 | — | IC50 | = | 109000.0 | nM | 3.96 |
| CHEMBL2029517 | — | IC50 | = | 122000.0 | nM | 3.91 |
| CHEMBL2029518 | — | IC50 | = | 154000.0 | nM | 3.81 |
| CHEMBL2029516 | — | IC50 | = | 273000.0 | nM | 3.56 |
| CHEMBL23507 | 5-FLUOROINDOLE-2-CARBOXYLIC ACID | IC50 | = | 297000.0 | nM | 3.53 |
| CHEMBL2029514 | — | IC50 | = | 302000.0 | nM | 3.52 |
| CHEMBL2029515 | — | IC50 | = | 402000.0 | nM | 3.40 |
| CHEMBL1877245 | — | IC50 | = | 461000.0 | nM | 3.34 |
| CHEMBL2029512 | — | IC50 | = | 472000.0 | nM | 3.33 |
| CHEMBL1891423 | — | IC50 | = | 492000.0 | nM | 3.31 |
| CHEMBL2029510 | — | IC50 | = | 828000.0 | nM | 3.08 |