Assay Detail
Binding
CHEMBL877132
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PDK-1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
[Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial (CHEMBL4766) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Substituted 3-imidazo[1,2-a]pyridin-3-yl- 4-(1,2,3,4-tetrahydro-[1,4]diazepino-[6,7,1-hi]indol-7-yl)pyrrole-2,5-diones as highly selective and potent inhibitors of glycogen synthase kinase-3.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 5 | 5.26 | 5.37 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL362588 | — | — | 1 | 5.37 |
| CHEMBL362558 | LY-2090314 | 2.0 | 1 | 5.21 |
| CHEMBL363058 | — | — | 1 | 5.19 |
| CHEMBL178737 | — | — | 1 | - |
| CHEMBL362814 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL362588 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL362558 | LY-2090314 | IC50 | = | 6200.0 | nM | 5.21 |
| CHEMBL363058 | — | IC50 | = | 6500.0 | nM | 5.19 |
| CHEMBL178737 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL362814 | — | IC50 | > | 20000.0 | nM | - |