Assay Detail
Binding
CHEMBL5167578
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human N-terminal His-tagged/ TEV cleavage fused DRAK1 (39 to 369 residues) expressed in Escherichia coli using KKLNRTLSFAEPG peptide as substrate in presence of [gamma-33P]ATP by radiometric based scintillation proximity assay
4
Total Activities
4
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
Illuminating the Dark: Highly Selective Inhibition of Serine/Threonine Kinase 17A with Pyrazolo[1,5-<i>a</i>]pyrimidine-Based Macrocycles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 7.36 | 7.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5191892 | — | — | 1 | 7.82 |
| CHEMBL5193635 | — | — | 1 | 7.51 |
| CHEMBL5087558 | — | — | 1 | 7.31 |
| CHEMBL5204528 | — | — | 1 | 6.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5191892 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5193635 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5087558 | — | IC50 | = | 49.0 | nM | 7.31 |
| CHEMBL5204528 | — | IC50 | = | 155.0 | nM | 6.81 |