Assay Detail
Binding
CHEMBL3772525
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant PAK1 kinase domain using coumarin/fluorescein-labeled FRET peptide as substrate preincubated for 10 mins followed by ATP addition measured after 60 mins by Z-LYTE assay
14
Total Activities
14
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 |
Target
Serine/threonine-protein kinase PAK 1 (CHEMBL4600) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 14 | 8.10 | 8.72 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3769478 | — | — | 1 | 8.72 |
| CHEMBL3770909 | — | — | 1 | 8.72 |
| CHEMBL3770588 | — | — | 1 | 8.68 |
| CHEMBL3770443 | — | — | 1 | 8.43 |
| CHEMBL3770363 | — | — | 1 | 8.37 |
| CHEMBL3769748 | — | — | 1 | 8.22 |
| CHEMBL3770369 | — | — | 1 | 8.21 |
| CHEMBL3769456 | — | — | 1 | 8.13 |
| CHEMBL3769552 | — | — | 1 | 8.10 |
| CHEMBL3770295 | — | — | 1 | 8.10 |
| CHEMBL3770943 | — | — | 1 | 7.72 |
| CHEMBL3770186 | — | — | 1 | 7.66 |
| CHEMBL3770806 | — | — | 1 | 7.19 |
| CHEMBL3769981 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3769478 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3770909 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL3770588 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL3770443 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL3770363 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL3769748 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL3770369 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL3769456 | — | Ki | = | 7.4 | nM | 8.13 |
| CHEMBL3769552 | — | Ki | = | 7.9 | nM | 8.10 |
| CHEMBL3770295 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL3770943 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3770186 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL3770806 | — | Ki | = | 64.0 | nM | 7.19 |
| CHEMBL3769981 | — | Ki | = | 66.0 | nM | 7.18 |