Assay Detail
Binding
CHEMBL4033368
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PAK4 kinase domain using coumarin and fluorescein-labeled ser/thr20 peptide as substrate preincubated for 15 mins followed by ATP addition measured after 60 mins by Z'-Lyte assay
38
Total Activities
38
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 4 (CHEMBL4482) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Structure-Based Design of 6-Chloro-4-aminoquinazoline-2-carboxamide Derivatives as Potent and Selective p21-Activated Kinase 4 (PAK4) Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 6.81 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4076860 | — | — | 1 | 8.22 |
| CHEMBL4081464 | — | — | 1 | 8.15 |
| CHEMBL4097816 | — | — | 1 | 8.05 |
| CHEMBL4089338 | — | — | 1 | 7.96 |
| CHEMBL4059493 | — | — | 1 | 7.80 |
| CHEMBL4076708 | — | — | 1 | 7.80 |
| CHEMBL4064068 | — | — | 1 | 7.80 |
| CHEMBL4090101 | — | — | 1 | 7.77 |
| CHEMBL4101547 | — | — | 1 | 7.77 |
| CHEMBL4063425 | — | — | 1 | 7.58 |
| CHEMBL4077032 | — | — | 1 | 7.55 |
| CHEMBL4068155 | — | — | 1 | 7.44 |
| CHEMBL4093999 | — | — | 1 | 7.35 |
| CHEMBL4079783 | — | — | 1 | 7.29 |
| CHEMBL4060217 | — | — | 1 | 7.11 |
| CHEMBL4091048 | — | — | 1 | 7.00 |
| CHEMBL4090268 | — | — | 1 | 6.94 |
| CHEMBL4062257 | — | — | 1 | 6.92 |
| CHEMBL4069022 | — | — | 1 | 6.82 |
| CHEMBL4095362 | — | — | 1 | 6.66 |
| CHEMBL4093805 | — | — | 1 | 6.59 |
| CHEMBL4059904 | — | — | 1 | 6.51 |
| CHEMBL4076937 | — | — | 1 | 6.49 |
| CHEMBL4069074 | — | — | 1 | 6.45 |
| CHEMBL4073477 | — | — | 1 | 6.24 |
| CHEMBL4102034 | — | — | 1 | 6.19 |
| CHEMBL4097984 | — | — | 1 | 6.17 |
| CHEMBL4102347 | — | — | 1 | 6.17 |
| CHEMBL4084054 | — | — | 1 | 6.15 |
| CHEMBL4066884 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4076860 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4081464 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL4097816 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL4089338 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL4059493 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4076708 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4064068 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL4090101 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4101547 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4063425 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL4077032 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL4068155 | — | Ki | = | 36.0 | nM | 7.44 |
| CHEMBL4093999 | — | Ki | = | 45.0 | nM | 7.35 |
| CHEMBL4079783 | — | Ki | = | 51.0 | nM | 7.29 |
| CHEMBL4060217 | — | Ki | = | 77.0 | nM | 7.11 |
| CHEMBL4091048 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL4090268 | — | Ki | = | 114.0 | nM | 6.94 |
| CHEMBL4062257 | — | Ki | = | 119.0 | nM | 6.92 |
| CHEMBL4069022 | — | Ki | = | 151.0 | nM | 6.82 |
| CHEMBL4095362 | — | Ki | = | 218.0 | nM | 6.66 |
| CHEMBL4093805 | — | Ki | = | 256.0 | nM | 6.59 |
| CHEMBL4059904 | — | Ki | = | 306.0 | nM | 6.51 |
| CHEMBL4076937 | — | Ki | = | 325.0 | nM | 6.49 |
| CHEMBL4069074 | — | Ki | = | 354.0 | nM | 6.45 |
| CHEMBL4073477 | — | Ki | = | 576.0 | nM | 6.24 |
| CHEMBL4102034 | — | Ki | = | 652.0 | nM | 6.19 |
| CHEMBL4097984 | — | Ki | = | 672.0 | nM | 6.17 |
| CHEMBL4102347 | — | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL4084054 | — | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL4066884 | — | Ki | = | 768.0 | nM | 6.12 |
| CHEMBL4087672 | — | Ki | = | 782.0 | nM | 6.11 |
| CHEMBL4097647 | — | Ki | = | 884.0 | nM | 6.05 |
| CHEMBL4071328 | — | Ki | = | 1440.0 | nM | 5.84 |
| CHEMBL4075754 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL4093649 | — | Ki | = | 2172.0 | nM | 5.66 |
| CHEMBL4095155 | — | Ki | = | 2408.0 | nM | 5.62 |
| CHEMBL4096333 | — | Ki | = | 3817.0 | nM | 5.42 |
| CHEMBL4078833 | — | Ki | = | 3890.0 | nM | 5.41 |