Assay Detail
ADMET
CHEMBL4033373
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PAK1 kinase domain using coumarin and fluorescein-labeled ser/thr19 peptide as substrate preincubated for 15 mins followed by ATP addition measured after 60 mins by Z'-Lyte assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| 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
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 | 26 | 6.03 | 6.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4076708 | — | — | 1 | 6.54 |
| CHEMBL4076860 | — | — | 1 | 6.43 |
| CHEMBL4063425 | — | — | 1 | 6.42 |
| CHEMBL4081464 | — | — | 1 | 6.40 |
| CHEMBL4059493 | — | — | 1 | 6.30 |
| CHEMBL4077032 | — | — | 1 | 6.16 |
| CHEMBL4101547 | — | — | 1 | 5.97 |
| CHEMBL4091048 | — | — | 1 | 5.72 |
| CHEMBL4090101 | — | — | 1 | 5.68 |
| CHEMBL4089338 | — | — | 1 | 5.68 |
| CHEMBL4064068 | — | — | 1 | 5.56 |
| CHEMBL4097816 | — | — | 1 | 5.51 |
| CHEMBL4102034 | — | — | 1 | - |
| CHEMBL4097647 | — | — | 1 | - |
| CHEMBL4071328 | — | — | 1 | - |
| CHEMBL4060217 | — | — | 1 | - |
| CHEMBL4093805 | — | — | 1 | - |
| CHEMBL4093999 | — | — | 1 | - |
| CHEMBL4095362 | — | — | 1 | - |
| CHEMBL4069022 | — | — | 1 | - |
| CHEMBL4079783 | — | — | 1 | - |
| CHEMBL4059904 | — | — | 1 | - |
| CHEMBL4062257 | — | — | 1 | - |
| CHEMBL4090268 | — | — | 1 | - |
| CHEMBL4084054 | — | — | 1 | - |
| CHEMBL4068155 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4076708 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL4076860 | — | Ki | = | 368.0 | nM | 6.43 |
| CHEMBL4063425 | — | Ki | = | 383.0 | nM | 6.42 |
| CHEMBL4081464 | — | Ki | = | 401.0 | nM | 6.40 |
| CHEMBL4059493 | — | Ki | = | 503.0 | nM | 6.30 |
| CHEMBL4077032 | — | Ki | = | 690.0 | nM | 6.16 |
| CHEMBL4101547 | — | Ki | = | 1072.0 | nM | 5.97 |
| CHEMBL4091048 | — | Ki | = | 1891.0 | nM | 5.72 |
| CHEMBL4090101 | — | Ki | = | 2080.0 | nM | 5.68 |
| CHEMBL4089338 | — | Ki | = | 2085.0 | nM | 5.68 |
| CHEMBL4064068 | — | Ki | = | 2750.0 | nM | 5.56 |
| CHEMBL4097816 | — | Ki | = | 3112.0 | nM | 5.51 |
| CHEMBL4102034 | — | Ki | - | — | - | |
| CHEMBL4097647 | — | Ki | - | — | - | |
| CHEMBL4071328 | — | Ki | - | — | - | |
| CHEMBL4060217 | — | Ki | - | — | - | |
| CHEMBL4093805 | — | Ki | - | — | - | |
| CHEMBL4093999 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4095362 | — | Ki | > | 4520.0 | nM | - |
| CHEMBL4069022 | — | Ki | > | 4520.0 | nM | - |
| CHEMBL4079783 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL4059904 | — | Ki | > | 4520.0 | nM | - |
| CHEMBL4062257 | — | Ki | - | — | - | |
| CHEMBL4090268 | — | Ki | > | 4520.0 | nM | - |
| CHEMBL4084054 | — | Ki | > | 10.0 | nM | - |
| CHEMBL4068155 | — | Ki | > | 4520.0 | nM | - |