Assay Detail
Binding
CHEMBL5146658
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human PAK4 assessed as enzymatic activity incubated for 20 mins by filter binding method
11
Total Activities
11
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
Synthesis and biological evaluation of 7H-pyrrolo [2,3-d] pyrimidine derivatives as potential p21-activated kinase 4 (PAK4) inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.07 | 8.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5180027 | — | — | 1 | 8.57 |
| CHEMBL4097816 | — | — | 1 | 8.05 |
| CHEMBL5183512 | — | — | 1 | 7.70 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 7.42 |
| CHEMBL5184137 | — | — | 1 | 7.30 |
| CHEMBL4297467 | PADNARSERTIB | 2.0 | 1 | 7.00 |
| CHEMBL5202902 | — | — | 1 | 6.78 |
| CHEMBL5170532 | — | — | 1 | 6.64 |
| CHEMBL5183475 | — | — | 1 | 6.64 |
| CHEMBL3799807 | — | — | 1 | 6.10 |
| CHEMBL5184873 | — | — | 1 | 5.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5180027 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4097816 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5183512 | — | IC50 | = | 20.2 | nM | 7.70 |
| CHEMBL3128043 | PF-03758309 | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5184137 | — | IC50 | = | 50.3 | nM | 7.30 |
| CHEMBL4297467 | PADNARSERTIB | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5202902 | — | IC50 | = | 164.5 | nM | 6.78 |
| CHEMBL5170532 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL5183475 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL3799807 | — | IC50 | = | 790.0 | nM | 6.10 |
| CHEMBL5184873 | — | IC50 | = | 2940.0 | nM | 5.53 |