Assay Detail
Binding
CHEMBL3598617
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of PAK1 (unknown origin) expressed in cryopreserved human MCF10A cells assessed as reduction in enzyme phosphorylation at Ser144 residue
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MCF-10A |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Serine/threonine-protein kinase PAK 1 (CHEMBL4600) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Identification and optimisation of 7-azaindole PAK1 inhibitors with improved potency and kinase selectivity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 6.34 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3597013 | — | — | 1 | 7.06 |
| CHEMBL3597011 | — | — | 1 | 6.85 |
| CHEMBL3596932 | — | — | 1 | 6.19 |
| CHEMBL3596899 | — | — | 1 | 6.06 |
| CHEMBL3596931 | — | — | 1 | 5.96 |
| CHEMBL3597012 | — | — | 1 | 5.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3597013 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3597011 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3596932 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3596899 | — | IC50 | = | 870.0 | nM | 6.06 |
| CHEMBL3596931 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL3597012 | — | IC50 | = | 1300.0 | nM | 5.89 |