Assay Detail
Binding
CHEMBL3865530
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Inhibition of PAK1 phosphorylation in human MCF10A cells
18
Total Activities
18
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
Optimization of Highly Kinase Selective Bis-anilino Pyrimidine PAK1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 6.32 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3923175 | — | — | 1 | 7.23 |
| CHEMBL3609327 | — | — | 1 | 7.06 |
| CHEMBL3964858 | — | — | 1 | 6.96 |
| CHEMBL3950903 | — | — | 1 | 6.89 |
| CHEMBL3896232 | — | — | 1 | 6.70 |
| CHEMBL3910608 | — | — | 1 | 6.66 |
| CHEMBL3914181 | — | — | 1 | 6.64 |
| CHEMBL3933198 | — | — | 1 | 6.57 |
| CHEMBL3891484 | — | — | 1 | 6.38 |
| CHEMBL3980696 | — | — | 1 | 6.32 |
| CHEMBL3924245 | — | — | 1 | 6.31 |
| CHEMBL3942173 | — | — | 1 | 6.28 |
| CHEMBL3962678 | — | — | 1 | 6.09 |
| CHEMBL3961614 | — | — | 1 | 6.07 |
| CHEMBL3935195 | — | — | 1 | 5.68 |
| CHEMBL1762546 | — | — | 1 | 5.51 |
| CHEMBL3969873 | — | — | 1 | 5.48 |
| CHEMBL3892617 | — | — | 1 | 4.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3923175 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3609327 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3964858 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3950903 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3896232 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL3910608 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL3914181 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3933198 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL3891484 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL3980696 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3924245 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3942173 | — | IC50 | = | 530.0 | nM | 6.28 |
| CHEMBL3962678 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3961614 | — | IC50 | = | 860.0 | nM | 6.07 |
| CHEMBL3935195 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL1762546 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL3969873 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3892617 | — | IC50 | = | 14000.0 | nM | 4.85 |