Assay Detail
Binding
CHEMBL3429155
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Inhibition of ACK1 kinase (unknown origin)
10
Total Activities
10
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Development of novel ACK1/TNK2 inhibitors using a fragment-based approach.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 7 | 7.75 | 8.70 |
| Kd | 2 | 8.46 | 8.70 |
| Ki | 1 | 9.52 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2087874 | — | — | 1 | 9.52 |
| CHEMBL487242 | — | — | 1 | 8.70 |
| CHEMBL1672987 | — | — | 1 | 8.70 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.57 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.22 |
| CHEMBL247479 | — | — | 1 | 7.96 |
| CHEMBL472392 | — | — | 1 | 7.70 |
| CHEMBL3426891 | — | — | 1 | 7.25 |
| CHEMBL3426892 | — | — | 1 | 7.09 |
| CHEMBL2325940 | — | — | 1 | 6.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2087874 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL487242 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1672987 | — | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL288441 | BOSUTINIB | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL5416410 | DASATINIB | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL247479 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL472392 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL3426891 | — | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL3426892 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2325940 | — | IC50 | = | 110.0 | nM | 6.96 |