Assay Detail
Binding
CHEMBL3429862
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Src
27
Total Activities
27
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
Proto-oncogene tyrosine-protein kinase Src (CHEMBL267) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, Synthesis, and Structure-Activity Relationship Studies of 3-(Phenylethynyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine Derivatives as a New Class of Src Inhibitors with Potent Activities in Models of Triple Negative Breast Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 8.05 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.52 |
| CHEMBL3426225 | — | — | 1 | 9.05 |
| CHEMBL3425518 | — | — | 1 | 9.00 |
| CHEMBL3426222 | — | — | 1 | 8.70 |
| CHEMBL3426217 | — | — | 1 | 8.70 |
| CHEMBL3426219 | — | — | 1 | 8.70 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 8.52 |
| CHEMBL3426220 | — | — | 1 | 8.52 |
| CHEMBL3426218 | — | — | 1 | 8.40 |
| CHEMBL3426223 | — | — | 1 | 8.40 |
| CHEMBL3426234 | — | — | 1 | 8.30 |
| CHEMBL3426224 | — | — | 1 | 8.15 |
| CHEMBL3426230 | — | — | 1 | 8.15 |
| CHEMBL3426229 | — | — | 1 | 8.15 |
| CHEMBL3426228 | — | — | 1 | 8.10 |
| CHEMBL3426226 | — | — | 1 | 8.05 |
| CHEMBL3426235 | — | — | 1 | 7.96 |
| CHEMBL3426232 | — | — | 1 | 7.92 |
| CHEMBL3426233 | — | — | 1 | 7.82 |
| CHEMBL3426227 | — | — | 1 | 7.72 |
| CHEMBL3426221 | — | — | 1 | 7.68 |
| CHEMBL3426239 | — | — | 1 | 7.23 |
| CHEMBL3426236 | — | — | 1 | 7.08 |
| CHEMBL3426237 | — | — | 1 | 5.85 |
| CHEMBL3426240 | — | — | 1 | 5.50 |
| CHEMBL3426231 | — | — | 1 | - |
| CHEMBL3426238 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL3426225 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL3425518 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3426222 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3426217 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3426219 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL1171837 | PONATINIB | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3426220 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3426218 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3426223 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3426234 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3426224 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3426230 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3426229 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3426228 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL3426226 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL3426235 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3426232 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3426233 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3426227 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3426221 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3426239 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL3426236 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL3426237 | — | IC50 | = | 1409.0 | nM | 5.85 |
| CHEMBL3426240 | — | IC50 | = | 3191.0 | nM | 5.50 |
| CHEMBL3426231 | — | IC50 | - | — | - | |
| CHEMBL3426238 | — | IC50 | - | — | - |