Assay Detail
Binding
CHEMBL997159
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of wild type chicken N-terminal His-tagged cSrc expressed in Escherichia coli BL21 (DE3)
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Gallus gallus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Proto-oncogene tyrosine-protein kinase Src (CHEMBL3655) ↗| Type | SINGLE PROTEIN |
| Organism | Gallus gallus |
Publication
Hybrid compound design to overcome the gatekeeper T338M mutation in cSrc.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 6.58 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.40 |
| CHEMBL510516 | — | — | 1 | 7.85 |
| CHEMBL497033 | — | — | 1 | 7.68 |
| CHEMBL526930 | — | — | 1 | 7.15 |
| CHEMBL526560 | — | — | 1 | 6.68 |
| CHEMBL497615 | — | — | 1 | 6.63 |
| CHEMBL188762 | — | — | 1 | 5.19 |
| CHEMBL498947 | — | — | 1 | 4.49 |
| CHEMBL522387 | — | — | 1 | 4.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | IC50 | = | 0.4 | nM | 9.40 |
| CHEMBL510516 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL497033 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL526930 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL526560 | — | IC50 | = | 207.0 | nM | 6.68 |
| CHEMBL497615 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL188762 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL498947 | — | IC50 | = | 32100.0 | nM | 4.49 |
| CHEMBL522387 | — | IC50 | = | 64100.0 | nM | 4.19 |