Assay Detail
Binding
CHEMBL997160
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Inhibition of chicken N-terminal His-tagged cSrc T338M mutant expressed in Escherichia coli BL21 (DE3)
6
Total Activities
6
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 | 6 | 6.24 | 7.64 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL510516 | — | — | 1 | 7.64 |
| CHEMBL497033 | — | — | 1 | 7.47 |
| CHEMBL526930 | — | — | 1 | 7.00 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.32 |
| CHEMBL498947 | — | — | 1 | 4.56 |
| CHEMBL497615 | — | — | 1 | 4.43 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL510516 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL497033 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL526930 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5416410 | DASATINIB | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL498947 | — | IC50 | = | 27800.0 | nM | 4.56 |
| CHEMBL497615 | — | IC50 | = | 36800.0 | nM | 4.43 |