Assay Detail
Binding
CHEMBL910551
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Inhibition of murine Lck in presence of ATP
19
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Mus musculus |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Proto-oncogene tyrosine-protein kinase LCK (CHEMBL2480) ↗| Type | SINGLE PROTEIN |
| Organism | Mus musculus |
Publication
2-aminothiazole as a novel kinase inhibitor template. Structure-activity relationship studies toward the discovery of N-(2-chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1- piperazinyl)]-2-methyl-4-pyrimidinyl]amino)]-1,3-thiazole-5-carboxamide (dasatinib, BMS-354825) as a potent pan-Src kinase inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 5.63 | 7.16 |
| Ki | 2 | 10.04 | 10.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 10.19 |
| CHEMBL364623 | — | — | 1 | 9.89 |
| CHEMBL131346 | — | — | 1 | 7.16 |
| CHEMBL217195 | — | — | 1 | 7.05 |
| CHEMBL215630 | — | — | 1 | 7.00 |
| CHEMBL338159 | — | — | 1 | 6.77 |
| CHEMBL130719 | — | — | 1 | 6.50 |
| CHEMBL214028 | — | — | 1 | 6.29 |
| CHEMBL128589 | — | — | 1 | 6.14 |
| CHEMBL340322 | — | — | 1 | 5.62 |
| CHEMBL66109 | — | — | 1 | 5.52 |
| CHEMBL307976 | — | — | 1 | 5.18 |
| CHEMBL129454 | — | — | 1 | 5.12 |
| CHEMBL334333 | — | — | 1 | 5.02 |
| CHEMBL132399 | — | — | 1 | 4.61 |
| CHEMBL216646 | — | — | 1 | 4.56 |
| CHEMBL214949 | — | — | 1 | 4.48 |
| CHEMBL336330 | — | — | 1 | 4.39 |
| CHEMBL128568 | — | — | 1 | 4.34 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Ki | = | 0.064 | nM | 10.19 |
| CHEMBL364623 | — | Ki | = | 0.13 | nM | 9.89 |
| CHEMBL131346 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL217195 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL215630 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL338159 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL130719 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL214028 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL128589 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL340322 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL66109 | — | IC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL307976 | — | IC50 | = | 6600.0 | nM | 5.18 |
| CHEMBL129454 | — | IC50 | = | 7500.0 | nM | 5.12 |
| CHEMBL334333 | — | IC50 | = | 9600.0 | nM | 5.02 |
| CHEMBL132399 | — | IC50 | = | 24300.0 | nM | 4.61 |
| CHEMBL216646 | — | IC50 | = | 27400.0 | nM | 4.56 |
| CHEMBL214949 | — | IC50 | = | 33320.0 | nM | 4.48 |
| CHEMBL336330 | — | IC50 | = | 40300.0 | nM | 4.39 |
| CHEMBL128568 | — | IC50 | = | 45700.0 | nM | 4.34 |