Assay Detail
Binding
CHEMBL3824531
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of C-terminal His-tagged full length human SRC expressed in insect cells preincubated for 20 mins using poly[Glu,Tyr]4:1 as substrate measured after 5 to 120 mins in presence of [gamma-33P]ATP by Kinome assay
18
Total Activities
18
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
Rapid Discovery and Structure-Activity Relationships of Pyrazolopyrimidines That Potently Suppress Breast Cancer Cell Growth via SRC Kinase Inhibition with Exceptional Selectivity over ABL Kinase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.47 | 9.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3823104 | — | — | 1 | 9.22 |
| CHEMBL3824116 | — | — | 1 | 9.00 |
| CHEMBL3823620 | — | — | 1 | 9.00 |
| CHEMBL3823543 | — | — | 1 | 8.46 |
| CHEMBL306380 | — | — | 1 | 7.77 |
| CHEMBL3823451 | — | — | 1 | 7.68 |
| CHEMBL3823861 | — | — | 1 | 7.57 |
| CHEMBL3824228 | — | — | 1 | 7.15 |
| CHEMBL3823255 | — | — | 1 | 6.94 |
| CHEMBL3823212 | — | — | 1 | 6.90 |
| CHEMBL3823711 | — | — | 1 | 6.71 |
| CHEMBL3823849 | — | — | 1 | 6.52 |
| CHEMBL3822591 | — | — | 1 | 5.98 |
| CHEMBL3799221 | — | — | 1 | 5.61 |
| CHEMBL3824233 | — | — | 1 | - |
| CHEMBL3824089 | — | — | 1 | - |
| CHEMBL3824021 | — | — | 1 | - |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3823104 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3824116 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3823620 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3823543 | — | IC50 | = | 3.5 | nM | 8.46 |
| CHEMBL306380 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3823451 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL3823861 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3824228 | — | IC50 | = | 71.0 | nM | 7.15 |
| CHEMBL3823255 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL3823212 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL3823711 | — | IC50 | = | 194.0 | nM | 6.71 |
| CHEMBL3823849 | — | IC50 | = | 303.0 | nM | 6.52 |
| CHEMBL3822591 | — | IC50 | = | 1040.0 | nM | 5.98 |
| CHEMBL3799221 | — | IC50 | = | 2453.0 | nM | 5.61 |
| CHEMBL3824233 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3824089 | — | IC50 | < | 0.5 | nM | - |
| CHEMBL3824021 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5416410 | DASATINIB | IC50 | < | 0.5 | nM | - |