Assay Detail
Binding
CHEMBL4357705
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human His-tagged full length SRC expressed in baculovirus expression system using tyrosine-2 peptide as substrate incubated for 1 hr by Z'-LYTE assay
30
Total Activities
30
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
Structure-Based Design of a Potent and Selective Covalent Inhibitor for SRC Kinase That Targets a P-Loop Cysteine.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 30 | 7.64 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4538743 | — | — | 1 | 8.70 |
| CHEMBL4574265 | — | — | 1 | 8.52 |
| CHEMBL4548584 | — | — | 1 | 8.52 |
| CHEMBL4515441 | — | — | 1 | 8.52 |
| CHEMBL4462060 | — | — | 1 | 8.52 |
| CHEMBL3883384 | — | — | 1 | 8.40 |
| CHEMBL4452399 | — | — | 1 | 8.40 |
| CHEMBL4460150 | — | — | 1 | 8.30 |
| CHEMBL4470506 | — | — | 1 | 8.30 |
| CHEMBL4442889 | — | — | 1 | 8.30 |
| CHEMBL4569421 | — | — | 1 | 8.22 |
| CHEMBL4562024 | — | — | 1 | 8.22 |
| CHEMBL4563120 | — | — | 1 | 8.22 |
| CHEMBL4537568 | — | — | 1 | 8.15 |
| CHEMBL4453645 | — | — | 1 | 8.10 |
| CHEMBL4578438 | — | — | 1 | 8.10 |
| CHEMBL4436957 | — | — | 1 | 8.05 |
| CHEMBL4442593 | — | — | 1 | 7.85 |
| CHEMBL4442601 | — | — | 1 | 7.66 |
| CHEMBL4517070 | — | — | 1 | 7.48 |
| CHEMBL4592277 | — | — | 1 | 7.10 |
| CHEMBL4463781 | — | — | 1 | 6.92 |
| CHEMBL4517370 | — | — | 1 | 6.65 |
| CHEMBL4528820 | — | — | 1 | 6.03 |
| CHEMBL4475369 | — | — | 1 | 6.00 |
| CHEMBL4447910 | — | — | 1 | 5.92 |
| CHEMBL4460793 | — | — | 1 | 5.45 |
| CHEMBL4561015 | — | — | 1 | 5.40 |
| CHEMBL4556686 | — | — | 1 | - |
| CHEMBL4443649 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4538743 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4574265 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4548584 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4515441 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4462060 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3883384 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4452399 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4460150 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4470506 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4442889 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4569421 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4562024 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4563120 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4537568 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4453645 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4578438 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4436957 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4442593 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4442601 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL4517070 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL4592277 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL4463781 | — | IC50 | = | 121.0 | nM | 6.92 |
| CHEMBL4517370 | — | IC50 | = | 226.0 | nM | 6.65 |
| CHEMBL4528820 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL4475369 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4447910 | — | IC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL4460793 | — | IC50 | = | 3580.0 | nM | 5.45 |
| CHEMBL4561015 | — | IC50 | = | 4010.0 | nM | 5.40 |
| CHEMBL4556686 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4443649 | — | IC50 | > | 3330.0 | nM | - |