Assay Detail
Binding
CHEMBL5738726
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In vitro kinase inhibition assay: An in vitro kinase assay was performed to evaluate the kinase suppression activity of the most promising cytotoxic candidates 4b, 4j against four different receptor tyrosine kinases (RTKs) - namely epidermal growth factor receptor (EGFR), human epidermal growth factor receptor (HER2), vascular endothelial growth factor receptor-2 (VEGFR-2) and platelet-derived growth factor receptor (PDGFR). The activities of the examined compounds against EGFR, HER2, PDGFR-β, and VEGFR2 were in vitro tested using Abcam's Human In cell ELISA Kit (ab 126419) for EGFR, ADP-Glo TM Kinase Assay for Her2, PDGFR-β, active, recombinant protein expressed in Sf9 cells for VEGFR2 (KDR) Kinase Assay Kit Catalog No. 40325, respectively.
9
Total Activities
3
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Receptor tyrosine-protein kinase erbB-2 (CHEMBL1824) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tetrahydroquinoline derivatives and a process of preparation thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 3 | 9.31 | 9.47 |
| kon | 3 | - | - |
| k_off | 3 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5977738 | — | — | 3 | 9.47 |
| CHEMBL1336 | SORAFENIB | 4.0 | 3 | 9.25 |
| CHEMBL5881155 | — | — | 3 | 9.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5977738 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL1336 | SORAFENIB | IC50 | = | 0.56 | nM | 9.25 |
| CHEMBL5881155 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL5881155 | — | kon | = | - | — | - |
| CHEMBL5881155 | — | k_off | = | - | s-1 | - |
| CHEMBL5977738 | — | kon | = | - | — | - |
| CHEMBL5977738 | — | k_off | = | - | s-1 | - |
| CHEMBL1336 | SORAFENIB | kon | = | - | — | - |
| CHEMBL1336 | SORAFENIB | k_off | = | - | s-1 | - |