Assay Detail
Functional
CHEMBL914745
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of VEGF-induced phosphorylation of human KDR expressed in mouse NIH3T3 cell line by ELISA
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NIH3T3 |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
1,4-Dihydroindeno[1,2-c]pyrazoles with acetylenic side chains as novel and potent multitargeted receptor tyrosine kinase inhibitors with low affinity for the hERG ion channel.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 7.03 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL225311 | — | — | 1 | 8.30 |
| CHEMBL225336 | — | — | 1 | 7.82 |
| CHEMBL223971 | — | — | 1 | 7.80 |
| CHEMBL225193 | — | — | 1 | 7.60 |
| CHEMBL426009 | — | — | 1 | 7.55 |
| CHEMBL390735 | — | — | 1 | 7.54 |
| CHEMBL390156 | — | — | 1 | 7.40 |
| CHEMBL225639 | — | — | 1 | 7.40 |
| CHEMBL224968 | — | — | 1 | 7.29 |
| CHEMBL223220 | — | — | 1 | 7.19 |
| CHEMBL376779 | — | — | 1 | 6.96 |
| CHEMBL387972 | — | — | 1 | 6.95 |
| CHEMBL213507 | — | — | 1 | 6.84 |
| CHEMBL225248 | — | — | 1 | 6.84 |
| CHEMBL224917 | — | — | 1 | 6.83 |
| CHEMBL225319 | — | — | 1 | 6.75 |
| CHEMBL375890 | — | — | 1 | 6.50 |
| CHEMBL225090 | — | — | 1 | 6.50 |
| CHEMBL387929 | — | — | 1 | 6.38 |
| CHEMBL223997 | — | — | 1 | 6.30 |
| CHEMBL223998 | — | — | 1 | 6.27 |
| CHEMBL225240 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL225311 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL225336 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL223971 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL225193 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL426009 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL390735 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL390156 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL225639 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL224968 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL223220 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL376779 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL387972 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL213507 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL225248 | — | IC50 | = | 146.0 | nM | 6.84 |
| CHEMBL224917 | — | IC50 | = | 148.0 | nM | 6.83 |
| CHEMBL225319 | — | IC50 | = | 178.0 | nM | 6.75 |
| CHEMBL375890 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL225090 | — | IC50 | = | 313.0 | nM | 6.50 |
| CHEMBL387929 | — | IC50 | = | 419.0 | nM | 6.38 |
| CHEMBL223997 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL223998 | — | IC50 | = | 542.0 | nM | 6.27 |
| CHEMBL225240 | — | IC50 | = | 2140.0 | nM | 5.67 |