Assay Detail
Binding
CHEMBL3364612
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Inhibition of KDR (unknown origin) by FRET-based homogeneous assay
17
Total Activities
17
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
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The discovery of Polo-like kinase 4 inhibitors: design and optimization of spiro[cyclopropane-1,3'[3H]indol]-2'(1'H).ones as orally bioavailable antitumor agents.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.20 | 7.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3353362 | — | — | 1 | 7.92 |
| CHEMBL2407897 | — | — | 1 | 7.66 |
| CHEMBL2407749 | — | — | 1 | 7.47 |
| CHEMBL3353347 | — | — | 1 | 6.96 |
| CHEMBL3353359 | — | — | 1 | 6.92 |
| CHEMBL2407900 | — | — | 1 | 6.32 |
| CHEMBL3353348 | — | — | 1 | 6.04 |
| CHEMBL3353340 | — | — | 1 | 5.89 |
| CHEMBL3353354 | — | — | 1 | 5.85 |
| CHEMBL3353341 | — | — | 1 | 5.70 |
| CHEMBL3353344 | — | — | 1 | 5.68 |
| CHEMBL3353337 | — | — | 1 | 5.60 |
| CHEMBL3353349 | — | — | 1 | 5.31 |
| CHEMBL3353358 | — | — | 1 | 5.10 |
| CHEMBL3353355 | — | — | 1 | 4.62 |
| CHEMBL3353339 | — | — | 1 | - |
| CHEMBL3353338 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3353362 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL2407897 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL2407749 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3353347 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL3353359 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2407900 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL3353348 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3353340 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL3353354 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3353341 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3353344 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL3353337 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL3353349 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3353358 | — | IC50 | = | 7900.0 | nM | 5.10 |
| CHEMBL3353355 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL3353339 | — | IC50 | - | — | - | |
| CHEMBL3353338 | — | IC50 | > | 10000.0 | nM | - |