Assay Detail
Binding
CHEMBL887077
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Inhibition of KDR after 90 mins by HTRF assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Intermediate |
Target
Vascular endothelial growth factor receptor 2 (CHEMBL279) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis, structural analysis, and SAR studies of triazine derivatives as potent, selective Tie-2 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.10 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221484 | — | — | 1 | 8.70 |
| CHEMBL394693 | — | — | 1 | 8.70 |
| CHEMBL245745 | — | — | 1 | 8.30 |
| CHEMBL246151 | — | — | 1 | 8.05 |
| CHEMBL246150 | — | — | 1 | 7.75 |
| CHEMBL245947 | — | — | 1 | 7.75 |
| CHEMBL245744 | — | — | 1 | 7.70 |
| CHEMBL394692 | — | — | 1 | 7.42 |
| CHEMBL245549 | — | — | 1 | 7.21 |
| CHEMBL245746 | — | — | 1 | 6.93 |
| CHEMBL394694 | — | — | 1 | 6.89 |
| CHEMBL397090 | — | — | 1 | 6.63 |
| CHEMBL397089 | — | — | 1 | 6.51 |
| CHEMBL246152 | — | — | 1 | 6.36 |
| CHEMBL245948 | — | — | 1 | 6.34 |
| CHEMBL246356 | — | — | 1 | 6.00 |
| CHEMBL246355 | — | — | 1 | 5.95 |
| CHEMBL245949 | — | — | 1 | 4.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221484 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL394693 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL245745 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL246151 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL246150 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL245947 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL245744 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL394692 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL245549 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL245746 | — | IC50 | = | 117.0 | nM | 6.93 |
| CHEMBL394694 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL397090 | — | IC50 | = | 233.0 | nM | 6.63 |
| CHEMBL397089 | — | IC50 | = | 309.0 | nM | 6.51 |
| CHEMBL246152 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL245948 | — | IC50 | = | 456.0 | nM | 6.34 |
| CHEMBL246356 | — | IC50 | = | 1002.0 | nM | 6.00 |
| CHEMBL246355 | — | IC50 | = | 1126.0 | nM | 5.95 |
| CHEMBL245949 | — | IC50 | = | 25000.0 | nM | 4.60 |