Assay Detail
Binding
CHEMBL4059305
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of KDR (unknown origin) expressed in mouse Ba/F3 cells
35
Total Activities
35
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 N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-Related Macular Degeneration.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 35 | 8.01 | 9.15 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4076909 | — | — | 1 | 9.15 |
| CHEMBL3746776 | — | — | 1 | 9.05 |
| CHEMBL4077373 | — | — | 1 | 8.89 |
| CHEMBL4080062 | BFH-772 | 2.0 | 1 | 8.89 |
| CHEMBL4104297 | — | — | 1 | 8.77 |
| CHEMBL4086718 | — | — | 1 | 8.70 |
| CHEMBL3808921 | — | — | 1 | 8.70 |
| CHEMBL4092692 | — | — | 1 | 8.68 |
| CHEMBL3746562 | — | — | 1 | 8.64 |
| CHEMBL4064471 | — | — | 1 | 8.60 |
| CHEMBL4079136 | — | — | 1 | 8.60 |
| CHEMBL4103267 | — | — | 1 | 8.55 |
| CHEMBL3747273 | — | — | 1 | 8.39 |
| CHEMBL4084937 | — | — | 1 | 8.39 |
| CHEMBL4102438 | — | — | 1 | 8.30 |
| CHEMBL4087814 | — | — | 1 | 8.24 |
| CHEMBL3746370 | — | — | 1 | 8.21 |
| CHEMBL4077291 | — | — | 1 | 8.10 |
| CHEMBL4074672 | — | — | 1 | 8.06 |
| CHEMBL4097955 | — | — | 1 | 8.03 |
| CHEMBL4065008 | — | — | 1 | 8.00 |
| CHEMBL3747063 | — | — | 1 | 7.95 |
| CHEMBL4103383 | — | — | 1 | 7.89 |
| CHEMBL4102888 | — | — | 1 | 7.89 |
| CHEMBL4076112 | — | — | 1 | 7.76 |
| CHEMBL4100555 | — | — | 1 | 7.75 |
| CHEMBL4079937 | — | — | 1 | 7.60 |
| CHEMBL3746122 | — | — | 1 | 7.58 |
| CHEMBL3745816 | — | — | 1 | 7.23 |
| CHEMBL4079318 | — | — | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4076909 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3746776 | — | IC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4077373 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4080062 | BFH-772 | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL4104297 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL4086718 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3808921 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4092692 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3746562 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL4064471 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4079136 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL4103267 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3747273 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4084937 | — | IC50 | = | 4.1 | nM | 8.39 |
| CHEMBL4102438 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4087814 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL3746370 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL4077291 | — | IC50 | = | 7.9 | nM | 8.10 |
| CHEMBL4074672 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4097955 | — | IC50 | = | 9.4 | nM | 8.03 |
| CHEMBL4065008 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL3747063 | — | IC50 | = | 11.2 | nM | 7.95 |
| CHEMBL4103383 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL4102888 | — | IC50 | = | 12.8 | nM | 7.89 |
| CHEMBL4076112 | — | IC50 | = | 17.4 | nM | 7.76 |
| CHEMBL4100555 | — | IC50 | = | 17.9 | nM | 7.75 |
| CHEMBL4079937 | — | IC50 | = | 25.2 | nM | 7.60 |
| CHEMBL3746122 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3745816 | — | IC50 | = | 59.4 | nM | 7.23 |
| CHEMBL4079318 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4079917 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4065713 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL4068360 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL4079003 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL4086998 | — | IC50 | = | 1720.0 | nM | 5.76 |