Assay Detail
Binding
CHEMBL678756
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Inhibition of fms-like tyrosine kinase receptor (Flt-1) kinase activity at a concentration of 2 uM of ATP
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel 4-anilinoquinazolines with C-7 basic side chains: design and structure activity relationship of a series of potent, orally active, VEGF receptor tyrosine kinase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 31 | 6.34 | 7.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2448066 | — | — | 1 | 7.70 |
| CHEMBL1202473 | — | — | 1 | 7.60 |
| CHEMBL25579 | — | — | 1 | 7.00 |
| CHEMBL24979 | — | — | 1 | 6.82 |
| CHEMBL26641 | — | — | 1 | 6.70 |
| CHEMBL24137 | — | — | 1 | 6.70 |
| CHEMBL2448067 | — | — | 1 | 6.70 |
| CHEMBL422758 | — | — | 1 | 6.52 |
| CHEMBL283088 | — | — | 1 | 6.52 |
| CHEMBL286160 | — | — | 1 | 6.40 |
| CHEMBL25450 | — | — | 1 | 6.35 |
| CHEMBL281990 | — | — | 1 | 6.30 |
| CHEMBL416191 | — | — | 1 | 6.30 |
| CHEMBL25425 | — | — | 1 | 6.30 |
| CHEMBL1907764 | — | — | 1 | 6.30 |
| CHEMBL1907944 | — | — | 1 | 6.30 |
| CHEMBL1202477 | — | — | 1 | 6.26 |
| CHEMBL1744347 | — | — | 1 | 6.22 |
| CHEMBL1202478 | — | — | 1 | 6.19 |
| CHEMBL428534 | — | — | 1 | 6.16 |
| CHEMBL281872 | ZD-4190 FREE BASE | 1.0 | 1 | 6.16 |
| CHEMBL1907763 | — | — | 1 | 6.16 |
| CHEMBL1744349 | — | — | 1 | 6.12 |
| CHEMBL279459 | — | — | 1 | 6.10 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.05 |
| CHEMBL2448064 | — | — | 1 | 6.00 |
| CHEMBL25610 | — | — | 1 | 5.96 |
| CHEMBL26050 | — | — | 1 | 5.82 |
| CHEMBL533849 | — | — | 1 | 5.80 |
| CHEMBL2448065 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2448066 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL1202473 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL25579 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL24979 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL26641 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL24137 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL2448067 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL422758 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL283088 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL286160 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL25450 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL281990 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL416191 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL25425 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1907764 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1907944 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL1202477 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL1744347 | — | IC50 | = | 600.0 | nM | 6.22 |
| CHEMBL1202478 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL1907763 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL281872 | ZD-4190 FREE BASE | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL428534 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL1744349 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL279459 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL24828 | VANDETANIB | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL2448064 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL25610 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL26050 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL533849 | — | IC50 | = | 1600.0 | nM | 5.80 |
| CHEMBL2448065 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL24026 | — | IC50 | = | 3900.0 | nM | 5.41 |