Assay Detail
Binding
CHEMBL1908550
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Binding constant for FLT1 kinase domain
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Vascular endothelial growth factor receptor 1 (CHEMBL1868) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.93 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 9.13 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.74 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.42 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.33 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 8.24 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.12 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 8.02 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 8.00 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 7.92 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.85 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.80 |
| CHEMBL386051 | — | — | 1 | 7.64 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.51 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.39 |
| CHEMBL1908395 | — | — | 1 | 7.28 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.20 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.16 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.14 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.07 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.00 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.96 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.92 |
| CHEMBL1908396 | — | — | 1 | 6.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 6.82 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.58 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 6.39 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.35 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.26 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.10 |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | Kd | = | 0.74 | nM | 9.13 |
| CHEMBL535 | SUNITINIB | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL1230609 | FORETINIB | Kd | = | 3.8 | nM | 8.42 |
| CHEMBL1721885 | SU-014813 | Kd | = | 4.7 | nM | 8.33 |
| CHEMBL1289926 | AXITINIB | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL223360 | LINIFANIB | Kd | = | 7.5 | nM | 8.12 |
| CHEMBL101253 | VATALANIB | Kd | = | 9.6 | nM | 8.02 |
| CHEMBL377300 | BRIVANIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL572881 | MOTESANIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL475251 | R-406 | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL386051 | — | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL1336 | SORAFENIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL1908395 | — | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL522892 | DOVITINIB | Kd | = | 69.0 | nM | 7.16 |
| CHEMBL1908397 | KW-2449 | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL574738 | AST-487 | Kd | = | 86.0 | nM | 7.07 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL1908396 | — | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL24828 | VANDETANIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL509032 | TAE-684 | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL558752 | RAF-265 | Kd | = | 800.0 | nM | 6.10 |
| CHEMBL259084 | MLN-8054 | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL1241674 | — | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 4300.0 | nM | 5.37 |
| CHEMBL553 | ERLOTINIB | Kd | = | 4400.0 | nM | 5.36 |
| CHEMBL5416410 | DASATINIB | Kd | = | 5000.0 | nM | 5.30 |
| CHEMBL31965 | CANERTINIB | Kd | = | 7500.0 | nM | 5.12 |
| CHEMBL296468 | BMS-387032 | Kd | = | 9900.0 | nM | 5.00 |
| CHEMBL255863 | NILOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 10000.0 | nM | - |