Assay Detail
Binding
CHEMBL1908488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for KIT(V559D) 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
Mast/stem cell growth factor receptor Kit (CHEMBL1936) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.65 | 9.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 9.57 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.39 |
| CHEMBL1908396 | — | — | 1 | 9.34 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 9.31 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 9.29 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.17 |
| CHEMBL386051 | — | — | 1 | 8.80 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.77 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.68 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 8.64 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 8.49 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.42 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.30 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.30 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 8.24 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.24 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.20 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.14 |
| CHEMBL1908395 | — | — | 1 | 8.11 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.82 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.82 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.82 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.80 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 7.77 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.64 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 7.46 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 7.42 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.34 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 7.24 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | Kd | = | 0.27 | nM | 9.57 |
| CHEMBL535 | SUNITINIB | Kd | = | 0.41 | nM | 9.39 |
| CHEMBL1908396 | — | Kd | = | 0.46 | nM | 9.34 |
| CHEMBL1289926 | AXITINIB | Kd | = | 0.49 | nM | 9.31 |
| CHEMBL1721885 | SU-014813 | Kd | = | 0.51 | nM | 9.29 |
| CHEMBL5416410 | DASATINIB | Kd | = | 0.68 | nM | 9.17 |
| CHEMBL386051 | — | Kd | = | 1.6 | nM | 8.80 |
| CHEMBL223360 | LINIFANIB | Kd | = | 1.7 | nM | 8.77 |
| CHEMBL1230609 | FORETINIB | Kd | = | 2.1 | nM | 8.68 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 2.3 | nM | 8.64 |
| CHEMBL572881 | MOTESANIB | Kd | = | 3.2 | nM | 8.49 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 3.8 | nM | 8.42 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL574738 | AST-487 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1908391 | MASITINIB | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL475251 | R-406 | Kd | = | 5.7 | nM | 8.24 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 6.3 | nM | 8.20 |
| CHEMBL522892 | DOVITINIB | Kd | = | 7.2 | nM | 8.14 |
| CHEMBL1908395 | — | Kd | = | 7.7 | nM | 8.11 |
| CHEMBL941 | IMATINIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 15.0 | nM | 7.82 |
| CHEMBL1336 | SORAFENIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL101253 | VATALANIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL1908397 | KW-2449 | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL377300 | BRIVANIB | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL255863 | NILOTINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL509032 | TAE-684 | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL558752 | RAF-265 | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL24828 | VANDETANIB | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 200.0 | nM | 6.70 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL1241674 | — | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL450786 | PHA-665752 | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL553 | ERLOTINIB | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL249697 | BMS-345541 | Kd | = | 5700.0 | nM | 5.24 |
| CHEMBL494089 | GSK-690693 | Kd | = | 7300.0 | nM | 5.14 |
| CHEMBL31965 | CANERTINIB | Kd | = | 7900.0 | nM | 5.10 |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |