Assay Detail
Binding
CHEMBL1908490
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for KIT(V559D,V654A) 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 | 7.11 | 9.68 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.68 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 9.60 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 9.51 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.57 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 8.51 |
| CHEMBL1908396 | — | — | 1 | 8.49 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 8.46 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.33 |
| CHEMBL1908395 | — | — | 1 | 8.22 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.12 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 7.92 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.68 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 7.64 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.58 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.54 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.52 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.44 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.42 |
| CHEMBL386051 | — | — | 1 | 7.17 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.12 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.04 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.00 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.89 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.68 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.62 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.58 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.42 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 6.39 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 6.32 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.25 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL535 | SUNITINIB | Kd | = | 0.21 | nM | 9.68 |
| CHEMBL1721885 | SU-014813 | Kd | = | 0.25 | nM | 9.60 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 0.31 | nM | 9.51 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2.7 | nM | 8.57 |
| CHEMBL522892 | DOVITINIB | Kd | = | 3.1 | nM | 8.51 |
| CHEMBL1908396 | — | Kd | = | 3.2 | nM | 8.49 |
| CHEMBL1289926 | AXITINIB | Kd | = | 3.5 | nM | 8.46 |
| CHEMBL1908391 | MASITINIB | Kd | = | 4.7 | nM | 8.33 |
| CHEMBL1908395 | — | Kd | = | 6.0 | nM | 8.22 |
| CHEMBL1230609 | FORETINIB | Kd | = | 7.6 | nM | 8.12 |
| CHEMBL377300 | BRIVANIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL223360 | LINIFANIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL572881 | MOTESANIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 30.0 | nM | 7.52 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 36.0 | nM | 7.44 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL386051 | — | Kd | = | 68.0 | nM | 7.17 |
| CHEMBL1908397 | KW-2449 | Kd | = | 76.0 | nM | 7.12 |
| CHEMBL941 | IMATINIB | Kd | = | 91.0 | nM | 7.04 |
| CHEMBL574738 | AST-487 | Kd | = | 100.0 | nM | 7.00 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL101253 | VATALANIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL1336 | SORAFENIB | Kd | = | 240.0 | nM | 6.62 |
| CHEMBL255863 | NILOTINIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL475251 | R-406 | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 480.0 | nM | 6.32 |
| CHEMBL24828 | VANDETANIB | Kd | = | 560.0 | nM | 6.25 |
| CHEMBL558752 | RAF-265 | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL509032 | TAE-684 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 2300.0 | nM | 5.64 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL494089 | GSK-690693 | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 3500.0 | nM | 5.46 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 4800.0 | nM | 5.32 |
| CHEMBL450786 | PHA-665752 | Kd | = | 7200.0 | nM | 5.14 |
| CHEMBL31965 | CANERTINIB | Kd | = | 7900.0 | nM | 5.10 |
| CHEMBL10 | SB-203580 | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 10000.0 | nM | - |