Assay Detail
Binding
CHEMBL1908486
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for KIT(D816V) 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 | 6.55 | 9.19 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 9.19 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 8.60 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 8.59 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.15 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 8.11 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.02 |
| CHEMBL1908395 | — | — | 1 | 7.75 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.58 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 7.54 |
| CHEMBL386051 | — | — | 1 | 7.46 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.33 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.14 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.09 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.89 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 6.82 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 6.80 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.80 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.54 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.54 |
| CHEMBL1241674 | — | — | 1 | 6.52 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.51 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.47 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 6.44 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.42 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.41 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.39 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.30 |
| CHEMBL1908396 | — | — | 1 | 6.24 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.23 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.64 | nM | 9.19 |
| CHEMBL475251 | R-406 | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2.6 | nM | 8.59 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 7.1 | nM | 8.15 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 7.7 | nM | 8.11 |
| CHEMBL1230609 | FORETINIB | Kd | = | 9.6 | nM | 8.02 |
| CHEMBL1908395 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL509032 | TAE-684 | Kd | = | 26.0 | nM | 7.58 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 29.0 | nM | 7.54 |
| CHEMBL386051 | — | Kd | = | 35.0 | nM | 7.46 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 47.0 | nM | 7.33 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL223360 | LINIFANIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL494089 | GSK-690693 | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL1908397 | KW-2449 | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL24828 | VANDETANIB | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL1241674 | — | Kd | = | 300.0 | nM | 6.52 |
| CHEMBL1336 | SORAFENIB | Kd | = | 310.0 | nM | 6.51 |
| CHEMBL1721885 | SU-014813 | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL574738 | AST-487 | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL535 | SUNITINIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 390.0 | nM | 6.41 |
| CHEMBL572881 | MOTESANIB | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 500.0 | nM | 6.30 |
| CHEMBL1908396 | — | Kd | = | 580.0 | nM | 6.24 |
| CHEMBL450786 | PHA-665752 | Kd | = | 590.0 | nM | 6.23 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 760.0 | nM | 6.12 |
| CHEMBL255863 | NILOTINIB | Kd | = | 770.0 | nM | 6.11 |
| CHEMBL941 | IMATINIB | Kd | = | 980.0 | nM | 6.01 |
| CHEMBL379218 | — | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1908391 | MASITINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 3100.0 | nM | 5.51 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL31965 | CANERTINIB | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL377300 | BRIVANIB | Kd | = | 4000.0 | nM | 5.40 |
| CHEMBL939 | GEFITINIB | Kd | = | 4300.0 | nM | 5.37 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 4600.0 | nM | 5.34 |
| CHEMBL558752 | RAF-265 | Kd | = | 6200.0 | nM | 5.21 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 7100.0 | nM | 5.15 |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |