Assay Detail
Binding
CHEMBL1908731
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for PDGFRA 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
Platelet-derived growth factor receptor alpha (CHEMBL2007) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.25 | 9.39 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 9.39 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.33 |
| CHEMBL1908396 | — | — | 1 | 9.31 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 9.29 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 9.10 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.96 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.62 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.38 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.35 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 8.31 |
| CHEMBL386051 | — | — | 1 | 8.25 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 8.00 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 8.00 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.96 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 7.96 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.80 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 7.60 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 7.57 |
| CHEMBL1908395 | — | — | 1 | 7.57 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.51 |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | 7.42 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.27 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.22 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.21 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 7.02 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.89 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.75 |
| CHEMBL1230020 | PLX-4720 | — | 1 | 6.72 |
| CHEMBL1241674 | — | — | 1 | 6.66 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL491473 | CEDIRANIB | Kd | = | 0.41 | nM | 9.39 |
| CHEMBL5416410 | DASATINIB | Kd | = | 0.47 | nM | 9.33 |
| CHEMBL1908396 | — | Kd | = | 0.49 | nM | 9.31 |
| CHEMBL1289926 | AXITINIB | Kd | = | 0.51 | nM | 9.29 |
| CHEMBL535 | SUNITINIB | Kd | = | 0.79 | nM | 9.10 |
| CHEMBL1721885 | SU-014813 | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL223360 | LINIFANIB | Kd | = | 4.2 | nM | 8.38 |
| CHEMBL1230609 | FORETINIB | Kd | = | 4.5 | nM | 8.35 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL386051 | — | Kd | = | 5.6 | nM | 8.25 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL572881 | MOTESANIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL377300 | BRIVANIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL1908391 | MASITINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL574738 | AST-487 | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL1908395 | — | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL941 | IMATINIB | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL522892 | DOVITINIB | Kd | = | 54.0 | nM | 7.27 |
| CHEMBL475251 | R-406 | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL1336 | SORAFENIB | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL101253 | VATALANIB | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL1908397 | KW-2449 | Kd | = | 130.0 | nM | 6.89 |
| CHEMBL255863 | NILOTINIB | Kd | = | 180.0 | nM | 6.75 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL1241674 | — | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL24828 | VANDETANIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL509032 | TAE-684 | Kd | = | 840.0 | nM | 6.08 |
| CHEMBL558752 | RAF-265 | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 1600.0 | nM | 5.80 |
| CHEMBL553 | ERLOTINIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL450786 | PHA-665752 | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 5100.0 | nM | 5.29 |
| CHEMBL31965 | CANERTINIB | Kd | = | 5200.0 | nM | 5.28 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 5900.0 | nM | 5.23 |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | = | 8800.0 | nM | 5.06 |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |