Assay Detail
Binding
CHEMBL1908692
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding constant for CSF1R 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
Macrophage colony-stimulating factor 1 receptor (CHEMBL1844) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.27 | 9.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.24 |
| CHEMBL386051 | — | — | 1 | 9.17 |
| CHEMBL1908396 | — | — | 1 | 9.08 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 8.74 |
| CHEMBL261849 | GW632580X | — | 1 | 8.66 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 8.60 |
| CHEMBL1908395 | — | — | 1 | 8.49 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 8.47 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 8.44 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 8.31 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 8.25 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 8.24 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.12 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 8.10 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 8.00 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.96 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.92 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.89 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 7.68 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 7.55 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.51 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 7.35 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 7.35 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.32 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.32 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 7.22 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.96 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 6.92 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.68 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 6.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5416410 | DASATINIB | Kd | = | 0.58 | nM | 9.24 |
| CHEMBL386051 | — | Kd | = | 0.67 | nM | 9.17 |
| CHEMBL1908396 | — | Kd | = | 0.83 | nM | 9.08 |
| CHEMBL1230609 | FORETINIB | Kd | = | 1.8 | nM | 8.74 |
| CHEMBL261849 | GW632580X | Kd | = | 2.2 | nM | 8.66 |
| CHEMBL535 | SUNITINIB | Kd | = | 2.5 | nM | 8.60 |
| CHEMBL1908395 | — | Kd | = | 3.2 | nM | 8.49 |
| CHEMBL223360 | LINIFANIB | Kd | = | 3.4 | nM | 8.47 |
| CHEMBL1721885 | SU-014813 | Kd | = | 3.6 | nM | 8.44 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 4.9 | nM | 8.31 |
| CHEMBL572881 | MOTESANIB | Kd | = | 5.6 | nM | 8.25 |
| CHEMBL574738 | AST-487 | Kd | = | 5.8 | nM | 8.24 |
| CHEMBL1908391 | MASITINIB | Kd | = | 7.6 | nM | 8.12 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 7.9 | nM | 8.10 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 10.0 | nM | 8.00 |
| CHEMBL941 | IMATINIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1289926 | AXITINIB | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL1336 | SORAFENIB | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL475251 | R-406 | Kd | = | 31.0 | nM | 7.51 |
| CHEMBL255863 | NILOTINIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL101253 | VATALANIB | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL509032 | TAE-684 | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL522892 | DOVITINIB | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL1908397 | KW-2449 | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 210.0 | nM | 6.68 |
| CHEMBL558752 | RAF-265 | Kd | = | 250.0 | nM | 6.60 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 330.0 | nM | 6.48 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 620.0 | nM | 6.21 |
| CHEMBL180022 | NERATINIB | Kd | = | 670.0 | nM | 6.17 |
| CHEMBL450786 | PHA-665752 | Kd | = | 700.0 | nM | 6.16 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | = | 2600.0 | nM | 5.58 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 2700.0 | nM | 5.57 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL1241674 | — | Kd | = | 3300.0 | nM | 5.48 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 8100.0 | nM | 5.09 |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 10000.0 | nM | - |