Assay Detail
Binding
CHEMBL1908547
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Binding constant for DDR1 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
Epithelial discoidin domain-containing receptor 1 (CHEMBL5319) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 7.15 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.70 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.16 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 9.16 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 9.15 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 8.96 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 8.82 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 8.77 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 8.72 |
| CHEMBL386051 | — | — | 1 | 8.62 |
| CHEMBL1908391 | MASITINIB | 3.0 | 1 | 8.06 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 8.03 |
| CHEMBL1908395 | — | — | 1 | 8.03 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.96 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.92 |
| CHEMBL1908396 | — | — | 1 | 7.92 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 7.89 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.72 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 7.55 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.24 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 7.24 |
| CHEMBL450786 | PHA-665752 | — | 1 | 7.16 |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | 7.09 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.92 |
| CHEMBL509032 | TAE-684 | — | 1 | 6.85 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 6.80 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.58 |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | 6.57 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 6.47 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 6.40 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 6.29 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1230609 | FORETINIB | Kd | = | 0.2 | nM | 9.70 |
| CHEMBL574738 | AST-487 | Kd | = | 0.69 | nM | 9.16 |
| CHEMBL5416410 | DASATINIB | Kd | = | 0.69 | nM | 9.16 |
| CHEMBL941 | IMATINIB | Kd | = | 0.7 | nM | 9.15 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1.1 | nM | 8.96 |
| CHEMBL1336 | SORAFENIB | Kd | = | 1.5 | nM | 8.82 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 1.7 | nM | 8.77 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 1.9 | nM | 8.72 |
| CHEMBL386051 | — | Kd | = | 2.4 | nM | 8.62 |
| CHEMBL1908391 | MASITINIB | Kd | = | 8.7 | nM | 8.06 |
| CHEMBL475251 | R-406 | Kd | = | 9.3 | nM | 8.03 |
| CHEMBL1908395 | — | Kd | = | 9.4 | nM | 8.03 |
| CHEMBL24828 | VANDETANIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1908396 | — | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL558752 | RAF-265 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 57.0 | nM | 7.24 |
| CHEMBL223360 | LINIFANIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL450786 | PHA-665752 | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL509032 | TAE-684 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL377300 | BRIVANIB | Kd | = | 160.0 | nM | 6.80 |
| CHEMBL572881 | MOTESANIB | Kd | = | 260.0 | nM | 6.58 |
| CHEMBL101253 | VATALANIB | Kd | = | 270.0 | nM | 6.57 |
| CHEMBL1289926 | AXITINIB | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL31965 | CANERTINIB | Kd | = | 400.0 | nM | 6.40 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 510.0 | nM | 6.29 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 510.0 | nM | 6.29 |
| CHEMBL1241674 | — | Kd | = | 740.0 | nM | 6.13 |
| CHEMBL553 | ERLOTINIB | Kd | = | 790.0 | nM | 6.10 |
| CHEMBL10 | SB-203580 | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 1400.0 | nM | 5.85 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL535 | SUNITINIB | Kd | = | 2000.0 | nM | 5.70 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 2400.0 | nM | 5.62 |
| CHEMBL522892 | DOVITINIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL1908397 | KW-2449 | Kd | = | 3200.0 | nM | 5.50 |
| CHEMBL259084 | MLN-8054 | Kd | = | 4200.0 | nM | 5.38 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 7200.0 | nM | 5.14 |
| CHEMBL221959 | TOFACITINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL91829 | RUBOXISTAURIN | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 10000.0 | nM | - |
| CHEMBL573339 | PI-103 | Kd | > | 10000.0 | nM | - |