Assay Detail
Binding
CHEMBL1908461
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Binding constant for CLK1 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
Dual specificity protein kinase CLK1 (CHEMBL4224) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.41 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL379218 | — | — | 1 | 8.85 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 8.06 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.02 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.92 |
| CHEMBL464552 | — | — | 1 | 7.68 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.66 |
| CHEMBL388978 | STAUROSPORINE | — | 1 | 7.50 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.19 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 7.18 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 6.96 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | 6.85 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 6.46 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.44 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.39 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.29 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.26 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 6.22 |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | 6.20 |
| CHEMBL608154 | — | — | 1 | 6.19 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.14 |
| CHEMBL1908395 | — | — | 1 | 6.05 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.04 |
| CHEMBL1241674 | — | — | 1 | 6.04 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 6.03 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 6.00 |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | 5.96 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.92 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.77 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.68 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.60 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL379218 | — | Kd | = | 1.4 | nM | 8.85 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 8.8 | nM | 8.06 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 9.6 | nM | 8.02 |
| CHEMBL509032 | TAE-684 | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL464552 | — | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL535 | SUNITINIB | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL388978 | STAUROSPORINE | Kd | = | 32.0 | nM | 7.50 |
| CHEMBL1908397 | KW-2449 | Kd | = | 64.0 | nM | 7.19 |
| CHEMBL384304 | RG-547 | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL574738 | AST-487 | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL230011 | TG100-115 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 350.0 | nM | 6.46 |
| CHEMBL1721885 | SU-014813 | Kd | = | 360.0 | nM | 6.44 |
| CHEMBL296468 | BMS-387032 | Kd | = | 410.0 | nM | 6.39 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 510.0 | nM | 6.29 |
| CHEMBL1230609 | FORETINIB | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 600.0 | nM | 6.22 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 630.0 | nM | 6.20 |
| CHEMBL608154 | — | Kd | = | 640.0 | nM | 6.19 |
| CHEMBL450786 | PHA-665752 | Kd | = | 730.0 | nM | 6.14 |
| CHEMBL1908395 | — | Kd | = | 900.0 | nM | 6.05 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 910.0 | nM | 6.04 |
| CHEMBL1241674 | — | Kd | = | 910.0 | nM | 6.04 |
| CHEMBL513909 | BI-2536 | Kd | = | 940.0 | nM | 6.03 |
| CHEMBL445813 | AT-7519 | Kd | = | 990.0 | nM | 6.00 |
| CHEMBL521851 | PICTILISIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL475251 | R-406 | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL255863 | NILOTINIB | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2500.0 | nM | 5.60 |
| CHEMBL573339 | PI-103 | Kd | = | 3900.0 | nM | 5.41 |
| CHEMBL941 | IMATINIB | Kd | = | 4500.0 | nM | 5.35 |
| CHEMBL1230020 | PLX-4720 | Kd | = | 6600.0 | nM | 5.18 |
| CHEMBL522892 | DOVITINIB | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL1336 | SORAFENIB | Kd | = | 7500.0 | nM | 5.12 |
| CHEMBL223360 | LINIFANIB | Kd | = | 8900.0 | nM | 5.05 |
| CHEMBL572881 | MOTESANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL386051 | — | Kd | > | 10000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL105442 | CI-1040 | Kd | > | 10000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 10000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 10000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 10000.0 | nM | - |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 10000.0 | nM | - |
| CHEMBL119385 | NEFLAMAPIMOD | Kd | > | 10000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 10000.0 | nM | - |
| CHEMBL259084 | MLN-8054 | Kd | > | 10000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 10000.0 | nM | - |