Assay Detail
Binding
CHEMBL1908727
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Binding constant for LOK 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 |
Publication
Comprehensive analysis of kinase inhibitor selectivity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 72 | 6.77 | 10.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | — | 1 | 10.43 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 9.28 |
| CHEMBL574738 | AST-487 | 1.0 | 1 | 9.04 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 8.24 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 8.15 |
| CHEMBL103667 | DORAMAPIMOD | 2.0 | 1 | 7.92 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 7.89 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 7.89 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 7.72 |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | 7.72 |
| CHEMBL1908396 | — | — | 1 | 7.66 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.64 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 7.36 |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | 7.22 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 7.16 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 7.16 |
| CHEMBL1241674 | — | — | 1 | 7.11 |
| CHEMBL509032 | TAE-684 | — | 1 | 7.09 |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | 7.09 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 7.08 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.06 |
| CHEMBL572878 | TOZASERTIB | 2.0 | 1 | 6.92 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.82 |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | 6.66 |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | 6.64 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 6.55 |
| CHEMBL450786 | PHA-665752 | — | 1 | 6.54 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 6.42 |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | 6.34 |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388978 | STAUROSPORINE | Kd | = | 0.037 | nM | 10.43 |
| CHEMBL1230609 | FORETINIB | Kd | = | 0.53 | nM | 9.28 |
| CHEMBL574738 | AST-487 | Kd | = | 0.92 | nM | 9.04 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 5.7 | nM | 8.24 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL103667 | DORAMAPIMOD | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL180022 | NERATINIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL1908397 | KW-2449 | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL535 | SUNITINIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL553 | ERLOTINIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL1908396 | — | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL558752 | RAF-265 | Kd | = | 60.0 | nM | 7.22 |
| CHEMBL475251 | R-406 | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 69.0 | nM | 7.16 |
| CHEMBL1241674 | — | Kd | = | 77.0 | nM | 7.11 |
| CHEMBL509032 | TAE-684 | Kd | = | 82.0 | nM | 7.09 |
| CHEMBL24828 | VANDETANIB | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 84.0 | nM | 7.08 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 87.0 | nM | 7.06 |
| CHEMBL572878 | TOZASERTIB | Kd | = | 120.0 | nM | 6.92 |
| CHEMBL1336 | SORAFENIB | Kd | = | 150.0 | nM | 6.82 |
| CHEMBL377300 | BRIVANIB | Kd | = | 220.0 | nM | 6.66 |
| CHEMBL1721885 | SU-014813 | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 280.0 | nM | 6.55 |
| CHEMBL450786 | PHA-665752 | Kd | = | 290.0 | nM | 6.54 |
| CHEMBL384304 | RG-547 | Kd | = | 380.0 | nM | 6.42 |
| CHEMBL223360 | LINIFANIB | Kd | = | 460.0 | nM | 6.34 |
| CHEMBL939 | GEFITINIB | Kd | = | 470.0 | nM | 6.33 |
| CHEMBL522892 | DOVITINIB | Kd | = | 550.0 | nM | 6.26 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 590.0 | nM | 6.23 |
| CHEMBL572881 | MOTESANIB | Kd | = | 1100.0 | nM | 5.96 |
| CHEMBL1289926 | AXITINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL5416410 | DASATINIB | Kd | = | 1200.0 | nM | 5.92 |
| CHEMBL525191 | — | Kd | = | 1300.0 | nM | 5.89 |
| CHEMBL1908395 | — | Kd | = | 1700.0 | nM | 5.77 |
| CHEMBL386051 | — | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL31965 | CANERTINIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL576982 | QUIZARTINIB | Kd | = | 2100.0 | nM | 5.68 |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | = | 2800.0 | nM | 5.55 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2900.0 | nM | 5.54 |
| CHEMBL259084 | MLN-8054 | Kd | = | 3700.0 | nM | 5.43 |
| CHEMBL1173655 | AFATINIB | Kd | = | 4300.0 | nM | 5.37 |
| CHEMBL554 | LAPATINIB | Kd | = | 4400.0 | nM | 5.36 |
| CHEMBL513909 | BI-2536 | Kd | = | 4900.0 | nM | 5.31 |
| CHEMBL255863 | NILOTINIB | Kd | = | 6800.0 | nM | 5.17 |
| CHEMBL124660 | TANDUTINIB | Kd | = | 9500.0 | nM | 5.02 |
| CHEMBL261849 | GW632580X | Kd | > | 10000.0 | nM | - |
| CHEMBL445813 | AT-7519 | Kd | > | 10000.0 | nM | - |