Assay Detail
Binding
CHEMBL3991735
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Kinobeads (epsilon), multiple immobilized ATP-competitive broad spectrum kinase inhibitors, used to assess residual binding of ~300 proteins simultaneously from cell lysate in the presence of a compound. Quantitative readout performed by mass spectrometry.
243
Total Activities
243
Compounds Tested
1
Activity Types
1
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | K-562, COLO 205, SK-N-BE(2) and MV-4-11 |
| Subcellular | Cell lysate |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Insulin-like growth factor 1 receptor (CHEMBL1957) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 5.91 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 8.30 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 6.86 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.12 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.66 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.57 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | 5.01 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.01 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | 4.72 |
| CHEMBL2376648 | — | — | 1 | - |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | - |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | - |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | - |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | - |
| CHEMBL2103875 | TRAMETINIB | 4.0 | 1 | - |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | - |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | - |
| CHEMBL576982 | QUIZARTINIB | 4.0 | 1 | - |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | - |
| CHEMBL3188267 | CAPMATINIB | 4.0 | 1 | - |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | - |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL2323775 | MK-8033 | 1.0 | 1 | - |
| CHEMBL1614707 | MUBRITINIB | 2.0 | 1 | - |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | - |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | - |
| CHEMBL571546 | TIRBANIBULIN | 4.0 | 1 | - |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | - |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | - |
| CHEMBL1090090 | VX-702 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL575448 | BMS-754807 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 138.0 | nM | 6.86 |
| CHEMBL3545085 | XL-228 | Kd | = | 754.0 | nM | 6.12 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2196.0 | nM | 5.66 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 2714.0 | nM | 5.57 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 9722.0 | nM | 5.01 |
| CHEMBL551064 | AEW-541 | Kd | = | 9769.0 | nM | 5.01 |
| CHEMBL2403108 | CERITINIB | Kd | = | 19217.0 | nM | 4.72 |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL2386889 | SCH-900776 | Kd | > | 30000.0 | nM | - |
| CHEMBL502835 | NINTEDANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1201182 | TEMSIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL3218575 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL571948 | Y-39983 | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |