Assay Detail
Binding
CHEMBL3991746
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
Serine/threonine-protein kinase LATS1 (CHEMBL6167) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.22 | 7.85 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3688339 | — | — | 1 | 7.85 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 7.60 |
| CHEMBL3544960 | AT-13148 | 1.0 | 1 | 7.57 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.35 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.18 |
| CHEMBL281948 | K-252A | — | 1 | 7.17 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 7.13 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.80 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 6.71 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.66 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.58 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.44 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.39 |
| CHEMBL3699142 | — | — | 1 | 6.20 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.17 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.13 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.02 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 5.72 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.67 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.56 |
| CHEMBL274654 | ORANTINIB | 3.0 | 1 | 5.52 |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | 5.45 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.42 |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | 5.41 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.38 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 5.34 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.04 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 4.97 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 4.85 |
| CHEMBL2403108 | CERITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3688339 | — | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL3544960 | AT-13148 | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL495727 | AT-9283 | Kd | = | 45.0 | nM | 7.35 |
| CHEMBL482967 | CYC-116 | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL281948 | K-252A | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL494089 | GSK-690693 | Kd | = | 74.0 | nM | 7.13 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 157.0 | nM | 6.80 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 195.0 | nM | 6.71 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 221.0 | nM | 6.66 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 261.0 | nM | 6.58 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 363.0 | nM | 6.44 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 406.0 | nM | 6.39 |
| CHEMBL3699142 | — | Kd | = | 635.0 | nM | 6.20 |
| CHEMBL564829 | MILCICLIB | Kd | = | 681.0 | nM | 6.17 |
| CHEMBL535 | SUNITINIB | Kd | = | 743.0 | nM | 6.13 |
| CHEMBL522892 | DOVITINIB | Kd | = | 955.0 | nM | 6.02 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1884.0 | nM | 5.72 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 2157.0 | nM | 5.67 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 2768.0 | nM | 5.56 |
| CHEMBL274654 | ORANTINIB | Kd | = | 3011.0 | nM | 5.52 |
| CHEMBL3137336 | UPROSERTIB | Kd | = | 3592.0 | nM | 5.45 |
| CHEMBL3545328 | XL-019 | Kd | = | 3790.0 | nM | 5.42 |
| CHEMBL551064 | AEW-541 | Kd | = | 3879.0 | nM | 5.41 |
| CHEMBL38380 | FASUDIL | Kd | = | 4170.0 | nM | 5.38 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 4616.0 | nM | 5.34 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 9050.0 | nM | 5.04 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 10733.0 | nM | 4.97 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 14103.0 | nM | 4.85 |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1645462 | AC-480 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545085 | XL-228 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |