Assay Detail
Binding
CHEMBL3991902
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.
242
Total Activities
242
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 TAO1 (CHEMBL5261) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 242 | 5.98 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 8.70 |
| CHEMBL3688339 | — | — | 1 | 7.77 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.97 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 6.64 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 6.47 |
| CHEMBL3590106 | ULIXERTINIB | 2.0 | 1 | 6.41 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 6.03 |
| CHEMBL3991933 | — | — | 1 | 5.96 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.91 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.72 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 5.69 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.68 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 5.67 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.66 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.66 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.65 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.49 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.49 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 5.47 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 5.01 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 4.75 |
| CHEMBL281948 | K-252A | — | 1 | 4.73 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | - |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | - |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | - |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | - |
| CHEMBL124660 | TANDUTINIB | 2.0 | 1 | - |
| CHEMBL2336325 | VISTUSERTIB | 2.0 | 1 | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | 4.0 | 1 | - |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3544966 | GSK-1059615 | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3688339 | — | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 107.0 | nM | 6.97 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 230.0 | nM | 6.64 |
| CHEMBL564829 | MILCICLIB | Kd | = | 342.0 | nM | 6.47 |
| CHEMBL3590106 | ULIXERTINIB | Kd | = | 388.0 | nM | 6.41 |
| CHEMBL445813 | AT-7519 | Kd | = | 933.0 | nM | 6.03 |
| CHEMBL3991933 | — | Kd | = | 1094.0 | nM | 5.96 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 1239.0 | nM | 5.91 |
| CHEMBL2140408 | AMG-900 | Kd | = | 1896.0 | nM | 5.72 |
| CHEMBL571948 | Y-39983 | Kd | = | 2030.0 | nM | 5.69 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 2080.0 | nM | 5.68 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 2138.0 | nM | 5.67 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 2195.0 | nM | 5.66 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 2174.0 | nM | 5.66 |
| CHEMBL495727 | AT-9283 | Kd | = | 2219.0 | nM | 5.65 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 3255.0 | nM | 5.49 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 3227.0 | nM | 5.49 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 3407.0 | nM | 5.47 |
| CHEMBL1789941 | RUXOLITINIB | Kd | = | 9790.0 | nM | 5.01 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 17866.0 | nM | 4.75 |
| CHEMBL281948 | K-252A | Kd | = | 18757.0 | nM | 4.73 |
| CHEMBL259084 | MLN-8054 | Kd | > | 30000.0 | nM | - |
| CHEMBL31965 | CANERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL462018 | TRICIRIBINE PHOSPHATE | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1078178 | MOMELOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL2048872 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3188267 | CAPMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL514201 | TALMAPIMOD | Kd | > | 30000.0 | nM | - |
| CHEMBL483321 | CP-724714 | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL513909 | BI-2536 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545157 | TIDEGLUSIB | Kd | > | 30000.0 | nM | - |