Assay Detail
Binding
CHEMBL3991844
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 |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.22 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 8.30 |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 7.68 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 7.47 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.42 |
| CHEMBL3544960 | AT-13148 | 1.0 | 1 | 7.36 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 7.17 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 7.17 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 7.14 |
| CHEMBL3688339 | — | — | 1 | 7.10 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.10 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.03 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.01 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.00 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 5.97 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.96 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.80 |
| CHEMBL2386889 | SCH-900776 | 2.0 | 1 | 5.79 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 5.76 |
| CHEMBL3991935 | — | — | 1 | 5.62 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 5.61 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 5.60 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 5.55 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.52 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.42 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.32 |
| CHEMBL3991934 | — | — | 1 | 5.29 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 5.04 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 4.88 |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL565612 | SOTRASTAURIN | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 21.0 | nM | 7.68 |
| CHEMBL571948 | Y-39983 | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL574737 | UCN-01 | Kd | = | 38.0 | nM | 7.42 |
| CHEMBL3544960 | AT-13148 | Kd | = | 44.0 | nM | 7.36 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL494089 | GSK-690693 | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL3688339 | — | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 795.0 | nM | 6.10 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 928.0 | nM | 6.03 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 974.0 | nM | 6.01 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 996.0 | nM | 6.00 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 1075.0 | nM | 5.97 |
| CHEMBL2140408 | AMG-900 | Kd | = | 1092.0 | nM | 5.96 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 1592.0 | nM | 5.80 |
| CHEMBL2386889 | SCH-900776 | Kd | = | 1641.0 | nM | 5.79 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 1741.0 | nM | 5.76 |
| CHEMBL3991935 | — | Kd | = | 2394.0 | nM | 5.62 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 2470.0 | nM | 5.61 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 2519.0 | nM | 5.60 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 2809.0 | nM | 5.55 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 2989.0 | nM | 5.52 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 3821.0 | nM | 5.42 |
| CHEMBL38380 | FASUDIL | Kd | = | 4789.0 | nM | 5.32 |
| CHEMBL3991934 | — | Kd | = | 5076.0 | nM | 5.29 |
| CHEMBL221959 | TOFACITINIB | Kd | = | 9206.0 | nM | 5.04 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 13314.0 | nM | 4.88 |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL281948 | K-252A | Kd | > | 30000.0 | nM | - |
| CHEMBL1738757 | REBASTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL1173655 | AFATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1171837 | PONATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |