Assay Detail
Binding
CHEMBL3991840
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.
241
Total Activities
241
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
5'-AMP-activated protein kinase subunit gamma-2 (CHEMBL2453) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 241 | 6.34 | 8.30 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 8.30 |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | 7.64 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 7.60 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 7.21 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 7.11 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 7.03 |
| CHEMBL3688339 | — | — | 1 | 6.68 |
| CHEMBL575448 | BMS-754807 | 2.0 | 1 | 6.57 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 6.46 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 6.29 |
| CHEMBL281948 | K-252A | — | 1 | 6.06 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.05 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.05 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 5.95 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 5.90 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.90 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 5.76 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.75 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.71 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 5.57 |
| CHEMBL3699142 | — | — | 1 | 5.56 |
| CHEMBL1236682 | REFAMETINIB | 2.0 | 1 | 5.55 |
| CHEMBL608533 | MIDOSTAURIN | 4.0 | 1 | 5.04 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | - |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | - |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | - |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | - |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | - |
| CHEMBL3218576 | COPANLISIB | 4.0 | 1 | - |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3128043 | PF-03758309 | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1952329 | SGI-1776 | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL574737 | UCN-01 | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL495727 | AT-9283 | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL494089 | GSK-690693 | Kd | = | 78.0 | nM | 7.11 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 93.0 | nM | 7.03 |
| CHEMBL3688339 | — | Kd | = | 208.0 | nM | 6.68 |
| CHEMBL575448 | BMS-754807 | Kd | = | 272.0 | nM | 6.57 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 344.0 | nM | 6.46 |
| CHEMBL3544932 | TAK-901 | Kd | = | 509.0 | nM | 6.29 |
| CHEMBL281948 | K-252A | Kd | = | 868.0 | nM | 6.06 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 895.0 | nM | 6.05 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 890.0 | nM | 6.05 |
| CHEMBL522892 | DOVITINIB | Kd | = | 1123.0 | nM | 5.95 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 1255.0 | nM | 5.90 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1266.0 | nM | 5.90 |
| CHEMBL535 | SUNITINIB | Kd | = | 1734.0 | nM | 5.76 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 1772.0 | nM | 5.75 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 1967.0 | nM | 5.71 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 2711.0 | nM | 5.57 |
| CHEMBL3699142 | — | Kd | = | 2749.0 | nM | 5.56 |
| CHEMBL1236682 | REFAMETINIB | Kd | = | 2817.0 | nM | 5.55 |
| CHEMBL608533 | MIDOSTAURIN | Kd | = | 9128.0 | nM | 5.04 |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL2403108 | CERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1091644 | LINSITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3989868 | TUCATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908391 | MASITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL601719 | CRIZOTINIB | Kd | > | 30000.0 | nM | - |