Assay Detail
Binding
CHEMBL3991908
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.
141
Total Activities
141
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
Dual specificity testis-specific protein kinase 2 (CHEMBL2069163) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 141 | 8.23 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 8.70 |
| CHEMBL3991933 | — | — | 1 | 7.75 |
| CHEMBL3545076 | LY-2584702 | 1.0 | 1 | - |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | - |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | - |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | - |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | - |
| CHEMBL101253 | VATALANIB | 3.0 | 1 | - |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | - |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | - |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | - |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | - |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | - |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | - |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL521851 | PICTILISIB | 2.0 | 1 | - |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | - |
| CHEMBL1952329 | SGI-1776 | 1.0 | 1 | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | - |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | - |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | - |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | - |
| CHEMBL2138625 | AV-412 FREE BASE | 1.0 | 1 | - |
| CHEMBL1614707 | MUBRITINIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1738757 | REBASTINIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL3991933 | — | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090479 | GSK-1070916 | Kd | > | 30000.0 | nM | - |
| CHEMBL575448 | BMS-754807 | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL603469 | LESTAURTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103839 | RIDAFOROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL592445 | GEDATOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991927 | HMN-214 | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1614701 | SELUMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL281948 | K-252A | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL1241855 | RIGOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3590106 | ULIXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL124660 | TANDUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL491473 | CEDIRANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL402548 | DANUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1721885 | SU-014813 | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |