Assay Detail
Binding
CHEMBL3991778
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.
238
Total Activities
238
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
MAP kinase-activated protein kinase 2 (CHEMBL2208) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 238 | 6.42 | 9.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1090090 | VX-702 | 2.0 | 1 | 9.52 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | 7.75 |
| CHEMBL514201 | TALMAPIMOD | 2.0 | 1 | 7.72 |
| CHEMBL1088752 | LOSMAPIMOD | 3.0 | 1 | 7.57 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 7.20 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 7.17 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 6.52 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.45 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 6.33 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.31 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.27 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.17 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 6.09 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 6.03 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 5.91 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 5.82 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 5.57 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.33 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.28 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.00 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 4.83 |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | - |
| CHEMBL411907 | SONOLISIB | 2.0 | 1 | - |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | - |
| CHEMBL2030402 | — | — | 1 | - |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | - |
| CHEMBL3991935 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1090090 | VX-702 | Kd | = | 0.3 | nM | 9.52 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL514201 | TALMAPIMOD | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL1088752 | LOSMAPIMOD | Kd | = | 27.0 | nM | 7.57 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL206834 | BAFETINIB | Kd | = | 304.0 | nM | 6.52 |
| CHEMBL3545328 | XL-019 | Kd | = | 354.0 | nM | 6.45 |
| CHEMBL1171837 | PONATINIB | Kd | = | 468.0 | nM | 6.33 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 490.0 | nM | 6.31 |
| CHEMBL5416410 | DASATINIB | Kd | = | 538.0 | nM | 6.27 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 682.0 | nM | 6.17 |
| CHEMBL1173655 | AFATINIB | Kd | = | 817.0 | nM | 6.09 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 934.0 | nM | 6.03 |
| CHEMBL253969 | OSI-632 | Kd | = | 1224.0 | nM | 5.91 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 1519.0 | nM | 5.82 |
| CHEMBL2140408 | AMG-900 | Kd | = | 2686.0 | nM | 5.57 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 4691.0 | nM | 5.33 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 5298.0 | nM | 5.28 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 10078.0 | nM | 5.00 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 14742.0 | nM | 4.83 |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301622 | GILTERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1079175 | MK-2206 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289494 | TIVOZANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL38380 | FASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL587723 | AEE-788 | Kd | > | 30000.0 | nM | - |
| CHEMBL603469 | LESTAURTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL215152 | DEFOSBARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |