Assay Detail
Binding
CHEMBL3991926
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 |
Target
Mitogen-activated protein kinase kinase kinase 20 (CHEMBL3886) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.10 | 7.39 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.39 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.28 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.19 |
| CHEMBL3688339 | — | — | 1 | 7.00 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 6.93 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.74 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.66 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.56 |
| CHEMBL3545396 | BMS-690514 | 2.0 | 1 | 6.55 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 6.50 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.41 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.35 |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | 6.32 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.16 |
| CHEMBL1336 | SORAFENIB | 4.0 | 1 | 6.14 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.11 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 6.06 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.00 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.98 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.95 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 5.92 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.90 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 5.77 |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | 5.55 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.53 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.53 |
| CHEMBL1289926 | AXITINIB | 4.0 | 1 | 5.34 |
| CHEMBL3186534 | RIVOCERANIB | 3.0 | 1 | 5.32 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.17 |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | 5.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1171837 | PONATINIB | Kd | = | 41.0 | nM | 7.39 |
| CHEMBL1230609 | FORETINIB | Kd | = | 53.0 | nM | 7.28 |
| CHEMBL206834 | BAFETINIB | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL3688339 | — | Kd | = | 101.0 | nM | 7.00 |
| CHEMBL572881 | MOTESANIB | Kd | = | 117.0 | nM | 6.93 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 184.0 | nM | 6.74 |
| CHEMBL5416410 | DASATINIB | Kd | = | 217.0 | nM | 6.66 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 274.0 | nM | 6.56 |
| CHEMBL3545396 | BMS-690514 | Kd | = | 282.0 | nM | 6.55 |
| CHEMBL1229517 | VEMURAFENIB | Kd | = | 316.0 | nM | 6.50 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 388.0 | nM | 6.41 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 450.0 | nM | 6.35 |
| CHEMBL2079588 | TELATINIB | Kd | = | 477.0 | nM | 6.32 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 695.0 | nM | 6.16 |
| CHEMBL1336 | SORAFENIB | Kd | = | 729.0 | nM | 6.14 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 785.0 | nM | 6.11 |
| CHEMBL607707 | PELITINIB | Kd | = | 875.0 | nM | 6.06 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 998.0 | nM | 6.00 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1052.0 | nM | 5.98 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 1113.0 | nM | 5.95 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 1213.0 | nM | 5.92 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 1254.0 | nM | 5.90 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 1705.0 | nM | 5.77 |
| CHEMBL31965 | CANERTINIB | Kd | = | 2819.0 | nM | 5.55 |
| CHEMBL217092 | SARACATINIB | Kd | = | 2985.0 | nM | 5.53 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 2978.0 | nM | 5.53 |
| CHEMBL1289926 | AXITINIB | Kd | = | 4615.0 | nM | 5.34 |
| CHEMBL3186534 | RIVOCERANIB | Kd | = | 4760.0 | nM | 5.32 |
| CHEMBL482967 | CYC-116 | Kd | = | 6839.0 | nM | 5.17 |
| CHEMBL1614710 | OSI-930 | Kd | = | 7731.0 | nM | 5.11 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 9540.0 | nM | 5.02 |
| CHEMBL587723 | AEE-788 | Kd | = | 13638.0 | nM | 4.87 |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL3128043 | PF-03758309 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544983 | TESEVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105759 | BARICITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482968 | ENMD-2076 | Kd | > | 30000.0 | nM | - |
| CHEMBL572878 | TOZASERTIB | Kd | > | 30000.0 | nM | - |