Assay Detail
Binding
CHEMBL3991766
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 kinase 3 (CHEMBL5432) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.00 | 7.48 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 7.48 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 7.31 |
| CHEMBL288441 | BOSUTINIB | 4.0 | 1 | 7.24 |
| CHEMBL607707 | PELITINIB | 2.0 | 1 | 6.72 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.44 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.39 |
| CHEMBL535 | SUNITINIB | 4.0 | 1 | 6.28 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.28 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.22 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.15 |
| CHEMBL4289017 | PF-03814735 | 1.0 | 1 | 6.12 |
| CHEMBL522892 | DOVITINIB | 3.0 | 1 | 6.08 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.07 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.92 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.82 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.81 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 5.80 |
| CHEMBL180022 | NERATINIB | 4.0 | 1 | 5.76 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 5.74 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 5.72 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.69 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 5.67 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 5.66 |
| CHEMBL281948 | K-252A | — | 1 | 5.62 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.59 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 5.55 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.54 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 5.49 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.03 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 4.81 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 49.0 | nM | 7.31 |
| CHEMBL288441 | BOSUTINIB | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL607707 | PELITINIB | Kd | = | 189.0 | nM | 6.72 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 363.0 | nM | 6.44 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 406.0 | nM | 6.39 |
| CHEMBL535 | SUNITINIB | Kd | = | 528.0 | nM | 6.28 |
| CHEMBL3545085 | XL-228 | Kd | = | 526.0 | nM | 6.28 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 605.0 | nM | 6.22 |
| CHEMBL574737 | UCN-01 | Kd | = | 706.0 | nM | 6.15 |
| CHEMBL4289017 | PF-03814735 | Kd | = | 766.0 | nM | 6.12 |
| CHEMBL522892 | DOVITINIB | Kd | = | 841.0 | nM | 6.08 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 1193.0 | nM | 5.92 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1524.0 | nM | 5.82 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1543.0 | nM | 5.81 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1565.0 | nM | 5.80 |
| CHEMBL180022 | NERATINIB | Kd | = | 1753.0 | nM | 5.76 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 1819.0 | nM | 5.74 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 1900.0 | nM | 5.72 |
| CHEMBL564829 | MILCICLIB | Kd | = | 2057.0 | nM | 5.69 |
| CHEMBL5416410 | DASATINIB | Kd | = | 2119.0 | nM | 5.67 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 2190.0 | nM | 5.66 |
| CHEMBL281948 | K-252A | Kd | = | 2374.0 | nM | 5.62 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 2587.0 | nM | 5.59 |
| CHEMBL253969 | OSI-632 | Kd | = | 2785.0 | nM | 5.55 |
| CHEMBL482967 | CYC-116 | Kd | = | 2855.0 | nM | 5.54 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 3219.0 | nM | 5.49 |
| CHEMBL3544932 | TAK-901 | Kd | = | 9285.0 | nM | 5.03 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 15435.0 | nM | 4.81 |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL460702 | BMS-777607 | Kd | > | 30000.0 | nM | - |
| CHEMBL553 | ERLOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289926 | AXITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL230011 | TG100-115 | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL477772 | PAZOPANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1171837 | PONATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |