Assay Detail
Binding
CHEMBL3991777
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 |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.06 | 8.70 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 8.70 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.83 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.51 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 6.47 |
| CHEMBL3688339 | — | — | 1 | 6.44 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 6.43 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.37 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.29 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.24 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.04 |
| CHEMBL281948 | K-252A | — | 1 | 6.01 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.01 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 5.94 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 5.84 |
| CHEMBL3991934 | — | — | 1 | 5.82 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.81 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.80 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 5.76 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.74 |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | 5.72 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 5.71 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.70 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 5.67 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 5.64 |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | 5.59 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.54 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 5.10 |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL411907 | SONOLISIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1950289 | TANZISERTIB | Kd | = | 2.0 | nM | 8.70 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 148.0 | nM | 6.83 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 312.0 | nM | 6.51 |
| CHEMBL1614713 | CC-401 | Kd | = | 340.0 | nM | 6.47 |
| CHEMBL3688339 | — | Kd | = | 364.0 | nM | 6.44 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 370.0 | nM | 6.43 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 430.0 | nM | 6.37 |
| CHEMBL495727 | AT-9283 | Kd | = | 509.0 | nM | 6.29 |
| CHEMBL482967 | CYC-116 | Kd | = | 575.0 | nM | 6.24 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 915.0 | nM | 6.04 |
| CHEMBL281948 | K-252A | Kd | = | 986.0 | nM | 6.01 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 980.0 | nM | 6.01 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 1137.0 | nM | 5.94 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 1430.0 | nM | 5.84 |
| CHEMBL3991934 | — | Kd | = | 1510.0 | nM | 5.82 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 1533.0 | nM | 5.81 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 1571.0 | nM | 5.80 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 1729.0 | nM | 5.76 |
| CHEMBL475251 | R-406 | Kd | = | 1827.0 | nM | 5.74 |
| CHEMBL488436 | AZD-5438 | Kd | = | 1898.0 | nM | 5.72 |
| CHEMBL1822792 | MK-2461 | Kd | = | 1931.0 | nM | 5.71 |
| CHEMBL1908397 | KW-2449 | Kd | = | 1985.0 | nM | 5.70 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 2149.0 | nM | 5.67 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 2307.0 | nM | 5.64 |
| CHEMBL1173655 | AFATINIB | Kd | = | 2543.0 | nM | 5.59 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 2856.0 | nM | 5.54 |
| CHEMBL1171837 | PONATINIB | Kd | = | 8025.0 | nM | 5.10 |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL3426621 | RIPASUDIL | Kd | > | 30000.0 | nM | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614707 | MUBRITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2048872 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL608533 | MIDOSTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3039525 | GOLVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544960 | AT-13148 | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2403108 | CERITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103851 | AMUVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3334567 | SAVOLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |