Assay Detail
Binding
CHEMBL3991749
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 | 5.67 | 7.09 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 7.09 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 7.02 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 6.69 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.32 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 6.01 |
| CHEMBL1950289 | TANZISERTIB | 2.0 | 1 | 5.74 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.59 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.46 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 5.42 |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | 5.36 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.35 |
| CHEMBL3545360 | ASP-3026 | 1.0 | 1 | 5.28 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 4.81 |
| CHEMBL587723 | AEE-788 | 2.0 | 1 | 4.66 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 4.28 |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
| CHEMBL3039517 | RABUSERTIB | 2.0 | 1 | - |
| CHEMBL1231124 | AZD-1480 | 2.0 | 1 | - |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | - |
| CHEMBL3688339 | — | — | 1 | - |
| CHEMBL939 | GEFITINIB | 4.0 | 1 | - |
| CHEMBL2107832 | PIMASERTIB | 2.0 | 1 | - |
| CHEMBL2376648 | — | — | 1 | - |
| CHEMBL270995 | BRIVANIB ALANINATE | 3.0 | 1 | - |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | - |
| CHEMBL3991935 | — | — | 1 | - |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | - |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | - |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2028663 | DABRAFENIB | Kd | = | 82.0 | nM | 7.09 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 96.0 | nM | 7.02 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 205.0 | nM | 6.69 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 477.0 | nM | 6.32 |
| CHEMBL5416410 | DASATINIB | Kd | = | 965.0 | nM | 6.01 |
| CHEMBL1950289 | TANZISERTIB | Kd | = | 1840.0 | nM | 5.74 |
| CHEMBL482967 | CYC-116 | Kd | = | 2547.0 | nM | 5.59 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 3505.0 | nM | 5.46 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 3758.0 | nM | 5.42 |
| CHEMBL601719 | CRIZOTINIB | Kd | = | 4340.0 | nM | 5.36 |
| CHEMBL495727 | AT-9283 | Kd | = | 4432.0 | nM | 5.35 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 5306.0 | nM | 5.28 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 15626.0 | nM | 4.81 |
| CHEMBL587723 | AEE-788 | Kd | = | 21770.0 | nM | 4.66 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 52056.0 | nM | 4.28 |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1873475 | IBRUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL223360 | LINIFANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218575 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL2017974 | BUPARLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |