Assay Detail
Binding
CHEMBL3991776
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 | 6.04 | 7.77 |
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 | 7.77 |
| CHEMBL3688339 | — | — | 1 | 6.82 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.80 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 6.53 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | — | 1 | 6.45 |
| CHEMBL281948 | K-252A | — | 1 | 6.26 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.22 |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | 6.20 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 6.14 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 6.13 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.11 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 6.07 |
| CHEMBL3600873 | MK-5108 | 1.0 | 1 | 5.94 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 5.84 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 5.83 |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | 5.78 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 5.73 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 5.71 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.70 |
| CHEMBL1908397 | KW-2449 | 1.0 | 1 | 5.69 |
| CHEMBL1287853 | FEDRATINIB | 4.0 | 1 | 5.65 |
| CHEMBL475251 | R-406 | 2.0 | 1 | 5.63 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 5.42 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 4.58 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | - |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | - |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL3188267 | CAPMATINIB | 4.0 | 1 | - |
| CHEMBL411907 | SONOLISIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1950289 | TANZISERTIB | Kd | = | 17.0 | nM | 7.77 |
| CHEMBL3688339 | — | Kd | = | 151.0 | nM | 6.82 |
| CHEMBL495727 | AT-9283 | Kd | = | 157.0 | nM | 6.80 |
| CHEMBL482967 | CYC-116 | Kd | = | 298.0 | nM | 6.53 |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | = | 356.0 | nM | 6.45 |
| CHEMBL281948 | K-252A | Kd | = | 551.0 | nM | 6.26 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 599.0 | nM | 6.22 |
| CHEMBL1614713 | CC-401 | Kd | = | 636.0 | nM | 6.20 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 731.0 | nM | 6.14 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 736.0 | nM | 6.13 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 783.0 | nM | 6.11 |
| CHEMBL3545328 | XL-019 | Kd | = | 844.0 | nM | 6.07 |
| CHEMBL3600873 | MK-5108 | Kd | = | 1148.0 | nM | 5.94 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 1457.0 | nM | 5.84 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 1471.0 | nM | 5.83 |
| CHEMBL488436 | AZD-5438 | Kd | = | 1676.0 | nM | 5.78 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 1865.0 | nM | 5.73 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 1957.0 | nM | 5.71 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 2011.0 | nM | 5.70 |
| CHEMBL1908397 | KW-2449 | Kd | = | 2027.0 | nM | 5.69 |
| CHEMBL1287853 | FEDRATINIB | Kd | = | 2223.0 | nM | 5.65 |
| CHEMBL475251 | R-406 | Kd | = | 2332.0 | nM | 5.63 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 3756.0 | nM | 5.42 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 26059.0 | nM | 4.58 |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545396 | BMS-690514 | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL575448 | BMS-754807 | Kd | > | 30000.0 | nM | - |
| CHEMBL1234354 | PF-04691502 | Kd | > | 30000.0 | nM | - |
| CHEMBL2323775 | MK-8033 | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL558752 | RAF-265 | Kd | > | 30000.0 | nM | - |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236682 | REFAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2396661 | ALPELISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1289601 | LENVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL415049 | BARASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | > | 30000.0 | nM | - |
| CHEMBL1233528 | VOLASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3184679 | AZD-4547 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2364611 | GALUNISERTIB | Kd | > | 30000.0 | nM | - |