Assay Detail
Binding
CHEMBL3991869
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
Receptor-interacting serine/threonine-protein kinase 3 (CHEMBL1795199) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.15 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.52 |
| CHEMBL2364611 | GALUNISERTIB | 2.0 | 1 | 7.96 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.64 |
| CHEMBL1873475 | IBRUTINIB | 4.0 | 1 | 7.07 |
| CHEMBL2103842 | VARLITINIB | 2.0 | 1 | 7.06 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.79 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 6.77 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.61 |
| CHEMBL2028663 | DABRAFENIB | 4.0 | 1 | 6.55 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 6.50 |
| CHEMBL3688339 | — | — | 1 | 6.49 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 6.44 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.43 |
| CHEMBL3545154 | POZIOTINIB | 3.0 | 1 | 6.41 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 6.30 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 6.18 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.01 |
| CHEMBL572881 | MOTESANIB | 3.0 | 1 | 5.98 |
| CHEMBL3989868 | TUCATINIB | 4.0 | 1 | 5.97 |
| CHEMBL2408045 | SAPITINIB | 2.0 | 1 | 5.93 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 5.89 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 5.89 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.88 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 5.87 |
| CHEMBL1614710 | OSI-930 | 1.0 | 1 | 5.77 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 5.75 |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | 5.75 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 5.73 |
| CHEMBL1229517 | VEMURAFENIB | 4.0 | 1 | 5.68 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.66 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL2364611 | GALUNISERTIB | Kd | = | 11.0 | nM | 7.96 |
| CHEMBL1171837 | PONATINIB | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL1873475 | IBRUTINIB | Kd | = | 85.0 | nM | 7.07 |
| CHEMBL2103842 | VARLITINIB | Kd | = | 88.0 | nM | 7.06 |
| CHEMBL1230609 | FORETINIB | Kd | = | 161.0 | nM | 6.79 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 170.0 | nM | 6.77 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 245.0 | nM | 6.61 |
| CHEMBL2028663 | DABRAFENIB | Kd | = | 283.0 | nM | 6.55 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 316.0 | nM | 6.50 |
| CHEMBL3688339 | — | Kd | = | 324.0 | nM | 6.49 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 366.0 | nM | 6.44 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 368.0 | nM | 6.43 |
| CHEMBL3545154 | POZIOTINIB | Kd | = | 392.0 | nM | 6.41 |
| CHEMBL206834 | BAFETINIB | Kd | = | 506.0 | nM | 6.30 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 662.0 | nM | 6.18 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 967.0 | nM | 6.01 |
| CHEMBL572881 | MOTESANIB | Kd | = | 1044.0 | nM | 5.98 |
| CHEMBL3989868 | TUCATINIB | Kd | = | 1065.0 | nM | 5.97 |
| CHEMBL2408045 | SAPITINIB | Kd | = | 1171.0 | nM | 5.93 |
| CHEMBL255863 | NILOTINIB | Kd | = | 1274.0 | nM | 5.89 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 1282.0 | nM | 5.89 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 1304.0 | nM | 5.88 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 1346.0 | nM | 5.87 |
| CHEMBL1614710 | OSI-930 | Kd | = | 1696.0 | nM | 5.77 |
| CHEMBL217092 | SARACATINIB | Kd | = | 1768.0 | nM | 5.75 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 1800.0 | nM | 5.75 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 1856.0 | nM | 5.73 |
| CHEMBL1229517 | VEMURAFENIB | Kd | = | 2079.0 | nM | 5.68 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 2177.0 | nM | 5.66 |
| CHEMBL31965 | CANERTINIB | Kd | = | 2254.0 | nM | 5.65 |
| CHEMBL3186534 | RIVOCERANIB | Kd | = | 2373.0 | nM | 5.62 |
| CHEMBL3991933 | — | Kd | = | 2375.0 | nM | 5.62 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 2459.0 | nM | 5.61 |
| CHEMBL939 | GEFITINIB | Kd | = | 2664.0 | nM | 5.57 |
| CHEMBL230011 | TG100-115 | Kd | = | 3668.0 | nM | 5.44 |
| CHEMBL2110732 | DACOMITINIB ANHYDROUS | Kd | = | 3637.0 | nM | 5.44 |
| CHEMBL482967 | CYC-116 | Kd | = | 4820.0 | nM | 5.32 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 6054.0 | nM | 5.22 |
| CHEMBL551064 | AEW-541 | Kd | = | 6453.0 | nM | 5.19 |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL565612 | SOTRASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL24828 | VANDETANIB | Kd | > | 30000.0 | nM | - |