Assay Detail
Binding
CHEMBL3991853
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.
235
Total Activities
235
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 | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 235 | 6.26 | 8.10 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | 8.10 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 7.64 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 6.61 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.51 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 6.39 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 6.24 |
| CHEMBL2325741 | CAPIVASERTIB | 4.0 | 1 | 6.06 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 6.00 |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | 5.74 |
| CHEMBL281948 | K-252A | — | 1 | 5.61 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 5.51 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.47 |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | 5.46 |
| CHEMBL507361 | MIRDAMETINIB | 2.0 | 1 | - |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | - |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | - |
| CHEMBL1614713 | CC-401 | 2.0 | 1 | - |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | - |
| CHEMBL496102 | AMG-208 | 2.0 | 1 | - |
| CHEMBL3991934 | — | — | 1 | - |
| CHEMBL2079588 | TELATINIB | 2.0 | 1 | - |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | - |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | - |
| CHEMBL551064 | AEW-541 | 1.0 | 1 | - |
| CHEMBL3184679 | AZD-4547 | — | 1 | - |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | - |
| CHEMBL3688339 | — | — | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL1614725 | TAK-285 | 1.0 | 1 | - |
| CHEMBL2107832 | PIMASERTIB | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL494089 | GSK-690693 | Kd | = | 23.0 | nM | 7.64 |
| CHEMBL38380 | FASUDIL | Kd | = | 247.0 | nM | 6.61 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 312.0 | nM | 6.51 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 411.0 | nM | 6.39 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 571.0 | nM | 6.24 |
| CHEMBL2325741 | CAPIVASERTIB | Kd | = | 879.0 | nM | 6.06 |
| CHEMBL495727 | AT-9283 | Kd | = | 998.0 | nM | 6.00 |
| CHEMBL3545137 | PF-00477736 | Kd | = | 1841.0 | nM | 5.74 |
| CHEMBL281948 | K-252A | Kd | = | 2436.0 | nM | 5.61 |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | = | 3070.0 | nM | 5.51 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 3419.0 | nM | 5.47 |
| CHEMBL3301622 | GILTERITINIB | Kd | = | 3429.0 | nM | 5.46 |
| CHEMBL14762 | SELICICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3137331 | DEFACTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545076 | LY-2584702 | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1201182 | TEMSIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2408045 | SAPITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3402762 | TEPOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1738797 | ALECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230607 | PHA-793887 | Kd | > | 30000.0 | nM | - |
| CHEMBL1231124 | AZD-1480 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL180022 | NERATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL403989 | TG100-801 | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL255863 | NILOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3039517 | RABUSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2030402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL3187723 | BINIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL521851 | PICTILISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL428690 | ALVOCIDIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545215 | BMS-911543 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991932 | PEXMETINIB | Kd | > | 30000.0 | nM | - |