Assay Detail
Binding
CHEMBL3991831
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 | 6.53 | 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 |
| CHEMBL3544960 | AT-13148 | 1.0 | 1 | 8.05 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 7.55 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.85 |
| CHEMBL574737 | UCN-01 | 2.0 | 1 | 6.85 |
| CHEMBL603469 | LESTAURTINIB | 3.0 | 1 | 6.79 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 6.57 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 6.54 |
| CHEMBL281948 | K-252A | — | 1 | 6.44 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.05 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 5.92 |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | 5.65 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.58 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.56 |
| CHEMBL2041933 | AZD-7762 | 1.0 | 1 | 5.51 |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | 2.0 | 1 | - |
| CHEMBL553 | ERLOTINIB | 4.0 | 1 | - |
| CHEMBL24828 | VANDETANIB | 4.0 | 1 | - |
| CHEMBL223360 | LINIFANIB | 3.0 | 1 | - |
| CHEMBL3545157 | TIDEGLUSIB | 2.0 | 1 | - |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | - |
| CHEMBL1721885 | SU-014813 | 2.0 | 1 | - |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | - |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | - |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | - |
| CHEMBL2103839 | RIDAFOROLIMUS | 3.0 | 1 | - |
| CHEMBL3688339 | — | — | 1 | - |
| CHEMBL3264002 | AVUTOMETINIB | 3.0 | 1 | - |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | - |
| CHEMBL2376648 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1667969 | SAR-407899 FREE BASE | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL3544960 | AT-13148 | Kd | = | 9.0 | nM | 8.05 |
| CHEMBL571948 | Y-39983 | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 141.0 | nM | 6.85 |
| CHEMBL574737 | UCN-01 | Kd | = | 142.0 | nM | 6.85 |
| CHEMBL603469 | LESTAURTINIB | Kd | = | 164.0 | nM | 6.79 |
| CHEMBL2105759 | BARICITINIB | Kd | = | 269.0 | nM | 6.57 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 285.0 | nM | 6.54 |
| CHEMBL281948 | K-252A | Kd | = | 361.0 | nM | 6.44 |
| CHEMBL494089 | GSK-690693 | Kd | = | 892.0 | nM | 6.05 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 1215.0 | nM | 5.92 |
| CHEMBL1233300 | HYDROXYFASUDIL | Kd | = | 2260.0 | nM | 5.65 |
| CHEMBL38380 | FASUDIL | Kd | = | 2599.0 | nM | 5.58 |
| CHEMBL495727 | AT-9283 | Kd | = | 2767.0 | nM | 5.56 |
| CHEMBL2041933 | AZD-7762 | Kd | = | 3095.0 | nM | 5.51 |
| CHEMBL3545308 | ROCILETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL3186534 | RIVOCERANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1879463 | DACTOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3544966 | GSK-1059615 | Kd | > | 30000.0 | nM | - |
| CHEMBL384304 | RG-547 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545154 | POZIOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL572881 | MOTESANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3408248 | AZD-8186 | Kd | > | 30000.0 | nM | - |
| CHEMBL3137336 | UPROSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3301607 | FILGOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991935 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3109738 | JNJ-26483327 | Kd | > | 30000.0 | nM | - |
| CHEMBL535 | SUNITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3218576 | COPANLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL288441 | BOSUTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL536151 | IMD-0354 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL575448 | BMS-754807 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL217092 | SARACATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1952329 | SGI-1776 | Kd | > | 30000.0 | nM | - |
| CHEMBL2220486 | LUCITANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |