Assay Detail
Binding
CHEMBL3991727
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 | 6.44 | 8.15 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 8.15 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 8.10 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 7.92 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 7.89 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 7.24 |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | 7.21 |
| CHEMBL3688339 | — | — | 1 | 7.10 |
| CHEMBL300138 | ENZASTAURIN | 3.0 | 1 | 6.72 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 6.52 |
| CHEMBL494089 | GSK-690693 | 1.0 | 1 | 6.37 |
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.37 |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 6.35 |
| CHEMBL3544964 | RAVOXERTINIB | 2.0 | 1 | 6.22 |
| CHEMBL3128043 | PF-03758309 | 1.0 | 1 | 6.18 |
| CHEMBL565612 | SOTRASTAURIN | 2.0 | 1 | 6.15 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 6.15 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 6.13 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 6.03 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.88 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 5.84 |
| CHEMBL3991935 | — | — | 1 | 5.57 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.31 |
| CHEMBL91829 | RUBOXISTAURIN | 3.0 | 1 | 5.30 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.21 |
| CHEMBL2030402 | — | — | 1 | 5.06 |
| CHEMBL2103851 | AMUVATINIB | 2.0 | 1 | - |
| CHEMBL3545076 | LY-2584702 | 1.0 | 1 | - |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | - |
| CHEMBL1233528 | VOLASERTIB | 3.0 | 1 | - |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL495727 | AT-9283 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 12.0 | nM | 7.92 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 13.0 | nM | 7.89 |
| CHEMBL445813 | AT-7519 | Kd | = | 58.0 | nM | 7.24 |
| CHEMBL488436 | AZD-5438 | Kd | = | 62.0 | nM | 7.21 |
| CHEMBL3688339 | — | Kd | = | 80.0 | nM | 7.10 |
| CHEMBL300138 | ENZASTAURIN | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL296468 | BMS-387032 | Kd | = | 299.0 | nM | 6.52 |
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 425.0 | nM | 6.37 |
| CHEMBL494089 | GSK-690693 | Kd | = | 428.0 | nM | 6.37 |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 447.0 | nM | 6.35 |
| CHEMBL3544964 | RAVOXERTINIB | Kd | = | 599.0 | nM | 6.22 |
| CHEMBL3128043 | PF-03758309 | Kd | = | 667.0 | nM | 6.18 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 707.0 | nM | 6.15 |
| CHEMBL565612 | SOTRASTAURIN | Kd | = | 709.0 | nM | 6.15 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 740.0 | nM | 6.13 |
| CHEMBL571948 | Y-39983 | Kd | = | 924.0 | nM | 6.03 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 1322.0 | nM | 5.88 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 1430.0 | nM | 5.84 |
| CHEMBL3991935 | — | Kd | = | 2722.0 | nM | 5.57 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 4850.0 | nM | 5.31 |
| CHEMBL91829 | RUBOXISTAURIN | Kd | = | 5063.0 | nM | 5.30 |
| CHEMBL3544932 | TAK-901 | Kd | = | 6168.0 | nM | 5.21 |
| CHEMBL2030402 | — | Kd | = | 8793.0 | nM | 5.06 |
| CHEMBL1236962 | OMIPALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1908394 | GSK-461364 | Kd | > | 30000.0 | nM | - |
| CHEMBL3182621 | AZD-8330 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545085 | XL-228 | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL206834 | BAFETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL939 | GEFITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1088751 | PH-797804 | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2105717 | CABOZANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL405130 | WHI-P131 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL483158 | ALISERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545307 | MERESTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL607707 | PELITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |