Assay Detail
Binding
CHEMBL3991663
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 | 6.41 | 9.00 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | 9.00 |
| CHEMBL2103840 | DINACICLIB | 3.0 | 1 | 8.15 |
| CHEMBL445813 | AT-7519 | 2.0 | 1 | 8.15 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 8.15 |
| CHEMBL384304 | RG-547 | 2.0 | 1 | 7.60 |
| CHEMBL3991935 | — | — | 1 | 7.55 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 7.48 |
| CHEMBL296468 | BMS-387032 | 1.0 | 1 | 7.47 |
| CHEMBL3688339 | — | — | 1 | 7.09 |
| CHEMBL3301610 | ABEMACICLIB | 4.0 | 1 | 6.76 |
| CHEMBL1230607 | PHA-793887 | 1.0 | 1 | 6.66 |
| CHEMBL488436 | AZD-5438 | 1.0 | 1 | 6.50 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 6.13 |
| CHEMBL2105728 | CRENOLANIB | 3.0 | 1 | 6.00 |
| CHEMBL2035187 | PACRITINIB | 4.0 | 1 | 6.00 |
| CHEMBL571948 | Y-39983 | 1.0 | 1 | 5.87 |
| CHEMBL1084546 | PF-00562271 | 1.0 | 1 | 5.87 |
| CHEMBL495727 | AT-9283 | 2.0 | 1 | 5.79 |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | 5.75 |
| CHEMBL3039513 | DECERNOTINIB | 2.0 | 1 | 5.73 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 5.45 |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | 5.44 |
| CHEMBL3545110 | RIBOCICLIB | 4.0 | 1 | 5.43 |
| CHEMBL38380 | FASUDIL | 3.0 | 1 | 5.37 |
| CHEMBL14762 | SELICICLIB | 2.0 | 1 | 5.31 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.02 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 5.00 |
| CHEMBL3426621 | RIPASUDIL | 3.0 | 1 | 4.88 |
| CHEMBL230011 | TG100-115 | 2.0 | 1 | - |
| CHEMBL217092 | SARACATINIB | 3.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1944698 | ZOTIRACICLIB | Kd | = | 1.0 | nM | 9.00 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL2103840 | DINACICLIB | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL445813 | AT-7519 | Kd | = | 7.0 | nM | 8.15 |
| CHEMBL384304 | RG-547 | Kd | = | 25.0 | nM | 7.60 |
| CHEMBL3991935 | — | Kd | = | 28.0 | nM | 7.55 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 33.0 | nM | 7.48 |
| CHEMBL296468 | BMS-387032 | Kd | = | 34.0 | nM | 7.47 |
| CHEMBL3688339 | — | Kd | = | 81.0 | nM | 7.09 |
| CHEMBL3301610 | ABEMACICLIB | Kd | = | 174.0 | nM | 6.76 |
| CHEMBL1230607 | PHA-793887 | Kd | = | 218.0 | nM | 6.66 |
| CHEMBL488436 | AZD-5438 | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL1078178 | MOMELOTINIB | Kd | = | 741.0 | nM | 6.13 |
| CHEMBL2105728 | CRENOLANIB | Kd | = | 988.0 | nM | 6.00 |
| CHEMBL2035187 | PACRITINIB | Kd | = | 1006.0 | nM | 6.00 |
| CHEMBL1084546 | PF-00562271 | Kd | = | 1354.0 | nM | 5.87 |
| CHEMBL571948 | Y-39983 | Kd | = | 1355.0 | nM | 5.87 |
| CHEMBL495727 | AT-9283 | Kd | = | 1640.0 | nM | 5.79 |
| CHEMBL3137331 | DEFACTINIB | Kd | = | 1790.0 | nM | 5.75 |
| CHEMBL3039513 | DECERNOTINIB | Kd | = | 1870.0 | nM | 5.73 |
| CHEMBL3545085 | XL-228 | Kd | = | 3512.0 | nM | 5.45 |
| CHEMBL3544932 | TAK-901 | Kd | = | 3609.0 | nM | 5.44 |
| CHEMBL3545110 | RIBOCICLIB | Kd | = | 3708.0 | nM | 5.43 |
| CHEMBL38380 | FASUDIL | Kd | = | 4251.0 | nM | 5.37 |
| CHEMBL14762 | SELICICLIB | Kd | = | 4860.0 | nM | 5.31 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 9492.0 | nM | 5.02 |
| CHEMBL482967 | CYC-116 | Kd | = | 9901.0 | nM | 5.00 |
| CHEMBL3426621 | RIPASUDIL | Kd | = | 13279.0 | nM | 4.88 |
| CHEMBL3545360 | ASP-3026 | Kd | > | 30000.0 | nM | - |
| CHEMBL494089 | GSK-690693 | Kd | > | 30000.0 | nM | - |
| CHEMBL3600873 | MK-5108 | Kd | > | 30000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3120215 | OSI-027 | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1236107 | SGX-523 | Kd | > | 30000.0 | nM | - |
| CHEMBL3348923 | TOVORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3989914 | GLESATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1090090 | VX-702 | Kd | > | 30000.0 | nM | - |
| CHEMBL1336 | SORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103830 | FOSTAMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL564829 | MILCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3545366 | VOXTALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL574737 | UCN-01 | Kd | > | 30000.0 | nM | - |
| CHEMBL400402 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |