Assay Detail
Binding
CHEMBL3991828
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.
240
Total Activities
240
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
Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma (CHEMBL1770034) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 240 | 5.88 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3688339 | — | — | 1 | 8.52 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | 7.17 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.96 |
| CHEMBL2133806 | JNJ-38877605 | 1.0 | 1 | 6.50 |
| CHEMBL3544966 | GSK-1059615 | 1.0 | 1 | 6.48 |
| CHEMBL1822792 | MK-2461 | 2.0 | 1 | 5.99 |
| CHEMBL1230165 | SILMITASERTIB | 2.0 | 1 | 5.95 |
| CHEMBL1236962 | OMIPALISIB | 2.0 | 1 | 5.86 |
| CHEMBL564829 | MILCICLIB | 2.0 | 1 | 5.84 |
| CHEMBL3545328 | XL-019 | 1.0 | 1 | 5.80 |
| CHEMBL189963 | PALBOCICLIB | 4.0 | 1 | 5.76 |
| CHEMBL3545083 | RGB-286638 | 1.0 | 1 | 5.66 |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | 5.61 |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | 5.58 |
| CHEMBL1908394 | GSK-461364 | 1.0 | 1 | 5.55 |
| CHEMBL428690 | ALVOCIDIB | 3.0 | 1 | 5.55 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 5.54 |
| CHEMBL3353410 | OSIMERTINIB | 4.0 | 1 | 5.53 |
| CHEMBL1094408 | NMS-1286937 | — | 1 | 5.40 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 5.36 |
| CHEMBL2087361 | ICOTINIB | 3.0 | 1 | 5.33 |
| CHEMBL3218578 | BGT-226 FREE BASE | 2.0 | 1 | 5.32 |
| CHEMBL3120215 | OSI-027 | 2.0 | 1 | 5.30 |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | 5.25 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 5.21 |
| CHEMBL2336325 | VISTUSERTIB | 2.0 | 1 | - |
| CHEMBL377300 | BRIVANIB | 3.0 | 1 | - |
| CHEMBL31965 | CANERTINIB | 3.0 | 1 | - |
| CHEMBL1976040 | ADAVOSERTIB | 2.0 | 1 | - |
| CHEMBL1236107 | SGX-523 | 1.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3688339 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL482967 | CYC-116 | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL1230609 | FORETINIB | Kd | = | 109.0 | nM | 6.96 |
| CHEMBL2133806 | JNJ-38877605 | Kd | = | 320.0 | nM | 6.50 |
| CHEMBL3544966 | GSK-1059615 | Kd | = | 331.0 | nM | 6.48 |
| CHEMBL1822792 | MK-2461 | Kd | = | 1027.0 | nM | 5.99 |
| CHEMBL1230165 | SILMITASERTIB | Kd | = | 1112.0 | nM | 5.95 |
| CHEMBL1236962 | OMIPALISIB | Kd | = | 1372.0 | nM | 5.86 |
| CHEMBL564829 | MILCICLIB | Kd | = | 1432.0 | nM | 5.84 |
| CHEMBL3545328 | XL-019 | Kd | = | 1595.0 | nM | 5.80 |
| CHEMBL189963 | PALBOCICLIB | Kd | = | 1721.0 | nM | 5.76 |
| CHEMBL3545083 | RGB-286638 | Kd | = | 2184.0 | nM | 5.66 |
| CHEMBL513909 | BI-2536 | Kd | = | 2440.0 | nM | 5.61 |
| CHEMBL2103830 | FOSTAMATINIB | Kd | = | 2635.0 | nM | 5.58 |
| CHEMBL428690 | ALVOCIDIB | Kd | = | 2845.0 | nM | 5.55 |
| CHEMBL1908394 | GSK-461364 | Kd | = | 2837.0 | nM | 5.55 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 2901.0 | nM | 5.54 |
| CHEMBL3353410 | OSIMERTINIB | Kd | = | 2973.0 | nM | 5.53 |
| CHEMBL1094408 | NMS-1286937 | Kd | = | 4015.0 | nM | 5.40 |
| CHEMBL941 | IMATINIB | Kd | = | 4342.0 | nM | 5.36 |
| CHEMBL2087361 | ICOTINIB | Kd | = | 4663.0 | nM | 5.33 |
| CHEMBL3218578 | BGT-226 FREE BASE | Kd | = | 4795.0 | nM | 5.32 |
| CHEMBL3120215 | OSI-027 | Kd | = | 4974.0 | nM | 5.30 |
| CHEMBL1091644 | LINSITINIB | Kd | = | 5572.0 | nM | 5.25 |
| CHEMBL206834 | BAFETINIB | Kd | = | 6185.0 | nM | 5.21 |
| CHEMBL1229517 | VEMURAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL495727 | AT-9283 | Kd | > | 30000.0 | nM | - |
| CHEMBL3544964 | RAVOXERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL2216870 | IDELALISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3813873 | PEXIDARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL283120 | AXL-1717 | Kd | > | 30000.0 | nM | - |
| CHEMBL554 | LAPATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1614713 | CC-401 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545110 | RIBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL300138 | ENZASTAURIN | Kd | > | 30000.0 | nM | - |
| CHEMBL1201182 | TEMSIROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL2105728 | CRENOLANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1922094 | APITOLISIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2029988 | CEP-32496 | Kd | > | 30000.0 | nM | - |
| CHEMBL296468 | BMS-387032 | Kd | > | 30000.0 | nM | - |
| CHEMBL1908360 | EVEROLIMUS | Kd | > | 30000.0 | nM | - |
| CHEMBL3301612 | ENCORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1944698 | ZOTIRACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL587723 | AEE-788 | Kd | > | 30000.0 | nM | - |
| CHEMBL1079175 | MK-2206 | Kd | > | 30000.0 | nM | - |
| CHEMBL2001019 | PF-04217903 | Kd | > | 30000.0 | nM | - |