Assay Detail
Binding
CHEMBL3991822
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.
179
Total Activities
179
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
Membrane-associated progesterone receptor component 1 (CHEMBL4105706) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 179 | 6.69 | 6.69 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3301612 | ENCORAFENIB | 4.0 | 1 | 6.69 |
| CHEMBL482967 | CYC-116 | 1.0 | 1 | - |
| CHEMBL601719 | CRIZOTINIB | 4.0 | 1 | - |
| CHEMBL1233300 | HYDROXYFASUDIL | — | 1 | - |
| CHEMBL3991933 | — | — | 1 | - |
| CHEMBL1091644 | LINSITINIB | 3.0 | 1 | - |
| CHEMBL558752 | RAF-265 | 2.0 | 1 | - |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | - |
| CHEMBL215152 | DEFOSBARASERTIB | 2.0 | 1 | - |
| CHEMBL259084 | MLN-8054 | 1.0 | 1 | - |
| CHEMBL2103830 | FOSTAMATINIB | 4.0 | 1 | - |
| CHEMBL3301622 | GILTERITINIB | 4.0 | 1 | - |
| CHEMBL1079175 | MK-2206 | 2.0 | 1 | - |
| CHEMBL513909 | BI-2536 | 2.0 | 1 | - |
| CHEMBL3544932 | TAK-901 | 1.0 | 1 | - |
| CHEMBL3545137 | PF-00477736 | 1.0 | 1 | - |
| CHEMBL3402762 | TEPOTINIB | 4.0 | 1 | - |
| CHEMBL3137336 | UPROSERTIB | 2.0 | 1 | - |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | - |
| CHEMBL1944698 | ZOTIRACICLIB | 2.0 | 1 | - |
| CHEMBL3137331 | DEFACTINIB | 3.0 | 1 | - |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | - |
| CHEMBL1173655 | AFATINIB | 4.0 | 1 | - |
| CHEMBL1614701 | SELUMETINIB | 4.0 | 1 | - |
| CHEMBL2107832 | PIMASERTIB | 2.0 | 1 | - |
| CHEMBL1801204 | AZD-8055 | 1.0 | 1 | - |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | - |
| CHEMBL3188551 | GSK-2636771 | 2.0 | 1 | - |
| CHEMBL1667969 | SAR-407899 FREE BASE | 2.0 | 1 | - |
| CHEMBL1234354 | PF-04691502 | 2.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3301612 | ENCORAFENIB | Kd | = | 204.0 | nM | 6.69 |
| CHEMBL941 | IMATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1287853 | FEDRATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL4084193 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL1822792 | MK-2461 | Kd | > | 30000.0 | nM | - |
| CHEMBL2087361 | ICOTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103840 | DINACICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3264002 | AVUTOMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2133806 | JNJ-38877605 | Kd | > | 30000.0 | nM | - |
| CHEMBL576982 | QUIZARTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL507361 | MIRDAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3353410 | OSIMERTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103842 | VARLITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2103875 | TRAMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2079588 | TELATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2041933 | AZD-7762 | Kd | > | 30000.0 | nM | - |
| CHEMBL488436 | AZD-5438 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991929 | Cerdulatinib Hydrochloride | Kd | > | 30000.0 | nM | - |
| CHEMBL1230165 | SILMITASERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL496102 | AMG-208 | Kd | > | 30000.0 | nM | - |
| CHEMBL253969 | OSI-632 | Kd | > | 30000.0 | nM | - |
| CHEMBL1230609 | FORETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL571546 | TIRBANIBULIN | Kd | > | 30000.0 | nM | - |
| CHEMBL274654 | ORANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1615025 | TAK-733 | Kd | > | 30000.0 | nM | - |
| CHEMBL598797 | CUDC-101 | Kd | > | 30000.0 | nM | - |
| CHEMBL2103882 | TIVANTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL3991931 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL2219422 | AFURESERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1946170 | REGORAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1614725 | TAK-285 | Kd | > | 30000.0 | nM | - |
| CHEMBL482767 | SNS-314 | Kd | > | 30000.0 | nM | - |
| CHEMBL4289017 | PF-03814735 | Kd | > | 30000.0 | nM | - |
| CHEMBL3545083 | RGB-286638 | Kd | > | 30000.0 | nM | - |
| CHEMBL3991934 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL536151 | IMD-0354 | Kd | > | 30000.0 | nM | - |
| CHEMBL3039525 | GOLVATINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2138625 | AV-412 FREE BASE | Kd | > | 30000.0 | nM | - |
| CHEMBL1084546 | PF-00562271 | Kd | > | 30000.0 | nM | - |
| CHEMBL1614766 | RO-4987655 | Kd | > | 30000.0 | nM | - |
| CHEMBL2146883 | COBIMETINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL475251 | R-406 | Kd | > | 30000.0 | nM | - |
| CHEMBL221959 | TOFACITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1976040 | ADAVOSERTIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2140408 | AMG-900 | Kd | > | 30000.0 | nM | - |
| CHEMBL3907479 | FGFR INHIBITOR DEBIO 1347 | Kd | > | 30000.0 | nM | - |
| CHEMBL372764 | PERIFOSINE | Kd | > | 30000.0 | nM | - |
| CHEMBL3699142 | — | Kd | > | 30000.0 | nM | - |
| CHEMBL522892 | DOVITINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2376648 | — | Kd | > | 30000.0 | nM | - |