Assay Detail
Binding
CHEMBL3991686
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 |
Target
Discoidin domain-containing receptor 2 (CHEMBL5122) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.20 | 8.40 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.40 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.80 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 7.41 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.32 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 7.19 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.16 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.06 |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | 7.03 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.92 |
| CHEMBL3991933 | — | — | 1 | 6.86 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.74 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 6.74 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 6.74 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 6.66 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 6.64 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 6.53 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.46 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.38 |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | 6.37 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.30 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.23 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 6.17 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.09 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.07 |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | 6.04 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 6.00 |
| CHEMBL3991932 | PEXMETINIB | 2.0 | 1 | 5.94 |
| CHEMBL3699142 | — | — | 1 | 5.93 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 5.90 |
| CHEMBL3989914 | GLESATINIB | 2.0 | 1 | 5.83 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 4.0 | nM | 8.40 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 16.0 | nM | 7.80 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL206834 | BAFETINIB | Kd | = | 48.0 | nM | 7.32 |
| CHEMBL460702 | BMS-777607 | Kd | = | 65.0 | nM | 7.19 |
| CHEMBL5416410 | DASATINIB | Kd | = | 70.0 | nM | 7.16 |
| CHEMBL1171837 | PONATINIB | Kd | = | 87.0 | nM | 7.06 |
| CHEMBL2220486 | LUCITANIB | Kd | = | 94.0 | nM | 7.03 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 121.0 | nM | 6.92 |
| CHEMBL3991933 | — | Kd | = | 139.0 | nM | 6.86 |
| CHEMBL1230609 | FORETINIB | Kd | = | 182.0 | nM | 6.74 |
| CHEMBL941 | IMATINIB | Kd | = | 181.0 | nM | 6.74 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 183.0 | nM | 6.74 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 218.0 | nM | 6.66 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 227.0 | nM | 6.64 |
| CHEMBL2140408 | AMG-900 | Kd | = | 298.0 | nM | 6.53 |
| CHEMBL255863 | NILOTINIB | Kd | = | 347.0 | nM | 6.46 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 421.0 | nM | 6.38 |
| CHEMBL482767 | SNS-314 | Kd | = | 423.0 | nM | 6.37 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 501.0 | nM | 6.30 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 592.0 | nM | 6.23 |
| CHEMBL253969 | OSI-632 | Kd | = | 669.0 | nM | 6.17 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 805.0 | nM | 6.09 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 850.0 | nM | 6.07 |
| CHEMBL3545307 | MERESTINIB | Kd | = | 908.0 | nM | 6.04 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 1000.0 | nM | 6.00 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 1138.0 | nM | 5.94 |
| CHEMBL3699142 | — | Kd | = | 1163.0 | nM | 5.93 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 1271.0 | nM | 5.90 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 1493.0 | nM | 5.83 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 1523.0 | nM | 5.82 |
| CHEMBL475251 | R-406 | Kd | = | 1913.0 | nM | 5.72 |
| CHEMBL1336 | SORAFENIB | Kd | = | 1950.0 | nM | 5.71 |
| CHEMBL3688339 | — | Kd | = | 2284.0 | nM | 5.64 |
| CHEMBL3544932 | TAK-901 | Kd | = | 2331.0 | nM | 5.63 |
| CHEMBL3991934 | — | Kd | = | 3250.0 | nM | 5.49 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 3421.0 | nM | 5.47 |
| CHEMBL1908391 | MASITINIB | Kd | = | 3956.0 | nM | 5.40 |
| CHEMBL564829 | MILCICLIB | Kd | = | 4289.0 | nM | 5.37 |
| CHEMBL3545085 | XL-228 | Kd | = | 4963.0 | nM | 5.30 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 12899.0 | nM | 4.89 |
| CHEMBL2180604 | TAK-593 | Kd | = | 19290.0 | nM | 4.71 |
| CHEMBL587723 | AEE-788 | Kd | = | 28192.0 | nM | 4.55 |
| CHEMBL217092 | SARACATINIB | Kd | = | 42280.0 | nM | 4.37 |
| CHEMBL3188551 | GSK-2636771 | Kd | > | 30000.0 | nM | - |
| CHEMBL101253 | VATALANIB | Kd | > | 30000.0 | nM | - |
| CHEMBL1983268 | ENTRECTINIB | Kd | > | 30000.0 | nM | - |
| CHEMBL189963 | PALBOCICLIB | Kd | > | 30000.0 | nM | - |
| CHEMBL2028663 | DABRAFENIB | Kd | > | 30000.0 | nM | - |
| CHEMBL377300 | BRIVANIB | Kd | > | 30000.0 | nM | - |