Assay Detail
Binding
CHEMBL3991685
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
Epithelial discoidin domain-containing receptor 1 (CHEMBL5319) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
The target landscape of clinical kinase drugs.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 243 | 6.60 | 8.52 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Direct Binder | Direct Binder | - | — | yes |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL400402 | — | — | 1 | 8.52 |
| CHEMBL3039525 | GOLVATINIB | 2.0 | 1 | 8.30 |
| CHEMBL1090479 | GSK-1070916 | 1.0 | 1 | 8.10 |
| CHEMBL206834 | BAFETINIB | 2.0 | 1 | 7.85 |
| CHEMBL2220486 | LUCITANIB | 2.0 | 1 | 7.85 |
| CHEMBL1171837 | PONATINIB | 4.0 | 1 | 7.75 |
| CHEMBL491473 | CEDIRANIB | 3.0 | 1 | 7.72 |
| CHEMBL502835 | NINTEDANIB | 4.0 | 1 | 7.70 |
| CHEMBL941 | IMATINIB | 4.0 | 1 | 7.66 |
| CHEMBL460702 | BMS-777607 | 2.0 | 1 | 7.41 |
| CHEMBL5416410 | DASATINIB | 4.0 | 1 | 7.37 |
| CHEMBL1289601 | LENVATINIB | 4.0 | 1 | 7.34 |
| CHEMBL3184679 | AZD-4547 | — | 1 | 7.25 |
| CHEMBL3348923 | TOVORAFENIB | 4.0 | 1 | 7.20 |
| CHEMBL1230609 | FORETINIB | 2.0 | 1 | 7.18 |
| CHEMBL253969 | OSI-632 | 2.0 | 1 | 7.17 |
| CHEMBL3544983 | TESEVATINIB | 3.0 | 1 | 7.14 |
| CHEMBL2140408 | AMG-900 | 1.0 | 1 | 6.96 |
| CHEMBL255863 | NILOTINIB | 4.0 | 1 | 6.94 |
| CHEMBL2029988 | CEP-32496 | 2.0 | 1 | 6.91 |
| CHEMBL477772 | PAZOPANIB | 4.0 | 1 | 6.88 |
| CHEMBL482767 | SNS-314 | 1.0 | 1 | 6.85 |
| CHEMBL402548 | DANUSERTIB | 2.0 | 1 | 6.85 |
| CHEMBL3545307 | MERESTINIB | 2.0 | 1 | 6.76 |
| CHEMBL1289494 | TIVOZANIB | 4.0 | 1 | 6.72 |
| CHEMBL2105717 | CABOZANTINIB | 4.0 | 1 | 6.68 |
| CHEMBL3545085 | XL-228 | 1.0 | 1 | 6.66 |
| CHEMBL1738757 | REBASTINIB | 2.0 | 1 | 6.57 |
| CHEMBL3991934 | — | — | 1 | 6.50 |
| CHEMBL1946170 | REGORAFENIB | 4.0 | 1 | 6.45 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL400402 | — | Kd | = | 3.0 | nM | 8.52 |
| CHEMBL3039525 | GOLVATINIB | Kd | = | 5.0 | nM | 8.30 |
| CHEMBL1090479 | GSK-1070916 | Kd | = | 8.0 | nM | 8.10 |
| CHEMBL2220486 | LUCITANIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL206834 | BAFETINIB | Kd | = | 14.0 | nM | 7.85 |
| CHEMBL1171837 | PONATINIB | Kd | = | 18.0 | nM | 7.75 |
| CHEMBL491473 | CEDIRANIB | Kd | = | 19.0 | nM | 7.72 |
| CHEMBL502835 | NINTEDANIB | Kd | = | 20.0 | nM | 7.70 |
| CHEMBL941 | IMATINIB | Kd | = | 22.0 | nM | 7.66 |
| CHEMBL460702 | BMS-777607 | Kd | = | 39.0 | nM | 7.41 |
| CHEMBL5416410 | DASATINIB | Kd | = | 43.0 | nM | 7.37 |
| CHEMBL1289601 | LENVATINIB | Kd | = | 46.0 | nM | 7.34 |
| CHEMBL3184679 | AZD-4547 | Kd | = | 56.0 | nM | 7.25 |
| CHEMBL3348923 | TOVORAFENIB | Kd | = | 63.0 | nM | 7.20 |
| CHEMBL1230609 | FORETINIB | Kd | = | 66.0 | nM | 7.18 |
| CHEMBL253969 | OSI-632 | Kd | = | 67.0 | nM | 7.17 |
| CHEMBL3544983 | TESEVATINIB | Kd | = | 73.0 | nM | 7.14 |
| CHEMBL2140408 | AMG-900 | Kd | = | 110.0 | nM | 6.96 |
| CHEMBL255863 | NILOTINIB | Kd | = | 115.0 | nM | 6.94 |
| CHEMBL2029988 | CEP-32496 | Kd | = | 124.0 | nM | 6.91 |
| CHEMBL477772 | PAZOPANIB | Kd | = | 132.0 | nM | 6.88 |
| CHEMBL482767 | SNS-314 | Kd | = | 140.0 | nM | 6.85 |
| CHEMBL402548 | DANUSERTIB | Kd | = | 142.0 | nM | 6.85 |
| CHEMBL3545307 | MERESTINIB | Kd | = | 174.0 | nM | 6.76 |
| CHEMBL1289494 | TIVOZANIB | Kd | = | 190.0 | nM | 6.72 |
| CHEMBL2105717 | CABOZANTINIB | Kd | = | 209.0 | nM | 6.68 |
| CHEMBL3545085 | XL-228 | Kd | = | 221.0 | nM | 6.66 |
| CHEMBL1738757 | REBASTINIB | Kd | = | 272.0 | nM | 6.57 |
| CHEMBL3991934 | — | Kd | = | 314.0 | nM | 6.50 |
| CHEMBL1946170 | REGORAFENIB | Kd | = | 358.0 | nM | 6.45 |
| CHEMBL3991932 | PEXMETINIB | Kd | = | 363.0 | nM | 6.44 |
| CHEMBL475251 | R-406 | Kd | = | 417.0 | nM | 6.38 |
| CHEMBL3699142 | — | Kd | = | 469.0 | nM | 6.33 |
| CHEMBL3688339 | — | Kd | = | 515.0 | nM | 6.29 |
| CHEMBL3989914 | GLESATINIB | Kd | = | 549.0 | nM | 6.26 |
| CHEMBL482968 | ENMD-2076 | Kd | = | 755.0 | nM | 6.12 |
| CHEMBL3991933 | — | Kd | = | 881.0 | nM | 6.05 |
| CHEMBL377300 | BRIVANIB | Kd | = | 1019.0 | nM | 5.99 |
| CHEMBL270995 | BRIVANIB ALANINATE | Kd | = | 1039.0 | nM | 5.98 |
| CHEMBL1908391 | MASITINIB | Kd | = | 1119.0 | nM | 5.95 |
| CHEMBL3600873 | MK-5108 | Kd | = | 1216.0 | nM | 5.92 |
| CHEMBL24828 | VANDETANIB | Kd | = | 1349.0 | nM | 5.87 |
| CHEMBL1336 | SORAFENIB | Kd | = | 1641.0 | nM | 5.79 |
| CHEMBL403989 | TG100-801 | Kd | = | 1725.0 | nM | 5.76 |
| CHEMBL575448 | BMS-754807 | Kd | = | 2383.0 | nM | 5.62 |
| CHEMBL3545360 | ASP-3026 | Kd | = | 4040.0 | nM | 5.39 |
| CHEMBL564829 | MILCICLIB | Kd | = | 4175.0 | nM | 5.38 |
| CHEMBL217092 | SARACATINIB | Kd | = | 4401.0 | nM | 5.36 |
| CHEMBL587723 | AEE-788 | Kd | = | 5223.0 | nM | 5.28 |
| CHEMBL3544932 | TAK-901 | Kd | = | 13766.0 | nM | 4.86 |