Assay Detail
Binding
CHEMBL5524487
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Binding affinity to human CRBN TBD assessed as inhibition constant using BODIPY-uracil as substrate by Microscale thermophoresis assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and characterization of potent spiro-isoxazole-based cereblon ligands with a novel binding mode.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 20 | 4.75 | 5.44 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5561114 | — | — | 1 | 5.44 |
| CHEMBL5563368 | — | — | 1 | 5.43 |
| CHEMBL5559649 | — | — | 1 | 5.42 |
| CHEMBL5549746 | — | — | 1 | 5.23 |
| CHEMBL5563976 | — | — | 1 | 5.15 |
| CHEMBL468 | THALIDOMIDE | 4.0 | 1 | 5.07 |
| CHEMBL5555248 | — | — | 1 | 5.06 |
| CHEMBL5555710 | — | — | 1 | 4.95 |
| CHEMBL5561864 | — | — | 1 | 4.80 |
| CHEMBL5559414 | — | — | 1 | 4.71 |
| CHEMBL5559886 | — | — | 1 | 4.69 |
| CHEMBL5557027 | — | — | 1 | 4.57 |
| CHEMBL5563024 | — | — | 1 | 4.52 |
| CHEMBL5563719 | — | — | 1 | 4.48 |
| CHEMBL5557543 | — | — | 1 | 4.38 |
| CHEMBL5562478 | — | — | 1 | 4.15 |
| CHEMBL5560360 | — | — | 1 | 4.11 |
| CHEMBL5565416 | — | — | 1 | 4.09 |
| CHEMBL3763941 | — | — | 1 | 4.03 |
| CHEMBL5561250 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5561114 | — | Ki | = | 3600.0 | nM | 5.44 |
| CHEMBL5563368 | — | Ki | = | 3700.0 | nM | 5.43 |
| CHEMBL5559649 | — | Ki | = | 3800.0 | nM | 5.42 |
| CHEMBL5549746 | — | Ki | = | 5900.0 | nM | 5.23 |
| CHEMBL5563976 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL468 | THALIDOMIDE | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL5555248 | — | Ki | = | 8800.0 | nM | 5.06 |
| CHEMBL5555710 | — | Ki | = | 11300.0 | nM | 4.95 |
| CHEMBL5561864 | — | Ki | = | 15800.0 | nM | 4.80 |
| CHEMBL5559414 | — | Ki | = | 19300.0 | nM | 4.71 |
| CHEMBL5559886 | — | Ki | = | 20400.0 | nM | 4.69 |
| CHEMBL5557027 | — | Ki | = | 27100.0 | nM | 4.57 |
| CHEMBL5563024 | — | Ki | = | 30100.0 | nM | 4.52 |
| CHEMBL5563719 | — | Ki | = | 33400.0 | nM | 4.48 |
| CHEMBL5557543 | — | Ki | = | 41600.0 | nM | 4.38 |
| CHEMBL5562478 | — | Ki | = | 70700.0 | nM | 4.15 |
| CHEMBL5560360 | — | Ki | = | 77400.0 | nM | 4.11 |
| CHEMBL5565416 | — | Ki | = | 80900.0 | nM | 4.09 |
| CHEMBL3763941 | — | Ki | = | 92500.0 | nM | 4.03 |
| CHEMBL5561250 | — | Ki | = | 102900.0 | nM | - |