Assay Detail
Binding
CHEMBL5375575
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of BODIPY-lenalidomide from human N-terminal NanoLuc-fused CRBN expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Covalent Stapling of the Cereblon Sensor Loop Histidine Using Sulfur-Heterocycle Exchange.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 6.55 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5279477 | — | — | 1 | 8.96 |
| CHEMBL5431754 | — | — | 1 | 7.68 |
| CHEMBL5439475 | — | — | 1 | 7.38 |
| CHEMBL5430120 | — | — | 1 | 7.36 |
| CHEMBL5419977 | — | — | 1 | 7.30 |
| CHEMBL5431074 | — | — | 1 | 7.26 |
| CHEMBL5420894 | — | — | 1 | 7.11 |
| CHEMBL5289875 | — | — | 1 | 6.59 |
| CHEMBL5429393 | — | — | 1 | 6.49 |
| CHEMBL5399248 | — | — | 1 | 6.34 |
| CHEMBL304572 | — | — | 1 | 6.22 |
| CHEMBL5397937 | — | — | 1 | 5.86 |
| CHEMBL5413999 | — | — | 1 | 5.79 |
| CHEMBL5415133 | — | — | 1 | 5.63 |
| CHEMBL5421432 | — | — | 1 | 5.43 |
| CHEMBL5410618 | — | — | 1 | 5.37 |
| CHEMBL5423386 | — | — | 1 | 4.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5279477 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5431754 | — | IC50 | = | 21.1 | nM | 7.68 |
| CHEMBL5439475 | — | IC50 | = | 41.9 | nM | 7.38 |
| CHEMBL5430120 | — | IC50 | = | 43.6 | nM | 7.36 |
| CHEMBL5419977 | — | IC50 | = | 50.4 | nM | 7.30 |
| CHEMBL5431074 | — | IC50 | = | 54.9 | nM | 7.26 |
| CHEMBL5420894 | — | IC50 | = | 77.9 | nM | 7.11 |
| CHEMBL5289875 | — | IC50 | = | 255.0 | nM | 6.59 |
| CHEMBL5429393 | — | IC50 | = | 324.0 | nM | 6.49 |
| CHEMBL5399248 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL304572 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL5397937 | — | IC50 | = | 1377.0 | nM | 5.86 |
| CHEMBL5413999 | — | IC50 | = | 1629.0 | nM | 5.79 |
| CHEMBL5415133 | — | IC50 | = | 2341.0 | nM | 5.63 |
| CHEMBL5421432 | — | IC50 | = | 3752.0 | nM | 5.43 |
| CHEMBL5410618 | — | IC50 | = | 4298.0 | nM | 5.37 |
| CHEMBL5423386 | — | IC50 | = | 28630.0 | nM | 4.54 |