Assay Detail
Binding
CHEMBL5037071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Cy5-O-Len probe from 6XHis-tagged CRBN/DDB1 (unknown origin) incubated in dark for 1 hr by fluorescence polarization assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Protein cereblon/DNA damage-binding protein 1 (CHEMBL4630734) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.41 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5084281 | — | — | 1 | 9.00 |
| CHEMBL5078971 | — | — | 1 | 8.52 |
| CHEMBL5078004 | — | — | 1 | 8.05 |
| CHEMBL5079426 | — | — | 1 | 8.00 |
| CHEMBL5073414 | — | — | 1 | 7.96 |
| CHEMBL5094191 | — | — | 1 | 7.82 |
| CHEMBL5084741 | — | — | 1 | 7.80 |
| CHEMBL4170596 | — | — | 1 | 7.75 |
| CHEMBL5074427 | — | — | 1 | 7.64 |
| CHEMBL848 | LENALIDOMIDE | 4.0 | 1 | 6.54 |
| CHEMBL5069911 | — | — | 1 | 6.47 |
| CHEMBL5090015 | — | — | 1 | 6.21 |
| CHEMBL4742712 | — | — | 1 | 6.08 |
| CHEMBL468 | THALIDOMIDE | 4.0 | 1 | 5.86 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5084281 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5078971 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5078004 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5079426 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5073414 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5094191 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5084741 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4170596 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5074427 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL848 | LENALIDOMIDE | IC50 | = | 286.0 | nM | 6.54 |
| CHEMBL5069911 | — | IC50 | = | 337.0 | nM | 6.47 |
| CHEMBL5090015 | — | IC50 | = | 612.0 | nM | 6.21 |
| CHEMBL4742712 | — | IC50 | = | 824.0 | nM | 6.08 |
| CHEMBL468 | THALIDOMIDE | IC50 | = | 1380.0 | nM | 5.86 |