Assay Detail
Binding
CHEMBL5037049
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PROTAC activity at human CRBN/HiBiT-fused GSPT1 transfected in HEK293T cells assessed as induction of GSPT1 degradation measured after 4 hrs by Nano-Glo HiBiT lytic assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293T |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Protein cereblon/GSPT1 (CHEMBL4296168) ↗| 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 |
|---|---|---|---|
| EC50 | 11 | 7.36 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5094191 | — | — | 1 | 10.00 |
| CHEMBL4742712 | — | — | 1 | 7.54 |
| CHEMBL5069911 | — | — | 1 | 7.28 |
| CHEMBL5084741 | — | — | 1 | 6.97 |
| CHEMBL5073414 | — | — | 1 | 5.03 |
| CHEMBL5078971 | — | — | 1 | - |
| CHEMBL5084281 | — | — | 1 | - |
| CHEMBL5079426 | — | — | 1 | - |
| CHEMBL5078004 | — | — | 1 | - |
| CHEMBL5090015 | — | — | 1 | - |
| CHEMBL5074427 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5094191 | — | EC50 | = | 0.1 | nM | 10.00 |
| CHEMBL4742712 | — | EC50 | = | 29.2 | nM | 7.54 |
| CHEMBL5069911 | — | EC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5084741 | — | EC50 | = | 108.0 | nM | 6.97 |
| CHEMBL5073414 | — | EC50 | = | 9320.0 | nM | 5.03 |
| CHEMBL5078971 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5084281 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5079426 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5078004 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5090015 | — | EC50 | > | 10000.0 | nM | - |
| CHEMBL5074427 | — | EC50 | > | 10000.0 | nM | - |