Assay Detail
Binding
CHEMBL5355404
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity to human CRBN thalidomide binding domain assessed as inhibition constant by microscale thermophoresis analysis
30
Total Activities
30
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
Synthesis of novel glutarimide ligands for the E3 ligase substrate receptor Cereblon (CRBN): Investigation of their binding mode and antiproliferative effects against myeloma cell lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 30 | 5.27 | 6.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5409302 | — | — | 1 | 6.30 |
| CHEMBL5413097 | — | — | 1 | 5.96 |
| CHEMBL5419709 | — | — | 1 | 5.52 |
| CHEMBL5435497 | — | — | 1 | 5.52 |
| CHEMBL5436622 | — | — | 1 | 5.52 |
| CHEMBL5397580 | — | — | 1 | 5.51 |
| CHEMBL5434742 | — | — | 1 | 5.48 |
| CHEMBL5439702 | — | — | 1 | 5.47 |
| CHEMBL5418463 | — | — | 1 | 5.46 |
| CHEMBL5418032 | — | — | 1 | 5.40 |
| CHEMBL5422899 | — | — | 1 | 5.32 |
| CHEMBL5406302 | — | — | 1 | 5.30 |
| CHEMBL5418739 | — | — | 1 | 5.29 |
| CHEMBL5418383 | — | — | 1 | 5.26 |
| CHEMBL5404825 | — | — | 1 | 5.22 |
| CHEMBL5436049 | — | — | 1 | 5.22 |
| CHEMBL5404837 | — | — | 1 | 5.16 |
| CHEMBL5428083 | — | — | 1 | 5.15 |
| CHEMBL5411137 | — | — | 1 | 5.15 |
| CHEMBL5398118 | — | — | 1 | 5.14 |
| CHEMBL5397775 | — | — | 1 | 5.13 |
| CHEMBL5416620 | — | — | 1 | 5.12 |
| CHEMBL5435385 | — | — | 1 | 5.11 |
| CHEMBL468 | THALIDOMIDE | 4.0 | 1 | 5.07 |
| CHEMBL5413552 | — | — | 1 | 5.05 |
| CHEMBL5429778 | — | — | 1 | 5.00 |
| CHEMBL5402303 | — | — | 1 | 4.89 |
| CHEMBL5419971 | — | — | 1 | 4.89 |
| CHEMBL5435212 | — | — | 1 | 4.70 |
| CHEMBL5420053 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5409302 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL5413097 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL5419709 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5435497 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5436622 | — | Ki | = | 3000.0 | nM | 5.52 |
| CHEMBL5397580 | — | Ki | = | 3100.0 | nM | 5.51 |
| CHEMBL5434742 | — | Ki | = | 3300.0 | nM | 5.48 |
| CHEMBL5439702 | — | Ki | = | 3400.0 | nM | 5.47 |
| CHEMBL5418463 | — | Ki | = | 3500.0 | nM | 5.46 |
| CHEMBL5418032 | — | Ki | = | 4000.0 | nM | 5.40 |
| CHEMBL5422899 | — | Ki | = | 4800.0 | nM | 5.32 |
| CHEMBL5406302 | — | Ki | = | 5000.0 | nM | 5.30 |
| CHEMBL5418739 | — | Ki | = | 5100.0 | nM | 5.29 |
| CHEMBL5418383 | — | Ki | = | 5500.0 | nM | 5.26 |
| CHEMBL5404825 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL5436049 | — | Ki | = | 6000.0 | nM | 5.22 |
| CHEMBL5404837 | — | Ki | = | 7000.0 | nM | 5.16 |
| CHEMBL5428083 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL5411137 | — | Ki | = | 7100.0 | nM | 5.15 |
| CHEMBL5398118 | — | Ki | = | 7300.0 | nM | 5.14 |
| CHEMBL5397775 | — | Ki | = | 7400.0 | nM | 5.13 |
| CHEMBL5416620 | — | Ki | = | 7500.0 | nM | 5.12 |
| CHEMBL5435385 | — | Ki | = | 7800.0 | nM | 5.11 |
| CHEMBL468 | THALIDOMIDE | Ki | = | 8500.0 | nM | 5.07 |
| CHEMBL5413552 | — | Ki | = | 9000.0 | nM | 5.05 |
| CHEMBL5429778 | — | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL5402303 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL5419971 | — | Ki | = | 13000.0 | nM | 4.89 |
| CHEMBL5435212 | — | Ki | = | 20000.0 | nM | 4.70 |
| CHEMBL5420053 | — | Ki | = | 21000.0 | nM | 4.68 |