Assay Detail
Binding
CHEMBL4715296
Review assay metadata, readout intent, target linkage, and publication context from the same page.
PROTAC activity at CRBN/JAK2 in human MHHCALL4 cells assessed as protein degradation by immunoblot analysis
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MHHCALL4 |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
Protein cereblon/Tyrosine-protein kinase JAK2 (CHEMBL4742263) ↗| Type | PROTEIN-PROTEIN INTERACTION |
| Organism | Homo sapiens |
Publication
PROTAC-Mediated Degradation of Janus Kinase as a Therapeutic Strategy for Cancer and Rheumatoid Arthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 12 | 8.01 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4741262 | — | — | 1 | 9.70 |
| CHEMBL4797017 | — | — | 1 | 9.30 |
| CHEMBL4790924 | — | — | 1 | 9.30 |
| CHEMBL4742130 | — | — | 1 | 9.27 |
| CHEMBL4789389 | — | — | 1 | 9.05 |
| CHEMBL4759504 | — | — | 1 | 8.57 |
| CHEMBL4784942 | — | — | 1 | 8.41 |
| CHEMBL4764854 | — | — | 1 | 7.82 |
| CHEMBL4744617 | — | — | 1 | 6.91 |
| CHEMBL4783150 | — | — | 1 | 6.14 |
| CHEMBL4781392 | — | — | 1 | 5.96 |
| CHEMBL4758582 | — | — | 1 | 5.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4741262 | — | EC50 | = | 0.2 | nM | 9.70 |
| CHEMBL4797017 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4790924 | — | EC50 | = | 0.5 | nM | 9.30 |
| CHEMBL4742130 | — | EC50 | = | 0.54 | nM | 9.27 |
| CHEMBL4789389 | — | EC50 | = | 0.9 | nM | 9.05 |
| CHEMBL4759504 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL4784942 | — | EC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4764854 | — | EC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4744617 | — | EC50 | = | 122.0 | nM | 6.91 |
| CHEMBL4783150 | — | EC50 | = | 720.0 | nM | 6.14 |
| CHEMBL4781392 | — | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4758582 | — | EC50 | = | 2300.0 | nM | 5.64 |