Assay Detail
Functional
CHEMBL5388153
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Cytotoxicity against human RPMI-8226 cells assessed as inhibition of cell proliferation incubated for 72 hrs by Cell Titer-Glo luminescence assay
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | RPMI-8226 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design and discovery of novel dipeptide boronic acid ester proteasome inhibitors, an oral slowly-released prodrug for the treatment of multiple myeloma.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.06 | 8.54 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5394365 | — | — | 1 | 8.54 |
| CHEMBL5440712 | — | — | 1 | 8.36 |
| CHEMBL5398681 | — | — | 1 | 8.31 |
| CHEMBL5431451 | — | — | 1 | 8.30 |
| CHEMBL5394458 | — | — | 1 | 8.28 |
| CHEMBL5419917 | — | — | 1 | 8.25 |
| CHEMBL5402052 | — | — | 1 | 8.17 |
| CHEMBL5423645 | — | — | 1 | 8.17 |
| CHEMBL5403296 | — | — | 1 | 8.16 |
| CHEMBL5412037 | — | — | 1 | 8.16 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 8.13 |
| CHEMBL5434607 | — | — | 1 | 8.12 |
| CHEMBL5433735 | — | — | 1 | 8.06 |
| CHEMBL5413513 | — | — | 1 | 7.87 |
| CHEMBL5406440 | — | — | 1 | 7.83 |
| CHEMBL5429323 | — | — | 1 | 7.74 |
| CHEMBL5410630 | — | — | 1 | 7.38 |
| CHEMBL5433547 | — | — | 1 | 7.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5394365 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5440712 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL5398681 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL5431451 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5394458 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL5419917 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL5402052 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL5423645 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5403296 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL5412037 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 7.4 | nM | 8.13 |
| CHEMBL5434607 | — | IC50 | = | 7.5 | nM | 8.12 |
| CHEMBL5433735 | — | IC50 | = | 8.7 | nM | 8.06 |
| CHEMBL5413513 | — | IC50 | = | 13.6 | nM | 7.87 |
| CHEMBL5406440 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL5429323 | — | IC50 | = | 18.4 | nM | 7.74 |
| CHEMBL5410630 | — | IC50 | = | 41.5 | nM | 7.38 |
| CHEMBL5433547 | — | IC50 | = | 57.9 | nM | 7.24 |