Assay Detail
Functional
CHEMBL4233076
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Cytotoxicity against human ARH77 cells assessed as reduction in cell viability after 72 hrs by CellTiter 96 aqueous one solution assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | ARH-77 |
| Confidence | 1 — Organism |
| Curated By | Intermediate |
Publication
Design, synthesis, in vitro and in vivo evaluation, and structure-activity relationship (SAR) discussion of novel dipeptidyl boronic acid proteasome inhibitors as orally available anti-cancer agents for the treatment of multiple myeloma and mechanism studies.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 7.99 | 8.43 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4248209 | — | — | 1 | 8.43 |
| CHEMBL4241473 | — | — | 1 | 8.33 |
| CHEMBL4246864 | — | — | 1 | 8.29 |
| CHEMBL4246480 | — | — | 1 | 8.27 |
| CHEMBL4245244 | — | — | 1 | 8.22 |
| CHEMBL4238198 | — | — | 1 | 8.12 |
| CHEMBL4243375 | — | — | 1 | 8.04 |
| CHEMBL4242666 | — | — | 1 | 8.02 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.02 |
| CHEMBL4249503 | — | — | 1 | 7.99 |
| CHEMBL4251272 | — | — | 1 | 7.84 |
| CHEMBL4249022 | — | — | 1 | 7.69 |
| CHEMBL1813256 | — | — | 1 | 7.36 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 7.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4248209 | — | IC50 | = | 3.68 | nM | 8.43 |
| CHEMBL4241473 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL4246864 | — | IC50 | = | 5.12 | nM | 8.29 |
| CHEMBL4246480 | — | IC50 | = | 5.32 | nM | 8.27 |
| CHEMBL4245244 | — | IC50 | = | 6.07 | nM | 8.22 |
| CHEMBL4238198 | — | IC50 | = | 7.59 | nM | 8.12 |
| CHEMBL4243375 | — | IC50 | = | 9.1 | nM | 8.04 |
| CHEMBL4242666 | — | IC50 | = | 9.51 | nM | 8.02 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 9.57 | nM | 8.02 |
| CHEMBL4249503 | — | IC50 | = | 10.34 | nM | 7.99 |
| CHEMBL4251272 | — | IC50 | = | 14.41 | nM | 7.84 |
| CHEMBL4249022 | — | IC50 | = | 20.55 | nM | 7.69 |
| CHEMBL1813256 | — | IC50 | = | 43.25 | nM | 7.36 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 65.5 | nM | 7.18 |