Assay Detail
Binding
CHEMBL4233071
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin-like activity of human 20S proteasome using Suc-Leu-Leu-Val-Tyr-AMC as substrate incubated for 10 mins followed by substrate addition measured after 1 hr by spectrofluorimetric method
26
Total Activities
26
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
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 | 26 | 7.84 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4249022 | — | — | 1 | 8.70 |
| CHEMBL4246480 | — | — | 1 | 8.64 |
| CHEMBL4238198 | — | — | 1 | 8.49 |
| CHEMBL4246864 | — | — | 1 | 8.45 |
| CHEMBL4241473 | — | — | 1 | 8.38 |
| CHEMBL4251272 | — | — | 1 | 8.32 |
| CHEMBL4245244 | — | — | 1 | 8.28 |
| CHEMBL4238378 | — | — | 1 | 8.23 |
| CHEMBL4248209 | — | — | 1 | 8.17 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.15 |
| CHEMBL2141296 | IXAZOMIB | 3.0 | 1 | 8.11 |
| CHEMBL4243375 | — | — | 1 | 8.09 |
| CHEMBL4242666 | — | — | 1 | 8.09 |
| CHEMBL1813256 | — | — | 1 | 8.07 |
| CHEMBL4249503 | — | — | 1 | 8.05 |
| CHEMBL4249917 | — | — | 1 | 7.89 |
| CHEMBL4238931 | — | — | 1 | 7.69 |
| CHEMBL4248689 | — | — | 1 | 7.67 |
| CHEMBL4246922 | — | — | 1 | 7.57 |
| CHEMBL4243132 | — | — | 1 | 7.56 |
| CHEMBL4249453 | — | — | 1 | 7.51 |
| CHEMBL4239365 | — | — | 1 | 7.37 |
| CHEMBL4250217 | — | — | 1 | 7.13 |
| CHEMBL1813227 | — | — | 1 | 6.52 |
| CHEMBL4244424 | — | — | 1 | 6.41 |
| CHEMBL4245648 | — | — | 1 | 6.23 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4249022 | — | IC50 | = | 1.98 | nM | 8.70 |
| CHEMBL4246480 | — | IC50 | = | 2.31 | nM | 8.64 |
| CHEMBL4238198 | — | IC50 | = | 3.22 | nM | 8.49 |
| CHEMBL4246864 | — | IC50 | = | 3.53 | nM | 8.45 |
| CHEMBL4241473 | — | IC50 | = | 4.16 | nM | 8.38 |
| CHEMBL4251272 | — | IC50 | = | 4.82 | nM | 8.32 |
| CHEMBL4245244 | — | IC50 | = | 5.26 | nM | 8.28 |
| CHEMBL4238378 | — | IC50 | = | 5.89 | nM | 8.23 |
| CHEMBL4248209 | — | IC50 | = | 6.74 | nM | 8.17 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 7.04 | nM | 8.15 |
| CHEMBL2141296 | IXAZOMIB | IC50 | = | 7.73 | nM | 8.11 |
| CHEMBL4243375 | — | IC50 | = | 8.21 | nM | 8.09 |
| CHEMBL4242666 | — | IC50 | = | 8.11 | nM | 8.09 |
| CHEMBL1813256 | — | IC50 | = | 8.44 | nM | 8.07 |
| CHEMBL4249503 | — | IC50 | = | 8.86 | nM | 8.05 |
| CHEMBL4249917 | — | IC50 | = | 12.89 | nM | 7.89 |
| CHEMBL4238931 | — | IC50 | = | 20.44 | nM | 7.69 |
| CHEMBL4248689 | — | IC50 | = | 21.17 | nM | 7.67 |
| CHEMBL4246922 | — | IC50 | = | 26.79 | nM | 7.57 |
| CHEMBL4243132 | — | IC50 | = | 27.75 | nM | 7.56 |
| CHEMBL4249453 | — | IC50 | = | 30.78 | nM | 7.51 |
| CHEMBL4239365 | — | IC50 | = | 42.79 | nM | 7.37 |
| CHEMBL4250217 | — | IC50 | = | 74.86 | nM | 7.13 |
| CHEMBL1813227 | — | IC50 | = | 303.8 | nM | 6.52 |
| CHEMBL4244424 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL4245648 | — | IC50 | = | 593.7 | nM | 6.23 |