Assay Detail
Binding
CHEMBL1027683
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of chymotrypsin-like activity of human 20s proteasome beta 5 subunit assessed as hydrolysis of fluorogenic substrate
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis, biological evaluation, and structure-activity relationship (SAR) discussion of dipeptidyl boronate proteasome inhibitors, part I: comprehensive understanding of the SAR of alpha-amino acid boronates.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 8.17 | 9.12 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL446130 | — | — | 1 | 9.12 |
| CHEMBL506562 | — | — | 1 | 8.95 |
| CHEMBL503813 | — | — | 1 | 8.94 |
| CHEMBL451354 | — | — | 1 | 8.94 |
| CHEMBL1169561 | — | — | 1 | 8.94 |
| CHEMBL499361 | — | — | 1 | 8.92 |
| CHEMBL472257 | — | — | 1 | 8.90 |
| CHEMBL1169560 | — | — | 1 | 8.87 |
| CHEMBL510808 | — | — | 1 | 8.84 |
| CHEMBL499504 | — | — | 1 | 8.80 |
| CHEMBL501663 | — | — | 1 | 8.72 |
| CHEMBL499581 | — | — | 1 | 8.72 |
| CHEMBL325041 | BORTEZOMIB | 3.0 | 1 | 8.72 |
| CHEMBL520016 | — | — | 1 | 8.63 |
| CHEMBL454027 | — | — | 1 | 8.61 |
| CHEMBL490471 | — | — | 1 | 8.56 |
| CHEMBL448833 | — | — | 1 | 8.49 |
| CHEMBL445552 | — | — | 1 | 8.48 |
| CHEMBL505554 | — | — | 1 | 8.47 |
| CHEMBL506549 | — | — | 1 | 8.44 |
| CHEMBL502598 | — | — | 1 | 8.38 |
| CHEMBL499743 | — | — | 1 | 8.37 |
| CHEMBL499083 | — | — | 1 | 8.36 |
| CHEMBL508194 | — | — | 1 | 8.31 |
| CHEMBL504464 | — | — | 1 | 8.29 |
| CHEMBL454503 | — | — | 1 | 8.28 |
| CHEMBL504301 | — | — | 1 | 8.21 |
| CHEMBL451526 | — | — | 1 | 8.17 |
| CHEMBL502349 | — | — | 1 | 8.16 |
| CHEMBL449261 | — | — | 1 | 8.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL446130 | — | IC50 | = | 0.76 | nM | 9.12 |
| CHEMBL506562 | — | IC50 | = | 1.12 | nM | 8.95 |
| CHEMBL451354 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL1169561 | — | IC50 | = | 1.16 | nM | 8.94 |
| CHEMBL503813 | — | IC50 | = | 1.15 | nM | 8.94 |
| CHEMBL499361 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL472257 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL1169560 | — | IC50 | = | 1.34 | nM | 8.87 |
| CHEMBL510808 | — | IC50 | = | 1.46 | nM | 8.84 |
| CHEMBL499504 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL325041 | BORTEZOMIB | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL499581 | — | IC50 | = | 1.92 | nM | 8.72 |
| CHEMBL501663 | — | IC50 | = | 1.92 | nM | 8.72 |
| CHEMBL520016 | — | IC50 | = | 2.34 | nM | 8.63 |
| CHEMBL454027 | — | IC50 | = | 2.46 | nM | 8.61 |
| CHEMBL490471 | — | IC50 | = | 2.73 | nM | 8.56 |
| CHEMBL448833 | — | IC50 | = | 3.21 | nM | 8.49 |
| CHEMBL445552 | — | IC50 | = | 3.34 | nM | 8.48 |
| CHEMBL505554 | — | IC50 | = | 3.37 | nM | 8.47 |
| CHEMBL506549 | — | IC50 | = | 3.67 | nM | 8.44 |
| CHEMBL502598 | — | IC50 | = | 4.18 | nM | 8.38 |
| CHEMBL499743 | — | IC50 | = | 4.26 | nM | 8.37 |
| CHEMBL499083 | — | IC50 | = | 4.37 | nM | 8.36 |
| CHEMBL508194 | — | IC50 | = | 4.85 | nM | 8.31 |
| CHEMBL504464 | — | IC50 | = | 5.17 | nM | 8.29 |
| CHEMBL454503 | — | IC50 | = | 5.24 | nM | 8.28 |
| CHEMBL504301 | — | IC50 | = | 6.12 | nM | 8.21 |
| CHEMBL451526 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL502349 | — | IC50 | = | 6.96 | nM | 8.16 |
| CHEMBL449261 | — | IC50 | = | 7.63 | nM | 8.12 |
| CHEMBL483963 | — | IC50 | = | 8.46 | nM | 8.07 |
| CHEMBL496682 | — | IC50 | = | 9.19 | nM | 8.04 |
| CHEMBL446964 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL490668 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL447614 | — | IC50 | = | 17.2 | nM | 7.76 |
| CHEMBL508062 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL464408 | — | IC50 | = | 41.2 | nM | 7.38 |
| CHEMBL521004 | — | IC50 | = | 49.5 | nM | 7.30 |
| CHEMBL446922 | — | IC50 | = | 114.0 | nM | 6.94 |
| CHEMBL490669 | — | IC50 | = | 120.2 | nM | 6.92 |
| CHEMBL490874 | — | IC50 | = | 471.0 | nM | 6.33 |
| CHEMBL524664 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL498735 | — | IC50 | = | 2290.0 | nM | 5.64 |