Assay Detail
Binding
CHEMBL4411752
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Inhibition of 20S proteosome beta 2 in human MOLT4 cells by ELISA
12
Total Activities
12
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
Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.33 | 7.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4465456 | — | — | 1 | 7.09 |
| CHEMBL4452892 | — | — | 1 | 6.38 |
| CHEMBL4297468 | ZETOMIPZOMIB | 2.0 | 1 | 6.22 |
| CHEMBL3237875 | — | — | 1 | 6.03 |
| CHEMBL4443505 | — | — | 1 | 5.93 |
| CHEMBL3319482 | — | — | 1 | - |
| CHEMBL4566534 | — | — | 1 | - |
| CHEMBL3319584 | — | — | 1 | - |
| CHEMBL4464640 | — | — | 1 | - |
| CHEMBL4454809 | — | — | 1 | - |
| CHEMBL4550864 | — | — | 1 | - |
| CHEMBL4441524 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4465456 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4452892 | — | IC50 | = | 413.0 | nM | 6.38 |
| CHEMBL4297468 | ZETOMIPZOMIB | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL3237875 | — | IC50 | = | 927.0 | nM | 6.03 |
| CHEMBL4443505 | — | IC50 | = | 1176.0 | nM | 5.93 |
| CHEMBL3319482 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4566534 | — | IC50 | - | — | - | |
| CHEMBL3319584 | — | IC50 | - | — | - | |
| CHEMBL4464640 | — | IC50 | - | — | - | |
| CHEMBL4454809 | — | IC50 | > | 25000.0 | nM | - |
| CHEMBL4550864 | — | IC50 | - | — | - | |
| CHEMBL4441524 | — | IC50 | > | 25000.0 | nM | - |