Compound Detail
CHEMBL5181539
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Basic Information
| ChEMBL ID | CHEMBL5181539 |
| Phase | Preclinical |
| Structure Type | MOL |
| InChI Key | AXRZDEGVEPTORD-KBPBESRZSA-N |
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names
Molecular Properties
303.1
MW (Da)
Drug Information
| Availability | Unknown |
| Chirality | Unknown |
Activity Summary
IC50 4 meas. best 6.72
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Proteasome subunit beta type-8 CHEMBL5620 | IC50 | 6.72 | 6.56 | 190.0 | 2 |
| Proteasome Macropain subunit MB1 CHEMBL4662 | IC50 | 4.82 | 4.72 | 15000.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Proteasome subunit beta type-8 | IC50 | = | 190.0 | nM | 6.72 | Inhibition of human 20S immunoproteasome beta-5i subunit using Suc-LLVY-AMC as s... | 34228444 |
| Proteasome subunit beta type-8 | IC50 | = | 400.0 | nM | 6.4 | Inhibition of 20S immunoproteasome beta-5i subunit in human PBMC using Ac-ANW-lu... | 34228444 |
| Proteasome Macropain subunit MB1 | IC50 | = | 15000.0 | nM | 4.82 | Inhibition of 20S proteasome beta5 subunit in human A549 cells using Suc-LLVY-lu... | 34228444 |
| Proteasome Macropain subunit MB1 | IC50 | = | 24000.0 | nM | 4.62 | Inhibition of human 20S proteasome beta5 subunit using Suc-LLVY-AMC as substrate... | 34228444 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 34228444 | 10.1021/acs.jmedchem.1c00604 | Proteasome subunit beta type-8 | 2 |
| 34228444 | 10.1021/acs.jmedchem.1c00604 | Proteasome Macropain subunit MB1 | 2 |
| 34228444 | 10.1021/acs.jmedchem.1c00604 | Unchecked | 2 |
| 34228444 | 10.1021/acs.jmedchem.1c00604 | ADMET | 2 |
| 34228444 | 10.1021/acs.jmedchem.1c00604 | No relevant target | 1 |
Data from ChEMBL 36 via Core Engine