Compound Detail
CHEMBL3545432
IXAZOMIB CITRATE 💊 Approved Drug
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💊 Approved Drug
CC(C)C[C@H](NC(=O)CNC(=O)c1cc(Cl)ccc1Cl)B1OC(=O)C(CC(=O)O)(CC(=O)O)O1
Basic Information
| ChEMBL ID | CHEMBL3545432 |
| Name | IXAZOMIB CITRATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | MBOMYENWWXQSNW-AWEZNQCLSA-N |
| Therapeutic | ✓ Yes |
| Active Moiety | CHEMBL2141296 |
2
Targets
4
Activities
2
Assay Types
0
PK Parameters
7
Publications
4
Known Names
15
Indications
1
Mechanisms
Molecular Properties
517.1
MW (Da)
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2015 |
| Availability | Prescription |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| 26S proteasome inhibitor | INHIBITOR | 26S proteasome | ✓ | ✓ |
Indications
Multiple Myeloma Bronchiolitis Obliterans Syndrome Leukemia, Plasma Cell Lymphoma Lymphoma, Mantle-Cell Plasmacytoma Sarcoma, Kaposi Waldenstrom Macroglobulinemia Amyloidosis, Familial Breast Neoplasms Leukemia, Myeloid, Acute Neoplasms Precursor Cell Lymphoblastic Leukemia-Lymphoma Precursor Cell Lymphoblastic Leukemia-Lymphoma Glioblastoma
Activity Summary
IC50 3 meas. best 8.47
Ki 1 meas. best 9.03
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Proteasome Macropain subunit MB1 CHEMBL4662 | Ki | 9.03 | 9.03 | 0.9 | 1 |
| Proteasome Macropain subunit MB1 CHEMBL4662 | IC50 | 8.47 | 8.47 | 3.4 | 1 |
| Unchecked CHEMBL612545 | IC50 | 7.51 | 6.485 | 31.0 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Proteasome Macropain subunit MB1 | Ki | = | 0.93 | nM | 9.03 | Binding affinity to 20s proteasome beta5 site (unknown origin) mediated chymotry... | 37210838 |
| Proteasome Macropain subunit MB1 | IC50 | = | 3.4 | nM | 8.47 | Inhibition of 20s proteasome beta5 site (unknown origin) mediated chymotrypsin-l... | 37210838 |
| Unchecked | IC50 | = | 31.0 | nM | 7.51 | Inhibition of 20s proteasome beta1 (unknown origin) mediated chymotrypsin-like a... | 37210838 |
| Unchecked | IC50 | = | 3500.0 | nM | 5.46 | Inhibition of 20s proteasome beta2 (unknown origin) mediated chymotrypsin-like a... | 37210838 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37210838 | 10.1016/j.ejmech.2023.115492 | Proteasome Macropain subunit MB1 | 2 |
| 37210838 | 10.1016/j.ejmech.2023.115492 | Unchecked | 2 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.1101/2020.04.21.054387 | SARS-CoV-2 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
Data from ChEMBL 36 via Core Engine