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Compound Detail

CHEMBL4297468

ZETOMIPZOMIB
🧪 Phase II
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🧪 Phase II
COc1ccc([C@@H](O)[C@H](NC(=O)[C@H](C)NC(=O)CN2CCOCC2)C(=O)N[C@@H](CC2=CCCC2)C(=O)[C@@]2(C)CO2)cc1
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL4297468
Name ZETOMIPZOMIB
Phase Phase II
Structure Type MOL
InChI Key GHYOCDFICYLMRF-UTIIJYGPSA-N

Known Names

Kzr-616 Zetomipzomib
11
Targets
19
Activities
1
Assay Types
0
PK Parameters
20
Publications
2
Known Names
8
Indications

Molecular Properties

586.7
MW (Da)
0.39
ALogP
9
HBA
4
HBD
158.8
PSA (Ų)
0.18
QED
1
Ro5 Violations
14
Rot. Bonds

Drug Information

Molecule Type Protein
Chirality Single Enantiomer
USAN Stem -zomib
USAN Year 2022

Extended Properties

Molecular Formula C30H42N4O8
MW 586.69
Aromatic Rings 1
Heavy Atoms 42
NP-Likeness -0.10

Indications

Anemia, Hemolytic, Autoimmune Dermatomyositis Hepatitis, Autoimmune Lupus Nephritis Polymyositis Purpura, Thrombocytopenic, Idiopathic Autoimmune Diseases Inflammation

Activity Summary

IC50 19 meas. best 9.88

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome subunit beta type-10
CHEMBL3317334
 IC50 9.88 8.045 0.1 2
Proteasome subunit beta type-9
CHEMBL1944495
 IC50 9.21 7.4467 0.6 3
Proteasome Macropain subunit
CHEMBL3492
 IC50 7.55 6.885 28.0 2
Proteasome subunit beta type-8
CHEMBL5620
 IC50 7.41 7.265 39.0 2
Proteasome subunit beta type-8
CHEMBL1944492
 IC50 7.24 7.24 57.0 1
Proteasome subunit beta type-9
CHEMBL1944491
 IC50 6.75 6.75 179.0 1
Proteasome component C5
CHEMBL4208
 IC50 6.37 6.37 430.0 1
Proteasome subunit beta type-5
CHEMBL1944494
 IC50 6.32 6.32 483.0 1
Proteasome subunit beta type-10
CHEMBL4523133
 IC50 6.28 6.28 522.0 1
Proteasome Macropain subunit MB1
CHEMBL4662
 IC50 6.16 6.15 688.0 2
Proteasome subunit beta type-2
CHEMBL3112378
 IC50 6.07 6.07 857.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteasome subunit beta type-10 IC50 = 0.131 nM 9.88 Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome subunit beta type-9 IC50 = 0.623 nM 9.21 Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome Macropain subunit IC50 = 28.0 nM 7.55 Inhibition of 20S proteasome beta 2c (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome subunit beta type-8 IC50 = 39.0 nM 7.41 Inhibition of LMP7 in human MOLT4 cells by ELISA 30380863
Proteasome subunit beta type-8 IC50 = 57.0 nM 7.24 Inhibition of LMP7 in mouse A20 cells by ELISA 30380863
Proteasome subunit beta type-8 IC50 = 75.0 nM 7.12 Inhibition of human LMP7 beta -5i subunit using Ac-ANW-AMC as substrate preincub... 38906067
Proteasome subunit beta type-9 IC50 = 131.0 nM 6.88 Inhibition of LMP2 in human MOLT4 cells by ELISA 30380863
Proteasome subunit beta type-9 IC50 = 179.0 nM 6.75 Inhibition of LMP2 in mouse A20 cells by ELISA 30380863
Proteasome component C5 IC50 = 430.0 nM 6.37 Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome subunit beta type-5 IC50 = 483.0 nM 6.32 Inhibition of 20S proteosome beta 5 in mouse A20 cells by ELISA 30380863
Proteasome subunit beta type-10 IC50 = 522.0 nM 6.28 Inhibition of MECL1 in mouse A20 cells by ELISA 30380863
Proteasome subunit beta type-9 IC50 = 557.0 nM 6.25 Inhibition of human LMP2 beta-1i subunit using Ac-PAL-AMC as substrate preincuba... 38906067
Proteasome Macropain subunit IC50 = 604.0 nM 6.22 Inhibition of 20S proteosome beta 2 in human MOLT4 cells by ELISA 30380863
Proteasome subunit beta type-10 IC50 = 623.0 nM 6.21 Inhibition of MECL1 in human MOLT4 cells by ELISA 30380863
Proteasome Macropain subunit MB1 IC50 = 688.0 nM 6.16 Inhibition of 20S proteosome beta 5 in human MOLT4 cells by ELISA 30380863
Proteasome Macropain subunit MB1 IC50 = 720.0 nM 6.14 Inhibition of human 20S proteosome beta5c subunit using Ac-WLA-AMC as substrate ... 38906067
Proteasome subunit beta type-2 IC50 = 857.0 nM 6.07 Inhibition of 20S proteosome beta 2 in mouse A20 cells by ELISA 30380863

Literature References

PubMed DOI Target Context # Activities
30380863 10.1021/acs.jmedchem.8b01201 PBMC 5
31521028 10.1016/j.ejmech.2019.111646 Unchecked 3
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-9 2
38906067 10.1016/j.bmc.2024.117790 Unchecked 2
30380863 10.1021/acs.jmedchem.8b01201 Mus musculus 2
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-10 2
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-8 2
30380863 10.1021/acs.jmedchem.8b01201 No relevant target 1
31521028 10.1016/j.ejmech.2019.111646 Proteasome subunit beta type-8 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome Macropain subunit MB1 1
31521028 10.1016/j.ejmech.2019.111646 Proteasome component C5 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome component C5 1
31521028 10.1016/j.ejmech.2019.111646 Proteasome Macropain subunit MB1 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome Macropain subunit 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-5 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-1 1
30380863 10.1021/acs.jmedchem.8b01201 Proteasome subunit beta type-2 1
31521028 10.1016/j.ejmech.2019.111646 Proteasome subunit beta type-10 1
31521028 10.1016/j.ejmech.2019.111646 Proteasome Macropain subunit 1
38906067 10.1016/j.bmc.2024.117790 Proteasome subunit beta type-8 1

Data from ChEMBL 36 via Core Engine