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Compound Detail

CHEMBL270515

DELANZOMIB
🧪 Phase II
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🧪 Phase II
CC(C)C[C@H](NC(=O)[C@@H](NC(=O)c1cccc(-c2ccccc2)n1)[C@@H](C)O)B(O)O
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL270515
Name DELANZOMIB
Phase Phase II
Structure Type MOL
InChI Key SJFBTAPEPRWNKH-CCKFTAQKSA-N

Known Names

CEP 18770 CEP-18770 CIP 18770 CIP-18770 CT 47098 CT-47098 Delanzomib NPH 007098 NPH-007098 NPH007098
13
Targets
24
Activities
2
Assay Types
18
PK Parameters
20
Publications
10
Known Names
1
Indications

Molecular Properties

413.3
MW (Da)

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product
USAN Stem -zomib

Extended Properties

Molecular Formula C21H28BN3O5
MW 413.28

Indications

Multiple Myeloma

Activity Summary

IC50 22 meas. best 9.0
EC50 2 meas. best 7.87

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Proteasome subunit beta type-9
CHEMBL1944495
 IC50 9.0 9.0 1.0 1
Proteasome Macropain subunit MB1
CHEMBL4662
 IC50 8.82 8.6 1.5 3
Proteasome subunit beta type-8
CHEMBL5620
 IC50 8.52 8.52 3.0 1
Unchecked
CHEMBL612545
 IC50 8.42 6.9833 3.8 6
Proteasome subunit beta type-10
CHEMBL3317334
 IC50 8.0 8.0 10.0 1
Cathepsin G
CHEMBL4071
 EC50 7.87 7.87 13.5 1
Unchecked
CHEMBL612545
 EC50 7.87 7.87 13.5 1
Cathepsin G
CHEMBL4071
 IC50 7.86 6.77 13.7 2
A2780
CHEMBL614004
 IC50 7.86 7.86 13.7 1
Proteasome component C5
CHEMBL4208
 IC50 7.51 7.51 31.0 1
SARS-CoV-2
CHEMBL4303835
 IC50 5.89 5.89 1300.0 2
Cytochrome P450 3A4
CHEMBL340
 IC50 5.46 5.46 3500.0 1
Proteasome Macropain subunit
CHEMBL3492
 IC50 5.46 5.46 3500.0 1
Neutrophil elastase
CHEMBL248
 IC50 5.45 5.45 3550.0 1
Chymase
CHEMBL4068
 IC50 5.45 5.45 3530.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1030.0 ng.hr.mL-1 Rattus norvegicus
AUC 2910.0 ng.hr.mL-1 Mus musculus
AUC 2200.0 ng.hr.mL-1 Rattus norvegicus
AUC 2850.0 ng.hr.mL-1 Mus musculus
CL 3.167 mL.min-1.kg-1 Rattus norvegicus
CL 23.33 mL.min-1.kg-1 Mus musculus
F 54.0 % Rattus norvegicus
F 39.0 % Mus musculus
F 54.0 % Rattus norvegicus
F 39.0 % Mus musculus
T1/2 71.0 hr Rattus norvegicus
T1/2 86.0 hr Rattus norvegicus
T1/2 15.0 hr Mus musculus
T1/2 53.0 hr Mus musculus
T1/2 0.6667 hr Mus musculus
T1/2 0.25 hr Rattus norvegicus
T1/2 0.6667 hr Canis lupus familiaris
T1/2 0.6667 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Proteasome subunit beta type-9 IC50 = 1.0 nM 9.0 Inhibition of 20S proteasome beta 1i (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome Macropain subunit MB1 IC50 = 1.5 nM 8.82 Inhibition of beta5 proteasome (unknown origin) 33656892
Proteasome Macropain subunit MB1 IC50 = 3.0 nM 8.52 Inhibition of 20S proteasome beta 5c (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome subunit beta type-8 IC50 = 3.0 nM 8.52 Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence... 31521028
Proteasome Macropain subunit MB1 IC50 = 3.5 nM 8.46 Reversible inhibition of human erythrocyte derived 20S proteasome subunit beta5 ... 22978849
Unchecked IC50 = 3.8 nM 8.42 Inhibition of chymotrypsin-like activity of human erythrocyte 20S proteasome 18247547
Unchecked IC50 = 10.0 nM 8.0 Inhibition of chymotrypsin-like activity of 20S proteasome in rabbit 20S proteas... 28642029
Proteasome subunit beta type-10 IC50 = 10.0 nM 8.0 Inhibition of 20S proteasome beta 2i (unknown origin) after 1 hr by fluorescence... 31521028
Cathepsin G EC50 = 13.5 nM 7.87 Inhibition of cathepsin G in human MOLT4 cells 20925433
Unchecked EC50 = 13.5 nM 7.87 Inhibition of chymotrypsin-like activity of human 20S proteasome in Molt4 cells 18247547
A2780 IC50 = 13.7 nM 7.86 Cytotoxicity against human A2780 cells 18247547
Cathepsin G IC50 = 13.7 nM 7.86 Inhibition of cathepsin G 20925433
Proteasome component C5 IC50 = 31.0 nM 7.51 Inhibition of 20S proteasome beta 1c (unknown origin) after 1 hr by fluorescence... 31521028
Unchecked IC50 = 59.0 nM 7.23 Inhibition of caspase-like activity of 20S proteasome in rabbit 20S proteasome p... 28642029
Unchecked IC50 = 70.0 nM 7.16 Inhibition of caspase-like activity of proteasome (unknown origin) 24524217
SARS-CoV-2 IC50 = 1300.0 nM 5.89 Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity o... -
SARS-CoV-2 IC50 = 1300.0 nM 5.89 Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity o... -
Unchecked IC50 = 1500.0 nM 5.82 Inhibition of bovine alpha chymotrypsin 18247547
Cathepsin G IC50 = 2110.0 nM 5.68 Inhibition of human cathepsin G 18247547
Cytochrome P450 3A4 IC50 = 3500.0 nM 5.46 Inhibition of human recombinant CYP3A4 18247547

Literature References

PubMed DOI Target Context # Activities
18247547 10.1021/jm7010589 Unchecked 9
18247547 10.1021/jm7010589 Mus musculus 8
18247547 10.1021/jm7010589 Rattus norvegicus 7
- 10.6019/CHEMBL4495565 SARS-CoV-2 4
18247547 10.1021/jm7010589 Plasma 4
18247547 10.1021/jm7010589 Neutrophil elastase 2
18247547 10.1021/jm7010589 Chymase 2
18247547 10.1021/jm7010589 Liver 2
- 10.6019/CHEMBL4495565 ADMET 2
18247547 10.1021/jm7010589 Liver microsomes 2
28642029 10.1016/j.bmc.2017.06.011 Unchecked 2
18247547 10.1021/jm7010589 Cathepsin G 2
- 10.6019/CHEMBL4495565 Vero C1008 2
20925433 10.1021/jm100189a Cathepsin G 2
18247547 10.1021/jm7010589 Cathepsin D 1
18247547 10.1021/jm7010589 Dipeptidyl peptidase 1 1
18247547 10.1021/jm7010589 Cathepsin B 1
- 10.6019/EOS300108 HepG2 1
18247547 10.1021/jm7010589 Cytochrome P450 1A2 1
18247547 10.1021/jm7010589 Cytochrome P450 2C19 1

Data from ChEMBL 36 via Core Engine