Molecule Details
InChIKeyBLMPQMFVWMYDKT-NZTKNTHTSA-N
Compound NameCarfilzomib
Canonical SMILESCC(C)C[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)CN1CCOCC1)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)[C@@]1(C)CO1
Clinical Status Data-mined Candidate
Targets (Human+Pathogen)43
Pfam Stratification Cross-Family
Avg pChEMBL7.82
SourceChEMBL;BindingDB
2D Structure
2D structure
Activity Profile
DrugBank Annotations
DrugBank ID DB08889
Drug NameCarfilzomib
CAS Number868540-17-4
Groups approved investigational
ATC Codes L01XG02
DescriptionCarfilzomib is an injectable antineoplastic agent (IV only). Chemically, it is a modified tetrapeptidyl epoxide and an analog of epoxomicin. It is also a selective proteasome inhibitor. FDA approved carfilzomib in July 2012 for the treatment of adults with relapsed or refractory multiple myeloma as ...

Categories: Amino Acids, Peptides, and Proteins Antineoplastic Agents Antineoplastic and Immunomodulating Agents Immunosuppressive Agents Myelosuppressive Agents Narrow Therapeutic Index Drugs P-glycoprotein inhibitors P-glycoprotein substrates P-glycoprotein substrates with a Narrow Therapeutic Index Peptides Proteasome Inhibitors
Cross-references: BindingDB: 50277889 ChEBI: 65347 CHEMBL451887 ChemSpider: 9731489 Drugs Product Database (DPD): 22678 D08880 PharmGKB: PA166165203 PubChem:11556711 PubChem:175427135 RxCUI: 1302966 Wikipedia: Carfilzomib ZINC: ZINC000049841054
Target Activities (43)
Target Gene Organism Category Pfam pChEMBL Type Source
P28074 PSMB5 Homo sapiens Human PF00227 8.1 IC50 ChEMBL;BindingDB
A5LHX3 PSMB11 Homo sapiens Human PF00227 8.1 IC50 ChEMBL
O00231 PSMD11 Homo sapiens Human PF01399 PF18503 PF18055 8.1 IC50 ChEMBL
O00232 PSMD12 Homo sapiens Human PF01399 PF22241 PF18098 8.1 IC50 ChEMBL
O00487 PSMD14 Homo sapiens Human PF01398 PF23594 8.1 IC50 ChEMBL
O14818 PSMA7 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
O43242 PSMD3 Homo sapiens Human PF01399 PF08375 PF25573 8.1 IC50 ChEMBL
P17980 PSMC3 Homo sapiens Human PF00004 PF17862 PF16450 8.1 IC50 ChEMBL
P20618 PSMB1 Homo sapiens Human PF00227 8.1 IC50 ChEMBL
P25786 PSMA1 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P25787 PSMA2 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P25788 PSMA3 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P25789 PSMA4 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P28066 PSMA5 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P28070 PSMB4 Homo sapiens Human PF00227 8.1 IC50 ChEMBL
P35998 PSMC2 Homo sapiens Human PF00004 PF17862 PF21236 8.1 IC50 ChEMBL
P43686 PSMC4 Homo sapiens Human PF00004 PF17862 PF16450 8.1 IC50 ChEMBL
P48556 PSMD8 Homo sapiens Human PF10075 8.1 IC50 ChEMBL
P49720 PSMB3 Homo sapiens Human PF00227 8.1 IC50 ChEMBL
P51665 PSMD7 Homo sapiens Human PF01398 PF13012 8.1 IC50 ChEMBL
P55036 PSMD4 Homo sapiens Human PF02809 PF13519 8.1 IC50 ChEMBL
P60896 SEM1 Homo sapiens Human PF05160 8.1 IC50 ChEMBL
P60900 PSMA6 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
P62191 PSMC1 Homo sapiens Human PF00004 PF17862 PF16450 8.1 IC50 ChEMBL
P62195 PSMC5 Homo sapiens Human PF00004 PF17862 PF16450 8.1 IC50 ChEMBL
P62333 PSMC6 Homo sapiens Human PF00004 PF17862 PF16450 8.1 IC50 ChEMBL
Q13200 PSMD2 Homo sapiens Human PF01851 PF18051 PF17781 8.1 IC50 ChEMBL
Q15008 PSMD6 Homo sapiens Human PF01399 PF10602 PF21154 8.1 IC50 ChEMBL
Q16186 ADRM1 Homo sapiens Human PF04683 PF16550 8.1 IC50 ChEMBL
Q8TAA3 PSMA8 Homo sapiens Human PF00227 PF10584 8.1 IC50 ChEMBL
Q99436 PSMB7 Homo sapiens Human PF12465 PF00227 8.1 IC50 ChEMBL;BindingDB
Q99460 PSMD1 Homo sapiens Human PF13646 PF01851 PF18004 PF21505 8.1 IC50 ChEMBL
Q9UNM6 PSMD13 Homo sapiens Human PF01399 PF22037 8.1 IC50 ChEMBL
P28065 PSMB9 Homo sapiens Human PF00227 7.9 IC50 ChEMBL
P28072 PSMB6 Homo sapiens Human PF00227 7.9 IC50 ChEMBL
P40306 PSMB10 Homo sapiens Human PF12465 PF00227 7.8 IC50 ChEMBL;BindingDB
P28062 PSMB8 Homo sapiens Human PF00227 7.6 IC50 ChEMBL;BindingDB
P78417 GSTO1 Homo sapiens Human PF14497 PF13409 6.8 IC50 ChEMBL;BindingDB
P49721 PSMB2 Homo sapiens Human PF00227 6.7 IC50 ChEMBL;BindingDB
P08684 CYP3A4 Homo sapiens Human PF00067 6.3 IC50 ChEMBL
P20815 CYP3A5 Homo sapiens Human PF00067 6.3 IC50 ChEMBL
P24462 CYP3A7 Homo sapiens Human PF00067 6.3 IC50 ChEMBL
Q9HB55 CYP3A43 Homo sapiens Human PF00067 6.3 IC50 ChEMBL
DrugBank Target Actions (8)
Target Gene Target Name Action Type
P20618 PSMB1 Proteasome subunit beta type-1 inhibitor targets
P28062 PSMB8 Proteasome subunit beta type-8 inhibitor targets
P28065 PSMB9 Proteasome subunit beta type-9 inhibitor targets
P28074 PSMB5 Proteasome subunit beta type-5 inhibitor targets
P40306 PSMB10 Proteasome subunit beta type-10 inhibitor targets
P49721 PSMB2 Proteasome subunit beta type-2 inhibitor targets
P08183 ABCB1 ATP-dependent translocase ABCB1 inhibitor transporters
P08183 ABCB1 ATP-dependent translocase ABCB1 substrate transporters