bortezomib
A pyrazine and boronic acid derivative that functions as a reversible PROTEASOME INHIBITOR. It is used as an ANTINEOPLASTIC AGENT in the treatment of MULTIPLE MYELOMA and MANTLE CELL LYMPHOMA.
Ligand Summary
UNII: 69G8BD63PP
PubChem: 387447
Guide to Pharmacology: 6391
ChEMBL: CHEMBL325041
DrugCentral: 391
LyCHI: HBWAWX2HPNMG
Target Activities
PSMB5
Proteasome subunit beta type-5
28 Activities
Items per page:
1 – 10 of 28
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.7 | |||||
IC50 | 9.3 | Eur J Med Chem, (2018) 146:None:636 | ||||
Ki | 9.26 | MedChemComm, (2012) 3:6:710 | ||||
Ki | 9.22 | Eur. J. Med. Chem., (2013) 64:None:23 | ||||
IC50 | 8.72 | Bioorg. Med. Chem. Lett., (2016) 26:8:1958 | ||||
IC50 | 8.72 | Bioorg. Med. Chem., (2016) 24:11:2576 | ||||
IC50 | 8.7 | MedChemComm, (2012) 3:6:710 | ||||
IC50 | 8.41 | MedChemComm, (2012) 3:6:710 | ||||
IC50 | 8.4 | Eur J Med Chem, (2017) 125:None:925 | ||||
IC50 | 8.4 | Eur J Med Chem, (2017) 135:None:142 | ||||
PSMB1
Proteasome subunit beta type-1
10 Activities
Items per page:
1 – 10 of 10
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 7.72 | Eur J Med Chem, (2018) 146:None:636 | ||||
IC50 | 7.52 | Eur J Med Chem, (2017) 125:None:925 | ||||
IC50 | 7.52 | Bioorg Med Chem, (2017) 25:15:4031 | ||||
IC50 | 7.28 | J. Med. Chem., (2012) 55:23:10317 | ||||
IC50 | 7.16 | Eur J Med Chem, (2019) 182:None:111646 | ||||
IC50 | 7.01 | Bioorg Med Chem, (2018) 26:14:3975 | ||||
IC50 | 6.98 | Eur J Med Chem, (2019) 164:None:423 | ||||
IC50 | 6.89 | J. Med. Chem., (2013) 56:9:3689 | ||||
IC50 | 6.16 | Eur J Med Chem, (2018) 146:None:636 | ||||
IC50 | 7.28 | INHIBITOR | ||||
PSMB8
Proteasome subunit beta type-8
6 Activities
Items per page:
1 – 6 of 6
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.48 | Eur J Med Chem, (2019) 182:None:111646 | ||||
IC50 | 8.4 | Eur J Med Chem, (2019) 164:None:423 | ||||
IC50 | 8.1 | Eur J Med Chem, (2019) 164:None:602 | ||||
IC50 | 8.09 | J. Med. Chem., (2009) 52:9:3028 | ||||
IC50 | 7.11 | J. Med. Chem., (2014) 57:6:2726 | ||||
IC50 | 8.09 | INHIBITOR | ||||
PSMB2
Proteasome subunit beta type-2
5 Activities
Items per page:
1 – 5 of 5
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.89 | Eur J Med Chem, (2019) 164:None:602 | ||||
IC50 | 6.36 | Eur J Med Chem, (2017) 125:None:925 | ||||
IC50 | 6.36 | Bioorg Med Chem, (2017) 25:15:4031 | ||||
IC50 | 6.23 | J. Med. Chem., (2012) 55:23:10317 | ||||
IC50 | 6.23 | INHIBITOR | ||||
CTSG
Cathepsin G
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.28 | J. Med. Chem., (2008) 51:4:1068 | ||||
Ki | 6.2 | Bioorg. Med. Chem. Lett., (1998) 8:4:333 | ||||
Ki | 6.2 | |||||
PSMB9
Proteasome subunit beta type-9
3 Activities
Items per page:
1 – 3 of 3
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.52 | Eur J Med Chem, (2019) 164:None:423 | ||||
IC50 | 8.26 | Eur J Med Chem, (2019) 182:None:111646 | ||||
IC50 | 8.52 | |||||
CTRB1
Chymotrypsinogen B
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 6.5 | Bioorg. Med. Chem. Lett., (1998) 8:4:333 | ||||
Ki | 6.49 | |||||
PSMB10
Proteasome subunit beta type-10
2 Activities
Items per page:
1 – 2 of 2
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 6.03 | Eur J Med Chem, (2019) 182:None:111646 | ||||
IC50 | 6.03 | |||||
PSMA1
Proteasome subunit alpha type-1
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
Ki | 9.21 | INHIBITOR | ||||
NFKB2
Nuclear factor NF-kappa-B p100 subunit
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.01 | |||||
RELA
Transcription factor p65
1 Activities
Items per page:
1 – 1 of 1
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) | ||
|---|---|---|---|---|---|---|
IC50 | 8.01 | |||||