Found 6 hits Enz. Inhib. hit(s) with Target = 'Proteasome subunit beta type-8' and Ligand = 'BDBM50277889' Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 3.20 | n/a | n/a | n/a | n/a | n/a | n/a |
TBA
| |
Citation and Details
Article DOI: 10.1021/acs.jmedchem.1c00604 BindingDB Entry DOI: 10.7270/Q200064W |
More data for this Ligand-Target Pair | |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 14 | n/a | n/a | n/a | n/a | n/a | n/a |
Proteolix, Inc.
Curated by ChEMBL
| Assay Description Inhibition of chymotrypsin-like activity of LMP7 immunoproteasome by proteasome active site ELISA |
J Med Chem 52: 3028-38 (2009)
Article DOI: 10.1021/jm801329v BindingDB Entry DOI: 10.7270/Q2ZW1KS0 |
More data for this Ligand-Target Pair | |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 27 | n/a | n/a | n/a | n/a | n/a | n/a |
Zhejiang University
Curated by ChEMBL
| Assay Description Inhibition of 20S immunoproteasome LMP7 (unknown origin) using Ac-ANW-AMC as substrate preincubated for 15 mins followed by substrate addition by flu... |
Eur J Med Chem 161: 543-558 (2019)
Article DOI: 10.1016/j.ejmech.2018.10.056 BindingDB Entry DOI: 10.7270/Q2QF8X4M |
More data for this Ligand-Target Pair | |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 33 | n/a | n/a | n/a | n/a | n/a | n/a |
Hangzhou Xixi Hospital
Curated by ChEMBL
| Assay Description Inhibition of 20S proteasome beta 5i (unknown origin) after 1 hr by fluorescence based assay |
Eur J Med Chem 182: (2019)
Article DOI: 10.1016/j.ejmech.2019.111646 BindingDB Entry DOI: 10.7270/Q2154MHB |
More data for this Ligand-Target Pair | |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 33 | n/a | n/a | n/a | n/a | n/a | n/a |
New Mexico Institute of Mining and Technology
Curated by ChEMBL
| Assay Description Inhibition of human immunoproteasome beta5 subunit using Suc-RLR-AMC as substrate pretreated for 30 mins followed by substrate addition and measured ... |
Eur J Med Chem 157: 962-977 (2018)
Article DOI: 10.1016/j.ejmech.2018.08.052 BindingDB Entry DOI: 10.7270/Q2028V7T |
More data for this Ligand-Target Pair | |
Proteasome subunit beta type-8
(Homo sapiens (Human)) | BDBM50277889
(CARFILZOMIB | CHEMBL451887)Show SMILES CC(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 |r| Show InChI InChI=1S/C40H57N5O7/c1-27(2)22-32(36(47)40(5)26-52-40)42-39(50)34(24-30-14-10-7-11-15-30)44-38(49)33(23-28(3)4)43-37(48)31(17-16-29-12-8-6-9-13-29)41-35(46)25-45-18-20-51-21-19-45/h6-15,27-28,31-34H,16-26H2,1-5H3,(H,41,46)(H,42,50)(H,43,48)(H,44,49)/t31-,32-,33-,34-,40+/m0/s1 | PDB
Reactome pathway KEGG
UniProtKB/SwissProt
B.MOAD DrugBank GoogleScholar AffyNet
| Purchase
CHEMBL DrugBank MCE PC cid PC sid UniChem
Patents
Similars
| DrugBank Article PubMed
| n/a | n/a | 34 | n/a | n/a | n/a | n/a | n/a | n/a |
Hangzhou Institute of Innovative Medicine
Curated by ChEMBL
| Assay Description Inhibition of human 20s immunoproteasome beta5i activity using Suc-LLVY-AMC as substrate preincubated for 15 mins followed by substrate addition |
Eur J Med Chem 164: 602-614 (2019)
Article DOI: 10.1016/j.ejmech.2018.12.064 BindingDB Entry DOI: 10.7270/Q2JM2F38 |
More data for this Ligand-Target Pair | |