Reaction Details Report a problem with these data
Target
Macrophage metalloelastase
Ligand
BDBM224012
Substrate
n/a
Meas. Tech.
MMP Activity Assay
pH
7.5±0
Temperature
310.15±0 K
IC50
>5.0e+4±n/a nM
Citation
 Li, J; Yakushi, T; Parlati, F; Mackinnon, AL; Perez, C; Ma, Y; Carter, KP; Colayco, S; Magnuson, G; Brown, B; Nguyen, K; Vasile, S; Suyama, E; Smith, LH; Sergienko, E; Pinkerton, AB; Chung, TDY; Palmer, AE; Pass, I; Hess, S; Cohen, SM; Deshaies, RJ Capzimin is a potent and specific inhibitor of proteasome isopeptidase Rpn11. Nat Chem Biol 13:486-493 (2017) [PubMed]  Article 
Target
Name:
Macrophage metalloelastase
Synonyms:
HME | MMP12 | MMP12_HUMAN | Matrix metalloproteinase 12 | Matrix metalloproteinase-12 (MMP 12) | Matrix metalloproteinase-12 (MMP-12) | Matrix metalloproteinase-12 (MMP12) | Matrix metalloproteinases 12 (MMP-12)
Type:
Enzyme
Mol. Mass.:
54012.99
Organism:
Homo sapiens (Human)
Description:
P39900
Residue:
470
Sequence:
MKFLLILLLQATASGALPLNSSTSLEKNNVLFGERYLEKFYGLEINKLPVTKMKYSGNLMKEKIQEMQHFLGLKVTGQLDTSTLEMMHAPRCGVPDVHHFREMPGGPVWRKHYITYRINNYTPDMNREDVDYAIRKAFQVWSNVTPLKFSKINTGMADILVVFARGAHGDFHAFDGKGGILAHAFGPGSGIGGDAHFDEDEFWTTHSGGTNLFLTAVHEIGHSLGLGHSSDPKAVMFPTYKYVDINTFRLSADDIRGIQSLYGDPKENQRLPNPDNSEPALCDPNLSFDAVTTVGNKIFFFKDRFFWLKVSERPKTSVNLISSLWPTLPSGIEAAYEIEARNQVFLFKDDKYWLISNLRPEPNYPKSIHSFGFPNFVKKIDAAVFNPRFYRTYFFVDNQYWRYDERRQMMDPGYPKLITKNFQGIGPKIDAVFYSKNKYYYFFQGSNQFEYDFLLQRITKTLKSNSWFGC
  
Inhibitor
Name:
BDBM224012
Synonyms:
Capzimin | US10005735, Compound 12
Type:
Small organic molecule
Emp. Form.:
C15H13N3OS2
Mol. Mass.:
315.413
SMILES:
Sc1cccc2cc(cnc12)C(=O)NCCc1nccs1
Structure:
Search PDB for entries with ligand similarity: