Reaction Details Report a problem with these data
Target
Procathepsin L
Ligand
BDBM19856
Substrate
BDBM19480
Meas. Tech.
Enzyme Inhibition Assay and Whole Cell Enzyme Occupancy Assay
pH
5.5000±n/a
Temperature
295.1500±n/a K
IC50
2600±250 nM
EC50
320±170 nM
Citation
 Falgueyret, JP; Desmarais, S; Oballa, R; Black, WC; Cromlish, W; Khougaz, K; Lamontagne, S; Massé, F; Riendeau, D; Toulmond, S; Percival, MD Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem 48:7535-43 (2005) [PubMed]  Article 
Target
Name:
Procathepsin L
Synonyms:
Cathepsin L1 | Cathepsin L | Cathepsin L1 heavy chain | Cathepsin L1 light chain | MEP | Major excreted protein | cathepsin L preproprotein | CTSL CTSL1 | CATL1_HUMAN | CTSL | CTSL1
Type:
Enzyme
Mol. Mass.:
37557.19
Organism:
Human
Description:
Purchased from Calbiochem (San Diego, CA).
Residue:
333
Sequence:
MNPTLILAAFCLGIASATLTFDHSLEAQWTKWKAMHNRLYGMNEEGWRRAVWEKNMKMIELHNQEYREGKHSFTMAMNAFGDMTSEEFRQVMNGFQNRKPRKGKVFQEPLFYEAPRSVDWREKGYVTPVKNQGQCGSCWAFSATGALEGQMFRKTGRLISLSEQNLVDCSGPQGNEGCNGGLMDYAFQYVQDNGGLDSEESYPYEATEESCKYNPKYSVANDTGFVDIPKQEKALMKAVATVGPISVAIDAGHESFLFYKEGIYFEPDCSSEDMDHGVLVVGYGFESTESDNNKYWLVKNSWGEEWGMGGYVKMAKDRRNHCGIASAASYPTV
  
Inhibitor
Name:
BDBM19856
Synonyms:
(2R)-N-(cyanomethyl)-4-methyl-2-{3-[4-(piperazin-1-yl)phenyl]phenyl}pentanamide | JMC463709 (R)-2 | CHEMBL184514 | piperazine-containing compound, 11
Type:
Small organic molecule
Emp. Form.:
C24H30N4O
Mol. Mass.:
390.24
SMILES:
CC(C)C[C@@H](C(=O)NCC#N)c1cccc(c1)-c1ccc(cc1)N1CCNCC1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM19480
Synonyms:
Fluorogenic substrate | Z-Leu-Arg-AMC | Cbz-Leu-Arg-AMC
Type:
n/a
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: