Target
Procathepsin L
Ligand
BDBM19855
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
503±80 nM
EC50
48±15 nM
Citation
 Falgueyret, JPDesmarais, SOballa, RBlack, WCCromlish, WKhougaz, KLamontagne, SMassé, FRiendeau, DToulmond, SPercival, 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:
BDBM19855
Synonyms:
N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl) | CHEMBL371064 | basic piperazine-containing compound, 10 | N-{1-[(cyanomethyl)carbamoyl]cyclohexyl}-4-(4-propylpiperazin-1-yl)benzamide | Balicatib
Type:
Small organic molecule
Emp. Form.:
C23H33N5O2
Mol. Mass.:
411.26
SMILES:
CCCN1CCN(CC1)c1ccc(cc1)C(=O)NC1(CCCCC1)C(=O)NCC#N
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: