Target
Calpain-1 catalytic subunit
Ligand
BDBM23862
Substrate
BDBM23856
Meas. Tech.
mu-Calpain Inhibition Assay
pH
7.4±n/a
Temperature
295.15±n/a K
Ki
2150±20 nM
Citation
 Donkor, IOAssefa, HLiu, J Structural basis for the potent calpain inhibitory activity of peptidyl alpha-ketoacids. J Med Chem 51:4346-50 (2008) [PubMed]  Article 
Target
Name:
Calpain-1 catalytic subunit
Synonyms:
CAN1_PIG | CANP 1 | CAPN1 | Calcium-activated neutral proteinase 1 | Calpain 1 | Calpain mu-type | Calpain-1 | Calpain-1 catalytic subunit | Calpain-1 large subunit | Micromolar-calpain | muCANP
Type:
Catalytic subunit; forms a heterodimer with a small (regulatory) subunit (CAPNS1)
Mol. Mass.:
81729.82
Organism:
Sus scrofa (pig)
Description:
Native calpain-1 from porcine erythrocytes, purchased from Calbiochem, was used in assay.
Residue:
714
Sequence:
MAEEVITPVYCTGVSAQVQKLRAKELGLGRHENAIKYLGQDYEQLRAHCLQSGSLFRDEAFPPVPQSLGFKELGPNSSKTYGVKWKRPTELFSNPQFIVDGATRTDICQGALGDCWLLAAIASLTLNDTLLHRVVPHGQSFQNGYAGIFHFQLWQFGEWVDVVVDDLLPTKDGKLVFVHSAQGNEFWSALLEKAYAKVNGSYEALSGGSTSEGFEDFTGGVTEWYELRKAPSDLYSIILKALERGSLLGCSIDISSVLDMEAVTFKKLVKGHAYSVTGAKQVNYQGQMVNLIRMRNPWGEVEWTGAWSDGSSEWNGVDPYQRDQLRVRMEDGEFWMSFRDFLREFTRLEICNLTPDALKSQRVRNWNTTLYEGTWRRGSTAGGCRNYPATFWVNPQFKIRLEETDDPEDDYGGRESGCSFVLALMQKHRRRERRFGRDMETIGFAVYEVPPELVGQPVHLKRDFFLANASRARSEQFINLREVSTRFRLPPGEYVVVPSTFEPNKEGDFVLRFFSEKKAGTQELDDQVQAILPDEQVLSEEEIDENFKALFRQLAGEDMEISVRELRTILNRIISKHKDLRTKGFSLESCRSMVNLMDRDGNGKLGLVEFNILWNRIRNYLSIFRKFDLDKSGSMSAYEMRMAIESAGFKLNKKLFELIITRYSEPDLAVDFDNFVCCLVRLETMFRFFKTLDTDLDGVVTFDLFKWLQLTMFA
  
Inhibitor
Name:
BDBM23862
Synonyms:
Peptidyl alpha-Ketoester, 1d | methyl 3-[(2S)-2-(3,3-diphenylpropanamido)-4-methylpentanamido]-2-oxo-4-phenylbutanoate
Type:
Small organic molecule
Emp. Form.:
C32H36N2O5
Mol. Mass.:
528.6386
SMILES:
COC(=O)C(=O)C(Cc1ccccc1)NC(=O)[C@H](CC(C)C)NC(=O)CC(c1ccccc1)c1ccccc1 |r|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM23856
Synonyms:
Suc-LY-AMC (AMC=7-Amino-4-methylcoumarin) | Suc-Leu-Tyr-AMC
Type:
Fluorogenic substrate
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
n/a
Structure: