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Target
Calpain-1 catalytic subunit
Ligand
BDBM50466175
Substrate
n/a
Meas. Tech.
ChEMBL_1791744 (CHEMBL4263663)
IC50
20500±n/a nM
Citation
Kalash, L; Cresser-Brown, J; Habchi, J; Morgan, C; Miller, DJ; Glen, RC; Allemann, RK; Bender, A Structure-based design of allosteric calpain-1 inhibitors populating a novel bioactivity space. Eur J Med Chem 157:1264-1275 (2018) [PubMed] Article
More Info.:
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