Reaction Details |
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Target | Calpain-1 catalytic subunit |
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Ligand | BDBM50326298 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_659958 (CHEMBL1247359) |
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Ki | 41±n/a nM |
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Citation | Ovat, A; Li, ZZ; Hampton, CY; Asress, SA; Fernández, FM; Glass, JD; Powers, JC Peptidyl alpha-ketoamides with nucleobases, methylpiperazine, and dimethylaminoalkyl substituents as calpain inhibitors. J Med Chem53:6326-36 (2010) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Calpain-1 catalytic subunit |
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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: | MAEEVITPVYCTGVSAQVQKLRAKELGLGRHENAIKYLGQDYEQLRAHCLQSGSLFRDEA
FPPVPQSLGFKELGPNSSKTYGVKWKRPTELFSNPQFIVDGATRTDICQGALGDCWLLAA
IASLTLNDTLLHRVVPHGQSFQNGYAGIFHFQLWQFGEWVDVVVDDLLPTKDGKLVFVHS
AQGNEFWSALLEKAYAKVNGSYEALSGGSTSEGFEDFTGGVTEWYELRKAPSDLYSIILK
ALERGSLLGCSIDISSVLDMEAVTFKKLVKGHAYSVTGAKQVNYQGQMVNLIRMRNPWGE
VEWTGAWSDGSSEWNGVDPYQRDQLRVRMEDGEFWMSFRDFLREFTRLEICNLTPDALKS
QRVRNWNTTLYEGTWRRGSTAGGCRNYPATFWVNPQFKIRLEETDDPEDDYGGRESGCSF
VLALMQKHRRRERRFGRDMETIGFAVYEVPPELVGQPVHLKRDFFLANASRARSEQFINL
REVSTRFRLPPGEYVVVPSTFEPNKEGDFVLRFFSEKKAGTQELDDQVQAILPDEQVLSE
EEIDENFKALFRQLAGEDMEISVRELRTILNRIISKHKDLRTKGFSLESCRSMVNLMDRD
GNGKLGLVEFNILWNRIRNYLSIFRKFDLDKSGSMSAYEMRMAIESAGFKLNKKLFELII
TRYSEPDLAVDFDNFVCCLVRLETMFRFFKTLDTDLDGVVTFDLFKWLQLTMFA
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BDBM50326298 |
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n/a |
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Name | BDBM50326298 |
Synonyms: | 3-(Benzyloxycarbonyl-L-leucylamino)-N-(3-(6-amino-2-methoxy-9H-purin-9-yl)propyl)-2-oxophenylbutanamide | CHEMBL1240874 |
Type | Small organic molecule |
Emp. Form. | C33H40N8O6 |
Mol. Mass. | 644.7207 |
SMILES | COc1nc(N)c2ncn(CCCNC(=O)C(=O)C(Cc3ccccc3)NC(=O)[C@H](CC(C)C)NC(=O)OCc3ccccc3)c2n1 |r| |
Structure |
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