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Target
Cathepsin D
Ligand
BDBM16755
Substrate
Cathepsin D/Pepsin Peptide Substrate
Meas. Tech.
FRET-based Peptide Cleavage Assay
pH
4.5±n/a
Temperature
295.15±n/a K
IC50
5900±300 nM
Citation
Cole, DC; Manas, ES; Stock, JR; Condon, JS; Jennings, LD; Aulabaugh, A; Chopra, R; Cowling, R; Ellingboe, JW; Fan, KY; Harrison, BL; Hu, Y; Jacobsen, S; Jin, G; Lin, L; Lovering, FE; Malamas, MS; Stahl, ML; Strand, J; Sukhdeo, MN; Svenson, K; Turner, MJ; Wagner, E; Wu, J; Zhou, P; Bard, J Acylguanidines as small-molecule beta-secretase inhibitors. J Med Chem 49:6158-61 (2006) [PubMed] Article
More Info.:
Target
Name:
Cathepsin D
Synonyms:
CATD_HUMAN | CPSD | CTSD | Cathepsin D [Precursor] | Cathepsin D heavy chain | Cathepsin D light chain | Cathepsin D precursor
Type:
Enzyme
Mol. Mass.:
44551.72
Organism:
Homo sapiens (Human)
Description:
Human proCathepsin D (SwissProt accession number P07339) was expressed in Sf9 cells, purified, and autoactivated.
Residue:
412
Sequence:
MQPSSLLPLALCLLAAPASALVRIPLHKFTSIRRTMSEVGGSVEDLIAKGPVSKYSQAVPAVTEGPIPEVLKNYMDAQYYGEIGIGTPPQCFTVVFDTGSSNLWVPSIHCKLLDIACWIHHKYNSDKSSTYVKNGTSFDIHYGSGSLSGYLSQDTVSVPCQSASSASALGGVKVERQVFGEATKQPGITFIAAKFDGILGMAYPRISVNNVLPVFDNLMQQKLVDQNIFSFYLSRDPDAQPGGELMLGGTDSKYYKGSLSYLNVTRKAYWQVHLDQVEVASGLTLCKEGCEAIVDTGTSLMVGPVDEVRELQKAIGAVPLIQGEYMIPCEKVSTLPAITLKLGGKGYKLSPEDYTLKVSQAGKTLCLSGFMGMDIPPPSGPLWILGDVFIGRYYTVFDRDNNRVGFAEAARL
Inhibitor
Name:
BDBM16755
Synonyms:
Acylguanidine, 10d | N-[(1Z)-amino[(3-hydroxypropyl)amino]methylidene]-2-[2-(2-chlorophenyl)-5-(4-propoxyphenyl)-1H-pyrrol-1-yl]acetamide
Type:
Small organic molecule
Emp. Form.:
C25H29ClN4O3
Mol. Mass.:
468.976
SMILES:
CCCOc1ccc(cc1)-c1ccc(-c2ccccc2Cl)n1CC(=O)NC(=N)NCCCO
Substrate
Name:
Cathepsin D/Pepsin Peptide Substrate
Synonyms:
n/a
Type:
Peptide
Mol. Mass.:
2478.43
Organism:
n/a
Description:
n/a
Residue:
21
Sequence:
MCACGKPILFFRLKDNPDRNH