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Target
Plasma kallikrein
Ligand
BDBM423188
Substrate
n/a
Meas. Tech.
Endpoint Assay
IC50
1.20±n/a nM
Citation
 Frattini, S; Lingard, I; Hamprecht, DW; Bakker, RA; Eckhardt, M; Gollner, A; Hehn, JP; Langkopf, E; Wagner, H; Wellenzohn, B; Wiedenmayer, D Heteroarylcarboxamide derivatives as plasma kallikrein inhibitors US Patent  US10501440 Publication Date 12/10/2019 
Target
Name:
Plasma kallikrein
Synonyms:
3.4.21.34 | Fletcher factor | KLKB1_RAT | Kininogenin | Klk3 | Klkb1 | Pk | Plasma kallikrein | Plasma kallikrein heavy chain | Plasma kallikrein light chain | Plasma prekallikrein
Type:
PROTEIN
Mol. Mass.:
71291.49
Organism:
Rattus norvegicus
Description:
ChEMBL_117397
Residue:
638
Sequence:
MILFKQVGYFVSLFATVSCGCLSQLYANTFFRGGDLAAIYTPDAQHCQKMCTFHPRCLLFSFLAVSPTKETDKRFGCFMKESITGTLPRIHRTGAISGHSLKQCGHQLSACHQDIYEGLDMRGSNFNISKTDSIEECQKLCTNNIHCQFFTYATKAFHRPEYRKSCLLKRSSSGTPTSIKPVDNLVSGFSLKSCALSEIGCPMDIFQHFAFADLNVSQVVTPDAFVCRTVCTFHPNCLFFTFYTNEWETESQRNVCFLKTSKSGRPSPPIIQENAVSGYSLFTCRKARPEPCHFKIYSGVAFEGEELNATFVQGADACQETCTKTIRCQFFTYSLLPQDCKAEGCKCSLRLSTDGSPTRITYEAQGSSGYSLRLCKVVESSDCTTKINARIVGGTNSSLGEWPWQVSLQVKLVSQNHMCGGSIIGRQWILTAAHCFDGIPYPDVWRIYGGILNLSEITNKTPFSSIKELIIHQKYKMSEGSYDIALIKLQTPLNYTEFQKPICLPSKADTNTIYTNCWVTGWGYTKERGETQNILQKATIPLVPNEECQKKYRDYVITKQMICAGYKEGGIDACKGDSGGPLVCKHSGRWQLVGITSWGEGCARKEQPGVYTKVAEYIDWILEKIQSSKERALETSPA
  
Inhibitor
Name:
BDBM423188
Synonyms:
N-[(5R)-1-Amino-3-methyl-5H,6H,7H-cyclopenta[c]pyridin-5-yl]-1-[(2-{3-azabicyclo[3.1.0]hexan-3-yl}-4-methylpyrimidin-5-yl)methyl]-1H-1,2,3-triazole-4-carboxamide | US10501440, Example 18
Type:
Small organic molecule
Emp. Form.:
C23H27N9O
Mol. Mass.:
445.5202
SMILES:
Cc1cc2[C@@H](CCc2c(N)n1)NC(=O)c1cn(Cc2cnc(nc2C)N2CC3CC3C2)nn1 |r|
Structure:
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