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Literature summary for 3.4.21.34 extracted from

  • Partridge, J.R.; Choy, R.M.; Silva-Garcia, A.; Yu, C.; Li, Z.; Sham, H.; Metcalf, B.
    Structures of full-length plasma kallikrein bound to highly specific inhibitors describe a new mode of targeted inhibition (2019), J. Struct. Biol., 206, 170-182 .
    View publication on PubMed
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Activating Compound

Activating Compound Comment Organism Structure
thrombin
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
enzyme bound to inhibitor, hanging drop vapor diffusion method, using 0.2 M potassium dihydrogen phosphate, 23% (w/v) PEG3350 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
BCX4161 low nanomolar inhibitory potency Homo sapiens
benzamidine
-
 Homo sapiens
N-[(6-amino-2,4-dimethylpyridin-3-yl)methyl]-1-[[4-(1H-pyrazol-1-ylmethyl)phenyl]methyl]-1H-pyrazole-4-carboxamide low nanomolar inhibitory potency Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
kininogen + H2O Homo sapiens
-
 bradykinin + fragments of kininogen
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P03952
-
-

Source Tissue

Source Tissue Comment Organism Textmining
HUVEC cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Pro-Phe-Arg-4-nitroanilide + H2O
-
 Homo sapiens D-Pro-Phe-Arg + 4-nitroaniline
-
 ?
kininogen + H2O
-
 Homo sapiens bradykinin + fragments of kininogen
-
 ?

Synonyms

Synonyms Comment Organism
PKal
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
 at pH 7.4 and 23°C Homo sapiens BCX4161
0.0000082
-
 at pH 7.4 and 23°C Homo sapiens N-[(6-amino-2,4-dimethylpyridin-3-yl)methyl]-1-[[4-(1H-pyrazol-1-ylmethyl)phenyl]methyl]-1H-pyrazole-4-carboxamide