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Literature summary for 3.4.21.21 extracted from

  • Shiraishi, T.; Kadono, S.; Haramura, M.; Kodama, H.; Ono, Y.; Iikura, H.; Esaki, T.; Koga, T.; Hattori, K.; Watanabe, Y.; Sakamoto, A.; Yoshihashi, K.; Kitazawa, T.; Esaki, K.; Ohta, M.; Sato, H.; Kozono, T.
    Design and synthesis of peptidomimetic factor VIIa inhibitors (2010), Chem. Pharm. Bull., 58, 38-44.
    View publication on PubMed
Search for more literature for 3.4.21.21

Cloned(Commentary)

Cloned (Comment) Organism
-
 Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
-
 Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
3-(3-[(R)-2-[(S)-1-(4-carbamimidoyl-benzylcarbamoyl)-3-carbamoylpropylcarbamoyl]-2-ethanesulfonylamino-ethyl]-1H-indol-5-yloxymethyl)-benzoic acid
-
 Homo sapiens
5-(4-carboxybutoxy)-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
 Homo sapiens
5-[(3-carboxybenzyl)oxy]-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
 Homo sapiens
D-prolyl-N-(4-carbamimidoylbenzyl)-L-prolinamide
-
 Homo sapiens
N-(ethylsulfonyl)-1-methyl-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
 Homo sapiens
N-(ethylsulfonyl)-5-hydroxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
 Homo sapiens
N-(ethylsulfonyl)-5-methoxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
-
 Homo sapiens
N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-L-glutamamide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Factor X + H2O Homo sapiens
-
 Factor Xa + ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P08709
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Factor X + H2O
-
 Homo sapiens Factor Xa + ?
-
 ?

Synonyms

Synonyms Comment Organism
FVIIa
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000039
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens 3-(3-[(R)-2-[(S)-1-(4-carbamimidoyl-benzylcarbamoyl)-3-carbamoylpropylcarbamoyl]-2-ethanesulfonylamino-ethyl]-1H-indol-5-yloxymethyl)-benzoic acid
0.000056
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens 5-[(3-carboxybenzyl)oxy]-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
0.000062
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-L-glutamamide
0.000065
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens N-(ethylsulfonyl)-5-methoxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
0.000069
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens N-(ethylsulfonyl)-1-methyl-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
0.00014
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens N-(ethylsulfonyl)-5-hydroxy-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
0.000204
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens 5-(4-carboxybutoxy)-N-(ethylsulfonyl)-D-tryptophyl-N1-(4-carbamimidoylbenzyl)-D-glutamamide
0.0024
-
 in 500 mM Tris-HCl, pH 7.5, 1.5 M NaCl, 50 mM CaCl2, temperature not specified in the publication Homo sapiens D-prolyl-N-(4-carbamimidoylbenzyl)-L-prolinamide

General Information

General Information Comment Organism
physiological function FVIIa in complex with tissue factor initiates the extrinsic coagulation pathway Homo sapiens