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Literature summary extracted from

  • Dennis, M.S.; Roberge, M.; Quan, C.; Lazarus, R.A.
    Selection and characterization of a new class of peptide exosite inhibitors of coagulation factor VIIa (2001), Biochemistry, 40, 9513-9521.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.21 EEWEVLCWTWETCER IC50: 1.6 nM, partial hyperbolic mixed-type inhibitor of factor X activation, partial competitive inhibitor of amidolytic activity. Inhibits activation of factor X and factor IX and amidolytic activity of Chromozym t-PA with IC50 values of 1.6 nM, 3.5 nM and 8.5 nM Homo sapiens
3.4.21.21 EEWEVLCWTWETCERGEG-(Z-domain of protein A) IC50: 3.8 nM Homo sapiens
3.4.21.21 EEWEVLCWTWETCERGEG-NH2 IC50: 1.5 nM Homo sapiens
3.4.21.21 EVLCWTWETCER-NH2 IC50: 470 nM Homo sapiens
3.4.21.21 EWEVLCWTWETCERGE-(Z-domain of protein A) IC50: 4.8 nM Homo sapiens
3.4.21.21 MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A) IC50: 5.9 nM Homo sapiens
3.4.21.21 SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A) IC50: 4400 nM Homo sapiens
3.4.21.21 SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A) IC50: 93 nM Homo sapiens
3.4.21.21 VLCWTWETCER-NH2 IC50: 0.022 nM Homo sapiens
3.4.21.21 WEVLCWTWETC-NH2 IC50: 0.013 mM Homo sapiens
3.4.21.21 WEVLCWTWETCE-NH2 IC50: 0.007 mM Homo sapiens
3.4.21.21 WEVLCWTWETCER-NH2 IC50: 2.5 nM Homo sapiens

KM Value [mM]

EC Number KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
3.4.21.21 0.0000184
-
 Factor X pH 7.8 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.21 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.21.21 blood plasma
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.21 chromozym t-PA + H2O
-
 Homo sapiens ?
-
 ?
3.4.21.21 factor IX + H2O
-
 Homo sapiens activated factor IX + ?
-
 ?
3.4.21.21 factor X + H2O
-
 Homo sapiens activated factor X
-
 ?

Turnover Number [1/s]

EC Number Turnover Number Minimum [1/s] Turnover Number Maximum [1/s] Substrate Comment Organism Structure
3.4.21.21 9.2
-
 Factor X pH 7.8 Homo sapiens

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
3.4.21.21 0.0000002
-
 EEWEVLCWTWETCER inhibition of amidolytic activity Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.21 0.000000022
-
 IC50: 0.022 nM Homo sapiens VLCWTWETCER-NH2
3.4.21.21 0.0000015
-
 IC50: 1.5 nM Homo sapiens EEWEVLCWTWETCERGEG-NH2
3.4.21.21 0.0000016
-
 IC50: 1.6 nM, partial hyperbolic mixed-type inhibitor of factor X activation, partial competitive inhibitor of amidolytic activity. Inhibits activation of factor X and factor IX and amidolytic activity of Chromozym t-PA with IC50 values of 1.6 nM, 3.5 nM Homo sapiens EEWEVLCWTWETCER
3.4.21.21 0.0000025
-
 IC50: 2.5 nM Homo sapiens WEVLCWTWETCER-NH2
3.4.21.21 0.0000038
-
 IC50: 3.8 nM Homo sapiens EEWEVLCWTWETCERGEG-(Z-domain of protein A)
3.4.21.21 0.0000048
-
 IC50: 4.8 nM Homo sapiens EWEVLCWTWETCERGE-(Z-domain of protein A)
3.4.21.21 0.0000059
-
 IC50: 5.9 nM Homo sapiens MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A)
3.4.21.21 0.000093
-
 IC50: 93 nM Homo sapiens SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A)
3.4.21.21 0.00047
-
 IC50: 470 nM Homo sapiens EVLCWTWETCER-NH2
3.4.21.21 0.0044
-
 IC50: 4400 nM Homo sapiens SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A)
3.4.21.21 0.007
-
 IC50: 0.007 mM Homo sapiens WEVLCWTWETCE-NH2
3.4.21.21 0.013
-
 IC50: 0.013 mM Homo sapiens WEVLCWTWETC-NH2