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Literature summary for 3.4.21.21 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

Inhibitors Comment Organism Structure
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
EEWEVLCWTWETCERGEG-(Z-domain of protein A) IC50: 3.8 nM Homo sapiens
EEWEVLCWTWETCERGEG-NH2 IC50: 1.5 nM Homo sapiens
EVLCWTWETCER-NH2 IC50: 470 nM Homo sapiens
EWEVLCWTWETCERGE-(Z-domain of protein A) IC50: 4.8 nM Homo sapiens
MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A) IC50: 5.9 nM Homo sapiens
SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A) IC50: 4400 nM Homo sapiens
SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A) IC50: 93 nM Homo sapiens
VLCWTWETCER-NH2 IC50: 0.022 nM Homo sapiens
WEVLCWTWETC-NH2 IC50: 0.013 mM Homo sapiens
WEVLCWTWETCE-NH2 IC50: 0.007 mM Homo sapiens
WEVLCWTWETCER-NH2 IC50: 2.5 nM Homo sapiens

KM Value [mM]

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood plasma
-
Homo sapiens
-

Substrates and Products (Substrate)

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

Turnover Number [1/s]

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

Ki Value [mM]

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

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000000022
-
IC50: 0.022 nM Homo sapiens VLCWTWETCER-NH2
0.0000015
-
IC50: 1.5 nM Homo sapiens EEWEVLCWTWETCERGEG-NH2
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
0.0000025
-
IC50: 2.5 nM Homo sapiens WEVLCWTWETCER-NH2
0.0000038
-
IC50: 3.8 nM Homo sapiens EEWEVLCWTWETCERGEG-(Z-domain of protein A)
0.0000048
-
IC50: 4.8 nM Homo sapiens EWEVLCWTWETCERGE-(Z-domain of protein A)
0.0000059
-
IC50: 5.9 nM Homo sapiens MEEWEVLCWTWETCERGEGQ-(Z-domain of protein A)
0.000093
-
IC50: 93 nM Homo sapiens SEEWEVLCWTWEDCRLEGLE-(Z-domain of protein A)
0.00047
-
IC50: 470 nM Homo sapiens EVLCWTWETCER-NH2
0.0044
-
IC50: 4400 nM Homo sapiens SAEWEVLCWTWEGCGSVGL-(Z-domain of protein A)
0.007
-
IC50: 0.007 mM Homo sapiens WEVLCWTWETCE-NH2
0.013
-
IC50: 0.013 mM Homo sapiens WEVLCWTWETC-NH2