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Literature summary for 3.4.21.6 extracted from

  • Yang, J.; Su, G.; Ren, Y.; Chen, Y.
    Synthesis of 3,4-diaminobenzoyl derivatives as factor Xa inhibitors (2015), Eur. J. Med. Chem., 101, 41-51 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
4-(4-(2-oxopyridin-1(2H)-yl)benzamido)-3-(3,4,5-trimethoxybenzamido)benzoic acid
-
Homo sapiens
4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
-
Homo sapiens
4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
-
Homo sapiens
apixaban
-
Homo sapiens
betrixaban
-
Homo sapiens
darexaban
-
Homo sapiens
edoxaban
-
Homo sapiens
ethyl-(4-(2-oxopyridin-1(2H)-yl)benzamido)-3-(3,4,5-trimethoxybenzamido)benzoate
-
Homo sapiens
N-(4-carbamoyl-2-(3,4,5-trimethoxybenzamido)phenyl)-2-oxo-1-phenyl-1,2-di-hydropyridine-4-carboxamide
-
Homo sapiens
N-(4-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopiperidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide highly potent, selective, direct inhibitor Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-chlorobenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-fluorobenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-formamidobenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-4-methoxybenzamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-5-chlorothio-phene-2-carboxamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-6-chloronicotinamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzo[d]oxa-zole-6-carboxamide
-
Homo sapiens
N-(5-carbamoyl-2-(4-(2-oxopyrrolidin-1-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
-
Homo sapiens
rivaroxaban
-
Homo sapiens
TAK-442
-
Homo sapiens
YM-222714
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
prothrombin + H2O Homo sapiens
-
thrombin + ?
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
prothrombin + H2O
-
Homo sapiens thrombin + ?
-
?
S-2765 + H2O
-
Homo sapiens Z-D-Arg-Gly-L-Arg + 4-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
factor Xa
-
Homo sapiens
FXa
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000065
-
at pH 6.0 and 25°C Homo sapiens rivaroxaban
0.0000065
-
at pH 6.0 and 25°C Homo sapiens N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dichlorobenzamide
0.0000156
-
at pH 6.0 and 25°C Homo sapiens 4-acetamido-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-benzamide
0.0000171
-
at pH 6.0 and 25°C Homo sapiens N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4-dimethoxybenzamide
0.0000259
-
at pH 6.0 and 25°C Homo sapiens 4-bromo-N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)benzamide
0.0000286
-
at pH 6.0 and 25°C Homo sapiens N-(5-carbamoyl-2-(4-(2-oxopyridin-1(2H)-yl)benzamido)phenyl)-3,4,5-trimethoxybenzamide
0.0000286
-
at pH 6.0 and 25°C Homo sapiens YM-222714
0.0000546
-
at pH 6.0 and 25°C Homo sapiens darexaban