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Literature summary for 3.4.21.69 extracted from

  • De Nanteuil, G.; Gloanec, P.; Beguin, S.; Giesen, P.L.; Hemker, H.C.; Mennecier, P.; Rupin, A.; Verbeuren, T.J.
    Low molecular weight activated protein C inhibitors as a potential treatment for hemophilic disorders (2006), J. Med. Chem., 49, 5047-5050.
    View publication on PubMed
Search for more literature for 3.4.21.69

Application

Application Comment Organism
medicine low molecular weight activated protein C inhibitors might be useful as potential treatment for hemophilic disorders Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
additional information inhibitor structure-activity relationship, overview Homo sapiens
N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2,2-dimethyl-4-oxobutyl)glycine
-
 Homo sapiens
N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-cyclohexyl-4-oxobutyl)glycine
-
 Homo sapiens
N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-4-oxobutyl)glycine
-
 Homo sapiens
N-[(2R)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-3-methylpentyl]glycine
-
 Homo sapiens
N-[(2R)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-4-methylpentyl]glycine
-
 Homo sapiens
N-[(2R)-2-benzyl-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-4-oxobutyl]glycine
-
 Homo sapiens
N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-(cyclohexylmethyl)-4-oxobutyl]glycine
-
 Homo sapiens
N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-ethyl-4-oxobutyl]glycine
-
 Homo sapiens
N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-methyl-4-oxobutyl]glycine
-
 Homo sapiens
N-[(2S)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-3,3-dimethylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([1-benzyl-2-[(4-carbamimidoylbenzyl)amino]-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)amino]-1-(2,3-dihydro-1H-inden-2-yl)-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)amino]-1-(diphenylmethyl)-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-cyclopenta[a]naphthalen-2-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-cyclopenta[b]naphthalen-2-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-phenalen-2-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-cyclopenta[b]pyridin-6-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-cyclopenta[c]pyridin-6-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-dibenzo[a,c][7]annulen-6-yl]carbamoyl)-3-methylbutyl]glycine
-
 Homo sapiens
N-[(2S)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-(1-methylethyl)-4-oxobutyl]glycine
-
 Homo sapiens
N-[(2S)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-cyclohexyl-4-oxobutyl]glycine
-
 Homo sapiens
N-[[1-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)cyclopentyl]methyl]glycine
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
Activated protein C
-
 Homo sapiens
APC
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0001
-
-
 Homo sapiens N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-(cyclohexylmethyl)-4-oxobutyl]glycine
0.00025
-
-
 Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-cyclopenta[a]naphthalen-2-yl]carbamoyl)-3-methylbutyl]glycine
0.00035
-
-
 Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)amino]-1-(2,3-dihydro-1H-inden-2-yl)-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
0.00043
-
-
 Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-phenalen-2-yl]carbamoyl)-3-methylbutyl]glycine
0.00071
-
-
 Homo sapiens N-[(2S)-2-([1-benzyl-2-[(4-carbamimidoylbenzyl)amino]-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
0.00075
-
-
 Homo sapiens N-[(2R)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-4-methylpentyl]glycine
0.0008
-
-
 Homo sapiens N-[(2S)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-(1-methylethyl)-4-oxobutyl]glycine
0.00082
-
-
 Homo sapiens N-[(2S)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-cyclohexyl-4-oxobutyl]glycine
0.0011
-
-
 Homo sapiens N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-cyclopenta[b]pyridin-6-yl]carbamoyl)-3-methylbutyl]glycine
0.00112
-
-
 Homo sapiens N-[(2R)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-3-methylpentyl]glycine
0.0017
-
-
 Homo sapiens N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-cyclopenta[c]pyridin-6-yl]carbamoyl)-3-methylbutyl]glycine
0.00204
-
-
 Homo sapiens N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-ethyl-4-oxobutyl]glycine
0.00383
-
-
 Homo sapiens N-[(2S)-2-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)-3,3-dimethylbutyl]glycine
0.00908
-
-
 Homo sapiens N-[(2R)-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-methyl-4-oxobutyl]glycine
0.00928
-
-
 Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-cyclopenta[b]naphthalen-2-yl]carbamoyl)-3-methylbutyl]glycine
0.01091
-
-
 Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)carbamoyl]-5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl]carbamoyl)-3-methylbutyl]glycine
0.01125
-
-
 Homo sapiens N-[(2R)-2-benzyl-4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-4-oxobutyl]glycine
0.01265
-
-
 Homo sapiens N-[(2S)-2-([6-[(4-carbamimidoylbenzyl)carbamoyl]-6,7-dihydro-5H-dibenzo[a,c][7]annulen-6-yl]carbamoyl)-3-methylbutyl]glycine
0.033
-
 above Homo sapiens N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-cyclohexyl-4-oxobutyl)glycine
0.033
-
 above Homo sapiens N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-4-oxobutyl)glycine
0.033
-
 above Homo sapiens N-[(2S)-2-([2-[(4-carbamimidoylbenzyl)amino]-1-(diphenylmethyl)-2-oxoethyl]carbamoyl)-3-methylbutyl]glycine
0.044
-
-
 Homo sapiens N-(4-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2,2-dimethyl-4-oxobutyl)glycine
0.053
-
-
 Homo sapiens N-[[1-(2-[2-[(4-carbamimidoylbenzyl)carbamoyl]-2,3-dihydro-1H-inden-2-yl]-2-oxoethyl)cyclopentyl]methyl]glycine