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Literature summary for 3.4.21.6 extracted from

  • Young, R.J.; Adams, C.; Blows, M.; Brown, D.; Burns-Kurtis, C.L.; Chan, C.; Chaudry, L.; Convery, M.A.; Davies, D.E.; Exall, A.M.; Foster, G.; Harling, J.D.; Hortense, E.; Irvine, S.; Irving, W.R.; Jackson, S.; Kleanthous, S.; Pateman, A.J.; Patikis, A.N.; Roethka, T.J.; Senger, S.; Stelman, G.J.; Toomey, J.R.
    Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs (2011), Bioorg. Med. Chem. Lett., 21, 1582-1587.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide
-
Homo sapiens
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
Homo sapiens
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
Homo sapiens
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide
-
Homo sapiens
additional information structure and property based design of factor Xa pyrrolidin-2-one inhibitors with aminoindane and phenylpyrrolidine P4 motifs, rational design, syntheses and evaluation, overview Homo sapiens
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide
-
Homo sapiens
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide
-
Homo sapiens
rivaroxaban
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
FXa
-
Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000003
-
3-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000001
-
3-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]-1H-indole-6-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000002
-
6-chloro-N-[(3S)-1-[(1R)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000002
-
6-chloro-N-[(3S)-1-[(1S)-1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000002
-
6-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000002
-
3-chloro-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000002
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000003
-
6-chloro-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000003
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2R)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000004
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[(2S)-1-(morpholin-4-yl)-1-oxopropan-2-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000004
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000004
-
6-chloro-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000004
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000005
-
6-chloro-N-[(3S)-1-[1-(methylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000005
-
N-[(3S)-1-(1-amino-2,3-dihydro-1H-inden-5-yl)-2-oxopyrrolidin-3-yl]-6-chloronaphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000005
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000006
-
6-chloro-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000006
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-2-oxo-1-[4-[(2S)-pyrrolidin-2-yl]phenyl]pyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.000009
-
6-chloro-N-[(3S)-1-[(1S)-1-(dimethylamino)-2,3-dihydro-1H-inden-5-yl]-2-oxopyrrolidin-3-yl]naphthalene-2-sulfonamide pH and temperature not specified in the publication Homo sapiens
0.000015
-
(E)-2-(5-chlorothiophen-2-yl)-N-[(3S)-1-[4-(1-methylpyrrolidin-2-yl)phenyl]-2-oxopyrrolidin-3-yl]ethenesulfonamide pH and temperature not specified in the publication Homo sapiens
0.0001
-
N-[(3S)-2-oxo-1-[4-(pyrrolidin-2-yl)phenyl]pyrrolidin-3-yl]-1H-indole-6-sulfonamide pH and temperature not specified in the publication Homo sapiens