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Literature summary for 3.4.21.6 extracted from

  • Pinto, D.J.; Galemmo, R.A.; Quan, M.L.; Orwat, M.J.; Clark, C.; Li, R.; Wells, B.; Woerner, F.; Alexander, R.S.; Rossi, K.A.; Smallwood, A.; Wong, P.C.; Luettgen, J.M.; Rendina, A.R.; Knabb, R.M.; He, K.; Wexler, R.R.; Lam, P.Y.
    Discovery of potent, efficacious, and orally bioavailable inhibitors of blood coagulation factor Xa with neutral P1 moieties (2006), Bioorg. Med. Chem. Lett., 16, 5584-5589.
    View publication on PubMed
Search for more literature for 3.4.21.6

Inhibitors

Inhibitors Comment Organism Structure
1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
 Homo sapiens
2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
3-[6-(2'-dimethylaminomethyl-biphenyl-4-yl)-7-oxo-3-trifluoromethyl-4,5,6,7-tetrahydro-pyrazolo[3,4-c]pyridine-1-yl]-benzamide the inhibitor shows good fXa potency, selectivity, in vivo efficacy and oral bioavailability Homo sapiens
3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
BMS-740808
-
 Homo sapiens
DPC423
-
 Homo sapiens
methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
 Homo sapiens
methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
 Homo sapiens
N-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]acetamide
-
 Homo sapiens
razaxaban i.e. BMS-561389 Homo sapiens
Trypsin
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Synonyms

Synonyms Comment Organism
FXa
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000003
-
 BMS-740808
-
 Homo sapiens
0.00000004
-
 1-(3-amino-1,2-benzisoxazol-5-yl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.00000012
-
 methyl 4'-[1-[2-[(aminooxy)sulfinyl]-4-methoxyphenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.00000018
-
 razaxaban
-
 Homo sapiens
0.00000018
-
 3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
0.00000018
-
 methyl 4'-[1-(2-carbamoyl-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.00000018
-
 methyl 4'-[1-(4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.0000002
-
 methyl 4'-[1-(2-amino-4-methoxyphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.00000035
-
 6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.00000072
-
 3-[6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
0.00000074
-
 methyl 4'-[1-[2-[(aminooxy)sulfinyl]phenyl]-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.00000076
-
 (R)-6-(2'-((3-hydroxypyrrolidin-1-yl)methyl)-[1,1'-biphenyl]-4-yl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-5,6-dihydro-1H-pyrazolo[3,4-c]pyridin-7(4H)-one
-
 Homo sapiens
0.00000082
-
 methyl 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzenesulfinate
-
 Homo sapiens
0.0000012
-
 6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-[3-(iminomethyl)phenyl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.0000012
-
 1-[2-[(aminooxy)sulfinyl]phenyl]-6-(2'-[[(3R)-3-hydroxypyrrolidin-1-yl]methyl]biphenyl-4-yl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.000002
-
 methyl 4'-[1-(2-carbamoylphenyl)-7-oxo-3-(trifluoromethyl)-1,4,5,7-tetrahydro-6H-pyrazolo[3,4-c]pyridin-6-yl]biphenyl-2-sulfinate
-
 Homo sapiens
0.000002
-
 1-(3-aminophenyl)-6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.0000026
-
 6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(4-ethylphenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.0000027
-
 2-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]benzamide
-
 Homo sapiens
0.00002
-
 6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-1-(3-nitrophenyl)-3-(trifluoromethyl)-1,4,5,6-tetrahydro-7H-pyrazolo[3,4-c]pyridin-7-one
-
 Homo sapiens
0.000047
-
 methyl [3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]amidosulfite
-
 Homo sapiens
0.000054
-
 1-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]urea
-
 Homo sapiens
0.000088
-
 N-[3-[6-[2'-[(dimethylamino)methyl]biphenyl-4-yl]-7-oxo-3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridin-1-yl]phenyl]acetamide
-
 Homo sapiens
0.01
-
 Trypsin above Homo sapiens