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Literature summary for 3.4.21.39 extracted from

  • Greco, M.N.; Hawkins, M.J.; Powell, E.T.; Almond, H.R.; de Garavilla, L.; Hall, J.; Minor, L.K.; Wang, Y.; Corcoran, T.W.; Di Cera, E.; Cantwell, A.M.; Savvides, S.N.; Damiano, B.P.; Maryanoff, B.E.
    Discovery of potent, selective, orally active, nonpeptide inhibitors of human mast cell chymase (2007), J. Med. Chem., 50, 1727-1730.
    View publication on PubMed
Search for more literature for 3.4.21.39

Inhibitors

Inhibitors Comment Organism Structure
methyl[1-naphthalen-2-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphinic acid
-
 Homo sapiens
[1-(1-benzofuran-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(2,3-dihydro-1H-benzotriazol-1-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid less than 50% inhibition at 0.01 mM Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl](2-phenylethyl)phosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]ethylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phenylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]ethylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chloro-5-fluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chlorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-methoxyphenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-benzothiophen-3-yl)-2-[[2-(3,4-difluorophenyl)ethyl]amino]-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
-
 Homo sapiens
[1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[1-naphthalen-1-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
-
 Homo sapiens
[2-(3-[methyl[1-(naphthalen-2-ylcarbonyl)piperidin-4-yl]carbamoyl]naphthalen-2-yl)-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
mast cell
-
 Homo sapiens
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0000035
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chlorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
0.0000045
-
-
 Homo sapiens [2-(3-[methyl[1-(naphthalen-2-ylcarbonyl)piperidin-4-yl]carbamoyl]naphthalen-2-yl)-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
0.00001
-
-
 Homo sapiens [1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
0.000011
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
0.000013
-
-
 Homo sapiens [1-(5-chloro-1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.000016
-
-
 Homo sapiens [1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
0.000017
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3-chloro-5-fluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
0.000021
-
-
 Homo sapiens [1-(5-chloro-1-methyl-1H-indol-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
0.000029
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.00005
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]methylphosphinic acid
0.000058
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]methylphosphinic acid
0.00006
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-oxo-2-[[(E)-2-phenylethenyl]amino]ethyl]phosphonic acid
0.000066
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-fluorophenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
0.00008
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]methylphosphinic acid
0.00009
-
-
 Homo sapiens [1-(1-methyl-1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.00012
-
-
 Homo sapiens [1-(1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.00016
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]ethylphosphinic acid
0.000165
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(3,4-difluorophenyl)ethenyl]amino]-2-oxoethyl]ethylphosphinic acid
0.00019
-
-
 Homo sapiens [1-naphthalen-1-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.00021
-
-
 Homo sapiens methyl[1-naphthalen-2-yl-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphinic acid
0.00024
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl](2-phenylethyl)phosphinic acid
0.00028
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[(E)-2-(4-methoxyphenyl)ethenyl]amino]-2-oxoethyl]phosphonic acid
0.00092
-
-
 Homo sapiens [1-(1H-indol-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.0021
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phenylphosphinic acid
0.0025
-
-
 Homo sapiens [1-(1-benzofuran-3-yl)-2-(naphthalen-2-ylamino)-2-oxoethyl]phosphonic acid
0.0104
-
-
 Homo sapiens [1-(5-chloro-1-benzothiophen-3-yl)-2-[[2-(3,4-difluorophenyl)ethyl]amino]-2-oxoethyl]methylphosphinic acid