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Literature summary for 3.4.11.18 extracted from

  • Wang, G.T.; Mantei, R.A.; Kawai, M.; Tedrow, J.S.; Barnes, D.M.; Wang, J.; Zhang, Q.; Lou, P.; Garcia, L.A.; Bouska, J.; Yates, M.; Park, C.; Judge, R.A.; Lesniewski, R.; Sheppard, G.S.; Bell, R.L.
    Lead optimization of methionine aminopeptidase-2 (MetAP2) inhibitors containing sulfonamides of 5,6-disubstituted anthranilic acids (2007), Bioorg. Med. Chem. Lett., 17, 2817-2822.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
2-(2-aminoethoxy)-3-ethyl-6-[[(2-propylphenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
2-(2-aminoethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
2-(2-aminoethoxy)-6-[([2-[3-(diethylamino)propyl]-4-fluorophenyl]sulfonyl)amino]-3-ethylbenzoic acid
-
Mus musculus
2-(carboxymethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
2-butyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
Mus musculus
2-chloro-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
2-ethenyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
Mus musculus
2-ethoxy-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methoxybenzoic acid
-
Mus musculus
2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
-
Mus musculus
2-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid potent inhibitor but lacks cellular activity and is highly protein bound Mus musculus
3-ethyl-2-methoxy-6-[[(2-[[2-(1-methylpyrrolidin-2-yl)ethyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
3-ethyl-2-methoxy-6-[[(2-[[3-(2-methylpiperidin-1-yl)propyl]amino]phenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
3-ethyl-2-methyl-6-[(pyridin-2-ylsulfonyl)amino]benzoic acid
-
Mus musculus
5-ethyl-2-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
-
Mus musculus
6-[([2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-ethyl-2-methoxybenzoic acid
-
Mus musculus
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-(1H-imidazol-4-yl)-3-methoxybenzoic acid
-
Mus musculus
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-2-yl-3-methoxybenzoic acid
-
Mus musculus
6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
-
Mus musculus
6-[[(2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-furan-3-yl-2-methoxybenzoic acid
-
Mus musculus
6-[[(2-[[3-(dimethylamino)propyl]amino]-4-fluorophenyl)sulfonyl]amino]-3-furan-3-yl-2-methoxybenzoic acid
-
Mus musculus
6-[[(2-[[4-(dimethylamino)butyl]amino]phenyl)sulfonyl]amino]-3-ethyl-2-methoxybenzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-2,3-dimethylbenzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(1-hydroxyethyl)-3-methylbenzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-2-(hydroxymethyl)-3-methylbenzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-2-methoxy-3-(1H-pyrazol-4-yl)benzoic acid
-
Mus musculus
6-[[(4-fluorophenyl)sulfonyl]amino]-3-methyl-2-propylbenzoic acid
-
Mus musculus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
Met-peptide + H2O Mus musculus
-
Met + peptide
-
?

Organism

Organism UniProt Comment Textmining
Mus musculus O08663
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Met-peptide + H2O
-
Mus musculus Met + peptide
-
?

Synonyms

Synonyms Comment Organism
MetAP2
-
Mus musculus
methionine aminopeptidase-2
-
Mus musculus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000008
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
0.000009
-
-
Mus musculus 2-[(phenylsulfonyl)amino]-5,6,7,8-tetrahydronaphthalene-1-carboxylic acid
0.00001
-
-
Mus musculus 6-[[(2-[[4-(dimethylamino)butyl]amino]phenyl)sulfonyl]amino]-3-ethyl-2-methoxybenzoic acid
0.000011
-
-
Mus musculus 2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methoxybenzoic acid
0.000015
-
-
Mus musculus 2-chloro-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
0.000015
-
-
Mus musculus 3-ethyl-2-methoxy-6-[[(2-[[2-(1-methylpyrrolidin-2-yl)ethyl]amino]phenyl)sulfonyl]amino]benzoic acid
0.000015
-
-
Mus musculus 6-[[(2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-furan-3-yl-2-methoxybenzoic acid
0.000016
-
-
Mus musculus 2-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
0.000016
-
-
Mus musculus 2-(2-aminoethoxy)-3-ethyl-6-[[(2-propylphenyl)sulfonyl]amino]benzoic acid
0.000017
-
-
Mus musculus 6-[[(2-[[3-(dimethylamino)propyl]amino]-4-fluorophenyl)sulfonyl]amino]-3-furan-3-yl-2-methoxybenzoic acid
0.000018
-
-
Mus musculus 3-ethyl-2-methoxy-6-[[(2-[[3-(2-methylpiperidin-1-yl)propyl]amino]phenyl)sulfonyl]amino]benzoic acid
0.00002
-
-
Mus musculus 6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-3-yl-3-methoxybenzoic acid
0.000024
-
-
Mus musculus 2-(2-aminoethoxy)-6-[([2-[3-(diethylamino)propyl]-4-fluorophenyl]sulfonyl)amino]-3-ethylbenzoic acid
0.000026
-
-
Mus musculus 6-[([2-[(1E)-3-(diethylamino)prop-1-en-1-yl]-4-fluorophenyl]sulfonyl)amino]-3-ethyl-2-methoxybenzoic acid
0.000038
-
-
Mus musculus 2-ethoxy-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
0.000046
-
-
Mus musculus 2-(2-aminoethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
0.000055
-
-
Mus musculus 5-ethyl-2-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
0.00006
-
-
Mus musculus 2-ethenyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
0.000067
-
-
Mus musculus 3-ethyl-2-methyl-6-[(pyridin-2-ylsulfonyl)amino]benzoic acid
0.000078
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-2,3-dimethylbenzoic acid
0.00015
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-3-methyl-2-propylbenzoic acid
0.00028
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-2-methoxy-3-(1H-pyrazol-4-yl)benzoic acid
0.001
-
-
Mus musculus 6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-furan-2-yl-3-methoxybenzoic acid
0.0013
-
-
Mus musculus 2-butyl-6-[[(4-fluorophenyl)sulfonyl]amino]-3-methylbenzoic acid
0.0025
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-2-(1-hydroxyethyl)-3-methylbenzoic acid
0.0058
-
-
Mus musculus 2-(carboxymethoxy)-3-ethyl-6-[[(4-fluorophenyl)sulfonyl]amino]benzoic acid
0.008
-
-
Mus musculus 6-[[(4-fluorophenyl)sulfonyl]amino]-2-(hydroxymethyl)-3-methylbenzoic acid
0.036
-
-
Mus musculus 6-[[(2-bromo-4-fluorophenyl)sulfonyl]amino]-2-(1H-imidazol-4-yl)-3-methoxybenzoic acid