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Literature summary for 3.4.24.17 extracted from

  • Jacobsen, E.J.; Mitchell, M.A.; Hendges, S.K.; Belonga, K.L.; Skaletzky, L.L.; Stelzer, L.S.; Lindberg, T.J.; Fritzen, E.L.; Schostarez, H.J.; O’Sullivan, T.J.; Maggiora, L.L.; Stuchly, C.W.; Laborde, A.L.; Kubicek, M.F.; Poorman, R.A.; Beck, J.M.; Miller, H.R.; Petzold, G.L.; Scott, P.S.; Truesdell, S.E.; Wallace, T.L.; Wilks, J.W.; Fisher, C.; Goodman, L.V.; Kaytes, P.S.; Ledbetter, S.R.; Powers, E.A.
    Synthesis of a series of stromelysin-selective thiadiazole urea matrix metalloproteinase inhibitors (1999), J. Med. Chem., 42, 1525-1536.
    View publication on PubMed
Search for more literature for 3.4.24.17

Inhibitors

Inhibitors Comment Organism Structure
(2S)-3-(4-fluorophenyl)-N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide
-
 Homo sapiens
(2S)-3-(benzyloxy)-N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide
-
 Homo sapiens
(2S)-3-phenyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide
-
 Homo sapiens
(2S)-N-methyl-3-(4-nitrophenyl)-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide
-
 Homo sapiens
(2S)-N-methyl-3-(pentafluorophenyl)-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide i.e. PNU-142372 Homo sapiens
(2S)-N-methyl-3-phenyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide i.e. PNU-107859 Homo sapiens
1-[(1S)-1-(4-fluorobenzyl)-2-oxo-2-(4-pyridin-2-ylpiperazin-1-yl)ethyl]-3-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)urea
-
 Homo sapiens
1-[(1S)-2-oxo-1-(pentafluorobenzyl)-2-(4-pyridin-2-ylpiperazin-1-yl)ethyl]-3-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)urea
-
 Homo sapiens
alpha-[[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]-carbonyl]amino]-3-hydroxy-N-methyl-(S)-propanamide
-
 Homo sapiens
alpha-[[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]amino]-N,N-dimethyl-(S)-benzenepropanamide
-
 Homo sapiens
N-(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)-N'-(2-phenethyl)urea
-
 Homo sapiens
N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)acetamide
-
 Homo sapiens
N-[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]-L-phenylalanine methyl ester
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
 truncated protein lacking C-terminus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
beta-casein + H2O
-
 Homo sapiens ?
-
 ?

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000014
-
 1-[(1S)-2-oxo-1-(pentafluorobenzyl)-2-(4-pyridin-2-ylpiperazin-1-yl)ethyl]-3-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)urea pH 7.6, 25°C Homo sapiens
0.000018
-
 (2S)-N-methyl-3-(pentafluorophenyl)-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.0001
-
 (2S)-3-(4-fluorophenyl)-N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.00027
-
 1-[(1S)-1-(4-fluorobenzyl)-2-oxo-2-(4-pyridin-2-ylpiperazin-1-yl)ethyl]-3-(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)urea pH 7.6, 25°C Homo sapiens
0.00029
-
 N-[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]-L-phenylalanine methyl ester pH 7.6, 25°C Homo sapiens
0.00033
-
 (2S)-N-methyl-3-(4-nitrophenyl)-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.00071
-
 (2S)-N-methyl-3-phenyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.002
-
 (2S)-3-(benzyloxy)-N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.0023
-
 alpha-[[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]carbonyl]amino]-N,N-dimethyl-(S)-benzenepropanamide pH 7.6, 25°C Homo sapiens
0.0033
-
 (2S)-3-phenyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)propanamide pH 7.6, 25°C Homo sapiens
0.007
-
 N-(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)-N'-(2-phenethyl)urea pH 7.6, 25°C Homo sapiens
0.031
-
 alpha-[[[(4,5-dihydro-5-thioxo-1,3,4-thiadiazol-2-yl)amino]-carbonyl]amino]-3-hydroxy-N-methyl-(S)-propanamide pH 7.6, 25°C Homo sapiens
0.166
-
 N-methyl-2-(([(5-thioxo-4,5-dihydro-1,3,4-thiadiazol-2-yl)amino]carbonyl)amino)acetamide pH 7.6, 25°C Homo sapiens