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Literature summary for 3.4.24.B4 extracted from

  • Gao, D.A.; Xiong, Z.; Heim-Riether, A.; Amodeo, L.; August, E.M.; Cao, X.; Ciccarelli, L.; Collins, B.K.; Harrington, K.; Haverty, K.; Hill-Drzewi, M.; Li, X.; Liang, S.; Margarit, S.M.; Moss, N.; Nagaraja, N.; Proudfoot, J.; Roman, R.; Schlyer, S.; Keenan, L.S.; Taylor, S.; Wellenzohn, B.; Wiedenmayer, D.; Li, J.; Farrow, N.A.
    SAR studies of non-zinc-chelating MMP-13 inhibitors: improving selectivity and metabolic stability (2010), Bioorg. Med. Chem. Lett., 20, 5039-5043.
    View publication on PubMed
Search for more literature for 3.4.24.B4

Inhibitors

Inhibitors Comment Organism Structure
2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
-
 Homo sapiens
2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
-
 Homo sapiens
5-(4-chlorophenyl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
 Homo sapiens
5-[3-[(acetylamino)methyl]phenyl]-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
-
 Homo sapiens
additional information selectivity and metabolic stability of non-zinc-chelating MMP-13 inhibitors, overview Homo sapiens
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(3-[[(furan-2-ylcarbonyl)amino]methyl]phenyl)furan-2-carboxamide
-
 Homo sapiens
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[3-([[(2-methylfuran-3-yl)carbonyl]amino]methyl)phenyl]furan-2-carboxamide
-
 Homo sapiens
N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(1,5-dimethyl-1H-pyrazol-3-yl)methoxy]phenyl]furan-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-imidazole-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-3-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-methyl-1,3-thiazole-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylfuran-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylpyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-ethylpyridine-3-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-methylfuran-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-methylpyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-7-methylimidazo[1,2-a]pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-8-methylimidazo[1,2-a]pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]imidazo[1,2-a]pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-3-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
 Homo sapiens
N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
-
 Homo sapiens
N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
-
 Homo sapiens

Metals/Ions

Metals/Ions Comment Organism Structure
Ca2+ dependent on Homo sapiens
Zn2+ dependent on Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
type II collagen + H2O Homo sapiens
-
 ?
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
type II collagen + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

Synonyms Comment Organism
MMP-13
-
 Homo sapiens
More MMP-13 belongs to the collagenase family Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000002
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
0.000002
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[2-(methylamino)-2-oxo-1-(tetrahydro-2H-pyran-4-yl)ethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
0.000003
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
0.000004
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[4-[(1,5-dimethyl-1H-pyrazol-3-yl)methoxy]phenyl]furan-2-carboxamide
0.000004
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-methylpyridine-2-carboxamide
0.000005
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
0.000006
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
0.000007
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
0.000008
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-2-carboxamide
0.000008
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-methyl-1,3-thiazole-4-carboxamide
0.000009
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
0.000009
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
0.00001
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyrimidine-4-carboxamide
0.000011
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-methylfuran-2-carboxamide
0.000024
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-3-carboxamide
0.000025
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[3-hydroxy-3-methyl-1-(methylamino)-1-oxobutan-2-yl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
0.000027
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-chloro-N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
0.000028
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-6-(trifluoromethyl)pyridine-2-carboxamide
0.000029
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-5-ethylpyridine-3-carboxamide
0.000031
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-4-carboxamide
0.000036
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[1-cyclopropyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-2-(trifluoromethyl)pyrimidine-4-carboxamide
0.000042
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]pyridine-3-carboxamide
0.000072
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1,5-dimethyl-1H-pyrazole-3-carboxamide
0.000075
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-(3-[[(furan-2-ylcarbonyl)amino]methyl]phenyl)furan-2-carboxamide
0.0001
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylpyridine-2-carboxamide
0.0001
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]imidazo[1,2-a]pyridine-2-carboxamide
0.00011
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-8-methylimidazo[1,2-a]pyridine-2-carboxamide
0.00014
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-7-methylimidazo[1,2-a]pyridine-2-carboxamide
0.00014
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-pyrazole-4-carboxamide
0.00018
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-3-methylfuran-2-carboxamide
0.00031
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[3-(5-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]furan-2-yl)benzyl]-1-methyl-1H-imidazole-2-carboxamide
0.00033
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]-5-[3-([[(2-methylfuran-3-yl)carbonyl]amino]methyl)phenyl]furan-2-carboxamide
0.00043
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-(4-chlorophenyl)-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide
0.0033
-
 pH not specified in the publication, temperature not specified in the publication Homo sapiens 5-[3-[(acetylamino)methyl]phenyl]-N-[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]furan-2-carboxamide