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Literature summary for 3.4.24.B12 extracted from

  • Cappelli, A.; Nannicini, C.; Valenti, S.; Giuliani, G.; Anzini, M.; Mennuni, L.; Giordani, A.; Caselli, G.; Stasi, L.P.; Makovec, F.; Giorgi, G.; Vomero, S.
    Design, synthesis, and preliminary biological evaluation of pyrrolo[3,4-c]quinolin-1-one and oxoisoindoline derivatives as aggrecanase inhibitors (2010), ChemMedChem, 5, 739-748.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2R,5R)-1-([4-[(2,4-dichlorobenzyl)oxy]phenyl]sulfonyl)-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamide
-
Homo sapiens
2-[4-(benzyloxy)phenyl]-2,3-dihydro-1-oxo-1H-pyrrolo[3,4-c]quinoline-4-carboxylate the inhibitor is unable to discriminate between ADAMTS-5 and ADAMTS-4 Homo sapiens
2-[4-(benzyloxy)phenyl]-2,3-dihydro-N-hydroxy-1-oxo-1Hpyrrolo[3,4-c]quinoline-4-carboxamide
-
Homo sapiens
2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid does not inhibit ADAMTS-4 Homo sapiens
2-[4-(benzyloxy)phenyl]-N-hydroxy-3-oxoisoindoline-4-carboxamide does not inhibit ADAMTS-4 Homo sapiens
additional information design of ADAMTS-5 inhibitors Homo sapiens
N2-(biphenyl-4-ylcarbonyl)-N-(2-phenylpropan-2-yl)-L-alpha-glutamine
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
aggrecan-interglobular domain + H2O cleavage site Glu373-Ala374 in aggrecan–interglobular domain Homo sapiens ?
-
?

Synonyms

Synonyms Comment Organism
ADAMTS-5
-
Homo sapiens
aggrecanase-2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
additional information
-
IC25-value: 0.0025 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50% Homo sapiens 2-[4-(benzyloxy)phenyl]-N-hydroxy-3-oxoisoindoline-4-carboxamide
additional information
-
IC25-value: 0.0075 mM, 37°C, pH and temperature not specified in the publication, plateau inhibition at about 50% Homo sapiens 2-[4-(benzyloxy)phenyl]-3-oxoisoindoline-4-carboxylic acid
0.0000014
-
37°C, pH and temperature not specified in the publication Homo sapiens (2R,5R)-1-([4-[(2,4-dichlorobenzyl)oxy]phenyl]sulfonyl)-N,5-dihydroxy-3,3-dimethylpiperidine-2-carboxamide
0.00095
-
37°C, pH and temperature not specified in the publication Homo sapiens 2-[4-(benzyloxy)phenyl]-2,3-dihydro-N-hydroxy-1-oxo-1Hpyrrolo[3,4-c]quinoline-4-carboxamide
0.0011
-
37°C, pH and temperature not specified in the publication Homo sapiens N2-(biphenyl-4-ylcarbonyl)-N-(2-phenylpropan-2-yl)-L-alpha-glutamine
0.012
-
37°C, pH and temperature not specified in the publication Homo sapiens 2-[4-(benzyloxy)phenyl]-2,3-dihydro-1-oxo-1H-pyrrolo[3,4-c]quinoline-4-carboxylate