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Literature summary for 3.4.24.B12 extracted from

  • Bursavich, M.G.; Gilbert, A.M.; Lombardi, S.; Georgiadis, K.E.; Reifenberg, E.; Flannery, C.R.; Morris, E.A.
    Synthesis and evaluation of aryl thioxothiazolidinone inhibitors of ADAMTS-5 (Aggrecanase-2) (2007), Bioorg. Med. Chem. Lett., 17, 1185-1188.
    View publication on PubMed
Search for more literature for 3.4.24.B12

Inhibitors

Inhibitors Comment Organism Structure
(5E)-2-thioxo-5-([3-[3-(trifluoromethyl)phenoxy]phenyl]methylidene)-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-3-benzyl-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-([3-methoxy-4-[(4-methoxybenzyl)oxy]phenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-([4-[(4-chlorobenzyl)oxy]-3-methoxyphenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[(3-phenoxyphenyl)methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-(2-phenylethyl)-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-methyl-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3,5-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(4-methoxyphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(4-methylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[3-(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5E)-5-[[4-(benzyloxy)-3-methoxyphenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-1-methyl-2-thioxoimidazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
-
 Homo sapiens
(5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
-
 Homo sapiens
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
-
 Homo sapiens
2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
-
 Homo sapiens
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
-
 Homo sapiens
2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
-
 Homo sapiens
3-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
-
 Homo sapiens
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
-
 Homo sapiens
[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
-
 Homo sapiens
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
-
 Homo sapiens
[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
a disintegrin and metalloproteinase with thrombospondin motifs 5
-
 Homo sapiens
ADAMTS-5
-
 Homo sapiens
aggrecanase-2
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0009
-
-
 Homo sapiens [(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
0.0011
-
-
 Homo sapiens 2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
0.0013
-
-
 Homo sapiens [(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl](phenyl)acetic acid
0.0013
-
-
 Homo sapiens 2-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
0.0014
-
-
 Homo sapiens (5E)-5-[[3,5-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0016
-
-
 Homo sapiens 2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-phenylpropanoic acid
0.0017
-
-
 Homo sapiens (5E)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0018
-
-
 Homo sapiens (5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0018
-
-
 Homo sapiens 2-[(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]-3-methylbutanoic acid
0.0025
-
-
 Homo sapiens (5E)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0032
-
-
 Homo sapiens (5E)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0035
-
-
 Homo sapiens (5E)-5-([4-[(4-chlorobenzyl)oxy]-3-methoxyphenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0049
-
-
 Homo sapiens (5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0053
-
-
 Homo sapiens (5E)-2-thioxo-5-([3-[3-(trifluoromethyl)phenoxy]phenyl]methylidene)-1,3-thiazolidin-4-one
0.0053
-
-
 Homo sapiens 3-[(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]propanoic acid
0.0067
-
-
 Homo sapiens [(5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
0.0068
-
-
 Homo sapiens (5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0092
-
-
 Homo sapiens (5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.01
-
-
 Homo sapiens (5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0111
-
-
 Homo sapiens [(5Z)-5-[[3-(3,4-dichlorophenoxy)phenyl]methylidene]-4-oxo-2-thioxo-1,3-thiazolidin-3-yl]acetic acid
0.0116
-
-
 Homo sapiens (5E)-5-([3-methoxy-4-[(4-methoxybenzyl)oxy]phenyl]methylidene)-2-thioxo-1,3-thiazolidin-4-one
0.0148
-
-
 Homo sapiens (5E)-5-[[3-(4-methylphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0162
-
-
 Homo sapiens (5E)-5-[[3-(4-methoxyphenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.0201
-
-
 Homo sapiens (5E)-5-[[3-(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.022
-
 IC50 above 0.022 mM Homo sapiens (5E)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.022
-
 IC50 above 0.022 mM Homo sapiens (5E)-5-[(3-phenoxyphenyl)methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.022
-
 IC50 above 0.022 mM Homo sapiens (5E)-5-[[4-(benzyloxy)-3-methoxyphenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.022
-
 IC50 above 0.022 mM Homo sapiens (5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-1-methyl-2-thioxoimidazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5E)-3-benzyl-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-2-thioxo-1,3-thiazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-(2-phenylethyl)-2-thioxo-1,3-thiazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-ethyl-2-thioxo-1,3-thiazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-methyl-2-thioxo-1,3-thiazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5E)-5-[[3,4-bis(benzyloxy)phenyl]methylidene]-3-phenyl-2-thioxo-1,3-thiazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5Z)-5-[[3-(3,5-dichlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5Z)-5-[[3-(4-chlorophenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one
0.067
-
 IC50 above 0.067 mM Homo sapiens (5Z)-5-[[3-(4-tert-butylphenoxy)phenyl]methylidene]-2-thioxoimidazolidin-4-one