Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.24.86 extracted from

  • Yu, W.; Tong, L.; Kim, S.; Wong, M.; Chen, L.; Yang, D.; Shankar, B.; Lavey, B.; Zhou, G.; Kosinski, A.; Rizvi, R.; Li, D.; Feltz, R.; Piwinski, J.; Rosner, K.; Shih, N.; Siddiqui, M.; Guo, Z.; Orth, P.; Shah, H.; Sun, J.; Umland, S.; Lundell, D.; Niu, X.
    Biaryl substituted hydantoin compounds as TACE inhibitors (2010), Bioorg. Med. Chem. Lett., 20, 5286-5289.
    View publication on PubMed
Search for more literature for 3.4.24.86

Inhibitors

Inhibitors Comment Organism Structure
(5R)-5-(2',4'-difluorobiphenyl-4-yl)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-(4'-chlorobiphenyl-4-yl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[2'-(1-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(trifluoromethyl)biphenyl-4-yl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(quinolin-6-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[3'-(2-methyl-1,3-thiazol-4-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(1H-pyrazol-3-yl)biphenyl-4-yl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1,3-thiazol-2-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methyl-2H-indazol-6-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methylpyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(3-phenyl-1,2-oxazol-5-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(4-methyl-2,5-dioxoimidazolidin-4-yl)phenyl]imidazolidine-2,4-dione (non-preferred name)
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrazin-2-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-2-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrimidin-5-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[4-(2-aminopyridin-4-yl)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5R)-5-[4-(5-chloro-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
(5S)-5-(4-fluorophenyl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxamide
-
 Homo sapiens
5-[(5-methoxy-3-oxo-1,3-dihydro-2H-indazol-2-yl)methyl]-5-phenylimidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(2-phenoxyphenyl)imidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(3-phenoxyphenyl)imidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-oxopyrrolidin-1-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(morpholin-4-yl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yloxy)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrrolidin-1-ylcarbonyl)phenyl]imidazolidine-2,4-dione
-
 Homo sapiens
5-[4-(cyclopentyloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
5-[4-(isoquinolin-7-yloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione
-
 Homo sapiens
methyl 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxylate
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
proTNF-alpha + H2O Homo sapiens
-
 soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
blood
-
 Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
proTNF-alpha + H2O
-
 Homo sapiens soluble TNF-alpha + 9000 Da membrane-bound fragment of TNF-alpha
-
 ?

Synonyms

Synonyms Comment Organism
TACE
-
 Homo sapiens
TNF-alpha converting enzyme
-
 Homo sapiens
tumor necrosis factor alpha converting enzyme
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000001
-
 (5R)-5-[4-(5-chloro-6-oxo-1,6-dihydropyridin-3-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000002
-
 (5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(6-oxo-1,6-dihydropyridin-3-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000005
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-2-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000005
-
 (5R)-5-[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000005
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methylpyridin-4-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000006
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000006
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1,3-thiazol-2-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000008
-
 (5S)-5-(4-fluorophenyl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000008
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000008
-
 (5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(quinolin-6-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000009
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrimidin-5-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000001
-
 (5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-3-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000012
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrazin-2-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000014
-
 (5R)-5-[4-(2-aminopyridin-4-yl)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000002
-
 (5R)-5-(2',4'-difluorobiphenyl-4-yl)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000002
-
 (5R)-5-(4'-chlorobiphenyl-4-yl)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000002
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrazol-4-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000002
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-methyl-2H-indazol-6-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000002
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(1H-pyrazol-3-yl)biphenyl-4-yl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.0000026
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(4-methyl-2,5-dioxoimidazolidin-4-yl)phenyl]imidazolidine-2,4-dione (non-preferred name) pH and temperature not specified in the publication Homo sapiens
0.000003
-
 5-[4-(cyclopentyloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000003
-
 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxamide pH and temperature not specified in the publication Homo sapiens
0.000003
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(1-methyl-1H-pyrrolo[2,3-c]pyridin-5-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000006
-
 5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(morpholin-4-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000006
-
 5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyrrolidin-1-ylcarbonyl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000006
-
 5-[(5-methoxy-3-oxo-1,3-dihydro-2H-indazol-2-yl)methyl]-5-phenylimidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000007
-
 5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(pyridin-4-yloxy)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000008
-
 5-[4-(isoquinolin-7-yloxy)phenyl]-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000008
-
 5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(2-oxopyrrolidin-1-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000009
-
 methyl 4'-[(4R)-4-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-2,5-dioxoimidazolidin-4-yl]biphenyl-4-carboxylate pH and temperature not specified in the publication Homo sapiens
0.00001
-
 (5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[2'-(1-methyl-1H-tetrazol-5-yl)biphenyl-4-yl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000018
-
 (5R)-5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4'-(trifluoromethyl)biphenyl-4-yl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000027
-
 5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(3-phenoxyphenyl)imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000028
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[4-(3-phenyl-1,2-oxazol-5-yl)phenyl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000029
-
 5-[(6-fluoro-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-(2-phenoxyphenyl)imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens
0.000031
-
 (5R)-5-[(6-methoxy-1-oxo-1,3-dihydro-2H-isoindol-2-yl)methyl]-5-[3'-(2-methyl-1,3-thiazol-4-yl)biphenyl-4-yl]imidazolidine-2,4-dione pH and temperature not specified in the publication Homo sapiens