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Literature summary for 2.7.7.48 extracted from

  • Slater, M.J.; Amphlett, E.M.; Andrews, D.M.; Bravi, G.; Burton, G.; Cheasty, A.G.; Corfield, J.A.; Ellis, M.R.; Fenwick, R.H.; Fernandes, S.; Guidetti, R.; Haigh, D.; Hartley, C.D.; Howes, P.D.; Jackson, D.L.; Jarvest, R.L.; Lovegrove, V.L.; Medhurst, K.J.; Parry, N.R.; Price, H.; Shah, P.; Singh, O.M.; Stocker, R.
    Optimization of novel acyl pyrrolidine inhibitors of hepatitis C virus RNA-dependent RNA polymerase leading to a development candidate (2007), J. Med. Chem., 50, 897-900.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)pyrrolidine-2,4-dicarboxylic acid
-
Hepacivirus C
(2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-thiophen-2-ylpyrrolidine-2,4-dicarboxylic acid
-
Hepacivirus C
(2S,4S,5R)-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-2,4-dicarboxylic acid
-
Hepacivirus C
(4R,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(ethoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4R,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(hydroxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(3-bromo-4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butyl-3-chlorophenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(ethoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(hydroxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(methoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C
(5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(methoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
Hepacivirus C

Organism

Organism UniProt Comment Textmining
Hepacivirus C
-
genotype 1b
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
nucleoside triphosphate + RNAn
-
Hepacivirus C diphosphate + RNAn+1
-
?

Synonyms

Synonyms Comment Organism
NS5B
-
Hepacivirus C
RDRP
-
Hepacivirus C
RNA-dependent RNA polymerase
-
Hepacivirus C

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000005
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.000014
-
-
Hepacivirus C (4S,5R)-1-[(3-bromo-4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.00002
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butyl-3-chlorophenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.00043
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(ethoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.00044
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(methoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.00073
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(hydroxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.00097
-
-
Hepacivirus C (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.001
-
-
Hepacivirus C (4R,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(hydroxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.0011
-
-
Hepacivirus C (2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-thiophen-2-ylpyrrolidine-2,4-dicarboxylic acid
0.0023
-
-
Hepacivirus C (5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(methoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.0032
-
-
Hepacivirus C (4R,5R)-1-[(4-tert-butyl-3-methoxyphenyl)carbonyl]-4-(ethoxymethyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
0.0038
-
-
Hepacivirus C (2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)pyrrolidine-2,4-dicarboxylic acid
0.02
-
-
Hepacivirus C (2S,4S,5R)-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-2,4-dicarboxylic acid