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Literature summary extracted from

  • Burton, G.; Ku, T.W.; Carr, T.J.; Kiesow, T.; Sarisky, R.T.; Lin-Goerke, J.; Hofmann, G.A.; Slater, M.J.; Haigh, D.; Dhanak, D.; Johnson, V.K.; Parry, N.R.; Thommes, P.
    Studies on acyl pyrrolidine inhibitors of HCV RNA-dependent RNA polymerase to identify a molecule with replicon antiviral activity (2007), Bioorg. Med. Chem. Lett., 17, 1930-1933.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.7.7.48 (2R,3S,5S)-5-(methoxycarbonyl)-5-(2-methylpropyl)-2-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-3-carboxylic acid
-
 Hepacivirus C
2.7.7.48 (2R,3S,5S)-5-[(aminooxy)carbonyl]-5-(2-methylpropyl)-2-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-3-carboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)pyrrolidine-2,4-dicarboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-thiophen-2-ylpyrrolidine-2,4-dicarboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-2,4-dicarboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-2-isobutyl-4-(2-phenylacetyl)-5-(thiophen-2-yl)-1-(4-(trifluoromethyl)benzoyl)pyrrolidine-2-carboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-2-isobutyl-5-(thiophen-2-yl)-1-(4-(trifluoromethyl)benzoyl)pyrrolidine-2,4-dicarboxylic acid
-
 Hepacivirus C
2.7.7.48 (2S,4S,5R)-4-acetyl-2-isobutyl-5-(thiophen-2-yl)-1-(4-(trifluoromethyl)benzoyl)pyrrolidine-2-carboxylic acid
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-4-(phenylcarbamoyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-4-[[(2-phenylethoxy)sulfinyl]carbamoyl]-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-(methylcarbamoyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-thiophen-2-yl-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-[(methoxysulfinyl)carbamoyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-2-(2-methylpropyl)-4-(phenylcarbamoyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-2-(2-methylpropyl)-4-[(2-phenylethyl)carbamoyl]-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-2-(2-methylpropyl)-5-thiophen-2-yl-4-[[(trifluoromethoxy)sulfinyl]carbamoyl]-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-(benzylcarbamoyl)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-(ethylcarbamoyl)-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-(methylcarbamoyl)-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-carbamoyl-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-[(1-methylethyl)carbamoyl]-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-[(methoxysulfinyl)carbamoyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-[(methoxysulfinyl)carbamoyl]-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]-L-proline
-
 Hepacivirus C
2.7.7.48 (4S,5R)-4-[[(benzyloxy)sulfinyl]carbamoyl]-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
-
 Hepacivirus C
2.7.7.48 dimethyl (2S,4S,5R)-2-(2-methylpropyl)-5-thiophen-2-yl-1-[[4-(trifluoromethyl)phenyl]carbonyl]pyrrolidine-2,4-dicarboxylate
-
 Hepacivirus C

Organism

EC Number Organism UniProt Comment Textmining
2.7.7.48 Hepacivirus C
-
 genotype 1b isolate J4 with 21 amino acid C-terminal truncation and genotype 1b isolate RB01
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
2.7.7.48 NS5B
-
 Hepacivirus C
2.7.7.48 RNA-dependent RNA polymerase
-
 Hepacivirus C

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.7.7.48 0.0031
-
 full-length enzyme Hepacivirus C (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-4-(phenylcarbamoyl)-5-(1,3-thiazol-2-yl)-L-proline
2.7.7.48 0.00315
-
 full-length enzyme Hepacivirus C (4S,5R)-4-[[(benzyloxy)sulfinyl]carbamoyl]-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
2.7.7.48 0.0038
-
 full-length enzyme Hepacivirus C (2S,4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)pyrrolidine-2,4-dicarboxylic acid
2.7.7.48 0.00423
-
 full-length enzyme Hepacivirus C (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-4-[[(2-phenylethoxy)sulfinyl]carbamoyl]-5-(1,3-thiazol-2-yl)-L-proline
2.7.7.48 0.0044
-
 full-length enzyme Hepacivirus C (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-carbamoyl-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
2.7.7.48 0.02
-
 full-length enzyme Hepacivirus C (2S,4S,5R)-2-isobutyl-5-(thiophen-2-yl)-1-(4-(trifluoromethyl)benzoyl)pyrrolidine-2,4-dicarboxylic acid
2.7.7.48 0.022
-
 full-length enzyme Hepacivirus C (4S,5R)-1-[(4-tert-butylphenyl)carbonyl]-4-(methylcarbamoyl)-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline
2.7.7.48 0.068
-
 full-length enzyme Hepacivirus C (4S,5R)-4-(benzylcarbamoyl)-1-[(4-tert-butylphenyl)carbonyl]-2-(2-methylpropyl)-5-(1,3-thiazol-2-yl)-L-proline