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Literature summary for 3.4.21.42 extracted from

  • Travins, J.M.; Ali, F.; Huang, H.; Ballentine, S.K.; Khalil, E.; Hufnagel, H.R.; Pan, W.; Gushue, J.; Leonard, K.; Bone, R.F.; Soll, R.M.; DesJarlais, R.L.; Crysler, C.S.; Ninan, N.; Kirkpatrick, J.; Cummings, M.D.; Huebert, N.; Molloy, C.J.; Gaul, M.; Tomczuk, B.E.; Subasinghe, N.L.
    Biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s (2008), Bioorg. Med. Chem. Lett., 18, 1603-1606.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-carboxylic acid
-
Rattus norvegicus
4-(biphenyl-3-ylsulfonyl)-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2'-chlorobiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2'-ethenylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(2-amino-6-methylphenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(3'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(3'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(3'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(3-bromophenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(4'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(4'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[(4'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[[2'-(hydroxymethyl)-6'-methylbiphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[[2'-(hydroxymethyl)biphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
4-[[3-(3-methylpyridin-2-yl)phenyl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
5-(methylsulfanyl)-4-[[2'-methyl-6'-([[2-(2H-tetrazol-5-yl)ethyl]carbamoyl]amino)biphenyl-3-yl]sulfonyl]thiophene-2-carboximidamide
-
Rattus norvegicus
6-[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)amino]-6-oxohexanoic acid
-
Rattus norvegicus
6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanoic acid
-
Rattus norvegicus
C1-esterase inhibitor
-
Rattus norvegicus
N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-2-(methylsulfonyl)acetamide
-
Rattus norvegicus
N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-4-(methylsulfonyl)butanamide
-
Rattus norvegicus
tert-butyl [[4-[(3-bromophenyl)sulfonyl]-5-(methylsulfanyl)thiophen-2-yl](imino)methyl]carbamate binding mode in the active site, structure, overview Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-

Synonyms

Synonyms Comment Organism
complement component C1s
-
Rattus norvegicus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000012
-
N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-2-(methylsulfonyl)acetamide
-
Rattus norvegicus
0.000014
-
N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-4-(methylsulfonyl)butanamide
-
Rattus norvegicus
0.00002
-
4-[(2-amino-6-methylphenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.000022
-
6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanoic acid
-
Rattus norvegicus
0.00003
-
4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00004
-
4-[(2'-chlorobiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00004
-
4-[[3-(3-methylpyridin-2-yl)phenyl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.000042
-
6-[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)amino]-6-oxohexanoic acid
-
Rattus norvegicus
0.00005
-
4-[[2'-(hydroxymethyl)-6'-methylbiphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.000064
-
5-(methylsulfanyl)-4-[[2'-methyl-6'-([[2-(2H-tetrazol-5-yl)ethyl]carbamoyl]amino)biphenyl-3-yl]sulfonyl]thiophene-2-carboximidamide
-
Rattus norvegicus
0.00012
-
4-[[2'-(hydroxymethyl)biphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00014
-
4-[(2'-ethenylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00015
-
3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-carboxylic acid
-
Rattus norvegicus
0.00015
-
4-[(3'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00019
-
4-[(4'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00025
-
4-[(4'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00026
-
4-(biphenyl-3-ylsulfonyl)-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00035
-
4-[(4'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00036
-
4-[(3-bromophenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00046
-
4-[(2'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00049
-
4-[(3'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00061
-
4-[(2'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus
0.00185
-
4-[(3'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
Rattus norvegicus