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Literature summary for 3.4.21.42 extracted from

  • Subasinghe, N.L.; Khalil, E.; Travins, J.M.; Ali, F.; Ballentine, S.K.; Hufnagel, H.R.; Pan, W.; Leonard, K.; Bone, R.F.; Soll, R.M.; Crysler, C.S.; Ninan, N.; Kirkpatrick, J.; Kolpak, M.X.; Diloreto, K.A.; Eisennagel, S.H.; Huebert, N.D.; Molloy, C.J.; Tomczuk, B.E.; Gaul, M.D.
    Design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s (2012), Bioorg. Med. Chem. Lett., 22, 5303-5307.
    View publication on PubMed
Search for more literature for 3.4.21.42

Inhibitors

Inhibitors Comment Organism Structure
2-bromo-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-2-methylbiphenyl-4-yl)acetamide
-
 Homo sapiens
2-bromo-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide
-
 Homo sapiens
4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
-
 Homo sapiens
additional information design and synthesis of polyethylene glycol-modified biphenylsulfonyl-thiophene-carboxamidine inhibitors of the complement component C1s, overview. Pegylation strategy to improve the pharmacokinetic properties of a potent C1s inhibitor 9. Analysis of the structure-activity relationship studies on the small molecule 1 Homo sapiens
N-PEG2000 6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide PEG size 20 kDa Homo sapiens
N-PEG2000 N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)dodecanediamide PEG size 20 kDa Homo sapiens
N-PEG4000 6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide PEG size 40 kDa Homo sapiens
N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide PEG size 10 kDa; PEG size 20 kDa Homo sapiens
N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-2-methylbiphenyl-4-yl)acetamide
-
 Homo sapiens
N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide PEG size 0.75 kDa Homo sapiens
PEG-linked bis(6-[[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide) PEG size 20 kDa Homo sapiens
PEG-linked bis(N-[6-amino-5-[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)amino]hept-6-en-1-yl]-6-[[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfanyl]biphenyl-2-yl)carbamoyl]amino]hexanamide)
-
 Homo sapiens
PEG-linked tetrakis(4-[[4'-carbamimidamido-2'-(carbamoylamino)biphenyl-3-yl]sulfanyl]-5-(methylsulfanyl)thiophene-2-carboximidamide) PEG size 20 kDa Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P09871
-
-

Synonyms

Synonyms Comment Organism
complement component C1s
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000018
-
 PEG-linked bis(N-[6-amino-5-[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)amino]hept-6-en-1-yl]-6-[[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfanyl]biphenyl-2-yl)carbamoyl]amino]hexanamide) pH and temperature not specified in the publication Homo sapiens
0.000029
-
 PEG-linked tetrakis(4-[[4'-carbamimidamido-2'-(carbamoylamino)biphenyl-3-yl]sulfanyl]-5-(methylsulfanyl)thiophene-2-carboximidamide) pH and temperature not specified in the publication Homo sapiens
0.00003
-
 4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide pH and temperature not specified in the publication Homo sapiens
0.000039
-
 PEG-linked bis(6-[[(4-carbamimidamido-3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide) pH and temperature not specified in the publication Homo sapiens
0.000055
-
 N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide pH and temperature not specified in the publication Homo sapiens
0.00006
-
 N-PEG2000 N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)dodecanediamide pH and temperature not specified in the publication Homo sapiens
0.000079
-
 N-PEG2000 6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide pH and temperature not specified in the publication Homo sapiens
0.000095
-
 N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide pH and temperature not specified in the publication Homo sapiens
0.00026
-
 N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-2-methylbiphenyl-4-yl)acetamide pH and temperature not specified in the publication Homo sapiens
0.00027
-
 N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide pH and temperature not specified in the publication Homo sapiens
0.000365
-
 N-PEG4000 6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanamide pH and temperature not specified in the publication Homo sapiens