3.4.21.42: complement subcomponent C1s
This is an abbreviated version!
For detailed information about complement subcomponent C1s, go to the full flat file.
Word Map on EC 3.4.21.42
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3.4.21.42
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angioedema
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hereditary
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lectin
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c1-inh
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edema
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swell
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mannose-binding
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masp-1
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mannan-binding
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coagulation
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kallikrein
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airway
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prophylaxis
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abdominal
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bradykinin
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life-threatening
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laryngeal
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angioneurotic
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lectin-associated
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c1-inhibitor
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danazol
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prophylactic
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ficolins
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plasma-derived
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urticaria
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icatibant
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antithrombin
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submucosal
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kinin
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fibrinolysis
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larynx
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kallikrein-kinin
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asphyxiation
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antifibrinolytic
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prekallikrein
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2-antiplasmin
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ecallantide
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2-macroglobulin
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tranexamic
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kininogens
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antihistamine
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pharmacology
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bradykinin-mediated
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serping1
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collectins
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behring
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c4d
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medicine
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collagen-like
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drug development
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tracheotomy
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fibrinogen-like
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stanozolol
- 3.4.21.42
- angioedema
- hereditary
- lectin
-
c1-inh
- edema
-
swell
-
mannose-binding
- masp-1
-
mannan-binding
-
coagulation
- kallikrein
-
airway
-
prophylaxis
- abdominal
- bradykinin
-
life-threatening
- laryngeal
-
angioneurotic
-
lectin-associated
- c1-inhibitor
- danazol
-
prophylactic
- ficolins
-
plasma-derived
- urticaria
- icatibant
- antithrombin
-
submucosal
- kinin
-
fibrinolysis
- larynx
-
kallikrein-kinin
-
asphyxiation
-
antifibrinolytic
- prekallikrein
-
2-antiplasmin
- ecallantide
-
2-macroglobulin
-
tranexamic
- kininogens
-
antihistamine
- pharmacology
-
bradykinin-mediated
-
serping1
-
collectins
-
behring
- c4d
- medicine
-
collagen-like
- drug development
-
tracheotomy
-
fibrinogen-like
-
stanozolol
Reaction
Cleavage of Arg-/-Ala bond in complement component C4 to form C4a and C4b, and Lys(or Arg)-/-Lys bond in complement component C2 to form C2a and C2b: the "classical" pathway C3 convertase =
Synonyms
activated complement C1s, C1 esterase, C1-esterase, C1g, C1s, C1s protease, C1s serine protease, complement 1s, complement C.hivin. 1s, complement C1s, complement C1s, activated, complement component 1 s, complement component 1 subcomponent s, complement component C1s, complement protease, complement protease C1s, complement subcomponent 1s, complement subcomponent C1sbar, esterase, C1, mannan-binding lectin-associated serine protease-2, MASP-2, MBL-associated serine protease-2, multiprotein complex C1, protease C1s, serine protease C1s
ECTree
3.4.21.42 complement subcomponent C1sAdvanced search results
results (
results (Inhibitors
Inhibitors on EC 3.4.21.42 - complement subcomponent C1s
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INHIBITOR 
ORGANISM
UNIPROT
COMMENTARY 
LITERATURE
IMAGE
2-bromo-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-2-methylbiphenyl-4-yl)acetamide
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2-bromo-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)acetamide
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3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-carboxylic acid
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4-(biphenyl-3-ylsulfonyl)-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-chloro-3-(3-isothiureidopropoxy)isocoumarin
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best inhibitor among substituted isocoumarins
4-[(2'-chlorobiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(2'-ethenylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(2'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(2'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(2-amino-6-methylphenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(3'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(3'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(3'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(3-bromophenyl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(4'-hydroxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(4'-methoxybiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(4'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[[2'-(hydroxymethyl)-6'-methylbiphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[[2'-(hydroxymethyl)biphenyl-3-yl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[[3-(3-methylpyridin-2-yl)phenyl]sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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5-(methylsulfanyl)-4-[[2'-methyl-6'-([[2-(2H-tetrazol-5-yl)ethyl]carbamoyl]amino)biphenyl-3-yl]sulfonyl]thiophene-2-carboximidamide
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6-[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)amino]-6-oxohexanoic acid
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6-[[(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)carbamoyl]amino]hexanoic acid
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C-1 esterase inhibitor
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main inhibitor of C1r and C1s of the complement system
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human C1-esterase inhibitor
C1-INH, a multifunctional plasma protein with a wide range of inhibitory and non-inhibitory properties, mainly recognized as a key downregulator of the complement and contact cascades. Potentiation of C1-INH by heparin and other glycosaminoglycans regulating a broad spectrum of C1-INH activities in vivo both in normal and disease states, interaction analysis via double capture SPR approach, surface plasmon resonance (using a CM5 sensor chip through amine coupling) and circular dichroism, overview. Heparin binding does not alter C1-INH secondary structure and does not affect the amidolytic activity of C1s, but does accelerate its consumption due to C1-INH potentiation
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N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-2-(methylsulfonyl)acetamide
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N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)-4-(methylsulfonyl)butanamide
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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
N-PEG2000 N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)-2,3-dihydrothiophen-3-yl]sulfonyl]-6-methylbiphenyl-2-yl)dodecanediamide
PEG size 20 kDa
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
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
N-PEG750 2-[(2-amino-2-oxoethyl)sulfanyl]-N-(3'-[[5-carbamimidoyl-2-(methylsulfanyl)thiophen-3-yl]sulfonyl]-2-methylbiphenyl-4-yl)acetamide
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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
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
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)
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PEG-linked tetrakis(4-[[4'-carbamimidamido-2'-(carbamoylamino)biphenyl-3-yl]sulfanyl]-5-(methylsulfanyl)thiophene-2-carboximidamide)
PEG size 20 kDa
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tert-butyl [[4-[(3-bromophenyl)sulfonyl]-5-(methylsulfanyl)thiophen-2-yl](imino)methyl]carbamate
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binding mode in the active site, structure, overview
TNT003
a mouse monoclonal antibody targeting the CP-specific serine protease C1s. TNT003 prevents cold agglutinin-mediated deposition of complement opsonins that promote phagocytosis of red blood cells. By preventing classical pathway activation, TNT003 also prevents cold agglutinin-driven generation of anaphylatoxins
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unconjugated bilirubin
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inhibits C1 esterase activity at pathological concentrations (above 17 micromol) and in a dose-dependent manner, due to a direct pigment-protein interaction. Maximal inhibitory activity is reached at an 85 micromol concentration. Inhibitory action exerted by unconjugated bilirubin on the classical pathway is not only due to an impairment of the interaction of the C1q subcomponent with IgM or IgG but also to a diminished enzymatic activity of the C1 esterase
4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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4-[(2'-methylbiphenyl-3-yl)sulfonyl]-5-(methylsulfanyl)thiophene-2-carboximidamide
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C1 esterase inhibitor
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severe abdominal attacks are effectively reverted with C1 inhibitor plasma concentrate
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C1 esterase inhibitor
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C1 esterase inhibitor inhibits components of the complement (specifically C1r and C1s), C1 esterase inhibitor concentrate given intravenously at a dose of 20 units/kg is an effective and safe treatment for acute abdominal and facial attacks in patients with hereditary angioedema
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C1 esterase inhibitor
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administration of C1 esterase inhibitor with factor XIII and of N-acetylcysteine with tirilazad mesylate both results in reduced leucocyte adherence and reduced levels of interleukin-1beta, but increases interleukin-6 levels
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C1-esterase inhibitor
inhibitory effect is increased by addition of heparin (5-500 nM)
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C1s-INH-248
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highly selective small molecule inhibitor. Blocking the classical complement pathway with a highly specific and potent synthetic inhibitor of the classical C1 complex appears to be an effective mean to preserve ischemic myocardium from injury following reperfusion
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C1s-INH-248
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highly selective small molecule inhibitor. Blocking the classical complement pathway with a highly specific and potent synthetic inhibitor of the classical C1 complex appears to be an effective mean to preserve ischemic myocardium from injury following reperfusion
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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
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additional information
engineering of a potenthuman antibody inhibitor of C1s protease activity, inhibition of recombinnat enzyme fragment CCP2-SP, overview. The C1 complex is a very attractive target for selective inhibition of the classical complement pathway because it is the only member of the classical pathway that does not participate in the other complement pathways
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additional information
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engineering of a potenthuman antibody inhibitor of C1s protease activity, inhibition of recombinnat enzyme fragment CCP2-SP, overview. The C1 complex is a very attractive target for selective inhibition of the classical complement pathway because it is the only member of the classical pathway that does not participate in the other complement pathways
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