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Literature summary extracted from

  • Vulpetti, A.; Ostermann, N.; Randl, S.; Yoon, T.; Mac Sweeney, A.; Cumin, F.; Lorthiois, E.; Ruedisser, S.; Erbel, P.; Maibaum, J.
    Discovery and design of first benzylamine-based ligands binding to an unlocked conformation of the complement factor D (2018), ACS Med. Chem. Lett., 9, 490-495 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.21.46 (1R,2S)-2-([4-[3-(aminomethyl)anilino]quinazolin-2-yl]amino)cyclohexane-1-carboxylic acid
-
 Homo sapiens
3.4.21.46 (2S)-2-([4-[3-(aminomethyl)anilino]pyrimidin-2-yl]amino)-3-methylbutanoic acid
-
 Homo sapiens
3.4.21.46 (2S)-2-([4-[3-(aminomethyl)anilino]quinazolin-2-yl]amino)-3-methylbutanoic acid
-
 Homo sapiens
3.4.21.46 1-(2-[(1R,3S,5R)-3-[(6-bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl)-1H-indazole-3-carboxamide
-
 Homo sapiens
3.4.21.46 1-[2-[(1R,3S,5R)-3-[[(1R)-1-(3-chloro-2-fluorophenyl)ethyl]carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
-
 Homo sapiens
3.4.21.46 3'-(aminomethyl)-5-(3-methylbutanamido)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)[1,1'-biphenyl]-3-carboxamide (incorrect configuration definition!)
-
 Homo sapiens
3.4.21.46 3'-(aminomethyl)-N-benzyl[1,1'-biphenyl]-3-carboxamide
-
 Homo sapiens
3.4.21.46 3'-(aminomethyl)-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl][1,1'-biphenyl]-3-carboxamide
-
 Homo sapiens
3.4.21.46 3'-(aminomethyl)-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl][1,1'-biphenyl]-3-carboxamide
-
 Homo sapiens
3.4.21.46 3-([3-[3-(aminomethyl)anilino]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino)phenol
-
 Homo sapiens
3.4.21.46 3-[[(2-carbamoyl-1H-indol-5-yl)oxy]methyl]benzoic acid
-
 Homo sapiens
3.4.21.46 methyl 2-([[(2S)-2-[[3-(trifluoromethoxy)phenyl]carbamoyl]pyrrolidine-1-carbonyl]amino]methyl)benzoate
-
 Homo sapiens
3.4.21.46 N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-2-phenylacetamide
-
 Homo sapiens
3.4.21.46 N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-3-methylbutanamide
-
 Homo sapiens
3.4.21.46 N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-3-phenylpropanamide
-
 Homo sapiens
3.4.21.46 N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]acetamide
-
 Homo sapiens
3.4.21.46 N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]benzamide
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.21.46 Homo sapiens P00746
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.21.46 benzyloxycarbonyl-Lys-thiobenzylester + H2O
-
 Homo sapiens ?
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.21.46 factor D
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.21.46 0.000006
-
 at pH 7.5 and 25°C Homo sapiens 1-(2-[(1R,3S,5R)-3-[(6-bromopyridin-2-yl)carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl)-1H-indazole-3-carboxamide
3.4.21.46 0.000017
-
 at pH 7.5 and 25°C Homo sapiens 1-[2-[(1R,3S,5R)-3-[[(1R)-1-(3-chloro-2-fluorophenyl)ethyl]carbamoyl]-2-azabicyclo[3.1.0]hexan-2-yl]-2-oxoethyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide
3.4.21.46 0.0034
-
 at pH 7.5 and 25°C Homo sapiens 3'-(aminomethyl)-5-(3-methylbutanamido)-N-(1,2,3,4-tetrahydronaphthalen-1-yl)[1,1'-biphenyl]-3-carboxamide (incorrect configuration definition!)
3.4.21.46 0.014
-
 at pH 7.5 and 25°C Homo sapiens methyl 2-([[(2S)-2-[[3-(trifluoromethoxy)phenyl]carbamoyl]pyrrolidine-1-carbonyl]amino]methyl)benzoate
3.4.21.46 0.02
-
 at pH 7.5 and 25°C Homo sapiens 3-([3-[3-(aminomethyl)anilino]-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino)phenol
3.4.21.46 0.043
-
 at pH 7.5 and 25°C Homo sapiens N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-2-phenylacetamide
3.4.21.46 0.044
-
 at pH 7.5 and 25°C Homo sapiens (2S)-2-([4-[3-(aminomethyl)anilino]pyrimidin-2-yl]amino)-3-methylbutanoic acid
3.4.21.46 0.054
-
 at pH 7.5 and 25°C Homo sapiens 3'-(aminomethyl)-N-[(1S)-1,2,3,4-tetrahydronaphthalen-1-yl][1,1'-biphenyl]-3-carboxamide
3.4.21.46 0.075
-
 at pH 7.5 and 25°C Homo sapiens (2S)-2-([4-[3-(aminomethyl)anilino]quinazolin-2-yl]amino)-3-methylbutanoic acid
3.4.21.46 0.084
-
 at pH 7.5 and 25°C Homo sapiens (1R,2S)-2-([4-[3-(aminomethyl)anilino]quinazolin-2-yl]amino)cyclohexane-1-carboxylic acid
3.4.21.46 0.098
-
 at pH 7.5 and 25°C Homo sapiens 3'-(aminomethyl)-N-[(1R)-1,2,3,4-tetrahydronaphthalen-1-yl][1,1'-biphenyl]-3-carboxamide
3.4.21.46 0.12
-
 at pH 7.5 and 25°C Homo sapiens N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-3-methylbutanamide
3.4.21.46 0.14
-
 at pH 7.5 and 25°C Homo sapiens N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]-3-phenylpropanamide
3.4.21.46 0.257
-
 at pH 7.5 and 25°C Homo sapiens N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]benzamide
3.4.21.46 0.31
-
 at pH 7.5 and 25°C Homo sapiens 3'-(aminomethyl)-N-benzyl[1,1'-biphenyl]-3-carboxamide
3.4.21.46 0.69
-
 at pH 7.5 and 25°C Homo sapiens N-[3'-(aminomethyl)[1,1'-biphenyl]-3-yl]acetamide