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Literature summary for 2.4.2.30 extracted from

  • Lindgren, A.E.; Karlberg, T.; Ekblad, T.; Spjut, S.; Thorsell, A.G.; Andersson, C.D.; Nhan, T.T.; Hellsten, V.; Weigelt, J.; Linusson, A.; Schueler, H.; Elofsson, M.
    Chemical probes to study ADP-ribosylation: synthesis and biochemical evaluation of inhibitors of the human ADP-ribosyltransferase ARTD3/PARP3 (2013), J. Med. Chem., 56, 9556-9568.
    View publication on PubMed

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors, sitting drop vapor diffusion method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-[[3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoyl]amino]-3-phenylpropanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1R)-1-(pyridin-2-yl)ethyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1R)-1-phenylethyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-(pyridin-2-yl)ethyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-phenylpropyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(4-sulfamoylphenyl)ethyl]propanamide
-
Homo sapiens
3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(pyridin-2-yl)ethyl]propanamide
-
Homo sapiens
methyl (2S)-2-[[3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoyl]amino]-3-phenylpropanoate
-
Homo sapiens
N-[(1R)-2,3-dihydro-1H-inden-1-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens
N-[(1S)-2,3-dihydro-1H-inden-1-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens
N-[(2S)-1-hydroxy-3-phenylpropan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens
N-[(2S)-1-hydroxybutan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens
N-[(2S)-1-hydroxypropan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens
N-[1-[4-(1H-imidazol-1-yl)phenyl]ethyl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
NAD+ + (ADP-D-ribosyl)n-acceptor Homo sapiens
-
nicotinamide + (ADP-D-ribosyl)n+1-acceptor + H+
-
?

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9Y6F1
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
NAD+ + (ADP-D-ribosyl)n-acceptor
-
Homo sapiens nicotinamide + (ADP-D-ribosyl)n+1-acceptor + H+
-
?

Synonyms

Synonyms Comment Organism
ADP-ribosyltransferase
-
Homo sapiens
ADP-ribosyltransferase 3
-
Homo sapiens
ARTD3
-
Homo sapiens
PARP3
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0009
-
pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-phenylethyl]propanamide
0.001
-
pH and temperature not specified in the publication Homo sapiens N-[(2S)-1-hydroxy-3-phenylpropan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
0.0013
-
pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-(pyridin-2-yl)ethyl]propanamide
0.0022
-
pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1S)-1-phenylpropyl]propanamide
0.0022
-
pH and temperature not specified in the publication Homo sapiens methyl (2S)-2-[[3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoyl]amino]-3-phenylpropanoate
0.0038
-
pH and temperature not specified in the publication Homo sapiens (2S)-2-[[3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanoyl]amino]-3-phenylpropanamide
0.0096
-
pH and temperature not specified in the publication Homo sapiens N-[(2S)-1-hydroxybutan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
0.0111
-
pH and temperature not specified in the publication Homo sapiens N-[(2S)-1-hydroxypropan-2-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
0.0132
-
pH and temperature not specified in the publication Homo sapiens N-[1-[4-(1H-imidazol-1-yl)phenyl]ethyl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
0.0144
-
pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[1-(4-sulfamoylphenyl)ethyl]propanamide
0.0152
-
pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1R)-1-phenylethyl]propanamide
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens 3-(4-oxo-3,4-dihydroquinazolin-2-yl)-N-[(1R)-1-(pyridin-2-yl)ethyl]propanamide
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens N-[(1R)-2,3-dihydro-1H-inden-1-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide
0.1
-
IC50 above 0.1 mM, pH and temperature not specified in the publication Homo sapiens N-[(1S)-2,3-dihydro-1H-inden-1-yl]-3-(4-oxo-3,4-dihydroquinazolin-2-yl)propanamide