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Literature summary for 3.1.3.5 extracted from

  • Rahimova, R.; Fontanel, S.; Lionne, C.; Jordheim, L.P.; Peyrottes, S.; Chaloin, L.
    Identification of allosteric inhibitors of the ecto-5'-nucleotidase (CD73) targeting the dimer interface (2018), PLoS Comput. Biol., 14, e1005943 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.1.3.5

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 insect cells Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(2E)-5-(5-methylfuran-2-yl)-N-(2-methylphenyl)-3-oxo-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidine-6-carboxamide 67% inhibition at 0.005 mM Homo sapiens
(2Z)-2-[[3-(3-fluoro-4-methoxyphenyl)-1-phenyl-1H-pyrazol-4-yl]methylidene]-6-[(4-methylphenyl)methyl]-7H-[1,3]thiazolo[3,2-b][1,2,4]triazine-3,7(2H)-dione 61% inhibition at 0.005 mM Homo sapiens
2,3,5-tri-O-benzyl-1-O-(4-nitrobenzoyl)-D-arabinofuranose 68% inhibition at 0.005 mM Homo sapiens
2-((4'-cyano-4,4''-dimethoxy-[1,1':3',1''-terphenyl]-5'-yl)thio)-N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)acetamide 73% inhibition at 0.005 mM Homo sapiens
2-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[4-[1-(4-methylbenzoyl)-2,3-dihydro-1H-indol-5-yl]-5-sulfanyl-1,3-thiazol-2-yl]acetamide 74% inhibition at 0.005 mM Homo sapiens
3-[4,5-di([1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl]-1H-indole 93% inhibition at 0.005 mM Homo sapiens
4-(4-[1-[(3-chlorophenyl)methyl]-4-hydroxy-1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl]piperidine-1-sulfonyl)-N-cycloheptylbenzene-1-sulfonamide 63% inhibition at 0.005 mM Homo sapiens
4-(6-[[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methyl]-1H-benzimidazol-2-yl)aniline 78% inhibition at 0.005 mM Homo sapiens
6-(4-ethoxyphenyl)-3-(4-methylphenyl)-N-(2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide 65% inhibition at 0.005 mM Homo sapiens
ADP competitive inhibitor Homo sapiens
alpha,beta-methylene-ADP competitive inhibitor Homo sapiens
ATP competitive inhibitor Homo sapiens
ethyl 4-(2-((4'-cyano-4''-methoxy-4-methyl-[1,1':3',1''-terphenyl]-5'-yl)thio)acetamido)benzoate 80% inhibition at 0.005 mM Homo sapiens
MEDI9447 non-competitive inhibitor Homo sapiens
N-(4-methylcyclohexyl)-1-(2-phenyl-1H-benzimidazole-5-sulfonyl)piperidine-3-carboxamide 17% inhibition at 0.005 mM Homo sapiens
N-[4-[5-([2-[2-(4-methoxybenzoyl)hydrazinyl]-2-oxoethyl]sulfanyl)-4-(4-methoxyphenyl)-4H-1,2,4-triazol-3-yl]phenyl]-4-methylbenzene-1-sulfonamide 64% inhibition at 0.005 mM Homo sapiens

Localization

Localization Comment Organism GeneOntology No. Textmining
cell surface
-
 Homo sapiens 9986
-
extracellular
-
 Homo sapiens
-
-

Organism

Organism UniProt Comment Textmining
Homo sapiens P21589
-
-

Purification (Commentary)

Purification (Comment) Organism
HisTrap column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5'-AMP + H2O
-
 Homo sapiens adenosine + phosphate
-
 ?

Synonyms

Synonyms Comment Organism
CD73
-
 Homo sapiens
ecto-5'-nucleotidase
-
 Homo sapiens

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00046
-
 4-(4-[1-[(3-chlorophenyl)methyl]-4-hydroxy-1H-[1,2,3]triazolo[4,5-c]pyridin-6-yl]piperidine-1-sulfonyl)-N-cycloheptylbenzene-1-sulfonamide at pH 7.0 and 37°C Homo sapiens
0.00053
-
 3-[4,5-di([1,1'-biphenyl]-4-yl)-1H-imidazol-2-yl]-1H-indole at pH 7.0 and 37°C Homo sapiens
0.00068
-
 ethyl 4-(2-((4'-cyano-4''-methoxy-4-methyl-[1,1':3',1''-terphenyl]-5'-yl)thio)acetamido)benzoate at pH 7.0 and 37°C Homo sapiens
0.0012
-
 2-((4'-cyano-4,4''-dimethoxy-[1,1':3',1''-terphenyl]-5'-yl)thio)-N-(3-cyano-4,5,6,7-tetrahydrobenzo[b]thiophen-2-yl)acetamide at pH 7.0 and 37°C Homo sapiens
0.00122
-
 2-(3,4-dihydroisoquinolin-2(1H)-yl)-N-[4-[1-(4-methylbenzoyl)-2,3-dihydro-1H-indol-5-yl]-5-sulfanyl-1,3-thiazol-2-yl]acetamide at pH 7.0 and 37°C Homo sapiens
0.0013
-
 (2E)-5-(5-methylfuran-2-yl)-N-(2-methylphenyl)-3-oxo-2-(2-oxo-1,2-dihydro-3H-indol-3-ylidene)-2,3-dihydro-5H-[1,3]thiazolo[3,2-a]pyrimidine-6-carboxamide at pH 7.0 and 37°C Homo sapiens
0.0027
-
 6-(4-ethoxyphenyl)-3-(4-methylphenyl)-N-(2-phenylethyl)-1H-pyrazolo[3,4-b]pyridine-4-carboxamide at pH 7.0 and 37°C Homo sapiens
0.0049
-
 N-[4-[5-([2-[2-(4-methoxybenzoyl)hydrazinyl]-2-oxoethyl]sulfanyl)-4-(4-methoxyphenyl)-4H-1,2,4-triazol-3-yl]phenyl]-4-methylbenzene-1-sulfonamide at pH 7.0 and 37°C Homo sapiens
0.0061
-
 4-(6-[[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methyl]-1H-benzimidazol-2-yl)aniline at pH 7.0 and 37°C Homo sapiens
0.00939
-
 N-(4-methylcyclohexyl)-1-(2-phenyl-1H-benzimidazole-5-sulfonyl)piperidine-3-carboxamide at pH 7.0 and 37°C Homo sapiens
0.0172
-
 2,3,5-tri-O-benzyl-1-O-(4-nitrobenzoyl)-D-arabinofuranose at pH 7.0 and 37°C Homo sapiens