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Literature summary for 2.7.1.20 extracted from

  • Toti, K.S.; Osborne, D.; Ciancetta, A.; Boison, D.; Jacobson, K.A.
    South (S)- and north (N)-methanocarba-7-deazaadenosine analogues as inhibitors of human adenosine kinase (2016), J. Med. Chem., 59, 6860-6877 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 2.7.1.20

Inhibitors

Inhibitors Comment Organism Structure
(1R,2R,3S,4R,5S)-4-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 82.5% inhibition Homo sapiens
(1R,2R,3S,4R,5S)-4-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 85.4% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(aminomethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 50.9% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(azidomethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 80.5% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 58.2% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-anilino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 85.1% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 88.3% inhibition Homo sapiens
(1R,2S,3R,4R,5S)-1-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 76.5% inhibition Homo sapiens
(1R,2S,3R,4S,5S)-1-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-methylbicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 88.1% inhibition Homo sapiens
(1R,2S,3R,4S,5S)-1-[4-(4-fluoroanilino)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-4-methylbicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 86.9% inhibition Homo sapiens
(1R,2S,3R,4S,5S)-1-[4-anilino-5-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-4-methylbicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 78.4% inhibition Homo sapiens
(1R,2S,3R,4S,5S)-4-amino-1-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)bicyclo[3.1.0]hexane-2,3-diol 0.05 mM, 60.4% inhibition Homo sapiens
(1S,2R,3S,5R)-3-amino-5-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol 0.05 mM, 88.4% inhibition Homo sapiens
5-iodo-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine 0.05 mM, 88.3% inhibition Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
ATP + adenosine Homo sapiens
-
 ADP + AMP
-
 ?

Organism

Organism UniProt Comment Textmining
Homo sapiens P55263
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + adenosine
-
 Homo sapiens ADP + AMP
-
 ?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000048
-
 37°C, pH not specified in the publication Homo sapiens (1S,2R,3S,5R)-3-amino-5-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)cyclopentane-1,2-diol
0.000088
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4S,5S)-1-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-methylbicyclo[3.1.0]hexane-2,3-diol
0.00011
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4S,5S)-1-[4-(4-fluoroanilino)-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-4-methylbicyclo[3.1.0]hexane-2,3-diol
0.000114
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4R,5S)-1-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol
0.000115
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4S,5S)-1-[4-anilino-5-(4-fluorophenyl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]-4-methylbicyclo[3.1.0]hexane-2,3-diol
0.00014
-
 37°C, pH not specified in the publication Homo sapiens (1R,2R,3S,4R,5S)-4-(4-anilino-5-phenyl-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol
0.00082
-
 37°C, pH not specified in the publication Homo sapiens 5-iodo-7-beta-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine
0.00224
-
 37°C, pH not specified in the publication Homo sapiens (1R,2R,3S,4R,5S)-4-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-1-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol
0.00334
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4R,5S)-1-(4-anilino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol
0.00538
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4R,5S)-1-(4-amino-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(azidomethyl)bicyclo[3.1.0]hexane-2,3-diol
0.00601
-
 37°C, pH not specified in the publication Homo sapiens (1R,2S,3R,4R,5S)-1-(4-chloro-5-iodo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-4-(hydroxymethyl)bicyclo[3.1.0]hexane-2,3-diol

General Information

General Information Comment Organism
drug target adenosine kinase inhibitors raise endogenous adenosine levels, particularly in disease states, and have potential for treatment of seizures, neurodegeneration, and inflammation Homo sapiens