CGS 15943   Click here for help

GtoPdb Ligand ID: 384

Synonyms: CGS 15943A | CGS-15943 | CGS15943
PDB Ligand
Compound class: Synthetic organic
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 4
Hydrogen bond donors 1
Rotatable bonds 1
Topological polar surface area 82.24
Molecular weight 285.04
XLogP 2.53
No. Lipinski's rules broken 0
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Canonical SMILES Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1
Isomeric SMILES Clc1ccc2c(c1)c1nc(nn1c(n2)N)c1ccco1
InChI InChI=1S/C13H8ClN5O/c14-7-3-4-9-8(6-7)12-17-11(10-2-1-5-20-10)18-19(12)13(15)16-9/h1-6H,(H2,15,16)
1. Alexander SP, Cooper J, Shine J, Hill SJ. (1996)
Characterization of the human brain putative A2B adenosine receptor expressed in Chinese hamster ovary (CHO.A2B4) cells.
Br J Pharmacol, 119 (6): 1286-90. [PMID:8937736]
2. Auchampach JA, Kreckler LM, Wan TC, Maas JE, van der Hoeven D, Gizewski E, Narayanan J, Maas GE. (2009)
Characterization of the A2B adenosine receptor from mouse, rabbit, and dog.
J Pharmacol Exp Ther, 329 (1): 2-13. [PMID:19141710]
3. Dionisotti S, Ongini E, Zocchi C, Kull B, Arslan G, Fredholm BB. (1997)
Characterization of human A2A adenosine receptors with the antagonist radioligand [3H]-SCH 58261.
Br J Pharmacol, 121 (3): 353-60. [PMID:9179373]
4. Ji X, Kim YC, Ahern DG, Linden J, Jacobson KA. (2001)
[3H]MRS 1754, a selective antagonist radioligand for A(2B) adenosine receptors.
Biochem Pharmacol, 61 (6): 657-63. [PMID:11266650]
5. Ji XD, Jacobson KA. (1999)
Use of the triazolotriazine [3H]ZM 241385 as a radioligand at recombinant human A2B adenosine receptors.
Drug Des Discov, 16 (3): 217-26. [PMID:10624567]
6. Kim J, Wess J, van Rhee AM, Schöneberg T, Jacobson KA. (1995)
Site-directed mutagenesis identifies residues involved in ligand recognition in the human A2a adenosine receptor.
J Biol Chem, 270 (23): 13987-97. [PMID:7775460]
7. Kim YC, Ji XD, Jacobson KA. (1996)
Derivatives of the triazoloquinazoline adenosine antagonist (CGS15943) are selective for the human A3 receptor subtype.
J Med Chem, 39 (21): 4142-8. [PMID:8863790]
8. Klotz KN, Hessling J, Hegler J, Owman C, Kull B, Fredholm BB, Lohse MJ. (1998)
Comparative pharmacology of human adenosine receptor subtypes - characterization of stably transfected receptors in CHO cells.
Naunyn Schmiedebergs Arch Pharmacol, 357 (1): 1-9. [PMID:9459566]
9. Müller CE. (2000)
A2A Adenosine receptor antagonists—future drugs for Parkinson’s disease?.
Drugs Future, (25): 1043-1052.
10. Ongini E, Dionisotti S, Gessi S, Irenius E, Fredholm BB. (1999)
Comparison of CGS 15943, ZM 241385 and SCH 58261 as antagonists at human adenosine receptors.
Naunyn Schmiedebergs Arch Pharmacol, 359 (1): 7-10. [PMID:9933143]
11. Stewart M, Steinig AG, Ma C, Song JP, McKibben B, Castelhano AL, MacLennan SJ. (2004)
[3H]OSIP339391, a selective, novel, and high affinity antagonist radioligand for adenosine A2B receptors.
Biochem Pharmacol, 68 (2): 305-12. [PMID:15194002]
12. Varani K, Merighi S, Gessi S, Klotz KN, Leung E, Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Borea PA. (2000)
[(3)H]MRE 3008F20: a novel antagonist radioligand for the pharmacological and biochemical characterization of human A(3) adenosine receptors.
Mol Pharmacol, 57 (5): 968-75. [PMID:10779381]