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Complex Information

Proteins used in this complex:


Adenosine receptor A2a (Homo sapiens)

Orthosteric ligand(s) in this complex:





Kd values:


Kd according to BindingDB: 632.0 nM Original page


Kd according to BindingDB: 4.4 nM Original page


Kd according to BindingDB: 4.4 nM Original page


Kd according to BindingDB: 4.4 nM Original page


Kd according to BindingDB: 7.6 nM Original page


Kd according to BindingDB: 27.0 nM Original page


Kd according to BindingDB: 7.6 nM Original page


Kd according to BindingDB: 74.0 nM Original page


Kd according to BindingDB: 4.3 nM Original page


Kd according to BindingDB: 12.0 nM Original page


Kd according to BindingDB: 99.0 nM Original page


Kd according to BindingDB: 36.0 nM Original page


Kd according to BindingDB: 22.0 nM Original page



Efficacy values:


EC50 according to BindingDB: 18.0 nM Original page


EC50 according to BindingDB: 18.0 nM Original page



Complex structures in which this complex is used:



Complex Structure ID: 43 using Specific State(s): Specific State ID: 5043




References for this complex:


Preti, D; Baraldi, PG; Saponaro, G; Romagnoli, R; Aghazadeh Tabrizi, M; Baraldi, S; Cosconati, S; Bruno, A; Novellino, E; Vincenzi, F; Ravani, A; Borea, PA; Varani, K. 2015. Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.. Journal of medicinal chemistry 58 (7). doi: 10.1021/acs.jmedchem.5b00215. Available in: Pubmed Link




Preti, D; Baraldi, PG; Saponaro, G; Romagnoli, R; Aghazadeh Tabrizi, M; Baraldi, S; Cosconati, S; Bruno, A; Novellino, E; Vincenzi, F; Ravani, A; Borea, PA; Varani, K. 2015. Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.. Journal of medicinal chemistry 58 (7). doi: 10.1021/acs.jmedchem.5b00215. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Moss, SM; Jayasekara, PS; Paoletta, S; Gao, ZG; Jacobson, KA. 2014. Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.. ACS medicinal chemistry letters 5 (9). doi: 10.1021/ml5002486. Available in: Pubmed Link




Moss, SM; Jayasekara, PS; Paoletta, S; Gao, ZG; Jacobson, KA. 2014. Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.. ACS medicinal chemistry letters 5 (9). doi: 10.1021/ml5002486. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link




Jiang, Q; Lee, BX; Glashofer, M; van Rhee, AM; Jacobson, KA. 1997. Mutagenesis reveals structure-activity parallels between human A2A adenosine receptors and biogenic amine G protein-coupled receptors.. Journal of medicinal chemistry 40 (16). doi: 10.1021/jm970084v. Available in: Pubmed Link





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