2-phenylethylyl-adenosine derivative | Ligand Activity Charts

2-phenylethylyl-adenosine derivative [Ligand Id: 5600] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL574602
A₁ receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] There should be some charts here, you may need to enable JavaScript!
A_2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] There should be some charts here, you may need to enable JavaScript!
A₃ receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
A₁ receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL	Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells	B	4.48	pKi	32800	nM	Ki	J Med Chem (2009) 52: 7897-7900 [PMID:19839592]
A_2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells	B	4.38	pKi	41700	nM	Ki	J Med Chem (2009) 52: 7897-7900 [PMID:19839592]
A₃ receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells	B	9.36	pKi	0.44	nM	Ki	J Med Chem (2009) 52: 7897-7900 [PMID:19839592]
ChEMBL	Binding affinity to human A3AR assessed as inhibitor constant	B	9.36	pKi	0.44	nM	Ki	ACS Med Chem Lett (2020) 11: 1935-1941 [PMID:33062176]
GtoPdb	-	-	9.36	pKi	0.44	nM	Ki	J Med Chem (2009) 52: 7897-900 [PMID:19839592]
ChEMBL	Binding affinity to human adenosine A3 receptor	B	9.36	pKi	0.44	nM	Ki	Bioorg Med Chem (2010) 18: 7923-7930 [PMID:20943397]
ChEMBL	Agonist activity at human recombinant adenosine A3 receptor expressed in CHO cells assessed as nonradiaoactive DELFIA Eu-GTP binding treated for 15 mins before addition of Eu-GTP measured after 45 mins by time-resolved fluorometric method	B	6.82	pEC50	151	nM	EC50	J Med Chem (2009) 52: 7897-7900 [PMID:19839592]

ChEMBL data shown on this page come from version 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]