ChEMBL ligand: CHEMBL447664 (Biib014, BIIB-014, BIIB014, CEB-4520, V-2006, V2006, VER-11135, VER-A-00049, VER-A00049, VER-A-00-11, VER-A00-11, VER-ADO-49, Vipadenant)
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!
A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] There should be some charts here, you may need to enable JavaScript!
A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] 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	Antagonist activity at human adenosine A1 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	F	7	pKd	100	nM	Kd	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Displacement of radioligand from human recombinant adenosine A1 receptor at 21 degC after 90 mins by cell-based microplate scintillation counting	B	7.17	pKi	68	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Inhibition of human recombinant adenosine A1 receptor	B	7.17	pKi	68	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb	-	-	7.17	pKi	68	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Antagonist activity at human adenosine A2A receptor expressed in CHO-K1 cells treated for 15 mins by calcium mobilization-based FLIPR assay	F	9.2	pKd	0.63	nM	Kd	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Displacement of radioligand from human recombinant adenosine A2A receptor at 21 degC after 90 mins by cell-based microplate scintillation counting	B	8.89	pKi	1.3	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Inhibition of human recombinant adenosine receptor A2a	F	8.89	pKi	1.3	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb	-	-	8.89	pKi	1.3	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL	Antagonist activity at human adenosine A2B receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	F	7.5	pKd	31.62	nM	Kd	J Med Chem (2009) 52: 33-47 [PMID:19072055]
GtoPdb	-	-	7.2	pKi	63	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Displacement of radioligand from human recombinant adenosine A2B receptor at 21 degC after 60 mins by cell-based microplate scintillation counting	B	7.2	pKi	63	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Inhibition of human recombinant adenosine receptor A2b	B	7.2	pKi	63	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Antagonist activity at human adenosine A3 receptor expressed in CHO-K1 cells by calcium mobilization-based FLIPR assay	F	5.8	pKd	1584.89	nM	Kd	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Displacement of radioligand from human recombinant adenosine A3 receptor at 21 degC after 60 mins by cell-based microplate scintillation counting	B	6	pKi	1005	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Inhibition of human recombinant adenosine A3 receptor	B	6	pKi	1005	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
GtoPdb	-	-	6	pKi	1005	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]

ChEMBL data shown on this page come from version 33:

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]