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]
ChEMBL	Antagonist activity at adenosine A2A receptor (unknown origin)	F	8.89	pKi	1.3	nM	Ki	Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
GtoPdb	-	-	8.89	pKi	1.3	nM	Ki	J Med Chem (2009) 52: 33-47 [PMID:19072055]
ChEMBL	Displacement of [3H]SCH5826 from human A2AAR incubated for 60 mins by scintillation counter analysis	B	9.1	pKi	0.79	nM	Ki	Eur J Med Chem (2022) 236: 114326-114326 [PMID:35390714]
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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]