ChEMBL ligand: CHEMBL2105747 (A-2A (3), A2A (3), A2A-(3), RO-4494351, RO4494351, RO-4494351-000, RO-4494351000, RO4494351-000, RO-4494351-002, RO4494351-002, SYN-115, SYN115, Tozadenant)
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] A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] 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	Displacement of [3H]-DPCPX from recombinant human A1 receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method	B	5.47	pKi	3380	nM	Ki	Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636]
ChEMBL	Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay	B	5.65	pKi	2240	nM	Ki	Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
ChEMBL	Displacement of [3H]-DPCPX from human adenosine A1 receptor expressed in HEK293 cell membranes measured after 90 mins	B	5.77	pKi	1700	nM	Ki	J Med Chem (2017) 60: 681-694 [PMID:28055204]
ChEMBL	Antagonist activity at human adenosine A1 receptor	F	5.77	pKi	1700	nM	Ki	Eur J Med Chem (2022) 237: 114378-114378 [PMID:35462165]
ChEMBL	Inhibition of human recombinant adenosine A1 receptor	B	5.87	pKi	1350	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Inhibition of human adenosine A1 receptor	B	5.87	pKi	1350	nM	Ki	J Med Chem (2020) 63: 12196-12212 [PMID:32667814]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membranes measured after 90 mins	B	7.96	pKi	11	nM	Ki	J Med Chem (2017) 60: 681-694 [PMID:28055204]
ChEMBL	Antagonist activity at human adenosine A2A receptor	F	7.96	pKi	11	nM	Ki	Eur J Med Chem (2022) 237: 114378-114378 [PMID:35462165]
ChEMBL	Displacement of [3H]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay	B	8.08	pKi	8.3	nM	Ki	Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
GtoPdb	-	-	8.3	pKi	5	nM	Ki	J Med Chem (2014) 57: 3623-50 [PMID:24164628]
ChEMBL	Antagonist activity at human adenosine 2A receptor (409 to 412 residues) expressed in CHO cells using Ysi-poly-1-lysine as substrate incubated for 1 hr in presence of 3H-SCH-58261 by scintillation counting method	B	8.3	pKi	5	nM	Ki	J Med Chem (2020) 63: 12196-12212 [PMID:32667814]
ChEMBL	Inhibition of human recombinant adenosine receptor A2a	F	8.3	pKi	5	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Antagonist activity at adenosine A2A receptor (unknown origin)	F	8.3	pKi	5	nM	Ki	Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
ChEMBL	Displacement of [3H]-ZM241385 from recombinant human A2A receptor expressed in CHO-K1 cells incubated for 70 mins by liquid scintillation counting method	B	8.41	pKi	3.9	nM	Ki	Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636]
ChEMBL	Binding affinity to human adenosine A2A receptor measured by radioligand-based affinity assay	B	8.47	pKi	3.4	nM	Ki	Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
ChEMBL	Antagonist activity at human adenosine A2A receptor expressed in HEK293 cell membranes assessed as decrease in CGS-21680/forskolin-induced cAMP level pretreated for 15 mins followed by agonist addition for 30 mins and subsequent forskolin stimulation measured after 30 mins	F	9.52	pKi	0.3	nM	Ki	J Med Chem (2017) 60: 681-694 [PMID:28055204]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Displacement of [3H]-ZM241385 from A2A receptor in rat brain corpora striata incubated for 70 mins by liquid scintillation counting method	B	7.73	pKi	18.7	nM	Ki	Eur J Med Chem (2021) 214: 113214-113214 [PMID:33548636]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL	Displacement of [3H]-MRS-1754 from human adenosine A2B receptor expressed in HEK293 cell membranes measured after 90 mins	B	5.3	pKi	5000	nM	Ki	J Med Chem (2017) 60: 681-694 [PMID:28055204]
ChEMBL	Inhibition of human recombinant adenosine receptor A2b	B	6.15	pKi	700	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Inhibition of human adenosine 2B receptor	B	6.15	pKi	700	nM	Ki	J Med Chem (2020) 63: 12196-12212 [PMID:32667814]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Displacement of [3H]-HEMADO from human adenosine A3 receptor expressed in HEK293 cell membranes measured after 90 mins	B	5.3	pKi	5000	nM	Ki	J Med Chem (2017) 60: 681-694 [PMID:28055204]
ChEMBL	Inhibition of human recombinant adenosine A3 receptor	B	5.8	pKi	1570	nM	Ki	J Med Chem (2014) 57: 3623-3650 [PMID:24164628]

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]