ChEMBL ligand: CHEMBL260331
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	Binding affinity towards human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX	B	6.61	pKi	248	nM	Ki	Bioorg Med Chem Lett (2004) 14: 3611-3614 [PMID:15177485]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	6.7	pKi	200	nM	Ki	Bioorg Med Chem (2008) 16: 2419-2430 [PMID:18077171]
ChEMBL	Displacement of specific [3H]DPCPX binding at human adenosine A1 receptor expressed in CHO cells	B	6.7	pKi	200	nM	Ki	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Antagonist activity against human adenosine A1 receptor	F	6.7	pKi	200	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells after 120 mins by scintillation counting	B	6.7	pKi	200	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	6.7	pKi	200	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	6.7	pKi	200	nM	Ki	J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
GtoPdb	-	-	6.7	pKi	-	-	-	Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]; J Med Chem (2004) 47: 1434-47 [PMID:14998332]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb	-	-	6	pKi	>1000	nM	Ki	J Med Chem (2004) 47: 1434-47 [PMID:14998332]
ChEMBL	Binding affinity of compound for displacement of specific [3H]ZM-241385 binding at human adenosine A2A receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem (2008) 16: 2419-2430 [PMID:18077171]
ChEMBL	Binding affinity to human adenosine A2A receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Antagonist activity against human adenosine A2A receptor	F	6	pKi	>1000	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL	Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in CHO cells after 120 mins by scintillation counting	B	6	pKi	>1000	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Binding affinity to human adenosine A2A receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Antagonist activity at adenosine A2A receptor (unknown origin)	F	8.26	pKi	5.5	nM	Ki	Eur J Med Chem (2022) 227: 113907-113907 [PMID:34695776]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL	Binding affinity of [3H]-MRE 2029-F20 towards human adenosine A2b receptor expressed in CHO cells	B	8.78	pKd	1.65	nM	Kd	Bioorg Med Chem Lett (2004) 14: 3611-3614 [PMID:15177485]
ChEMBL	Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Antagonist activity against human Adenosine A2b receptor	F	8.26	pKi	5.5	nM	Ki	J Med Chem (2005) 48: 6813-6820 [PMID:16250640]
ChEMBL	Displacement of [3H]MRE2029F20 from human adenosine A2B receptor expressed in HEK293 cells	B	8.26	pKi	5.5	nM	Ki	Bioorg Med Chem (2008) 16: 2419-2430 [PMID:18077171]
ChEMBL	Binding affinity to human adenosine A2B receptor	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Antagonist activity against human adenosine A2B receptor	F	8.26	pKi	5.5	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL	Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells after 120 mins by scintillation counting	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Displacement of [3H]MRE2029-F20 from human recombinant adenosine A2B receptor expressed in CHO cells	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Displacement of [3H] DPCPX from human recombinant Adenosine A2B receptor expressed in HEK293 cells after 60 mins	B	8.26	pKi	5.5	nM	Ki	J Med Chem (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL	Displacement of [3H]DPCPX from human adenosine receptor A2b expressed in HEK293 cell membranes	B	8.26	pKi	5.5	nM	Ki	Eur J Med Chem (2017) 127: 986-996 [PMID:27842891]
GtoPdb	-	-	8.5	pKi	-	-	-	Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]; J Med Chem (2004) 47: 1434-47 [PMID:14998332]
ChEMBL	Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor	F	7.42	pIC50	38	nM	IC50	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Antagonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-induced [3H]cAMP production after 150 mins by scintillation counting	F	7.42	pIC50	38	nM	IC50	J Med Chem (2012) 55: 797-811 [PMID:22148859]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb	-	-	6	pKi	>1000	nM	Ki	J Med Chem (2004) 47: 1434-47 [PMID:14998332]
ChEMBL	Binding affinity of compound for displacement of specific [3H]MRE3008-F20 binding at human A3 receptors expressed in CHO cells	B	6	pKi	>1000	nM	Ki	J Med Chem (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL	Displacement of [3H]MRE3008F20 from human adenosine A3 receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	Bioorg Med Chem (2008) 16: 2419-2430 [PMID:18077171]
ChEMBL	Binding affinity to human adenosine A3 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Antagonist activity against human adenosine A3 receptor	F	6	pKi	>1000	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL	Displacement of [3H]MRE3008-F20 from human recombinant adenosine A3 receptor expressed in CHO cells after 120 mins by scintillation counting	B	6	pKi	>1000	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]
ChEMBL	Binding affinity to human adenosine A3 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2012) 55: 797-811 [PMID:22148859]

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]