ChEMBL ligand: CHEMBL88147 (MRS-1220)
A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] 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!
A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] There should be some charts here, you may need to enable JavaScript!
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275] 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 after 60 mins by gamma counter	B	6.64	pKi	231	nM	Ki	J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Displacement of [3H]-(R)-PIA from Adenosine A1 receptor of rat cerebral cortex membranes	B	6.52	pKi	305	nM	Ki	J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL	Displacement of specific [3H](R)-PIA binding at adenosine A1 receptor from rat brain membranes.	B	6.52	pKi	305	nM	Ki	J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL	Inhibition of [3H]DPCPX binding to rat Adenosine A1 receptor expressed in CHO cells	B	6.52	pKi	305	nM	Ki	J Med Chem (2002) 45: 3703-3708 [PMID:12166943]
ChEMBL	Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter	B	7.28	pKi	53	nM	Ki	J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL	Binding affinity was determined in radioligand binding assay at rat brain adenosine A1 receptor vs [3H]R-PIA	B	7.28	pKi	52.7	nM	Ki	J Med Chem (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL	Displacement of [3H]DPCPX from Adenosine A1 receptor of rat brain membranes	B	7.28	pKi	52.7	nM	Ki	J Med Chem (1999) 42: 4473-4478 [PMID:10579811]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter	B	7.6	pKi	25	nM	Ki	J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Displacement of [3H]-CGH 21680 from Adenosine A2A receptor of rat striatal membranes	B	7.28	pKi	52	nM	Ki	J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL	Displacement of specific [3H]-CGS- 21680 binding at Adenosine A2A receptor in rat striatal membranes.	B	7.28	pKi	52	nM	Ki	J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL	Inhibition of [3H]CGS-21680 binding to rat Adenosine A2A receptor expressed in HEK293 cells	B	7.28	pKi	52	nM	Ki	J Med Chem (2002) 45: 3703-3708 [PMID:12166943]
ChEMBL	Binding affinity was determined in radioligand binding assay at rat striatal Adenosine A2A receptor vs [3H]-CGS- 21680	B	7.99	pKi	10.3	nM	Ki	J Med Chem (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL	Displacement of [3H]-SCH- 58261 from Adenosine A2A receptor in rat striatal membranes	B	7.99	pKi	10.3	nM	Ki	J Med Chem (1999) 42: 4473-4478 [PMID:10579811]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Displacement of [3H]NECA from human adenosine A3 receptor expressed in human HeLa cells incubated for 30 mins by fluorescence polarization binding assay	B	5.77	pKi	1700	nM	Ki	ACS Med Chem Lett (2022) 13: 243-249 [PMID:35178181]
ChEMBL	Displacement of CELT-228 from human adenosine A3 receptor expressed in human HeLa cells incubated for 30 mins by fluorescence polarization binding assay	B	5.85	pKi	1400	nM	Ki	ACS Med Chem Lett (2022) 13: 243-249 [PMID:35178181]
ChEMBL	Antagonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cell membrane assessed as inhibition of NECA-induced cAMP accumulation in presence of forskolin measured after 40 mins by alpha screen LANCE assay	F	8.3	pKi	5	nM	Ki	J Med Chem (2021) 64: 8161-8178 [PMID:34120444]
ChEMBL	Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449	B	8.46	pKi	3.46	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay	B	8.49	pKi	3.24	nM	Ki	ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351]
ChEMBL	Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay	B	8.53	pKi	2.97	nM	Ki	ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351]
ChEMBL	Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in human HeLa cell membrane	B	8.61	pKi	2.48	nM	Ki	Bioorg Med Chem (2010) 18: 2081-2088 [PMID:20202853]
ChEMBL	Bnding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL	Binding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor in the presence of GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL	Antagonist activity at human recombinant adenosine A3 receptor	B	9.19	pKi	0.65	nM	Ki	Bioorg Med Chem (2015) 23: 9-21 [PMID:25497490]
ChEMBL	Antagonist activity at human adenosine A3 receptor	F	9.19	pKi	0.65	nM	Ki	Bioorg Med Chem Lett (2011) 21: 2898-2905 [PMID:21511471]
ChEMBL	Binding affinity at cloned human adenosine A3 receptor expressed in HEK293 cells was determined using [125I]AB-MECA as radioligand	B	9.19	pKi	0.65	nM	Ki	J Med Chem (1998) 41: 2835-2845 [PMID:9667972]
ChEMBL	Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor.	B	9.19	pKi	0.65	nM	Ki	J Med Chem (1997) 40: 2596-2608 [PMID:9258367]
ChEMBL	In vitro binding affinity against human Adenosine A3 receptor	B	9.19	pKi	0.65	nM	Ki	Bioorg Med Chem Lett (2000) 10: 31-34 [PMID:10636237]
ChEMBL	Displacement of [125]AB-MECA from human Adenosine A3 receptor expressed in HEK293 cells	B	9.19	pKi	0.65	nM	Ki	J Med Chem (1999) 42: 4473-4478 [PMID:10579811]
ChEMBL	Inhibition of [125I]AB-MECA binding to human Adenosine A3 receptor expressed in HEK cells	B	9.19	pKi	0.65	nM	Ki	J Med Chem (2002) 45: 3703-3708 [PMID:12166943]
ChEMBL	Displacement of [3H]MRE 3008F20 from human adenosine A3 receptor expressed in CHO cells	B	9.19	pKi	0.65	nM	Ki	J Med Chem (2006) 49: 4085-4097 [PMID:16821770]
ChEMBL	In vitro binding affinity at human Adenosine A3 receptor from HEK293 cells by [125I]AB-MECA displacement.	B	9.19	pKi	0.65	nM	Ki	J Med Chem (1996) 39: 4142-4148 [PMID:8863790]
ChEMBL	Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis	B	9.19	pKi	0.65	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
GtoPdb	-	-	9.2	pKi	0.63	nM	Ki	Neuropharmacology (1997) 36: 1157-65 [PMID:9364471]; J Med Chem (1996) 39: 4142-8 [PMID:8863790]; Auton Autacoid Pharmacol (2006) 26: 191-200 [PMID:16553647]; Br J Pharmacol (2001) 132: 1017-26 [PMID:11226132]
ChEMBL	Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter	B	9.23	pKi	0.59	nM	Ki	J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL	Antagonist activity at human adenosine A3 receptor expressed in CHO cells by [S35]GTPgammaS binding assay	F	8.14	pIC50	7.2	nM	IC50	J Med Chem (2012) 55: 5676-5703 [PMID:22468757]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL	Binding affinity of adenosine derivative for endogenous rat Adenosine A3 receptor expressed on CHO cell	B	8	pKi	>10	nM	Ki	J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb	-	-	6.5	pKi	-	-	-	Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]

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]