ChEMBL ligand: CHEMBL183 (GNF-Pf-2224)
A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190] A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] 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] A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] 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!
μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] There should be some charts here, you may need to enable JavaScript!
Plasmodium falciparum [ChEMBL: CHEMBL364] 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	pA2 against human brain adenosine A1 receptor	B	8.43	pKd	3.71	nM	Kd	Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL	The A1-StaR receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore.	B	8.57	pKd	2.7	nM	Kd	K4DD drug target binding kinetics data
ChEMBL	Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHOK1 cells by scintillation counting	B	7.02	pKi	95	nM	Ki	Eur J Med Chem (2009) 44: 2122-2127 [PMID:19036477]
ChEMBL	Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay	B	7.4	pKi	39.81	nM	Ki	J Med Chem (2021) 64: 6670-6695 [PMID:33724031]
ChEMBL	Binding affinity to adenosine receptor A1	B	7.89	pKi	12.9	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control	B	7.92	pKi	12.02	nM	Ki	Medchemcomm (2012) 3: 333-338
ChEMBL	Binding affinity for human Adenosine A1 receptor	B	7.92	pKi	12	nM	Ki	J Med Chem (2004) 47: 663-672 [PMID:14736246]
ChEMBL	Binding affinity towards human A1 receptor (hA1) was measured through displacement of [3H]-DPCPX using mammalian cell membranes	B	8.15	pKi	7	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL	Binding affinity against adenosine A1 receptor in human cortical membranes using [3H]CHA as radioligand	B	8.17	pKi	6.7	nM	Ki	J Med Chem (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL	Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX	B	8.19	pKi	6.5	nM	Ki	J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL	Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells	B	8.21	pKi	6.1	nM	Ki	J Med Chem (2005) 48: 2045-2053 [PMID:15771447]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	8.21	pKi	6.1	nM	Ki	Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane	B	8.21	pKi	6.1	nM	Ki	J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL	Displacement of radiolabeled DPCPX from human adenosine A1 receptor	B	8.38	pKi	4.2	nM	Ki	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells	B	8.4	pKi	4	nM	Ki	Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	8.41	pKi	3.9	nM	Ki	J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL	Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]CHA	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Displacement of [3H]CHA from cloned human adenosine A1 receptor expressed in CHO cells	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	8.49	pKi	3.2	nM	Ki	J Med Chem (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL	Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells	B	8.49	pKi	3.2	nM	Ki	Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO-A1 cells after 60 mins	B	8.49	pKi	3.2	nM	Ki	Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins	B	8.49	pKi	3.2	nM	Ki	Eur J Med Chem (2015) 89: 32-41 [PMID:25462223]
ChEMBL	Inhibitory constant aganist human adenosine A1 receptor	B	8.52	pKi	3	nM	Ki	J Med Chem (2007) 50: 65-73 [PMID:17201410]
ChEMBL	Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A1 receptor	B	8.6	pKi	2.52	nM	Ki	J Med Chem (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting method	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes after 60 mins	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL	Displacement [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting method	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL	Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membrane incubated for 60 mins by microbeta trilux scintillation counter analysis	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2022) 65: 2091-2106 [PMID:35068155]
ChEMBL	Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells after 60 mins	B	8.66	pKi	2.2	nM	Ki	J Med Chem (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL	Binding affinity at human Adenosine A1 receptor expressed in CHO cells	B	8.67	pKi	2.13	nM	Ki	J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293 cells	B	8.8	pKi	1.6	nM	Ki	J Med Chem (2008) 51: 400-406 [PMID:18189346]
ChEMBL	Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membranes measured after 90 mins by scintillation counting method	B	8.96	pKi	1.09	nM	Ki	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
ChEMBL	Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2006) 49: 3682-3692 [PMID:16759111]
ChEMBL	Antagonist activity against human adenosine A1 receptor	F	9.05	pKi	0.9	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
GtoPdb	-	-	9.2	pKi	0.63	nM	Ki	J Biol Chem (1999) 274: 3617-21 [PMID:9920910]; J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]; Eur J Pharmacol (2005) 510: 1-8 [PMID:15740718]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; Br J Pharmacol (1994) 111: 1252-6 [PMID:8032613]
ChEMBL	Binding affinity to human adenosine A1 receptor by radioligand displacement assay	B	9.25	pKi	0.56	nM	Ki	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL	Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins	B	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL	Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL	Antagonist activity against adenosine A1 receptor in human platelets	F	9.33	pKi	0.47	nM	Ki	J Med Chem (1990) 33: 1906-1910 [PMID:1694546]
ChEMBL	Inhibition of human adenosine A1 receptor	B	7.6	pIC50	25	nM	IC50	Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL	Binding affinity against human A1 receptor (hA1) was measured through displacement of [3H]DPCPX using yeast cell membranes	B	7.85	pIC50	14	nM	IC50	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL	Inhibitory activity against human A1 receptor (hA1) on membranes from yeast cells	B	7.89	pIC50	13	nM	IC50	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL	Inhibition of human adenosine A1 receptor	B	7.89	pIC50	13	nM	IC50	J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL	Displacement of radiolabeled DPCPX from human adenosine A1 receptor	B	8.17	pIC50	6.7	nM	IC50	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Binding affinity to human adenosine A1 receptor by radioligand displacement assay	B	9.05	pIC50	0.89	nM	IC50	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Binding affinity to human adenosine A1 receptor by radioligand displacement assay	B	9.06	pIC50	0.87	nM	IC50	Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL	Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells measured after 60 mins by scintillation counting method	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL	Inverse agonist activity at human A1AR expressed in CHO cells assessed as increase in forskolin-stimulated cAMP production by alphascreen assay	F	8.82	pEC50	1.52	nM	EC50	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL	Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane	B	9.3	pKi	0.5	nM	Ki	Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement.	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptor in bovine brain membranes	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptor in bovine cerebral cortical membranes	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [3H]DPCPX from adenosine A1 receptor in bovine brain membranes	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [3H]DPCPX from bovine brain cortical membrane adenosine A1 receptor	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes	B	9.3	pKi	0.5	nM	Ki	J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL	Binding affinity at bovine Adenosine A1 receptor.	B	9.34	pKi	0.46	nM	Ki	J Med Chem (2002) 45: 4875-4887 [PMID:12383013]
ChEMBL	Affinity to A1 adenosine receptor was measured by the displacement of [3H]PIA in bovine brain cortical membrane	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL	Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand	B	9.6	pKi	0.25	nM	Ki	J Med Chem (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL	Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes	B	9.77	pKi	0.17	nM	Ki	J Med Chem (1998) 41: 555-563 [PMID:9484505]
ChEMBL	Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes	B	9.81	pKi	0.15	nM	Ki	J Med Chem (1998) 41: 555-563 [PMID:9484505]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	pA2 against rat brain adenosine A1 receptor	B	8.24	pKd	5.75	nM	Kd	Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL	Binding affinity for Adenosine A1 receptor of rat forebrain	B	8.42	pKi	3.77	nM	Ki	J Med Chem (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL	Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates.	B	8.82	pKi	1.5	nM	Ki	J Med Chem (1996) 39: 1164-1171 [PMID:8676354]
ChEMBL	Binding affinity at rat Adenosine A1 receptor in the absence of GTP	B	8.84	pKi	1.46	nM	Ki	J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL	Binding affinity at rat Adenosine A1 receptor in the presence of GTP	B	8.92	pKi	1.2	nM	Ki	J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL	Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells	B	9	pKi	1	nM	Ki	J Med Chem (2002) 45: 2131-2138 [PMID:12014951]
ChEMBL	Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes	B	9.05	pKi	0.9	nM	Ki	J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat cortical membranes using N6-[3H]cyclohexyladenosine as radioligand	B	9.05	pKi	0.9	nM	Ki	J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes	B	9.05	pKi	0.9	nM	Ki	J Med Chem (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL	Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex membrane	B	9.05	pKi	0.9	nM	Ki	Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Inhibition of [3H]CCPA binding to rat adenosine A1 receptor	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2002) 45: 1500-1510 [PMID:11906291]
ChEMBL	Inhibition of [3H]CCPA binding to adenosine A1 receptor	B	9.05	pKi	0.9	nM	Ki	J Med Chem (2005) 48: 2108-2114 [PMID:15771453]
ChEMBL	Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes	B	9.05	pKi	0.9	nM	Ki	J Med Chem (1989) 32: 1873-1879 [PMID:2754711]
ChEMBL	GTP-induced shift at rat Adenosine A1 receptor (A1AR)	B	9.11	pKi	0.77	nM	Ki	J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL	Evaluated for binding affinity against Adenosine A1 receptor	B	9.21	pKi	0.62	nM	Ki	J Med Chem (1992) 35: 629-635 [PMID:1542091]
ChEMBL	Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane	B	9.22	pKi	0.6	nM	Ki	J Med Chem (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat whole brain membranes	B	9.25	pKi	0.56	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes	B	9.26	pKi	0.55	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in absence of GTP	B	9.26	pKi	0.55	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by scintillation counting	B	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2010) 45: 1739-1745 [PMID:20116907]
ChEMBL	Displacement of [3H]CCPA from rat adenosine A1 receptor	B	9.3	pKi	0.5	nM	Ki	Eur J Med Chem (2008) 43: 614-620 [PMID:17602796]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine	B	9.31	pKi	0.49	nM	Ki	J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in presence of 0.1 mM GTP	B	9.32	pKi	0.48	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL	Binding affinity against adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1992) 35: 924-930 [PMID:1548682]
ChEMBL	Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1992) 35: 407-422 [PMID:1738138]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL	Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay	B	9.4	pKi	0.4	nM	Ki	Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL	Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes in presence of GTP by radioligand competition assay	B	9.4	pKi	0.4	nM	Ki	Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL	Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes	B	9.52	pKi	0.3	nM	Ki	Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL	Displacement of [3H]-PIA from Adenosine A1 receptor in Wistar rat brain membranes	B	9.52	pKi	0.3	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Adenosine A1 receptor binding using [3H]DPCPX in rat cortical membranes	B	9.55	pKi	0.28	nM	Ki	J Med Chem (1999) 42: 779-783 [PMID:10072675]
ChEMBL	Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from rat cortical membranes	B	9.64	pKi	0.23	nM	Ki	J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Binding affinity against adenosine A1 receptor in rat cortex by the displacement of [3H]cyclohexyladenosine (CHA).	B	9.64	pKi	0.23	nM	Ki	J Med Chem (1991) 34: 1431-1435 [PMID:2016719]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in absence of GTP	B	9.64	pKi	0.23	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in presence of 0.1 mM GTP	B	9.68	pKi	0.21	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
GtoPdb	-	-	9.74	pKi	0.18	nM	Ki	ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Naunyn Schmiedebergs Arch Pharmacol (1991) 343: 196-201 [PMID:2067592]
ChEMBL	Antagonist activity at adenosine A1 receptor in rat cortical membrane assessed as reduction of [35S]GTPgammaS binding	F	8.22	pIC50	6	nM	IC50	J Nat Prod (2002) 65: 1479-1485 [PMID:12398547]
ChEMBL	Inhibitory activity against Adenosine A1 Receptor using [3H]CHA in rat cortical membranes	B	8.33	pIC50	4.7	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1979-1984 [PMID:10450966]
ChEMBL	Inhibition of [3H]-CHA binding against Adenosine A1 receptors of rat cortical membranes; Not tested	B	8.33	pIC50	4.7	nM	IC50	Bioorg Med Chem Lett (1996) 6: 2059-2062
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL	Displacement of N6-[3H]cyclohexyladenosine from adenosine receptor A1 in guinea pig forebrain membranes by liquid scintillation counting method	B	8.19	pKi	6.4	nM	Ki	J Med Chem (2020) 63: 13291-13315 [PMID:32805118]
ChEMBL	Binding affinity towards adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig forebrain membranes	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1992) 35: 3578-3581 [PMID:1404238]
ChEMBL	Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1991) 34: 466-469 [PMID:1992150]
ChEMBL	Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Binding affinity against adenosine A1 receptor using N6-[3H]cyclohexyladenosine as radioligand in guinea pig forebrain membranes	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1992) 35: 924-930 [PMID:1548682]
ChEMBL	Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement.	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL	Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand.	B	8.19	pKi	6.4	nM	Ki	J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Binding affinity for Adenosine A1 receptor from Guinea pig membranes	B	8.53	pKi	2.93	nM	Ki	J Med Chem (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL	Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor)	F	8.88	pIC50	1.31	nM	IC50	Bioorg Med Chem Lett (1996) 6: 2059-2062
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Then it has been reconstituted into rHDLs membrane discs.Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction.	B	6.97	pKd	106.44	nM	Kd	K4DD drug target binding kinetics data
ChEMBL	The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction.	B	7.12	pKd	76.29	nM	Kd	K4DD drug target binding kinetics data
ChEMBL	Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells	B	6.1	pKi	788	nM	Ki	J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL	Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346	B	6.2	pKi	630	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane	B	6.47	pKi	340	nM	Ki	J Med Chem (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins	B	6.47	pKi	337	nM	Ki	Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane	B	6.47	pKi	337	nM	Ki	J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes	B	6.47	pKi	337	nM	Ki	J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes.	B	6.47	pKi	337	nM	Ki	J Med Chem (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.47	pKi	337	nM	Ki	J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.47	pKi	337	nM	Ki	J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.47	pKi	337	nM	Ki	J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL	Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes	B	6.47	pKi	337	nM	Ki	J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes	B	6.47	pKi	337	nM	Ki	J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane	B	6.47	pKi	337	nM	Ki	J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL	Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells	B	6.54	pKi	291	nM	Ki	J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells after 120 mins	B	6.58	pKi	260.3	nM	Ki	Eur J Med Chem (2015) 89: 32-41 [PMID:25462223]
ChEMBL	Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells	B	6.59	pKi	260	nM	Ki	Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Displacement of [3H]NECA from cloned human adenosine A2A receptor expressed in CHO cells	B	6.59	pKi	260	nM	Ki	J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.59	pKi	260	nM	Ki	J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.59	pKi	260	nM	Ki	J Med Chem (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL	Displacement of [3H]NECA from human cloned adenosine A2A receptor expressed in CHO cells	B	6.59	pKi	260	nM	Ki	J Med Chem (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2a receptor expressed in HeLa cells after 30 mins	B	6.59	pKi	260	nM	Ki	Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL	Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells	B	6.65	pKi	226	nM	Ki	J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL	Binding affinity against adenosine A2 receptor in bovine striatal membranes using [3H]-CGS-21,680 as radioligand	B	6.7	pKi	200	nM	Ki	J Med Chem (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL	Displacement [3H]ZM241385 from adenosine A2A receptor in human HeLa cell membranes incubated for 30 mins by scintillation counting method	B	6.8	pKi	157	nM	Ki	J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL	Displacement of [3H]4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol from human adenosine A2A receptor expressed in human Hela cell membranes after 30 mins	B	6.8	pKi	157	nM	Ki	J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL	Displacement of [3H]ZM241385 from human Adenosine A2A receptor expressed in HeLa cells after 30 mins	B	6.8	pKi	157	nM	Ki	J Med Chem (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL	Displacement of [3H]HZ241385 from human A2AAR expressed in HeLa cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis	B	6.8	pKi	157	nM	Ki	J Med Chem (2022) 65: 2091-2106 [PMID:35068155]
ChEMBL	Displacement of [3H]ZM2421385 from adenosine A2A receptor expressed in human HeLa cell membranes incubated for 30 mins by scintillation counting method	B	6.8	pKi	157	nM	Ki	J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL	Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand	B	6.84	pKi	144	nM	Ki	J Med Chem (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL	Displacement of [3H]ZM-241385 from human cloned adenosine A2A receptor expressed in HEK293 cells by scintillation counting	B	6.89	pKi	130	nM	Ki	Eur J Med Chem (2009) 44: 2122-2127 [PMID:19036477]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane	B	6.89	pKi	130	nM	Ki	J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL	Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells	B	6.89	pKi	130	nM	Ki	J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL	Displacement of [3H]-ZM 241385 binding to human adenosine A2A receptor expressed in CHO cells	B	6.89	pKi	129	nM	Ki	J Med Chem (2005) 48: 2045-2053 [PMID:15771447]
ChEMBL	Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis	B	6.89	pKi	129	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in HEK293 cells	B	6.89	pKi	129	nM	Ki	Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439]
ChEMBL	Displacement of [3H]ZM241385 from human A2AR expressed in CHO cell membranes measured after 60 mins by scintillation counting method	B	7.01	pKi	97	nM	Ki	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
ChEMBL	Binding affinity towards human A2 receptor (hA2) was measured through displacement of [3H]-CGS-21,680 using yeast cell membranes	B	7.15	pKi	70	nM	Ki	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
GtoPdb	-	-	7.2	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 7-10 [PMID:9933143]; Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]
ChEMBL	Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680	B	7.25	pKi	56	nM	Ki	J Med Chem (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL	Inhibitory activity against membranes from HEK293 cells stably expressing the human A2a receptor (hA2a)	B	6.58	pIC50	261	nM	IC50	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL	Binding affinity against human A2 receptor (hA2) was measured through displacement of [3H]CGS-21680 using yeast cell membranes	B	6.66	pIC50	217	nM	IC50	Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL	Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay	F	6.88	pIC50	132	nM	IC50	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal homogenates.	B	6.15	pKi	706	nM	Ki	J Med Chem (1996) 39: 1164-1171 [PMID:8676354]
ChEMBL	Displacement of [3H]NECA from adenosine A2A receptor in rat striatal membranes by radioligand competition assay	B	6.26	pKi	545	nM	Ki	Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL	Displacement of [3H]-NECA from Adenosine A2A receptor in Sprague-Dawley rat striatal membranes	B	6.28	pKi	530	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement.	B	6.3	pKi	500	nM	Ki	J Med Chem (2002) 45: 2131-2138 [PMID:12014951]
ChEMBL	Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor	B	6.33	pKi	470	nM	Ki	J Med Chem (2002) 45: 1500-1510 [PMID:11906291]
ChEMBL	Inhibition of [3H]MSX-2 binding to adenosine A2a receptor	B	6.33	pKi	470	nM	Ki	J Med Chem (2005) 48: 2108-2114 [PMID:15771453]
ChEMBL	Displacement of [3H]DPCPX from adenosine A2A receptor in rat striatal membranes	B	6.47	pKi	340	nM	Ki	Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane	B	6.47	pKi	340	nM	Ki	J Med Chem (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL	Displacement of [3H]-NECA from Adenosine A2A receptor in rat striatal membranes	B	6.47	pKi	340	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL	Displacement of [3H]-NECA from Adenosine A2A receptor in Wistar rat striatal membranes	B	6.47	pKi	340	nM	Ki	Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
GtoPdb	-	-	6.8	pKi	157	nM	Ki	J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Eur J Pharm Sci (2000) 10: 259-65 [PMID:10838015]
ChEMBL	Displacement of [3H]MSX2 from rat adenosine A2A receptor	B	6.8	pKi	157	nM	Ki	Eur J Med Chem (2008) 43: 614-620 [PMID:17602796]
ChEMBL	Displacement of [3H]MSX-2 from adenosine A2A receptor in rat brain striatal membrane after 30 mins by scintillation counting	B	6.8	pKi	157	nM	Ki	Eur J Med Chem (2010) 45: 1739-1745 [PMID:20116907]
ChEMBL	Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatum membrane	B	6.8	pKi	157	nM	Ki	Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Inhibitory activity against Adenosine A2a receptor using [3H]NECA in rat striatal membranes	B	5.96	pIC50	1100	nM	IC50	Bioorg Med Chem Lett (1999) 9: 1979-1984 [PMID:10450966]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method	B	5.14	pKi	7324	nM	Ki	J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL	Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity	F	6	pKi	1000	nM	Ki	Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184]
ChEMBL	Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method	B	7.14	pKi	73.24	nM	Ki	J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL	Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis	B	7.14	pKi	73.24	nM	Ki	J Med Chem (2022) 65: 2091-2106 [PMID:35068155]
ChEMBL	Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins	B	7.14	pKi	73.24	nM	Ki	J Med Chem (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins	B	7.14	pKi	73.2	nM	Ki	J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL	Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand	B	7.2	pKi	63.8	nM	Ki	J Med Chem (2002) 45: 2131-2138 [PMID:12014951]
ChEMBL	Antagonist activity against human adenosine A2B receptor	F	7.25	pKi	56	nM	Ki	Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
ChEMBL	Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells	B	7.25	pKi	56	nM	Ki	J Med Chem (2006) 49: 3682-3692 [PMID:16759111]
ChEMBL	Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins	B	7.29	pKi	51	nM	Ki	Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL	Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptor	B	7.29	pKi	51	nM	Ki	J Med Chem (2005) 48: 2108-2114 [PMID:15771453]
ChEMBL	Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor	B	7.29	pKi	51	nM	Ki	J Med Chem (2002) 45: 1500-1510 [PMID:11906291]
GtoPdb	-	-	7.3	pKi	-	-	-	J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]; Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 2131-8 [PMID:12014951]
ChEMBL	Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay	F	7.37	pIC50	43	nM	IC50	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
ChEMBL	Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method	B	8.42	pIC50	3.8	nM	IC50	J Med Chem (2018) 61: 4301-4316 [PMID:29681156]
ChEMBL	Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay	F	6	pEC50	>1000	nM	EC50	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb	-	-	7.06	pKi	86.2	nM	Ki	J Pharmacol Exp Ther (2009) 329: 2-13 [PMID:19141710]
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
GtoPdb	-	-	6.73	pKi	186	nM	Ki	J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Eur J Pharmacol (2003) 475: 79-84 [PMID:12954362]
ChEMBL	Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells	B	6.73	pKi	186	nM	Ki	J Med Chem (2002) 45: 2131-2138 [PMID:12014951]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL	Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane	B	5	pKi	>10000	nM	Ki	J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL	Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX	B	5	pKi	>10000	nM	Ki	J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	5.4	pKi	4000	nM	Ki	J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL	Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells	B	5.4	pKi	4000	nM	Ki	Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184]
ChEMBL	Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis	B	5.4	pKi	3980	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Displacement of [3H]NECA from adenosine A3 receptor expressed in human HeLa cell membranes incubated for 180 mins by scintillation counting method	B	5.76	pKi	1722	nM	Ki	J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL	Displacement of [3H]NECA from human A3AR expressed in HeLa cell membrane incubated for 180 mins by microbeta trilux scintillation counter analysis	B	5.76	pKi	1722	nM	Ki	J Med Chem (2022) 65: 2091-2106 [PMID:35068155]
ChEMBL	Displacement of [3H]NECA from human Adenosine A3 receptor expressed in HeLa cells after 30 mins	B	5.76	pKi	1722	nM	Ki	J Med Chem (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL	Displacement [3H]NECA from adenosine A3 receptor in human HeLa cell membranes incubated for 180 mins by scintillation counting method	B	5.76	pKi	1722	nM	Ki	J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL	Displacement of [3H]NECA from human adenosine A3 receptor expressed in human Hela cell membranes after 180 mins	B	5.76	pKi	1722	nM	Ki	J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL	Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cells	B	5.77	pKi	1700	nM	Ki	Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439]
ChEMBL	Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cell membrane	B	5.77	pKi	1700	nM	Ki	J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL	Displacement of [125I]-AB-MECA binding to human adenosine A3 receptor expressed in HEK 293 cells	B	5.77	pKi	1700	nM	Ki	J Med Chem (2005) 48: 2045-2053 [PMID:15771447]
ChEMBL	Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK 293 cells.	B	5.77	pKi	1700	nM	Ki	J Med Chem (1998) 41: 3987-3993 [PMID:9767636]
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	5.88	pKi	1320	nM	Ki	Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells	B	5.89	pKi	1300	nM	Ki	J Med Chem (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	Binding affinity against human adenosine A3 receptor expressed in CHO cells by [125I]AB-MECA displacement.	B	5.89	pKi	1300	nM	Ki	J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells.	B	5.89	pKi	1300	nM	Ki	J Med Chem (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	5.89	pKi	1300	nM	Ki	J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	5.89	pKi	1300	nM	Ki	J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	5.89	pKi	1300	nM	Ki	J Med Chem (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL	Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells	B	5.89	pKi	1300	nM	Ki	Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells after 180 mins	B	5.89	pKi	1300	nM	Ki	Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins	B	6	pKi	>1000	nM	Ki	Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL	Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins	B	6	pKi	>1000	nM	Ki	Medchemcomm (2018) 9: 81-86 [PMID:30108902]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL	Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	6	pKi	>1000	nM	Ki	J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL	Displacement of [125I]ABMECA from human A3R expressed in CHO cell membranes measured after 120 mins by scintillation counting method	B	6.01	pKi	985	nM	Ki	J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
ChEMBL	Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor	B	6.1	pKi	795	nM	Ki	J Med Chem (2002) 45: 1500-1510 [PMID:11906291]
ChEMBL	Displacement of [125I]ABA from human adenosine A3 receptor expressed in CHO cells	B	6.12	pKi	759	nM	Ki	J Med Chem (1998) 41: 3987-3993 [PMID:9767636]
ChEMBL	Inhibition of [3H]PSB-11 binding to adenosine A3 receptor	B	6.12	pKi	759	nM	Ki	J Med Chem (2005) 48: 2108-2114 [PMID:15771453]
GtoPdb	-	-	6.61	pKi	243	nM	Ki	Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Mol Pharmacol (2000) 57: 968-75 [PMID:10779381]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 1500-10 [PMID:11906291]; Mol Pharmacol (1997) 52: 846-60 [PMID:9351976]
ChEMBL	Displacement of [3H]PSB-11 from human adenosine A3 receptor expressed in CHO cells	B	6.61	pKi	243	nM	Ki	Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells	B	6.7	pKi	200	nM	Ki	J Med Chem (1998) 41: 3987-3993 [PMID:9767636]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL	Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA	B	5.28	pKi	5290	nM	Ki	J Med Chem (1994) 37: 3373-3382 [PMID:7932565]
GtoPdb	-	-	7.6	pKi	-	-	Ki	J Biol Chem (1994) 269: 24692-8 [PMID:7929142]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; Mol Pharmacol (1997) 52: 846-60 [PMID:9351976]
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
ChEMBL	Binding affinity to mu opioid receptor	B	4	pKi	>100000	nM	Ki	Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay	F	4.9	pIC50	12589.25	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay	F	5.1	pIC50	7943.28	nM	IC50	Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL	NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay	F	6.12	pEC50	764	nM	EC50	Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]
ChEMBL	NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay	F	6.46	pEC50	346	nM	EC50	Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783]

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]