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	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 cell membrane	B	8.21	pKi	6.1	nM	Ki	J. Med. Chem. (2008) 51: 4449-4455 [PMID:18637670]
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 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 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 [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	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]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 [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 cells	B	8.49	pKi	3.2	nM	Ki	J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
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]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	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 cells after 60 mins	B	8.66	pKi	2.2	nM	Ki	J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
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	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 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]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]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	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 cells	B	9.3	pKi	0.5	nM	Ki	J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
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