ChEMBL ligand: CHEMBL190 (Elixophyllin sr, Theophyl, Elixicon, Bronkodyl, Somophyllin-t, Aerolate iii, Somophyllin-crt, Theophylline-sr, Accurbron, Theolair-sr, Aerolate jr, Theophylline melting point standard, Theochron, Theoclear-100, Slo-phyllin, Theoclear-80, Theograd, Aerolate, NSC-2066, Theocin, Nuelin, Theoclear-200, Nuelin sa-250, Pro-vent, Theovent, Uni-dur, Aquaphyllin, Theo-24, Lasma, Theophylline monohydrate, Theophylline, T-phyl, Theo-dur, Quibron-t/sr, Theolair, Uniphyl, Respbid, Quibron, Uniphyllin continus, Labid, Slo-bid, Quibron-t, Theobid, Duraphyl, Theophyl-sr, Dimethylxanthine, Theoclear l.a.-260, Theolixir, Aerolate sr, Elixophyllin, Sustaire, Elixomin, Theoclear l.a.-130, Theophyl-225, Lanophyllin, Nuelin sa, Theobid jr.)
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] Adenosine A2a receptor in Guinea pig [ChEMBL: CHEMBL2605] [UniProtKB: P46616] 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!
Alkaline phosphatase, tissue-nonspecific isozyme in Human [ChEMBL: CHEMBL5979] [UniProtKB: P05186] There should be some charts here, you may need to enable JavaScript!
CYP3A4/Cytochrome P450 3A4 in Human [ChEMBL: CHEMBL340] [GtoPdb: 1337] [UniProtKB: P08684] There should be some charts here, you may need to enable JavaScript!
Intestinal alkaline phosphatase in Human [ChEMBL: CHEMBL5573] [UniProtKB: P09923] There should be some charts here, you may need to enable JavaScript!
Phosphodiesterase 3B in Bovine [ChEMBL: CHEMBL5129] [UniProtKB: E1BN64] There should be some charts here, you may need to enable JavaScript!
Phospholipase A-2-activating protein in Human [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] There should be some charts here, you may need to enable JavaScript!
Transmembrane domain-containing protein TMIGD3 in Human [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9] 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	Dissociation constant against Adenosine A1 receptor	B	4.92	pKd	12000	nM	Kd	J. Med. Chem. (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL	Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO-A1 cell membrane	B	5	pKi	10100	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853]
ChEMBL	DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)	B	5	pKi	9977	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to adenosine A1 receptor	B	5.07	pKi	8500	nM	Ki	J. Nat. Prod. (2000) 63: 315-317 [PMID:10757709]
ChEMBL	Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells	B	5.16	pKi	6920	nM	Ki	J. Med. Chem. (2006) 49: 3682-3692 [PMID:16759111]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	5.17	pKi	6770	nM	Ki	Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167]
ChEMBL	Displacement of [3H]CCPA from human A1 adenosine receptor expressed in CHO cells	B	5.17	pKi	6770	nM	Ki	MedChemComm (2016) 7: 845-852
ChEMBL	Binding affinity to human adenosine A1 receptor by radioligand displacement assay	B	5.17	pKi	6770	nM	Ki	MedChemComm (2018) 9: 951-962
ChEMBL	Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes by radioligand competition assay	B	5.17	pKi	6770	nM	Ki	J Med Chem (2020) 63: 2577-2587 [PMID:31738058]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	5.17	pKi	6770	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
GtoPdb	-	-	5.2	pKi	-	-	-	J Biol Chem (1994) 269: 32077-84 [PMID:7798201]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]; Biochem Pharmacol (2001) 62: 1163-73 [PMID:11705449]
ChEMBL	Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells	B	5.21	pKi	6200	nM	Ki	Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Displacement of [3H]CHA from cloned human adenosine A1 receptor expressed in CHO cells	B	5.21	pKi	6200	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	5.21	pKi	6200	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	5.21	pKi	6200	nM	Ki	J. Med. Chem. (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL	Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells	B	5.21	pKi	6200	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	5.21	pKi	6200	nM	Ki	J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Binding affinity to human adenosine A1 receptor	B	5.21	pKi	6200	nM	Ki	J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Binding affinity for adenosine A1 receptor by using as [3H]CPX iradioligand n membranes from Chinese hamster ovary cells	B	9.22	pKi	0.6	nM	Ki	Bioorg. Med. Chem. Lett. (2005) 15: 609-612 [PMID:15664822]
ChEMBL	DRUGMATRIX: Adenosine A1 radioligand binding (ligand: DPCPX)	B	4.77	pIC50	17104	nM	IC50	DrugMatrix in vitro pharmacology data
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL	Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain	B	4.7	pKi	20000	nM	Ki	J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
ChEMBL	Affinity to A1 adenosine receptor was measured by the displacement of [3H]PIA in bovine brain cortical membrane	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL	Displacement of [3H]CPX from adenosine A1 receptor of calf brain cortical membrane	B	5.22	pKi	6000	nM	Ki	J. Med. Chem. (1991) 34: 1202-1206 [PMID:2002461]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptor in bovine brain membranes	B	5.42	pKi	3800	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	5.42	pKi	3800	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	5.42	pKi	3800	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	5.42	pKi	3800	nM	Ki	J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane	B	5.42	pKi	3800	nM	Ki	Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL	Binding affinity towards adenosine A1 receptor of bovine brain membrane using [3H]-CHA at 20 uM	B	5.42	pKi	3800	nM	Ki	J. Med. Chem. (2000) 43: 1158-1164 [PMID:10737748]
ChEMBL	Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement.	B	5.42	pKi	3800	nM	Ki	J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Binding affinity against bovine brain adenosine A1 receptor using N6-[3H]- cyclohexyladenosine	B	4.9	pIC50	12700	nM	IC50	J. Med. Chem. (1985) 28: 1071-1079 [PMID:2991519]
ChEMBL	Binding affinity against bovine brain adenosine A1 receptor using N6-[3H]- cyclohexyladenosine	B	5.61	pIC50	2430	nM	IC50	J. Med. Chem. (1985) 28: 1071-1079 [PMID:2991519]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL	Displacement of [3H]CHA from adenosine A1 receptor in rat brain cortical membrane	B	4.59	pKi	26000	nM	Ki	J. Nat. Prod. (1998) 61: 301-305 [PMID:9514015]
ChEMBL	Ability to inhibit binding of [3H]CHA to adenosine A1 receptor in rat brain cortical membranes.	B	4.77	pKi	17000	nM	Ki	J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909]
ChEMBL	Binding affinity to rat adenosine A1 receptor	B	4.85	pKi	14000	nM	Ki	Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167]
ChEMBL	Ability to inhibit binding of [3H]R-PIA to Adenosine A1 receptor in rat brain cortical membranes	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909]
ChEMBL	Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1993) 36: 3341-3349 [PMID:8230124]
ChEMBL	Ability to inhibit binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptor in rat cerebral cortical membranes	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1986) 29: 1305-1308 [PMID:3806581]
ChEMBL	Binding affinity to A1 adenosine receptor from rat cortical membrane in presence of [3H]R-(phenylisopropyl)-adenosine	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1994) 37: 1526-1534 [PMID:8182711]
ChEMBL	Binding affinity for Adenosine A1 receptor from rat brain using [3H]-PIA as radioligand	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1990) 33: 2818-2821 [PMID:2213834]
ChEMBL	Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1985) 28: 487-492 [PMID:2984420]
ChEMBL	Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976]
ChEMBL	Binding of 1 nM [3H]CHA to Adenosine A1 receptor of rat cerebral cortical membranes	B	4.85	pKi	14000	nM	Ki	J. Med. Chem. (1988) 31: 2034-2039 [PMID:3172141]
ChEMBL	Binding affinity to rat adenosine A1 receptor	B	4.85	pKi	14000	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes	B	4.89	pKi	13000	nM	Ki	J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes	B	4.89	pKi	13000	nM	Ki	J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine	B	5.01	pKi	9700	nM	Ki	J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Displacement of [3H]CPX from adenosine A1 receptor of rat brain cortical membrane	B	5.04	pKi	9200	nM	Ki	J. Med. Chem. (1991) 34: 1202-1206 [PMID:2002461]
GtoPdb	-	-	5.06	pKi	8740	nM	Ki	Drug Dev Res (1999) : 45-53; J Med Chem (1993) 36: 3341-9 [PMID:8230124]
ChEMBL	Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane	B	5.06	pKi	8700	nM	Ki	J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL	Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL	Binding affinity to rat adenosine A1 receptor	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL	Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (1989) 32: 2247-2254 [PMID:2795597]
ChEMBL	Inhibition of [3H]CHA binding to Adenosine A1 receptor in rat brain membranes	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (1990) 33: 1708-1713 [PMID:2342066]
ChEMBL	Inhibition of rat recombinant adenosine A1 receptor	B	5.07	pKi	8500	nM	Ki	J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes	B	5.07	pKi	8470	nM	Ki	J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Binding affinity against Adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes	B	5.07	pKi	8470	nM	Ki	J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL	Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand	B	5.07	pKi	8470	nM	Ki	J. Med. Chem. (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL	Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes	B	5.07	pKi	8470	nM	Ki	J. Med. Chem. (1989) 32: 1873-1879 [PMID:2754711]
ChEMBL	Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine	B	5.07	pKi	8470	nM	Ki	J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	In vitro binding affinity to Adenosine A1 receptor of rat cerebral cortical membranes using 1 nM [3H]PIA	B	5.13	pKi	7400	nM	Ki	J. Med. Chem. (1988) 31: 2034-2039 [PMID:3172141]
ChEMBL	Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells	B	5.16	pKi	6920	nM	Ki	J. Med. Chem. (2002) 45: 2131-2138 [PMID:12014951]
ChEMBL	Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor	B	6.15	pKi	700	nM	Ki	J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897]
ChEMBL	Antagonism of adenosine A1 receptor assessed from the ability to inhibit binding of [3H]cyclohexyladenosine to rat cerebral cortical membranes	B	4.55	pIC50	28000	nM	IC50	J. Med. Chem. (1984) 27: 1364-1367 [PMID:6090665]
ChEMBL	Binding affinity against adenosine A1 receptor in rat brain membrane preparations using N6-[3H]cyclohexyladenosine as a radioligand	B	4.7	pIC50	20000	nM	IC50	J. Med. Chem. (1987) 30: 91-96 [PMID:3806606]
ChEMBL	Inhibition of adenosine binding to A1 receptor of rat brain homogenates	B	4.72	pIC50	19000	nM	IC50	J. Med. Chem. (1994) 37: 476-485 [PMID:8120866]
ChEMBL	Inhibition of binding towards adenosine A1 receptor using [3H]N-cyclohexyladenosine ([3H]CHA) in rat whole brain membranes.	B	5	pIC50	>10000	nM	IC50	J. Med. Chem. (1988) 31: 1014-1020 [PMID:3361572]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL	Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand.	B	4.64	pKi	23000	nM	Ki	J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL	Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor	B	4.64	pKi	23000	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	4.64	pKi	23000	nM	Ki	J. Med. Chem. (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL	Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand	B	4.64	pKi	23000	nM	Ki	J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL	Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor	B	4.64	pKi	23000	nM	Ki	J. Med. Chem. (1991) 34: 466-469 [PMID:1992150]
ChEMBL	Binding affinity against Adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig membranes	B	4.89	pKi	13000	nM	Ki	J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL	Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX.	B	5.01	pKi	9800	nM	Ki	J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453]
ChEMBL	Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand	B	5.01	pKi	9800	nM	Ki	J. Med. Chem. (1993) 36: 1380-1386 [PMID:8496906]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL	Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method	B	5.5	pKd	3162.28	nM	Kd	J. Med. Chem. (2011) 54: 4312-4323 [PMID:21661720]
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	5.78	pKd	1642.33	nM	Kd	K4DD drug target binding kinetics data
ChEMBL	Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane	B	4.6	pKi	25000	nM	Ki	J. Med. Chem. (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes.	B	4.68	pKi	21000	nM	Ki	J. Med. Chem. (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL	Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes	B	4.68	pKi	21000	nM	Ki	J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL	Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes	B	4.68	pKi	21000	nM	Ki	J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes	B	4.68	pKi	21000	nM	Ki	J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL	Displacement of [3H]ZM241385 from human recombinant adenosine A2A receptor expressed in in human HeLa cell membrane	B	4.73	pKi	18500	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2081-2088 [PMID:20202853]
ChEMBL	Displacement of [3H]ZM241385 from stabilized human adenosine receptor A2a expressed in HEK293 cells followed by receptor capturing on Biocore chips by SPR method	B	5	pKi	>10000	nM	Ki	J. Med. Chem. (2011) 54: 4312-4323 [PMID:21661720]
ChEMBL	Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells	B	5.1	pKi	7900	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	5.1	pKi	7900	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	5.1	pKi	7900	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	5.1	pKi	7900	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	5.1	pKi	7900	nM	Ki	J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL	DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)	B	5.17	pKi	6741	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Binding affinity to human adenosine A2A receptor	B	5.17	pKi	6700	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Displacement of [3H]ZM-241385 from human adenosine A2a receptor expressed in HEK cells	B	5.17	pKi	6700	nM	Ki	J. Med. Chem. (2006) 49: 3682-3692 [PMID:16759111]
ChEMBL	Binding affinity to human adenosine A2A receptor	B	5.17	pKi	6700	nM	Ki	Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167]
ChEMBL	Binding affinity to human adenosine A2A receptor	B	5.38	pKi	4200	nM	Ki	J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
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	5.69	pKi	2030	nM	Ki	Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL	Displacement of [3H]NECA from human adenosine receptor A2A expressed in CHO cell membranes by radioligand competition assay	B	5.77	pKi	1710	nM	Ki	J Med Chem (2020) 63: 2577-2587 [PMID:31738058]
ChEMBL	Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cells	B	5.77	pKi	1710	nM	Ki	MedChemComm (2016) 7: 845-852
ChEMBL	Binding affinity to human adenosine A2A receptor by radioligand displacement assay	B	5.77	pKi	1710	nM	Ki	MedChemComm (2018) 9: 951-962
ChEMBL	Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis	B	5.77	pKi	1700	nM	Ki	Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
GtoPdb	-	-	5.8	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]; Drug Dev Res (1999) : 45-53
ChEMBL	Binding affinity for adenosine A2a receptor by using as [3H]ZM-241385 radioligand in membranes from HEK-A2A cells	B	9.22	pKi	0.6	nM	Ki	Bioorg. Med. Chem. Lett. (2005) 15: 609-612 [PMID:15664822]
ChEMBL	DRUGMATRIX: Adenosine A2A radioligand binding (ligand: AB-MECA)	B	4.92	pIC50	12007	nM	IC50	DrugMatrix in vitro pharmacology data
ChEMBL	Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains.	F	4.55	pEC50	28200	nM	EC50	J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL	Binding affinity to rat adenosine A2A receptor	B	4.6	pKi	25000	nM	Ki	J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL	Inhibition of rat recombinant adenosine receptor A2a	B	4.6	pKi	25000	nM	Ki	J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL	Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane	B	4.6	pKi	25000	nM	Ki	J. Med. Chem. (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL	Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane	B	4.66	pKi	22000	nM	Ki	J. Nat. Prod. (1998) 61: 301-305 [PMID:9514015]
ChEMBL	Binding affinity to rat adenosine A2A receptor	B	4.66	pKi	22000	nM	Ki	Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL	Binding affinity to rat adenosine A2A receptor	B	4.66	pKi	22000	nM	Ki	Bioorg. Med. Chem. (2013) 21: 7435-7452 [PMID:24139167]
GtoPdb	-	-	4.66	pKi	22000	nM	Ki	Drug Dev Res (1999) : 45-53; J Med Chem (1993) 36: 3341-9 [PMID:8230124]
ChEMBL	Ability to inhibit binding of [3H]NECA to Adenosine A2A receptor in rat brain striatal membranes	B	4.72	pKi	19000	nM	Ki	J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909]
ChEMBL	Ability to inhibit binding of [3H]-CGS- 21680 to adenosine A2A receptor in rat brain striatal membranes.	B	5.03	pKi	9400	nM	Ki	J. Med. Chem. (1997) 40: 4396-4405 [PMID:9435909]
ChEMBL	Binding affinity for adenosine A2A receptor from rat brain membranes using [3H]CGS-21680	B	5.1	pKi	8000	nM	Ki	J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976]
ChEMBL	Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement.	B	5.17	pKi	6700	nM	Ki	J. Med. Chem. (2002) 45: 2131-2138 [PMID:12014951]
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
ChEMBL