theophylline [Ligand Id: 413] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL190 (Accurbron, Aerolate, Aerolate iii, Aerolate jr, Aerolate sr, Aquaphyllin, Bronkodyl, Dimethylxanthine, Doxophylline metabolite m3, Duraphyl, Elixicon, Elixomin, Elixophyllin, Elixophyllin sr, Labid, Lanophyllin, Lasma, NSC-2066, NSC-757346, Nuelin, Nuelin sa, Nuelin sa-250, Pro-vent, Quibron, Quibron-t, Quibron-t/sr, Respbid, Slo-bid, Slo-phyllin, Somophyllin-crt, Somophyllin-t, Sustaire, Theo-24, Theobid, Theobid jr., Theochron, Theocin, Theoclear-100, Theoclear-200, Theoclear-80, Theoclear l.a.-130, Theoclear l.a.-260, Theo-dur, Theograd, Theolair, Theolair-sr, Theolixir, Theophyl, Theophyl-225, Theophylline, Theophylline anhydrous, Theophylline,anhydrous, Theophylline, anhydrous, Theophylline melting point standard, Theophylline monohydrate, Theophylline-sr, Theophyl-sr, Theovent, T-phyl, Uni-dur, Uniphyl, Uniphyllin continus)
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  • 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]
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  • 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]
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  • 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]
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  • Alkaline phosphatase, tissue-nonspecific isozyme in Human [ChEMBL: CHEMBL5979] [UniProtKB: P05186]
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  • Intestinal alkaline phosphatase in Human [ChEMBL: CHEMBL5573] [UniProtKB: P09923]
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  • Phospholipase A-2-activating protein in Human [ChEMBL: CHEMBL6114] [UniProtKB: Q9Y263]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
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  • Transmembrane domain-containing protein TMIGD3 in Human [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9]
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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 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 Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes incubated for 90 mins by radioligand competition assay B 5.17 pKi 6770 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 5.17 pKi 6770 nM Ki MedChemComm (2018) 9: 951-962 [PMID:30108984]
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 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 Binding affinity to human adenosine A1 receptor B 5.21 pKi 6200 nM Ki J. Med. Chem. (2009) 52: 3994-4006 [PMID:19569717]
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 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 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 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. (2010) 18: 2195-2203 [PMID:20188574]
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 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. (2013) 21: 7435-7452 [PMID:24139167]
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 Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortex membranes incubated for 90 mins by radioligand competition assay B 4.85 pKi 14000 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
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 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 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 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 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 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 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 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 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 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 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 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 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 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 [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 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. (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 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 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 A2A adenosine receptor expressed in CHO cells B 5.77 pKi 1710 nM Ki MedChemComm (2016) 7: 845-852
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]MSX2 from human adenosine receptor A2A expressed in HEK293 cell membranes incubated for 30 mins by radioligand competition assay B 5.77 pKi 1710 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
ChEMBL Binding affinity to human adenosine A2A receptor by radioligand displacement assay B 5.77 pKi 1710 nM Ki MedChemComm (2018) 9: 951-962 [PMID:30108984]
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]MSX2 from adenosine receptor A2A in rat brain striatum membranes incubated for 30 mins by radioligand competition assay B 4.66 pKi 22000 nM Ki Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082]
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