DPCPX [Ligand Id: 386] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL183 (GNF-Pf-2224)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: 114] [GtoPdb: 18] [UniProtKB: P30542]
  • Adenosine A1 receptor in Bovine [ChEMBL: 12265] [UniProtKB: P28190]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: 12512] [GtoPdb: 18] [UniProtKB: P25099]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: 105567] [UniProtKB: P47745]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: 252] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: 11736] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: 278] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: 12854] [GtoPdb: 20] [UniProtKB: P29276]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: 280] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: 12171] [GtoPdb: 21] [UniProtKB: P28647]
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  • μ receptor/Mu opioid receptor in Human [ChEMBL: 129] [GtoPdb: 319] [UniProtKB: P35372]
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DB Assay description Assay Type Standard value Standard activity Original value Original units Original activity Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: 114] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL pA2 against human brain adenosine A1 receptor B 8.43 pKd 3.72 nM Kd Bioorg. Med. Chem. Lett. (1998) 8: 691-694 [PMID:9871584]
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 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 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 [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 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 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 B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
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 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 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 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 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]
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 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]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. (2005) 48: 8253-8260 [PMID:16366607]
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 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]
GtoPdb - - 9.2 pKi 0.63 nM Ki J. Biol. Chem. (1999) 274: 3617-3621 [PMID:9920910];
J Pharmacol Exp Ther (2005) 315: 329-336 [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 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]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: 12265] [UniProtKB: P28190]
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 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]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]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]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 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 [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 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 at bovine Adenosine A1 receptor. B 9.34 pKi 0.46 nM Ki J. Med. Chem. (2002) 45: 4875-4887 [PMID:12383013]
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 0.16 nM Ki J. Med. Chem. (1998) 41: 555-563 [PMID:9484505]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: 12512] [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 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 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 [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 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 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 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 (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 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 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]-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]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 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 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 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 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 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 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 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 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]-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 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
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]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: 105567] [UniProtKB: P47745]
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 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 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 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 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 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: 252] [GtoPdb: 19] [UniProtKB: P29274]
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 cells B 6.47 pKi 337 nM Ki J. Med. Chem. (2008) 51: 1764-1770 [PMID:18269230]
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 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]-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 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 in bovine striatal membranes B 6.47 pKi 337 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 6.47 pKi 337 nM Ki J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918]
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]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]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 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 [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 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 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]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 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 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 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]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]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]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 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]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 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 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]
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]
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: 353-360 [PMID:9179373];
ChemMedChem (2006) 1: 891-902 [PMID:16902942]
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]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: 11736] [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 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 adenosine A2a receptor B 6.33 pKi 470 nM Ki J. Med. Chem. (2005) 48: 2108-2114 [PMID:15771453]
ChEMBL Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor B 6.33 pKi 470 nM