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

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ChEMBL ligand: CHEMBL183 (GNF-Pf-2224)
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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]
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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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  • μ receptor/Mu opioid receptor in Human [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372]
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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 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 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 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 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]CHA from cloned human adenosine A1 receptor expressed in CHO cells B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]CHA B 8.49 pKi 3.2 nM Ki J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells B 8.49 pKi 3.2 nM Ki Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO-A1 cells after 60 mins B 8.49 pKi 3.2 nM Ki Bioorg. Med. Chem. (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins B 8.49 pKi 3.2 nM Ki Eur. J. Med. Chem. (2015) 89: 32-41 [PMID:25462223]
ChEMBL Inhibitory constant aganist human adenosine A1 receptor B 8.52 pKi 3 nM Ki J. Med. Chem. (2007) 50: 65-73 [PMID:17201410]
ChEMBL Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A1 receptor B 8.6 pKi 2.52 nM Ki J. Med. Chem. (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO 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 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]
GtoPdb - - 9.2 pKi 0.63 nM Ki J. Biol. Chem. (1999) 274: 3617-21 [PMID:9920910];
J. Pharmacol. Exp. Ther. (2005) 315: 329-36 [PMID:16020631];
Eur. J. Pharmacol. (2005) 510: 1-8 [PMID:15740718];
ChemMedChem (2006) 1: 891-902 [PMID:16902942];
Br. J. Pharmacol. (1994) 111: 1252-6 [PMID:8032613]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 9.25 pKi 0.56 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [3H]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 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. (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]
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 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 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 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 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 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 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 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 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 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 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 for Adenosine A1 receptor from Guinea pig membranes B 8.53 pKi 2.93 nM Ki J. Med. Chem. (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor) F 8.88 pIC50 1.31 nM IC50 Bioorg. Med. Chem. Lett. (1996) 6: 2059-2062
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Then it has been reconstituted into rHDLs membrane discs.Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. B 6.97 pKd 106.44 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. B 7.12 pKd 76.29 nM Kd K4DD drug target binding kinetics data
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 6.1 pKi 788 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 B 6.2 pKi 630 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane B 6.47 pKi 340 nM Ki J. Med. Chem. (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins B 6.47 pKi 337 nM Ki Eur. J. Med. Chem. (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane B 6.47 pKi 337 nM Ki J. Med. Chem. (2001) 44: 316-327 [PMID:11462973]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes B 6.47 pKi 337 nM Ki J. Med. Chem. (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes. B 6.47 pKi 337 nM Ki J. Med. Chem. (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J. Med. Chem. (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J. Med. Chem. (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes B 6.47 pKi 337 nM Ki J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes B 6.47 pKi 337 nM Ki J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane B 6.47 pKi 337 nM Ki J. Med. Chem. (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 6.54 pKi 291 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells after 120 mins B 6.58 pKi 260.3 nM Ki Eur. J. Med. Chem. (2015) 89: 32-41 [PMID:25462223]
ChEMBL Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells B 6.59 pKi 260 nM Ki Bioorg. Med. Chem. (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL Displacement of [3H]NECA from cloned human adenosine A2A receptor expressed in CHO cells B 6.59 pKi 260 nM Ki J. Med. Chem. (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.59 pKi 260 nM Ki J. Med. Chem. (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.59 pKi 260 nM Ki J. Med. Chem. (2007) 50: 4061-4074 [PMID:17665891]
ChEMBL Displacement of [3H]NECA from human cloned adenosine A2A receptor expressed in CHO cells B 6.59 pKi 260 nM Ki J. Med. Chem. (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL Displacement of [3H]ZM241385 from human adenosine A2a receptor expressed in HeLa cells after 30 mins B 6.59 pKi 260 nM Ki Bioorg. Med. Chem. (2010) 18: 7890-7899 [PMID:20937560]
ChEMBL Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 6.65 pKi 226 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity against adenosine A2 receptor in bovine striatal membranes using [3H]-CGS-21,680 as radioligand B 6.7 pKi 200 nM Ki J. Med. Chem. (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL Displacement of [3H]4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol from human adenosine A2A receptor expressed in human Hela cell membranes after 30 mins B 6.8 pKi 157 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement of [3H]ZM241385 from human Adenosine A2A receptor expressed in HeLa cells after 30 mins B 6.8 pKi 157 nM Ki J. Med. Chem. (2016) 59: 1967-1983 [PMID:26824742]
ChEMBL Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand B 6.84 pKi 144 nM