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 Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay B 7.4 pKi 39.81 nM Ki J Med Chem (2021) 64: 6670-6695 [PMID:33724031]
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 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 [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 [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 cell membranes incubated for 60 mins by scintillation counting method B 8.66 pKi 2.2 nM Ki J Med Chem (2021) 64: 458-480 [PMID:33372800]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes after 60 mins B 8.66 pKi 2.2 nM Ki J Med Chem (2017) 60: 3372-3382 [PMID:28368607]
ChEMBL Displacement [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting method B 8.66 pKi 2.2 nM Ki J Med Chem (2020) 63: 7721-7739 [PMID:32573250]
ChEMBL Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membrane incubated for 60 mins by microbeta trilux scintillation counter analysis B 8.66 pKi 2.2 nM Ki J Med Chem (2022) 65: 2091-2106 [PMID:35068155]
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 Binding affinity at human Adenosine A1 receptor expressed in CHO cells B 8.67 pKi 2.13 nM Ki J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293 cells B 8.8 pKi 1.6 nM Ki J Med Chem (2008) 51: 400-406 [PMID:18189346]
ChEMBL Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membranes measured after 90 mins by scintillation counting method B 8.96 pKi 1.09 nM Ki J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
ChEMBL Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells B 9.05 pKi 0.9 nM Ki J Med Chem (2006) 49: 3682-3692 [PMID:16759111]
ChEMBL Antagonist activity against human adenosine A1 receptor F 9.05 pKi 0.9 nM Ki Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438]
GtoPdb - - 9.2 pKi 0.63 nM Ki J Biol Chem (1999) 274: 3617-21 [PMID:9920910];
J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631];
Eur J Pharmacol (2005) 510: 1-8 [PMID:15740718];
ChemMedChem (2006) 1: 891-902 [PMID:16902942];
Br J Pharmacol (1994) 111: 1252-6 [PMID:8032613]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 9.25 pKi 0.56 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
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]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]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 Antagonist activity against adenosine A1 receptor in human platelets F 9.33 pKi 0.47 nM Ki J Med Chem (1990) 33: 1906-1910 [PMID:1694546]
ChEMBL Inhibition of human adenosine A1 receptor B 7.6 pIC50 25 nM IC50 Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Binding affinity against human A1 receptor (hA1) was measured through displacement of [3H]DPCPX using yeast cell membranes B 7.85 pIC50 14 nM IC50 Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL Inhibitory activity against human A1 receptor (hA1) on membranes from yeast cells B 7.89 pIC50 13 nM IC50 Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879]
ChEMBL Inhibition of human adenosine A1 receptor B 7.89 pIC50 13 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of radiolabeled DPCPX from human adenosine A1 receptor B 8.17 pIC50 6.7 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 9.05 pIC50 0.89 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human adenosine A1 receptor by radioligand displacement assay B 9.06 pIC50 0.87 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells measured after 60 mins by scintillation counting method B 9.3 pIC50 0.5 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Inverse agonist activity at human A1AR expressed in CHO cells assessed as increase in forskolin-stimulated cAMP production by alphascreen assay F 8.82 pEC50 1.52 nM EC50 J Med Chem (2019) 62: 6894-6912 [PMID:31306001]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane B 9.3 pKi 0.5 nM Ki Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446]
ChEMBL Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement. B 9.3 pKi 0.5 nM Ki J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor in bovine brain membranes B 9.3 pKi 0.5 nM Ki J Med Chem (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor in bovine cerebral cortical membranes B 9.3 pKi 0.5 nM Ki J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in bovine brain membranes B 9.3 pKi 0.5 nM Ki J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL Displacement of [3H]DPCPX from bovine brain cortical membrane adenosine A1 receptor B 9.3 pKi 0.5 nM Ki J Med Chem (2009) 52: 2407-2419 [PMID:19301821]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes B 9.3 pKi 0.5 nM Ki J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL Binding affinity at bovine Adenosine A1 receptor. B 9.34 pKi 0.46 nM Ki J Med Chem (2002) 45: 4875-4887 [PMID:12383013]
ChEMBL Affinity to A1 adenosine receptor was measured by the displacement of [3H]PIA in bovine brain cortical membrane B 9.34 pKi 0.46 nM Ki J Med Chem (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand B 9.6 pKi 0.25 nM Ki J Med Chem (2004) 47: 3019-3031 [PMID:15163184]
ChEMBL Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes B 9.77 pKi 0.17 nM Ki J Med Chem (1998) 41: 555-563 [PMID:9484505]
ChEMBL Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes B 9.81 pKi 0.15 nM Ki J Med Chem (1998) 41: 555-563 [PMID:9484505]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL pA2 against rat brain adenosine A1 receptor B 8.24 pKd 5.75 nM Kd Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL Binding affinity for Adenosine A1 receptor of rat forebrain B 8.42 pKi 3.77 nM Ki J Med Chem (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates. B 8.82 pKi 1.5 nM Ki J Med Chem (1996) 39: 1164-1171 [PMID:8676354]
ChEMBL Binding affinity at rat Adenosine A1 receptor in the absence of GTP B 8.84 pKi 1.46 nM Ki J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL Binding affinity at rat Adenosine A1 receptor in the presence of GTP B 8.92 pKi 1.2 nM Ki J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells B 9 pKi 1 nM Ki J Med Chem (2002) 45: 2131-2138 [PMID:12014951]
ChEMBL Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes B 9.05 pKi 0.9 nM Ki J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Binding affinity towards adenosine A1 receptor in rat cortical membranes using N6-[3H]cyclohexyladenosine as radioligand B 9.05 pKi 0.9 nM Ki J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes B 9.05 pKi 0.9 nM Ki J Med Chem (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex membrane B 9.05 pKi 0.9 nM Ki Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Inhibition of [3H]CCPA binding to rat adenosine A1 receptor B 9.05 pKi 0.9 nM Ki J Med Chem (2002) 45: 1500-1510 [PMID:11906291]
ChEMBL Inhibition of [3H]CCPA binding to adenosine A1 receptor B 9.05 pKi 0.9 nM Ki J Med Chem (2005) 48: 2108-2114 [PMID:15771453]
ChEMBL Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes B 9.05 pKi 0.9 nM Ki J Med Chem (1989) 32: 1873-1879 [PMID:2754711]
ChEMBL GTP-induced shift at rat Adenosine A1 receptor (A1AR) B 9.11 pKi 0.77 nM Ki J Med Chem (2002) 45: 1845-1852 [PMID:11960496]
ChEMBL Evaluated for binding affinity against Adenosine A1 receptor B 9.21 pKi 0.62 nM Ki J Med Chem (1992) 35: 629-635 [PMID:1542091]
ChEMBL Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane B 9.22 pKi 0.6 nM Ki J Med Chem (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat whole brain membranes B 9.25 pKi 0.56 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes B 9.26 pKi 0.55 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in absence of GTP B 9.26 pKi 0.55 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by scintillation counting B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2010) 45: 1739-1745 [PMID:20116907]
ChEMBL Displacement of [3H]CCPA from rat adenosine A1 receptor B 9.3 pKi 0.5 nM Ki Eur J Med Chem (2008) 43: 614-620 [PMID:17602796]
ChEMBL Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine B 9.31 pKi 0.49 nM Ki J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in presence of 0.1 mM GTP B 9.32 pKi 0.48 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand B 9.34 pKi 0.46 nM Ki J Med Chem (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL Binding affinity against adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes B 9.34 pKi 0.46 nM Ki J Med Chem (1992) 35: 924-930 [PMID:1548682]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 9.34 pKi 0.46 nM Ki J Med Chem (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine B 9.34 pKi 0.46 nM Ki J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane B 9.34 pKi 0.46 nM Ki J Med Chem (1994) 37: 3373-3382 [PMID:7932565]
ChEMBL Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes B 9.34 pKi 0.46 nM Ki J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay B 9.4 pKi 0.4 nM Ki Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes in presence of GTP by radioligand competition assay B 9.4 pKi 0.4 nM Ki Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes B 9.52 pKi 0.3 nM Ki Medchemcomm (2019) 10: 300-309 [PMID:30881617]
ChEMBL Displacement of [3H]-PIA from Adenosine A1 receptor in Wistar rat brain membranes B 9.52 pKi 0.3 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Adenosine A1 receptor binding using [3H]DPCPX in rat cortical membranes B 9.55 pKi 0.28 nM Ki J Med Chem (1999) 42: 779-783 [PMID:10072675]
ChEMBL Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from rat cortical membranes B 9.64 pKi 0.23 nM Ki J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Binding affinity against adenosine A1 receptor in rat cortex by the displacement of [3H]cyclohexyladenosine (CHA). B 9.64 pKi 0.23 nM Ki J Med Chem (1991) 34: 1431-1435 [PMID:2016719]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in absence of GTP B 9.64 pKi 0.23 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in presence of 0.1 mM GTP B 9.68 pKi 0.21 nM Ki Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370]
GtoPdb - - 9.74 pKi 0.18 nM Ki ChemMedChem (2006) 1: 891-902 [PMID:16902942];
J Med Chem (2002) 45: 2131-8 [PMID:12014951];
Naunyn Schmiedebergs Arch Pharmacol (1991) 343: 196-201 [PMID:2067592]
ChEMBL Antagonist activity at adenosine A1 receptor in rat cortical membrane assessed as reduction of [35S]GTPgammaS binding F 8.22 pIC50 6 nM IC50 J Nat Prod (2002) 65: 1479-1485 [PMID:12398547]
ChEMBL Inhibitory activity against Adenosine A1 Receptor using [3H]CHA in rat cortical membranes B 8.33 pIC50 4.7 nM IC50 Bioorg Med Chem Lett (1999) 9: 1979-1984 [PMID:10450966]
ChEMBL Inhibition of [3H]-CHA binding against Adenosine A1 receptors of rat cortical membranes; Not tested B 8.33 pIC50 4.7 nM IC50 Bioorg Med Chem Lett (1996) 6: 2059-2062
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Displacement of N6-[3H]cyclohexyladenosine from adenosine receptor A1 in guinea pig forebrain membranes by liquid scintillation counting method B 8.19 pKi 6.4 nM Ki J Med Chem (2020) 63: 13291-13315 [PMID:32805118]
ChEMBL Binding affinity towards adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig forebrain membranes B 8.19 pKi 6.4 nM Ki J Med Chem (1992) 35: 3578-3581 [PMID:1404238]
ChEMBL Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor B 8.19 pKi 6.4 nM Ki J Med Chem (1991) 34: 466-469 [PMID:1992150]
ChEMBL Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand B 8.19 pKi 6.4 nM Ki J Med Chem (1992) 35: 3066-3075 [PMID:1501234]
ChEMBL Binding affinity against adenosine A1 receptor using N6-[3H]cyclohexyladenosine as radioligand in guinea pig forebrain membranes B 8.19 pKi 6.4 nM Ki J Med Chem (1992) 35: 924-930 [PMID:1548682]
ChEMBL Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement. B 8.19 pKi 6.4 nM Ki J Med Chem (1993) 36: 2508-2518 [PMID:8355252]
ChEMBL Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand. B 8.19 pKi 6.4 nM Ki J Med Chem (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Binding affinity for Adenosine A1 receptor from Guinea pig membranes B 8.53 pKi 2.93 nM Ki J Med Chem (1997) 40: 1773-1778 [PMID:9191953]
ChEMBL Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor) F 8.88 pIC50 1.31 nM IC50 Bioorg Med Chem Lett (1996) 6: 2059-2062
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Then it has been reconstituted into rHDLs membrane discs.Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. B 6.97 pKd 106.44 nM Kd K4DD drug target binding kinetics data
ChEMBL The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. B 7.12 pKd 76.29 nM Kd K4DD drug target binding kinetics data
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 6.1 pKi 788 nM Ki J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 B 6.2 pKi 630 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane B 6.47 pKi 340 nM Ki J Med Chem (1994) 37: 2970-2975 [PMID:8071944]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins B 6.47 pKi 337 nM Ki Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane B 6.47 pKi 337 nM Ki J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes B 6.47 pKi 337 nM Ki J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes. B 6.47 pKi 337 nM Ki J Med Chem (2000) 43: 3118-3124 [PMID:10956220]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.47 pKi 337 nM Ki J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes B 6.47 pKi 337 nM Ki J Med Chem (2005) 48: 7932-7945 [PMID:16335918]
ChEMBL Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes B 6.47 pKi 337 nM Ki J Med Chem (2006) 49: 3916-3925 [PMID:16789747]
ChEMBL Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane