cyclopentyladenosine [Ligand Id: 380] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL68738 (CCPA, Cyclopentyladenosine)
1 CHEMBL68738_lig_chart_1 A1 adenosine receptor Pig
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
  • A1 receptor/Adenosine A1 receptor in Mouse [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
  • 9.1
2 CHEMBL68738_lig_chart_2 Adenosine A1 receptor HumanBovineMouseRatGuinea pig
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Mouse [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
  • 6.24
3 CHEMBL68738_lig_chart_3 Adenosine A2a receptor HumanMouseRat
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • 4.7
4 CHEMBL68738_lig_chart_4 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Mouse [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
  • 6.82
5 CHEMBL68738_lig_chart_5 Adenosine A3 receptor HumanMouseRat
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  • Equilibrative nucleoside transporter 1 in Human [ChEMBL: CHEMBL1997] [GtoPdb: 1117] [UniProtKB: Q99808]
  • This target only has 1 pki data point
  • 5.96
6 CHEMBL68738_lig_chart_6 Equilibrative nucleoside transporter 1 Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
  • 0
7 CHEMBL68738_lig_chart_7 Plasmodium falciparum Plasmodium falciparum
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11]
ChEMBL Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane B 6.09 pKi 810 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane B 9.28 pKi 0.53 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Agonist activity at adenosine A1 receptor in pig cortical membrane assessed as stimulation of GTPgammaS binding B 8.1 pEC50 7.9 nM EC50 Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Displacement of [3H]CPX from adenosine A1 receptor in DDT1MF-2 cells B 7.67 pKi 21.5 nM Ki Bioorg. Med. Chem. (2008) 16: 1861-1873 [PMID:18042389]
ChEMBL Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells B 8 pKi 10 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 pKi 10 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 pKi 10 nM Ki J. Med. Chem. (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Binding affinity to adenosine A1 receptor (unknown origin) B 8.23 pKi 5.9 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Displacement of [3H]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 8.64 pKi 2.3 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of [3H]DPCPX from recombinant human A1 receptor expressed in CHO cell membranes B 8.64 pKi 2.3 nM Ki MedChemComm (2018) 9: 1920-1932
ChEMBL Radioligand Binding Assay: Membranes for radioligand binding experiments are prepared from fresh or frozen cells as described in Klotz et al., Naunyn-Schmiedeberg's Arch. Pharmacol, 357:1-9 (1998). The cell suspension is then homogenized in ice-cold hypotonic buffer (5 mM Tris/HCl, 2 mM EDTA, pH 7.4) and the homogenate is spun for 10 minutes (4° C.) at 1,000 g. The membranes are then sedimented from the supernatant for 30 minutes at 100,000 g and resuspended in 50 mM Tris/HCl buffer pH 7.4 (for A3 adenosine receptors: 50 mM Tris/HCl, 10 mM MgCl2, 1 mM EDTA, pH 8.25), frozen in liquid nitrogen at a protein concentration of 1-3 mg/mL and stored at −80° C. Dissociation constants of unlabeled compounds (Ki-values) are determined in competition experiments in 96-well microplates using the A1 selective agonist 2-chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA, 1 nM) for the characterization of A1 receptor binding. Nonspecific binding is determined in the presence of 100 μM R-PM and 1 mM theophylline, respectively. B 8.64 pKi 2.3 nM Ki US-8470800-B2. Method of reducing intraocular pressure in humans (2013)
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells B 8.65 pKi 2.25 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A1 receptor in CHO cells B 9.35 pKi 0.45 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
GtoPdb - - 9.4 pKi - - - Biochem Pharmacol (1998) 56: 1437-45 [PMID:9827575];
Eur J Pharmacol (2005) 510: 1-8 [PMID:15740718];
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
Br J Pharmacol (2006) 147: 533-41 [PMID:16444290];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376];
J Biol Chem (1994) 269: 32077-84 [PMID:7798201];
J Biol Chem (1999) 274: 3617-21 [PMID:9920910]
ChEMBL Agonist activity at adenosine A1 receptor assessed as inhibition of isoproterenol-stimulated cAMP accumulation in DDT1MF-2 cells F 8.57 pIC50 2.7 nM IC50 Bioorg. Med. Chem. (2008) 16: 1861-1873 [PMID:18042389]
ChEMBL Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay F 8.2 pEC50 6.3 nM EC50 J. Med. Chem. (2012) 55: 6467-6477 [PMID:22738238]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding to human adenosine A1 receptor F 8.38 pEC50 4.15 nM EC50 J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Compound was evaluated for the Adenosine A1 receptor agonist potency. F 9.72 pEC50 0.19 nM EC50 Bioorg. Med. Chem. Lett. (1996) 6: 811-814
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane B 5.91 pKi 1220 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane B 9.4 pKi 0.4 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 9.52 pKi 0.3 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
ChEMBL Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 9.66 pKi 0.22 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity for Adenosine A1 receptor in corpora striata of rats using [3H]NECA B 6.34 pKi 462 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Binding affinity towards rat Adenosine A1 receptor using [3H]-DPCPX B 6.64 pKi 230 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 815-818 [PMID:11277527]
ChEMBL Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX B 6.89 pKi 130 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in presence of 0.1 mM GTP B 7 pKi 99.21 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes in presence of GTP by radioligand competition assay B 7 pKi 99 nM Ki MedChemComm (2019) 10: 300-309
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in presence of 0.1 mM GTP B 7.2 pKi 63.08 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the presence of GTP. B 7.45 pKi 35.2 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the presence of GTP. B 7.45 pKi 35.2 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Affinity for the Adenosine A1 receptor in the presence of GTP (A1+GTP) by using [3H]-DPCPX as radioligand B 7.45 pKi 35.2 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat brain cortical membranes in presence of GTP B 7.45 pKi 35.2 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]DPCPX (with GTP) from Adenosine A1 receptor of rat cortical membrane B 7.46 pKi 35 nM Ki J. Med. Chem. (1996) 39: 1463-1471 [PMID:8691477]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes B 7.82 pKi 15.3 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 7.82 pKi 15.3 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 after 1 hr by scintillation counting analysis B 7.98 pKi 10.4 nM Ki Eur. J. Med. Chem. (2015) 104: 177-188 [PMID:26462195]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in Sprague-Dawley rat whole brain after 1 hr by scintillation counting B 8.07 pKi 8.48 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 734-738 [PMID:26776359]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor in rat brain membranes B 8.1 pKi 7.9 nM Ki MedChemComm (2019) 10: 300-309
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat whole brain membranes B 8.1 pKi 7.9 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Affinity towards adenosine A1 receptor from rat cortical membranes using [3H]DPCPX B 8.15 pKi 7.14 nM Ki J. Med. Chem. (2001) 44: 2966-2975 [PMID:11520205]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay B 8.17 pKi 6.8 nM Ki MedChemComm (2019) 10: 300-309
ChEMBL Displacement of [3H]DPCPX (without GTP) from Adenosine A1 receptor of rat cortical membrane B 8.23 pKi 5.9 nM Ki J. Med. Chem. (1996) 39: 1463-1471 [PMID:8691477]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat brain cortical membranes in absence of GTP B 8.23 pKi 5.9 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the absence of GTP B 8.23 pKi 5.9 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Displacement of [3H]DPCPX from rat cortical membranes Adenosine A1 receptor B 8.23 pKi 5.9 nM Ki J. Med. Chem. (1999) 42: 1393-1400 [PMID:10212125]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the absence of GTP B 8.23 pKi 5.9 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Affinity for the Adenosine A1 receptor in the absence of GTP (A1-GTP) by using [3H]DPCPX as radioligand B 8.23 pKi 5.9 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Binding affinity for Adenosine A1 receptor of rat cortical membrane by displacing [3H]DPCPX B 8.23 pKi 5.9 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2141-2144 [PMID:10999489]
ChEMBL Binding affinity for adenosine A1 receptor was assayed by displacement of [3H]DPCPX from rat cortical membranes. B 8.29 pKi 5.07 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in absence of GTP B 8.35 pKi 4.43 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 8.92 pKi 1.21 nM Ki J. Med. Chem. (1992) 35: 241-252 [PMID:1732541]
ChEMBL Tested for inhibition of adenosine A1 receptor binding to rat brain B 8.92 pKi 1.2 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2661-2666
ChEMBL Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1999) 42: 3463-3477 [PMID:10479279]
ChEMBL Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA B 9.1 pKi 0.8 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex membrane B 9.1 pKi 0.8 nM Ki Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes B 9.1 pKi 0.8 nM Ki J. Med. Chem. (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX B 9.1 pKi 0.8 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine binding to rat brain membranes B 9.22 pKi 0.6 nM Ki Bioorg. Med. Chem. Lett. (1991) 1: 481-486
ChEMBL Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1988) 31: 271-273 [PMID:3336027]
ChEMBL Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity against Adenosine A1 receptor using N6-[3H]cyclohexyladenosine in rat brain membranes B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL Binding affinity against Adenosine A1 receptor using [3H]CHA in rat brain membranes B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1989) 32: 8-11 [PMID:2909748]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1985) 28: 1383-1384 [PMID:2995663]
ChEMBL Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. B 9.23 pKi 0.59 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor B 9.35 pKi 0.45 nM Ki J. Med. Chem. (1991) 34: 3388-3390 [PMID:1766003]
ChEMBL Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor B 9.49 pKi 0.32 nM Ki J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897]
ChEMBL Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor B 9.52 pKi 0.3 nM Ki J. Med. Chem. (2002) 45: 1196-1202 [PMID:11881988]
ChEMBL Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor B 4.85 pIC50 14000 nM IC50 J. Med. Chem. (1988) 31: 752-756 [PMID:3351851]
ChEMBL Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor B 4.96 pIC50 11000 nM IC50 J. Med. Chem. (1988) 31: 752-756 [PMID:3351851]
ChEMBL Binding affinity towards adenosine A1 receptor rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding B 6.14 pIC50 720 nM IC50 J. Med. Chem. (1988) 31: 745-751 [PMID:3351850]
ChEMBL Evaluated for the binding affinity towards the Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. B 6.19 pIC50 640 nM IC50 J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain cortical membrane in presence of 100 uM GTP B 6.81 pIC50 154 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor B 7.24 pIC50 58 nM IC50 J. Med. Chem. (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain cortical membrane in absence of 100 uM GTP B 8.15 pIC50 7.09 nM IC50 Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
ChEMBL Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor B 9 pIC50 1 nM IC50 J. Med. Chem. (1991) 34: 2570-2579 [PMID:1875349]
ChEMBL Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding B 9.46 pIC50 0.35 nM IC50 J. Med. Chem. (1988) 31: 745-751 [PMID:3351850]
ChEMBL Evaluated for binding affinity against Adenosine A1 receptor B 9.49 pIC50 0.32 nM IC50 J. Med. Chem. (1992) 35: 629-635 [PMID:1542091]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding to adenosine A1 receptor of rat cerebral cortical membrane F 7.69 pEC50 20.3 nM EC50 J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Agonist activity at adenosine A1 receptor in rat cortical membrane by [35S]GTPgammaS binding assay F 7.77 pEC50 16.9 nM EC50 J. Nat. Prod. (2002) 65: 1479-1485 [PMID:12398547]
ChEMBL Effective concentration for [35S]GTP-gamma-S, binding to adenosine A1 receptor in rat brain membranes F 7.84 pEC50 14.3 nM EC50 J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Effective concentration for [35S]GTP-gamma-S, binding to adenosine A1 receptor in rat brain membranes F 7.84 pEC50 14.3 nM EC50 J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding to rat brain membranes by adenosine A1 receptor activation F 7.88 pEC50 13.3 nM EC50 J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]CPX in guinea pig DDT membrane; 19.5+/-12.0 B 7.71 pKi 19.5 nM Ki low Bioorg. Med. Chem. Lett. (2004) 14: 3793-3797 [PMID:15203164]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]CCPA in guinea pig DDT membrane B 9.1 pKi 0.8 nM Ki high Bioorg. Med. Chem. Lett. (2004) 14: 3793-3797 [PMID:15203164]
ChEMBL Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor B 9.49 pKi 0.32 nM Ki J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation F 7.9 pEC50 12.59 nM EC50 J. Med. Chem. (1991) 34: 1334-1339 [PMID:2016707]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane B 5.77 pKi 1700 nM Ki J. Med. Chem. (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in HEK293 cells B 5.78 pKi 1652 nM Ki Bioorg. Med. Chem. (2008) 16: 2741-2752 [PMID:18258439]
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 6.09 pKi 814 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
GtoPdb - - 6.1 pKi - - - Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay B 6.1 pKi 794 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells B 6.1 pKi 794 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer B 6.1 pKi 794 nM Ki J. Med. Chem. (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis B 6.1 pKi 794 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 6.1 pKi 790 nM Ki J. Med. Chem. (2005) 48: 2045-2053 [PMID:15771447]
ChEMBL Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A2A receptor in CHO cells B 6.34 pKi 462 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
ChEMBL Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes B 6.41 pKi 390 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 6.41 pKi 385 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from mouse A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay B 6.09 pKi 808 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes. B 5.47 pKi 3370 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatum membrane B 5.61 pKi 2470 nM Ki Bioorg. Med. Chem. (2010) 18: 2195-2203 [PMID:20188574]
GtoPdb - - 6.02 pKi 950 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
ChEMBL Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes B 6.07 pKi 857 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Binding affinity for adenosine A2A receptor of rat striatal membrane by displacing [3H]-ZM 241385 B 6.24 pKi 580 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 2141-2144 [PMID:10999489]
ChEMBL Binding affinity against Adenosine A2A receptor using [3H]-CGS- 21680 as the radioligand in rat striatal membranes B 6.24 pKi 580 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Binding affinity against Adenosine A2A receptor using [3H]-CGS- 21680 as the radioligand in rat striatal membranes B 6.24 pKi 580 nM Ki J. Med. Chem. (1998) 41: 102-108 [PMID:9438026]
ChEMBL Displacement of [3H]-CGS- 21980 from Adenosine A2A receptor of rat striatal membranes B 6.24 pKi 580 nM Ki J. Med. Chem. (1999) 42: 1393-1400 [PMID:10212125]
ChEMBL Binding affinity against Adenosine A2A receptor by using [3H]CGS-21680 as radioligand B 6.24 pKi 580 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 6.34 pKi 462 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Displacement of [3H]-NECA from Adenosine A2A receptor in rat striatal membranes B 6.34 pKi 460 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Affinity to Adenosine A2A receptor of rat brain striatum using [3H]-CGS- 21680 B 6.42 pKi 380 nM Ki J. Med. Chem. (2002) 45: 1196-1202 [PMID:11881988]
ChEMBL Displacement of [3H]-NECA from Adenosine A2A receptor in Sprague-Dawley rat striatal membranes B 6.48 pKi 331 nM Ki Bioorg. Med. Chem. (2015) 23: 6641-6649 [PMID:26392370]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue B 6.49 pKi 321 nM Ki J. Med. Chem. (1999) 42: 3463-3477 [PMID:10479279]
ChEMBL Displacement of [3H]NECA from adenosine A2A receptor in rat striatal membranes by radioligand competition assay B 6.79 pKi 163 nM Ki MedChemComm (2019) 10: 300-309
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells B 4.67 pKi 21200 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
GtoPdb - - 4.7 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity F 7.37 pKi 43 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells B 4.73 pKi