(R)-PIA [Ligand Id: 414] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL139000 (R-N6-(Phenylisopropyl)Adenosine)
  • 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 Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
1 CHEMBL139000_lig_chart_1 Adenosine A1 receptor HumanBovineRat
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
  • Adenosine A2a receptor in Guinea pig [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
2 CHEMBL139000_lig_chart_2 Adenosine A2a receptor HumanRatGuinea pig
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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]
3 CHEMBL139000_lig_chart_3 Adenosine A2b receptor HumanMouse
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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]
4 CHEMBL139000_lig_chart_4 Adenosine A3 receptor HumanRat
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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 Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells after 90 mins B 6.31 pKi 490 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells B 8.7 pKi 2 nM Ki J. Med. Chem. (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Binding affinity to adenosine A1 receptor (unknown origin) B 8.7 pKi 2 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
GtoPdb - - 8.7 pKi - - - J. Biol. Chem. (1994) 269: 32077-84 [PMID:7798201];
J. Biol. Chem. (1999) 274: 3617-21 [PMID:9920910];
J. Biol. Chem. (1994) 269: 2373-6 [PMID:8300561];
Biochem. Pharmacol. (2004) 68: 1985-93 [PMID:15476669];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells after 90 mins B 6.08 pIC50 830 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells B 5.92 pEC50 1200 nM EC50 J. Nat. Prod. (2006) 69: 432-435 [PMID:16562853]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Intrinsic activity towards Adenosine A1 receptor as displacement of [3H]DPCPX from bovine cortical membranes with 1 mM GTP B 7.7 pKi 19.9 nM Ki J. Med. Chem. (2001) 44: 316-327 [PMID:11462973]
ChEMBL Intrinsic activity towards Adenosine A1 receptor as displacement of [3H]DPCPX from bovine cortical membranes without GTP B 8.38 pKi 4.2 nM Ki J. Med. Chem. (2001) 44: 316-327 [PMID:11462973]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 9.22 pKi 0.6 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 9.22 pKi 0.6 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain B 9.6 pKi 0.25 nM Ki J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX B 6.7 pKi 200 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Affinity for the Adenosine A1 receptor in the presence of GTP (A1+GTP) by using [3H]-DPCPX as radioligand B 7.21 pKi 62 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Affinity for the Adenosine A1 receptor in the absence of GTP (A1-GTP) by using [3H]DPCPX as radioligand B 7.96 pKi 11 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. B 8.52 pKi 3 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain B 8.59 pKi 2.6 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 8.89 pKi 1.3 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1988) 31: 1179-1183 [PMID:3373486]
GtoPdb - - 8.92 pKi 1.2 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Binding affinity to adenosine A1 receptor in rat whole brain membranes by [3H]N6-cyclohexyladenosine displacement. B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1987) 30: 1709-1711 [PMID:2888894]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1988) 31: 271-273 [PMID:3336027]
ChEMBL Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1991) 34: 3388-3390 [PMID:1766003]
ChEMBL Binding affinity for Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]-CHA B 8.93 pKi 1.17 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. B 8.93 pKi 1.17 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 8.94 pKi 1.15 nM Ki J. Med. Chem. (1985) 28: 1383-1384 [PMID:2995663]
ChEMBL Binding affinity for adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1986) 29: 346-353 [PMID:3005574]
ChEMBL Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX B 9 pKi 1 nM Ki J. Med. Chem. (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor B 9.22 pKi 0.6 nM Ki J. Med. Chem. (2002) 45: 1196-1202 [PMID:11881988]
ChEMBL Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor B 7.4 pIC50 40 nM IC50 J. Med. Chem. (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor B 8.3 pIC50 5 nM IC50 J. Med. Chem. (1991) 34: 2570-2579 [PMID:1875349]
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 8.62 pIC50 2.4 nM IC50 J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells B 6.05 pKi 884 nM Ki J. Med. Chem. (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 6.12 pKi 750 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes B 6.12 pKi 750 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]
GtoPdb - - 6.2 pKi - - - Biochem. Pharmacol. (2004) 68: 1985-93 [PMID:15476669];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566];
J. Biol. Chem. (1995) 270: 13987-97 [PMID:7775460];
Biochem. Pharmacol. (1999) 57: 65-75 [PMID:9920286];
Br. J. Pharmacol. (1997) 121: 353-60 [PMID:9179373]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 6.66 pKi 220 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Binding affinity against Adenosine A2A receptor by using [3H]CGS-21680 as radioligand B 6.85 pKi 140 nM Ki J. Med. Chem. (1995) 38: 4000-4006 [PMID:7562934]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue B 6.93 pKi 117 nM Ki J. Med. Chem. (1999) 42: 3463-3477 [PMID:10479279]
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to guinea pig brain B 8.48 pKi 3.3 nM Ki J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 5.5 pKi - - - Biochem. Pharmacol. (2005) 70: 1601-12 [PMID:16219300];
Mol. Pharmacol. (1999) 56: 705-13 [PMID:10496952];
Biochem. Pharmacol. (2001) 61: 657-63 [PMID:11266650];
Mol. Pharmacol. (2000) 58: 1349-56 [PMID:11093773];
Can. J. Physiol. Pharmacol. (1980) 58: 673-91 [PMID:6253037]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase F 3.23 pEC50 -3.23 - logEC50 J. Med. Chem. (2008) 51: 2088-2099 [PMID:18321038]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production F 5.77 pEC50 1680 nM EC50 J. Med. Chem. (2007) 50: 1810-1827 [PMID:17378544]
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 4.72 pKi 19000 nM Ki Biochem. Pharmacol. (1994) 47: 801-14 [PMID:8135856]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity to adenosine A3 receptor (unknown origin) B 7.8 pKi 16 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 8.06 pKi 8.7 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.06 pKi 8.7 nM Ki J. Med. Chem. (2007) 50: 1810-1827 [PMID:17378544]
GtoPdb - - 8.1 pKi - - - Proc. Natl. Acad. Sci. U.S.A. (1993) 90: 10365-9 [PMID:8234299];
Biochem. Pharmacol. (2004) 68: 1985-93 [PMID:15476669];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566];
Mol. Pharmacol. (2000) 57: 968-75 [PMID:10779381];
Neuropharmacology (1997) 36: 1157-65 [PMID:9364471]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 7.57 pEC50 27 nM EC50 J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
GtoPdb - - 6.8 pKi - - - J. Biol. Chem. (1994) 269: 24692-8 [PMID:7929142];
Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 7.28 pKi 53 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Affinity to Adenosine A3 receptor of rat testis membrane using [3H](R)-PIA with 150 nM DPCPX B 7.28 pKi 53 nM Ki J. Med. Chem. (2002) 45: 1196-1202 [PMID:11881988]
ChEMBL Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes B 7.28 pKi 53 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]