(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]
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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]
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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]
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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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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 USA (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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]