(S)-PIA [Ligand Id: 415] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL420705
  • A1 receptor in Human [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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  • 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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  • A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542]
GtoPdb - - 6 pKi - - - J Biol Chem (1994) 269: 32077-84 [PMID:7798201];
J Biol Chem (1994) 269: 2373-6 [PMID:8300561]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes B 7.92 pKi 12 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 7.93 pKi 11.7 nM Ki J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain B 8.1 pKi 8 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 Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. B 6.7 pKi 200 nM Ki J Med Chem (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor B 7.3 pKi 50 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 7.31 pKi 49.3 nM Ki J Med Chem (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Binding affinity to adenosine A1 receptor in rat whole brain membranes by [3H]N6-cyclohexyladenosine displacement. B 7.31 pKi 49 nM Ki J Med Chem (1987) 30: 1709-1711 [PMID:2888894]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 7.32 pKi 47.6 nM Ki J Med Chem (1985) 28: 1383-1384 [PMID:2995663]
ChEMBL Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor B 7.96 pKi 11 nM Ki J Med Chem (2002) 45: 1196-1202 [PMID:11881988]
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 6.98 pIC50 105 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]
GtoPdb - - 5.1 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 5.74 pKi 1800 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 5.74 pKi 1800 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Inhibition of [3H]- NECA binding to adenosine receptor A2A B 5.52 pKi 3000 nM Ki J Med Chem (1991) 34: 3388-3390 [PMID:1766003]
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 6.89 pKi 130 nM Ki J Med Chem (1982) 25: 197-207 [PMID:6279840]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 7.17 pKi 68 nM Ki J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
GtoPdb - - 7.4 pKi - - - Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Mol Pharmacol (2000) 57: 968-75 [PMID:10779381]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 6.68 pEC50 210 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]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 6.62 pKi 241 nM Ki J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes B 6.62 pKi 241 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Affinity to Adenosine A3 receptor of rat testis membrane using [3H](R)-PIA with 150 nM DPCPX B 6.62 pKi 240 nM Ki J Med Chem (2002) 45: 1196-1202 [PMID:11881988]
A2B receptor in Human [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 5.2 pKi - - - Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300];
Mol Pharmacol (1999) 56: 705-13 [PMID:10496952]

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]