(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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]