N(6)-cyclohexyladenosine [Ligand Id: 423] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL45891
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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]
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  • A3 receptor in Human [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
Adenosine A1 receptor in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2114] [UniProtKB: P49892]
ChEMBL Displacement of [125I]ABA from adenosine A1 receptor of chick cerebellar membrane B 8.6 pIC50 2.5 nM IC50 J. Med. Chem. (1987) 30: 954-956 [PMID:3572985]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain B 8.6 pKi 2.5 nM Ki J. Med. Chem. (1982) 25: 197-207 [PMID:6279840]
ChEMBL Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes B 8.89 pKi 1.3 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H] CGS 21680 from rat hippocampus adenosine A1 receptor B 8.89 pKd 1.3 nM Kd J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Binding affinity for adenosine A1 receptor was assayed by displacement of [3H]DPCPX from rat cortical membranes. B 7.68 pKi 21 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Binding affinity for Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA B 8.52 pKi 3 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 8.85 pKi 1.42 nM Ki J. Med. Chem. (1989) 32: 1667-1673 [PMID:2754691]
ChEMBL Binding affinity for Adenosine A1 receptor in corpora striata of rats using [3H]NECA B 8.88 pKi 1.31 nM Ki J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 8.88 pKi 1.31 nM Ki J. Med. Chem. (1985) 28: 1383-1384 [PMID:2995663]
ChEMBL Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine binding to rat brain membranes B 8.89 pKi 1.3 nM Ki Bioorg. Med. Chem. Lett. (1991) 1: 481-486
ChEMBL Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
GtoPdb - - 9.07 pKi 0.85 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
ChEMBL Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor B 9.07 pKi 0.85 nM Ki J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897]
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 Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. B 8.7 pIC50 2 nM IC50 J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. B 8.77 pIC50 1.7 nM IC50 J. Med. Chem. (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Evaluated for binding affinity against Adenosine A1 receptor B 9.07 pIC50 0.85 nM IC50 J. Med. Chem. (1992) 35: 629-635 [PMID:1542091]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 5.9 pKi - - - Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286];
Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]
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]
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 6.22 pKi 600 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
GtoPdb - - 6.34 pKi 460 nM Ki Pharmacology (1993) 46: 91-100 [PMID:8441759]
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 8.3 pKi 5 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 - - 3.8 pKi 160000 nM Ki 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 4.28 pEC50 -4.28 - logEC50 J. Med. Chem. (2008) 51: 2088-2099 [PMID:18321038]
A3 receptor in Human [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 5.99 pKi 1025 nM Ki J Immunol (1996) 156: 3435-42 [PMID:8617970]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
GtoPdb - - 6.75 pKi 176 nM Ki Mol Pharmacol (1994) 45: 1101-11 [PMID:8022403]
ChEMBL Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes B 7.6 pKi 25 nM Ki J. Med. Chem. (2000) 43: 2814-2823 [PMID:10956189]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]