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 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]