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ChEMBL ligand: CHEMBL139000 (R-N6-(Phenylisopropyl)Adenosine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
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]