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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 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]