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ChEMBL ligand: CHEMBL45891 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]