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ChEMBL ligand: CHEMBL1950554 (Binodenoson, Corvue, MRE-0470, MRE0470, Wrc0470) |
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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]CCPA from human recombinant adenosine A1 receptor | B | 4.32 | pKi | 48000 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Binding affinity to human recombinant adenosine A1 receptor | B | 4.32 | pKi | 48000 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
GtoPdb | - | - | 4.32 | pKi | 48000 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells 90 mins by liquid scintillation counting analysis | B | 6.77 | pKi | 169 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis | B | 7.15 | pKi | 70.8 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | In vitro prolonging of the stimulus-QRS interval in guinea pig heart. | B | 5.45 | pEC50 | 3548.13 | nM | EC50 | J Med Chem (1992) 35: 4557-4561 [PMID:1469687] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Binding affinity to A2A adenosine receptor | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells | B | 6.57 | pKi | 270 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Binding affinity to human recombinant adenosine receptor A2a | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Binding affinity to human adenosine A2A receptor | B | 6.57 | pKi | 270 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
GtoPdb | - | - | 6.57 | pKi | 270 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells after 60 mins by liquid scintillation counting | B | 7.09 | pKi | 81 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis | B | 7.59 | pKi | 25.5 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
GtoPdb | - | - | 3.37 | pKi | 430000 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation counting analysis | B | 5 | pKi | >10000 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Agonist activity at human recombinant adenosine receptor A2b by cAMP assay | F | 4 | pEC50 | >100000 | nM | EC50 | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
GtoPdb | - | - | 6.04 | pKi | 903 | nM | Ki | Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor | B | 6.04 | pKi | 903 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Binding affinity to human recombinant adenosine A3 receptor | B | 6.04 | pKi | 903 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells after 180 mins by liquid scintillation counting analysis | B | 7.28 | pKi | 52.6 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
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]