tecadenoson [Ligand Id: 5592] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL392149 (CVT-510, Tecadenoson) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| A1 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11] | ||||||||
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane | B | 5.01 | pKi | 9756 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane | B | 8.12 | pKi | 7.6 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Agonist activity at adenosine A1 receptor in pig cortical membrane assessed as stimulation of GTPgammaS binding | F | 7.5 | pEC50 | 31.6 | nM | EC50 | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
| ChEMBL | Displacement of [3H]CPX from adenosine A1 receptor expressed in DDT1 MF2 cells | B | 7.19 | pKi | 65 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| ChEMBL | Binding affinity for adenosine A1 receptor determined using hamster DDT1 cell membranes with [3H]CCPA as radioligand | B | 8.52 | pKi | 3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 535-539 [PMID:14698198] |
| ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 8.69 | pKi | 2.05 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Agonist activity at adenosine A1 receptor expressed in DDT1 MF2 cells assessed as inhibition of (-)-isoproterenol-stimulated cAMP accumulation | F | 8.09 | pIC50 | 8.2 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| A1 receptor in Pig [GtoPdb: 18] | ||||||||
| GtoPdb | - | - | 8.19 | pKi | 6.5 | nM | Ki |
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]; Biochim Biophys Acta (2011) 1808: 1290-308 [PMID:21185259] |
| Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane | B | 5.14 | pKi | 7300 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane | B | 8.51 | pKi | 3.1 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
| ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CPX in guinea pig DDT membrane; 543+/-182 | B | 6.27 | pKi | 543 | nM | Ki low | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CCPA in guinea pig DDT membrane; 3.25+/-0.74 | B | 8.49 | pKi | 3.25 | nM | Ki high | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| ChEMBL | Agonistic activity against adenosine A1 receptor in guinea pig isolated hearts | F | 7.39 | pEC50 | 41 | nM | EC50 | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
| A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
| ChEMBL | Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 5.19 | pKi | 6390 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A2A receptor in Pig [GtoPdb: 19] | ||||||||
| GtoPdb | - | - | 5.64 | pKi | 2315 | nM | Ki |
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]; Biochim Biophys Acta (2011) 1808: 1290-308 [PMID:21185259] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity | F | 6.64 | pKi | 227 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
| A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells | B | 4.59 | pKi | 25800 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
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]
