tecadenoson [Ligand Id: 5592] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL392149 (CVT-510, Tecadenoson)
There should be some charts here, you may need to enable JavaScript!
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor in Pig [GtoPdb: 18]
  • Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor in Pig [GtoPdb: 19]
There should be some charts here, you may need to enable JavaScript!
  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
There should be some charts here, you may need to enable JavaScript!
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 32:

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]