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

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ChEMBL ligand: CHEMBL392149 (Tecadenoson, CVT-510)
1 CHEMBL392149_lig_chart_1 A1 adenosine receptor Pig
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  • 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]
2 CHEMBL392149_lig_chart_2 Adenosine A1 receptor HumanPigBovineGuinea pig
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor in Pig [GtoPdb: 19]
3 CHEMBL392149_lig_chart_3 Adenosine A2a receptor HumanPig
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • This target only has 1 pki data point
4 CHEMBL392149_lig_chart_4 Adenosine A2b receptor Human
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • This target only has 1 pki data point
5 CHEMBL392149_lig_chart_5 Adenosine A3 receptor Human
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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 B 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 27:

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]