PENECA [Ligand Id: 378] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL223270
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
GtoPdb - - 6.2 pKi - - - J Med Chem (2002) 45: 3271-9 [PMID:12109910]
ChEMBL Binding affinity against Human recombinant Adenosine A1 receptor stably transfected in CHO cells using [3H]CCPA as radioligand B 6.25 pKi 560 nM Ki J. Med. Chem. (2002) 45: 3271-3279 [PMID:12109910]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells B 6.25 pKi 560 nM Ki J. Med. Chem. (2007) 50: 1222-1230 [PMID:17309246]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity towards adenosine A1 receptor in rat brain cortex B 6.16 pKi 698 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor of rat brain B 6.16 pKi 698 nM Ki J. Med. Chem. (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. B 6.16 pKi 698 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Functional activity against adenosine A1 receptor from rat atria. F 5 pEC50 >10000 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria F 9 pEC50 >1 nM EC50 J. Med. Chem. (1996) 39: 4211-4217 [PMID:8863798]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 6.2 pKi - - - J Med Chem (2002) 45: 3271-9 [PMID:12109910]
ChEMBL Binding affinity against Human recombinant Adenosine A2A receptor stably transfected in CHO cells using [3H]NECA as radioligand B 6.21 pKi 620 nM Ki J. Med. Chem. (2002) 45: 3271-3279 [PMID:12109910]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells B 6.21 pKi 620 nM Ki J. Med. Chem. (2007) 50: 1222-1230 [PMID:17309246]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity towards adenosine A2A receptor in rat brain striatum B 6.92 pKi 120 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. B 6.92 pKi 120 nM Ki J. Med. Chem. (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. B 6.92 pKi 120 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Functional activity against adenosine A2a receptor from rat aorta. F 5.82 pEC50 1500 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Vasorelaxation as Adenosine A2A receptor activity in rat aorta F 9 pEC50 >1 nM EC50 J. Med. Chem. (1996) 39: 4211-4217 [PMID:8863798]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Receptor-stimulated activity in CHO cells stably transfected with Human recombinant Adenosine A2B receptor using [3H]NECA as radioligand B 4 pEC50 >100000 nM EC50 J. Med. Chem. (2002) 45: 3271-3279 [PMID:12109910]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 8.2 pKi - - - J Med Chem (2002) 45: 3271-9 [PMID:12109910]
ChEMBL Binding affinity against Human recombinant Adenosine A3 receptor stably transfected in CHO cells using [3H]NECA as radioligand B 8.21 pKi 6.2 nM Ki J. Med. Chem. (2002) 45: 3271-3279 [PMID:12109910]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells B 8.21 pKi 6.2 nM Ki J. Med. Chem. (2007) 50: 1222-1230 [PMID:17309246]

ChEMBL data shown on this page come from version 28:

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]