PSB-10 [Ligand Id: 5619] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1562432
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
1 CHEMBL1562432_lig_chart_1 Adenosine A3 receptor Human
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  • A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542]
  • A1 receptor in Rat [GtoPdb: 18] [UniProtKB: P25099]
2 CHEMBL1562432_lig_chart_2 A1 receptor HumanRat
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  • A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor in Rat [GtoPdb: 19] [UniProtKB: P30543]
3 CHEMBL1562432_lig_chart_3 A2A receptor HumanRat
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  • A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
  • This target only has 1 pki data point
4 CHEMBL1562432_lig_chart_4 A2B receptor Mouse
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 B 8.02 pKi 9.54 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 9.36 pKi 0.44 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
GtoPdb - - 9.36 pKi 0.44 nM Ki J. Med. Chem. (2002) 45: 3440-50 [PMID:12139454]
ChEMBL Inverse agonist activity at human recombinant A3 adenosine receptor expressed CHO cells by [35S]GTPgammaS binding assay F 8.4 pIC50 4 nM IC50 J. Med. Chem. (2011) 54: 5205-5220 [PMID:21675777]
A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542]
GtoPdb - - 5.77 pKi 1700 nM Ki Bioorg. Med. Chem. (2003) 11: 347-56 [PMID:12517430]
A1 receptor in Rat [GtoPdb: 18] [UniProtKB: P25099]
GtoPdb - - 6.09 pKi 805 nM Ki J. Med. Chem. (2002) 45: 3440-50 [PMID:12139454]
A2A receptor in Human [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 5.57 pKi 2700 nM Ki Bioorg. Med. Chem. (2003) 11: 347-56 [PMID:12517430]
A2A receptor in Rat [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 5.22 pKi 6040 nM Ki J. Med. Chem. (2002) 45: 3440-50 [PMID:12139454]
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 5.68 pKi 2100 nM Ki J. Med. Chem. (2002) 45: 3440-50 [PMID:12139454]

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]