AS100 [Ligand Id: 381] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL32802
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
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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 - - 6.5 pKi - - - Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]
ChEMBL Displacement of specific [3H]DPCPX binding at human adenosine A1 receptor expressed in CHO cells B 6.52 pKi 300 nM Ki J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Binding affinity of compound for displacement of specific [3H]ZM-241385 binding at human adenosine A2A receptor expressed in CHO cells B 6 pKi >1000 nM Ki J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Binding affinity of compound for displacement of specific [3H]- DPCPX binding at human A2B receptors expressed in HEK293 cells B 7.8 pKi 16 nM Ki J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]
ChEMBL Binding affinity of compound for displacement of [3H]DPCPX binding in HEK293 membranes expressing human A2B adenosine receptors B 7.8 pKi 16 nM Ki J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]
GtoPdb - - 8.2 pKi - - - Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]
ChEMBL Inhibitory activity against cAMP production in CHO cells transfected with human A2B adenosine receptor F 7.22 pIC50 60 nM IC50 J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity of compound for displacement of specific [3H]MRE3008-F20 binding at human A3 receptors expressed in CHO cells B 6 pKi >1000 nM Ki J. Med. Chem. (2004) 47: 1434-1447 [PMID:14998332]

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]