8-cyclopentyltheophylline [Ligand Id: 385] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL106265
  • A1 receptor in Human [GtoPdb: 18] [UniProtKB: P30542]
  • Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
  • A1 receptor/Adenosine A1 receptor in Rat [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
  • Adenosine A1 receptor in Guinea pig [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
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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 in Human [GtoPdb: 18] [UniProtKB: P30542]
GtoPdb - - 8 pKi - - - Biochem Pharmacol (1998) 56: 1437-45 [PMID:9827575]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Binding affinity towards adenosine A1 receptor of bovine brain membrane using [3H]-CHA at 20 uM B 9.3 pKi 0.5 nM Ki J. Med. Chem. (2000) 43: 1158-1164 [PMID:10737748]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes B 7.62 pKi 24 nM Ki J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 7.96 pKi 11 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes B 7.96 pKi 10.9 nM Ki J. Med. Chem. (1989) 32: 1873-1879 [PMID:2754711]
ChEMBL Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor B 9.34 pKi 0.46 nM Ki J. Med. Chem. (1990) 33: 3127-3130 [PMID:2258897]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand B 7.02 pKi 95 nM Ki J. Med. Chem. (1992) 35: 3066-3075 [PMID:1501234]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Binding affinity towards human adenosine A3 receptor expressed in HEK293 cells using [125I]AB-MECA at 1 uM B 5.89 pKi 1300 nM Ki J. Med. Chem. (2000) 43: 1158-1164 [PMID:10737748]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]