CPX [Ligand Id: 427] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL157655
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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]
  • Adenosine A2a receptor in Guinea pig [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
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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 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 fat cell membrane B 5.8 pKi 1600 nM Ki J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes B 6.15 pKi 710 nM Ki J. Med. Chem. (1989) 32: 1231-1237 [PMID:2724296]
ChEMBL Binding of 1 nM [3H]CHA to Adenosine A1 receptor of rat cerebral cortical membranes B 6.15 pKi 700 nM Ki J. Med. Chem. (1988) 31: 2034-2039 [PMID:3172141]
ChEMBL Ability to inhibit binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptor in rat cerebral cortical membranes B 6.15 pKi 700 nM Ki J. Med. Chem. (1986) 29: 1305-1308 [PMID:3806581]
ChEMBL Binding affinity to A1 adenosine receptor from rat cortical membrane in presence of [3H]R-(phenylisopropyl)-adenosine B 6.15 pKi 700 nM Ki J. Med. Chem. (1994) 37: 1526-1534 [PMID:8182711]
ChEMBL Antagonism of binding of 1 nM [3H]cyclohexyladenosine to adenosine A1 receptors on rat cortical membranes B 6.15 pKi 700 nM Ki J. Med. Chem. (1985) 28: 487-492 [PMID:2984420]
ChEMBL Binding affinity for adenosine A1 receptor from rat brain membranes using [3H]PIA as radioligand B 6.15 pKi 700 nM Ki J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976]
ChEMBL Binding affinity at Adenosine A1 receptor in rat brain cortical membrane using [3H]N6-R-phenylisopropyladenosine (R-PIA) as radioligand B 6.15 pKi 700 nM Ki J. Med. Chem. (1993) 36: 3341-3349 [PMID:8230124]
ChEMBL Binding affinity against Adenosine A1 receptor in rat brain membrane, using [3H]N6-cyclohexyladenosine as the radioligand B 6.35 pKi 450 nM Ki J. Med. Chem. (1989) 32: 2247-2254 [PMID:2795597]
ChEMBL Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes B 6.35 pKi 450 nM Ki J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes B 6.35 pKi 450 nM Ki J. Med. Chem. (1989) 32: 1873-1879 [PMID:2754711]
ChEMBL Binding affinity against Adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes B 6.35 pKi 450 nM Ki J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL Antagonism of adenosine A1 receptor assessed from the ability to inhibit binding of [3H]cyclohexyladenosine to rat cerebral cortical membranes B 5.82 pIC50 1500 nM IC50 J. Med. Chem. (1984) 27: 1364-1367 [PMID:6090665]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor B 5.85 pKi 1400 nM Ki J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor B 5.92 pKi 1200 nM Ki J. Med. Chem. (1991) 34: 466-469 [PMID:1992150]
ChEMBL Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand. B 5.92 pKi 1200 nM Ki J. Med. Chem. (1992) 35: 2342-2345 [PMID:1613758]
ChEMBL Binding affinity against Adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig membranes B 6 pKi 1000 nM Ki J. Med. Chem. (1992) 35: 924-930 [PMID:1548682]
ChEMBL Binding affinity against adenosine A1 receptor of cerebral cortex using [3H]CPX as a radioligand B 6.68 pKi 210 nM Ki J. Med. Chem. (1993) 36: 1380-1386 [PMID:8496906]
ChEMBL Affinity against adenosine A1 receptor in the brain membranes by the displacement of [3H]CPX. B 6.7 pKi 200 nM Ki J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
GtoPdb - - 6.2 pKi - - - J Biol Chem (1995) 270: 13987-97 [PMID:7775460]
ChEMBL Relaxant activity on the spontaneous tone of isolated guinea pig tracheal ring chains. F 7.3 pEC50 50 nM EC50 J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity for adenosine A2A receptor from rat brain membranes using [3H]CGS-21680 B 5.59 pKi 2600 nM Ki J. Med. Chem. (1993) 36: 2639-2644 [PMID:8410976]
Adenosine A2a receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2605] [UniProtKB: P46616]
ChEMBL Affinity against adenosine A2 receptor in the brain membranes measured by the displacement of [3H]-CPX B 5.52 pKi 3000 nM Ki J. Med. Chem. (1992) 35: 4039-4044 [PMID:1331453]
ChEMBL Compound was evaluated for its ability to antagonise cyclic [3H]AMP accumulation in [3H]adenine-labeled guinea pig cerebral cortical slices. F 5.57 pKi 2700 nM Ki J. Med. Chem. (1986) 29: 1305-1308 [PMID:3806581]
ChEMBL Antagonism of cyclic [3H]AMP accumulation in guinea pig cerebral cortical slices (elicited by 15 uM 2-chloroadenosine at adenosine A2 receptor) F 5.57 pKi 2700 nM Ki J. Med. Chem. (1985) 28: 487-492 [PMID:2984420]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand B 5.95 pKi 1110 nM Ki J. Med. Chem. (2002) 45: 2131-2138 [PMID:12014951]
GtoPdb - - 7.3 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Biochem Pharmacol (2001) 61: 657-63 [PMID:11266650]

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]