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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]