[3H]CCPA [Ligand Id: 379] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL284969
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  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • Adenosine A1 receptor in Bovine [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
  • A1 receptor/Adenosine A1 receptor in Mouse [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
  • 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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  • 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]
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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]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11]
ChEMBL Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane B 6.19 pKi 650 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane B 9.52 pKi 0.3 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
GtoPdb - - 9.2 pKd 0.63 nM Kd J. Biol. Chem. (1999) 274: 3617-21 [PMID:9920910];
Naunyn Schmiedebergs Arch. Pharmacol. (1998) 357: 1-9 [PMID:9459566]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 90 mins B 7.82 pKi 15.3 nM Ki J. Med. Chem. (2012) 55: 7719-7735 [PMID:22889387]
ChEMBL Binding affinity to human adenosine A1 receptor expressed in CHO cells B 7.82 pKi 15.1 nM Ki J. Med. Chem. (2008) 51: 5875-5879 [PMID:18729349]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes B 7.83 pKi 14.9 nM Ki J. Med. Chem. (2014) 57: 7673-7686 [PMID:25181013]
ChEMBL In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. B 8.19 pKi 6.4 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A1 receptor in CHO cells B 9.08 pKi 0.83 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells B 9.08 pKi 0.83 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1495-1498 [PMID:15006389]
ChEMBL Radioligand Binding Assay: Membranes for radioligand binding experiments are prepared from fresh or frozen cells as described in Klotz et al., Naunyn-Schmiedeberg's Arch. Pharmacol, 357:1-9 (1998). The cell suspension is then homogenized in ice-cold hypotonic buffer (5 mM Tris/HCl, 2 mM EDTA, pH 7.4) and the homogenate is spun for 10 minutes (4° C.) at 1,000 g. The membranes are then sedimented from the supernatant for 30 minutes at 100,000 g and resuspended in 50 mM Tris/HCl buffer pH 7.4 (for A3 adenosine receptors: 50 mM Tris/HCl, 10 mM MgCl2, 1 mM EDTA, pH 8.25), frozen in liquid nitrogen at a protein concentration of 1-3 mg/mL and stored at −80° C. Dissociation constants of unlabeled compounds (Ki-values) are determined in competition experiments in 96-well microplates using the A1 selective agonist 2-chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA, 1 nM) for the characterization of A1 receptor binding. Nonspecific binding is determined in the presence of 100 μM R-PM and 1 mM theophylline, respectively. B 9.08 pKi 0.83 nM Ki US-8470800-B2. Method of reducing intraocular pressure in humans (2013)
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells B 9.1 pKi 0.8 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Inhibition of cAMP formation in CHO cells expressing adenosine A1 receptor B 8.89 pIC50 1.3 nM IC50 J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis B 9.3 pIC50 0.5 nM IC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay B 6.7 pEC50 199.53 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of isoproterenol-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay F 7.85 pEC50 14 nM EC50 J. Med. Chem. (2012) 55: 6467-6477 [PMID:22738238]
ChEMBL Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay F 8.34 pEC50 4.6 nM EC50 J. Med. Chem. (2012) 55: 6467-6477 [PMID:22738238]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane B 6.14 pKi 730 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 9.46 pKi 0.35 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane B 9.47 pKi 0.34 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612]
ChEMBL Agonist activity at mouse adenosine A1 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA F 7.75 pEC50 17.7 nM EC50 J. Med. Chem. (2013) 56: 5949-5963 [PMID:23789857]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Affinity towards adenosine A1 receptor from rat cortical membranes using [3H]DPCPX B 8.02 pKi 9.47 nM Ki J. Med. Chem. (2001) 44: 2966-2975 [PMID:11520205]
ChEMBL Binding affinity for adenosine A1 receptor was assayed by displacement of [3H]DPCPX from rat cortical membranes. B 8.13 pKi 7.43 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Tested for inhibition of adenosine A1 receptor binding to rat brain B 8.82 pKi 1.5 nM Ki Bioorg. Med. Chem. Lett. (1993) 3: 2661-2666
ChEMBL Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor B 8.88 pKi 1.33 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1994) 37: 1720-1726 [PMID:8201607]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor of rat brain B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. B 8.89 pKi 1.3 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1991) 34: 3388-3390 [PMID:1766003]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 9.22 pKi 0.6 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Functional activity against adenosine A1 receptor from rat atria. F 5.09 pEC50 8200 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Stimulation of [35S]GTP-gamma-S, binding to rat brain membranes by adenosine A1 receptor activation F 7.52 pEC50 30 nM EC50 J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria F 8.09 pEC50 8.2 nM EC50 J. Med. Chem. (1994) 37: 1720-1726 [PMID:8201607]
ChEMBL Activity at Adenosine A1 receptor of rat atria F 8.09 pEC50 8.2 nM EC50 J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Ex vivo inhibition of guinea pig ileum twitch via Adenosine A1 receptor. B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 403-406 [PMID:10714510]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells B 5.64 pKi 2300 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor in stably transfected CHO cells B 5.64 pKi 2270 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1495-1498 [PMID:15006389]
ChEMBL Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer B 5.64 pKi 2270 nM Ki J. Med. Chem. (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A2A receptor in CHO cells B 5.64 pKi 2270 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
ChEMBL Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand B 6.19 pKi 639 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 6.24 pKi 580 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL In vitro inhibition of human neutrophil activation via Adenosine A2A receptor. B 7.77 pKi 17 nM Ki Bioorg. Med. Chem. Lett. (2000) 10: 403-406 [PMID:10714510]
ChEMBL Agonist activity at human Adenosine A2A receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay B 5 pEC50 10000 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 6.02 pKi 950 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. B 6.19 pKi 650 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum B 6.19 pKi 650 nM Ki J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes. B 6.19 pKi 640 nM Ki J. Med. Chem. (2000) 43: 250-260 [PMID:10649980]
ChEMBL Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes B 6.22 pKi 605 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta F 5 pEC50 >10000 nM EC50 J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Functional activity against adenosine A2a receptor from rat aorta. F 8 pEC50 >10 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells B 4.69 pKi 20400 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity F 7.38 pKi 42 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay B 4.14 pEC50 72443.6 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells B 4.73 pKi 18800 nM Ki Bioorg. Med. Chem. (2008) 16: 336-353 [PMID:17933541]
ChEMBL Binding affinity towards Adenosine A3 receptor (H95A mutant receptor) B 6.1 pKi 796 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor B 6.55 pKi 281 nM Ki J. Med. Chem. (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Affinity towards Adenosine A3 receptor expressed in HEK 293 cells using [125I]AB-MECA radioligand B 6.69 pKi 204 nM Ki J. Med. Chem. (2001) 44: 2966-2975 [PMID:11520205]
ChEMBL Binding affinity towards human Adenosine A3 receptor wild type B 6.94 pKi 114 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity towards Adenosine A3 receptor (W243 mutant receptor) B 7 pKi 100 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Displacement of [3H]NECA from human adenosine A3 receptor in stably transfected HEK cells B 7.37 pKi 42.3 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 1495-1498 [PMID:15006389]
ChEMBL Binding affinity to Adenosine receptor A3 (unknown origin) B 7.42 pKi 38 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 7.42 pKi 38 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity to human adenosine A3 receptor in CHO cells B 7.42 pKi 38 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
ChEMBL Bnding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand B 7.42 pKi 38 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor in the presence of GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand B 7.47 pKi 34 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis B 7.95 pIC50 11.22 nM IC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA B 6.63 pKi 237 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Displacement of [125I]- AB-MECA from rat adenosine A3 receptor expressed in HEK cells B 6.63 pKi 237 nM Ki J. Med. Chem. (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Binding affinity to rat adenosine A3 receptor in CHO cells B 6.63 pKi 237 nM Ki J. Med. Chem. (2005) 48: 8103-8107 [PMID:16366590]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 7.52 pKi 30 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]

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, 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]