CCPA [Ligand Id: 374] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL284969
There should be some charts here, you may need to enable JavaScript!
  • 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]
There should be some charts here, you may need to enable JavaScript!
  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Mouse [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
There should be some charts here, you may need to enable JavaScript!
  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
There should be some charts here, you may need to enable JavaScript!
  • A3 receptor/Adenosine A3 receptor in Human [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
  • A3 receptor/Adenosine A3 receptor in Mouse [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
There should be some charts here, you may need to enable JavaScript!
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]
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]
GtoPdb - - 8.1 pKi - - - J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
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]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 8.92 pKi 1.2 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
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]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 9.08 pKi 0.83 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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 F 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 Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 9.68 pKi 0.21 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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]
GtoPdb - - 8.89 pKi 1.3 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
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]
ChEMBL Agonist activity at rat A1A adenosine receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay F 8.78 pEC50 1.65 nM EC50 J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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]
GtoPdb - - 5.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
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]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay B 5.64 pKi 2270 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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 Displacement of [3H]-NECA from human A2A receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 5.69 pKi 2050 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
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 Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from mouse A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay B 6.01 pKi 988 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
GtoPdb - - 6.02 pKi 950 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
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]
GtoPdb - - 4.7 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
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]
GtoPdb - - 7.4 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from human A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 7.42 pKi 38 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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 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 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 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 Displacement of [3H]-HEMADO from human A3 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 7.59 pKi 26 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
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 F 7.95 pIC50 11.22 nM IC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
ChEMBL Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from mouse A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 7.77 pKi 17 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
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]
GtoPdb - - 6.63 pKi 237 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
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 32:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]