CGS 21680 [Ligand Id: 375] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL331372 (CGS-21680)
  • A1 receptor/Adenosine A1 receptor in Human [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
  • 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]
  • A2B receptor in Rat [GtoPdb: 20] [UniProtKB: P29276]
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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 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method B 5 pKi >10000 nM Ki J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
GtoPdb - - 6.4 pKi - - - Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells B 6.42 pKi 380 nM Ki ACS Med. Chem. Lett. (2014) 5: 1043-1048 [PMID:25221664]
ChEMBL Displacement of [3H]N6-phenylisopropyladenosine from human A1 adenosine receptor expressed in CHO cell membranes after 60 mins B 6.42 pKi 380 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells B 6.52 pKi 302 nM Ki J. Med. Chem. (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Agonist activity at human adenosine receptor A1 B 6.54 pKi 290 nM Ki Eur J Med Chem (2019) 179: 310-324 [PMID:31255928]
ChEMBL Binding affinity to human recombinant adenosine A1 receptor B 6.54 pKi 290 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor B 6.54 pKi 289 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor B 6.54 pKi 289 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity for human adenosine A1 receptor B 6.54 pKi 289 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay B 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Binding against human adenosine A1 receptor B 5.19 pEC50 6437 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 691-694 [PMID:9871584]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay F 6.3 pEC50 501.19 nM EC50 MedChemComm (2014) 5: 192-196
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain B 5 pKi 9900 nM Ki J. Med. Chem. (1999) 42: 3463-3477 [PMID:10479279]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 5.59 pKi 2600 nM Ki J. Med. Chem. (1992) 35: 407-422 [PMID:1738138]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor in rat cortical membrane B 5.59 pKi 2600 nM Ki J. Med. Chem. (2002) 45: 420-429 [PMID:11784146]
ChEMBL Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor B 5.59 pKi 2600 nM Ki J. Med. Chem. (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL Displacement of [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane B 5.59 pKi 2600 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 5.59 pKi 2600 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
GtoPdb - - 5.74 pKi 1800 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis B 5.74 pKi 1800 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity towards adenosine A1 receptor in rat brain cortex B 5.74 pKi 1800 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex B 5.74 pKi 1800 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine B 5.85 pKi 1408 nM Ki J. Med. Chem. (1990) 33: 1919-1924 [PMID:2362269]
ChEMBL Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 5.91 pKi 1232 nM Ki J. Med. Chem. (1992) 35: 241-252 [PMID:1732541]
ChEMBL Inhibition of [3H]CHA binding to adenosine A1 receptor from rat brain membranes B 5.91 pKi 1232 nM Ki J. Med. Chem. (1992) 35: 2253-2260 [PMID:1613750]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. B 5.94 pKi 1138 nM Ki J. Med. Chem. (1992) 35: 2881-2890 [PMID:1495019]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. B 6.24 pKi 569 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor of rat brain B 6.24 pKi 569 nM Ki J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Functional activity against adenosine A1 receptor from rat atria. F 5 pEC50 >10000 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Activity at Adenosine A1 receptor of rat atria F 5 pEC50 >10000 nM EC50 J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL [S]GTP gamma-S binding against adenosine A1 receptor in rat brain B 7 pEC50 >100 nM EC50 Bioorg. Med. Chem. Lett. (1998) 8: 691-694 [PMID:9871584]
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745]
ChEMBL Prolongation of the stimulus-QRS interval by 50% of the maximum response at the Adenosine A1 receptor in langendorff guinea pig heart preparation F 4.61 pEC50 24547.09 nM EC50 J. Med. Chem. (1991) 34: 1334-1339 [PMID:2016707]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Saturation binding of wild type human Adenosine A2A receptor at pH 8.4 B 6.2 pKd 632 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding of human Adenosine A2A receptor H250N at pH 8.4 B 7 pKd 99 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding characteristics of wild type human Adenosine A2A receptor at pH 7.5 B 7.13 pKd 74 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding of wild type human Adenosine A2A receptor at pH 6.8 B 7.44 pKd 36.4 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Kd in saturation experiments using [3H]CGS-21680 at WT receptor in COS-7 cells B 7.44 pKd 36.4 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Kd in saturation experiments using [3H]CGS-21680 at V84L mutant receptor in COS-7 cells B 7.56 pKd 27.3 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding characteristics of wild type human Adenosine A2A receptor at pH 5.5 B 7.66 pKd 22 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding of human Adenosine A2A receptor H250N at pH 7.5 B 7.94 pKd 11.6 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Saturation binding of human Adenosine A2A receptor (H250N) at pH 6.8 B 8.12 pKd 7.6 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Kd in saturation experiments using [3H]CGS-21680 at H250N mutant receptor in COS-7 cells B 8.12 pKd 7.6 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Displacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from wild type human adenosine A2a receptor expressed in HEK293 cells assessed as radioligand Kd compound preincubated for 30 mins B 8.36 pKd 4.36 nM Kd ACS Med. Chem. Lett. (2014) 5: 1043-1048 [PMID:25221664]
ChEMBL Saturation binding of mutant human Adenosine A2A receptor (H250N) at pH 5.5 B 8.37 pKd 4.3 nM Kd J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Displacement of [3H]-ZM24135 from human adenosine A2A receptor expressed in HEK293 cells after 1 hr by scintillation counting B 6.3 pKi 503 nM Ki Eur. J. Med. Chem. (2015) 106: 15-25 [PMID:26513641]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from human adenosine A2a receptor expressed in HEK293 cells B 7.15 pKi 70 nM Ki ACS Med. Chem. Lett. (2014) 5: 1043-1048 [PMID:25221664]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamido-adenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins B 7.15 pKi 70 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Inhibition of [3H]ZM-241385 binding to human adenosine A2A receptor expressed in HeLa cells B 7.3 pKi 50 nM Ki J. Med. Chem. (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells by scintillation counting B 7.34 pKi 46.2 nM Ki Bioorg. Med. Chem. (2009) 17: 4280-4284 [PMID:19481943]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells B 7.34 pKi 46.2 nM Ki Bioorg. Med. Chem. (2008) 16: 3825-3830 [PMID:18262425]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells B 7.34 pKi 46.2 nM Ki Bioorg. Med. Chem. (2007) 15: 3235-3240 [PMID:17350268]
ChEMBL Binding affinity for human adenosine A2A receptor B 7.57 pKi 27.1 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Agonist activity at human adenosine receptor A2A B 7.57 pKi 27 nM Ki Eur J Med Chem (2019) 179: 310-324 [PMID:31255928]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor B 7.57 pKi 27 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells B 7.57 pKi 27 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity to human recombinant adenosine receptor A2a B 7.57 pKi 27 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine 2A receptor after 60 mins by gamma counting analysis B 7.57 pKi 27 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in Sf21 cells co-expressing GalphaS2, beta4, gamma2 B 7.68 pKi 21 nM Ki Bioorg. Med. Chem. Lett. (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method B 7.9 pKi 12.48 nM Ki J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
GtoPdb - - 8.1 pKi 7.94 nM Ki J Med Chem (2004) 47: 4041-53 [PMID:15267242];
Br J Pharmacol (1997) 121: 353-60 [PMID:9179373];
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376];
J Biol Chem (1995) 270: 13987-97 [PMID:7775460];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286];
J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]
ChEMBL Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay F 7.72 pIC50 19 nM IC50 Bioorg. Med. Chem. Lett. (2010) 20: 1219-1224 [PMID:20031406]
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 4.7 pEC50 19952.62 nM EC50 J. Med. Chem. (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method B 7.73 pEC50 18.47 nM EC50 J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay F 7.9 pEC50 12.59 nM EC50 MedChemComm (2014) 5: 192-196
ChEMBL Agonist activity at human adenosine A2a receptor expressed in CHO cells assessed as stimulation of cAMP formation after 24 hrs B 8.67 pEC50 2.12 nM EC50 ACS Med. Chem. Lett. (2014) 5: 1043-1048 [PMID:25221664]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Displacement of [3H]CGS21680 from A2A adenosine receptor expressed in rat striatal membranes after 30 mins by liquid scintillation counting B 7.57 pKi 27 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
GtoPdb - - 7.72 pKi 19 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
ChEMBL Binding affinity towards adenosine A2A receptor in rat brain striatum B 7.72 pKi 19 nM Ki J. Med. Chem. (2001) 44: 531-539 [PMID:11170643]
ChEMBL Binding affinity to rat recombinant adenosine receptor A2a B 7.72 pKi 19 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatum B 7.74 pKi 18 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis B 7.74 pKi 18 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 7.82 pKi 15 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane B 7.82 pKi 15 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [3H]NECA from Adenosine A2A receptor in rat striatal membrane B 7.82 pKi 15 nM Ki J. Med. Chem. (2002) 45: 420-429 [PMID:11784146]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue B 7.96 pKi 11 nM Ki J. Med. Chem. (1999) 42: 3463-3477 [PMID:10479279]
ChEMBL Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum B 7.96 pKi 11 nM Ki J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. B 7.96 pKi 11 nM Ki J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Functional activity against adenosine A2a receptor from rat aorta. F 6.94 pEC50 115 nM EC50 J. Med. Chem. (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta F 6.94 pEC50 115 nM EC50 J. Med. Chem. (1995) 38: 3581-3585 [PMID:7658444]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 5 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Mol Pharmacol (2000) 58: 1349-56 [PMID:11093773];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells B 5 pKi >10000 nM Ki J. Med. Chem. (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay B 5 pKi >10000 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay F 5 pEC50 >10000 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method B 5 pEC50 >10000 nM EC50 J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay F 7.4 pEC50 39.81 nM EC50 MedChemComm (2014) 5: 192-196
A2B receptor in Rat [GtoPdb: 20] [UniProtKB: P29276]
GtoPdb - - 5 pKi >10000 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
ChEMBL Displacement of [125I]APNEA from human Adenosine A3 receptor expressed in HEK 293 cells B 6.23 pKi 584 nM Ki J. Med. Chem. (2002) 45: 420-429 [PMID:11784146]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells B 6.24 pKi 570 nM Ki ACS Med. Chem. Lett. (2014) 5: 1043-1048 [PMID:25221664]
ChEMBL Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins B 6.24 pKi 570 nM Ki J. Med. Chem. (2012) 55: 538-552 [PMID:22104008]
ChEMBL Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method B 6.42 pKi 384 nM Ki J. Med. Chem. (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis B 6.94 pKi 114 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
ChEMBL Displacement of [125I]-AB-MECA from human recombinant adenosine A3 receptor B 6.94 pKi 114 nM Ki ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
ChEMBL Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells B 7.17 pKi 68 nM Ki J. Med. Chem. (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [125I]AB-MECA from membranes of HEK 293 cells expressing human Adenosine A3 receptor B 7.17 pKi 67.1 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Binding affinity to human recombinant adenosine A3 receptor B 7.17 pKi 67 nM Ki J. Med. Chem. (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [125I]I-AB-MECA from recombinant human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis B 7.17 pKi 67 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
GtoPdb - - 7.2 pKi - - - Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Mol Pharmacol (2000) 57: 968-75 [PMID:10779381];
J Med Chem (2004) 47: 4041-53 [PMID:15267242];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay B 6.21 pEC50 613 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay F 8 pEC50 10 nM EC50 MedChemComm (2014) 5: 192-196
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
GtoPdb - - 6.23 pKi 584 nM Ki . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010)
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 6.23 pKi 584 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity for rat adenosine A3 receptor B 6.23 pKi 584 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]

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]