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 Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669];
J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631];
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
J Med Chem (2004) 47: 4041-53 [PMID:15267242];
J Biol Chem (1995) 270: 13987-97 [PMID:7775460];
Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286];
Br J Pharmacol (1997) 121: 353-60 [PMID:9179373];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
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 F 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 F 8.67 pEC50 2.12 nM EC50 ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664]
ChEMBL Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay F 8.85 pEC50 1.41 nM EC50 J Med Chem (2021) 64: 3827-3842 [PMID:33764785]
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 F 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 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]