[3H]NECA [Ligand Id: 425] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL464859 (5'-N-Ethylcarboxamidoadenosine, NECA)
  • Adenosine A1 receptor in Chicken [ChEMBL: CHEMBL2114] [UniProtKB: P49892]
  • 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]
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [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 Mouse [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
  • A3 receptor/Adenosine A3 receptor in Rat [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
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  • oxoglutarate receptor/G protein-coupled receptor 80 in Rat [ChEMBL: CHEMBL2325] [GtoPdb: 162] [UniProtKB: Q6Y1R5]
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  • heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • Transmembrane domain-containing protein TMIGD3 in Human [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Adenosine A1 receptor in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2114] [UniProtKB: P49892]
ChEMBL Displacement of [125I]ABA from adenosine A1 receptor of chick cerebellar membrane B 7.77 pIC50 17 nM IC50 J Med Chem (1987) 30: 954-956 [PMID:3572985]
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Binding affinity to A1R E172 5.30A mutant (unknown origin) by saturation NanoBRET binding assay B 5.38 pKd 4168.69 nM Kd J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor in CHO cells B 6.24 pKd 575.44 nM Kd J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL Binding affinity to A1R S267 7.32A mutant (unknown origin) in by saturation NanoBRET binding assay B 6.31 pKd 489.78 nM Kd J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay B 6.63 pKd 234.42 nM Kd J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Binding affinity to wild type A1R (unknown origin) by saturation NanoBRET binding assay B 6.67 pKd 213.8 nM Kd J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Binding affinity to A1R H251 6.52A mutant (unknown origin) by saturation NanoBRET binding assay B 8.04 pKd 9.12 nM Kd J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Dissociation constant against Adenosine A1 receptor B 8.07 pKd 8.6 nM Kd J Med Chem (2005) 48: 2026-2035 [PMID:15771445]
ChEMBL Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay B 5.3 pKi 5011.87 nM Ki J Med Chem (2021) 64: 6670-6695 [PMID:33724031]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control B 5.95 pKi 1122.02 nM Ki Medchemcomm (2012) 3: 333-338
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused human adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay B 6.61 pKi 245.47 nM Ki J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Displacement of CA200645 from NLuc human A1 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay B 6.69 pKi 204.17 nM Ki ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
ChEMBL Affinity for Adenosine A1 receptor by displacement of [3H]DPCPX from human cerebral cortex B 6.7 pKi >200 nM Ki Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602]
ChEMBL Binding affinity to wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay B 7.08 pKi 83.18 nM Ki J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells B 7.74 pKi 18.3 nM Ki J Med Chem (2007) 50: 374-380 [PMID:17228880]
ChEMBL Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells B 7.74 pKi 18.2 nM Ki J Med Chem (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells B 7.74 pKi 18.2 nM Ki Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548]
ChEMBL Displacement of [3H]-CCPA from CHO cells expressing human recombinant Adenosine A1 receptor B 7.85 pKi 14 nM Ki Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 7.85 pKi 14 nM Ki J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 7.85 pKi 14 nM Ki J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells B 7.85 pKi 14 nM Ki J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 7.85 pKi 14 nM Ki J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane B 7.85 pKi 14 nM Ki J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins B 7.85 pKi 14 nM Ki Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL Binding affinity to human recombinant adenosine A1 receptor B 7.85 pKi 14 nM Ki J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membrane assessed as inhibition constant incubated for 60 mins by competitive binding assay B 7.85 pKi 14 nM Ki J Med Chem (2023) 66: 890-912 [PMID:36517209]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor B 7.87 pKi 13.6 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity for human adenosine A1 receptor B 7.87 pKi 13.6 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [3H]CCPA from human recombinant adenosine A1 receptor B 7.87 pKi 13.6 nM Ki Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX; Range = 9.6-15 nM B 7.92 pKi 12 nM Ki J Med Chem (2004) 47: 3707-3709 [PMID:15239649]
ChEMBL In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. B 7.92 pKi 12 nM Ki J Med Chem (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method B 8.06 pKi 8.62 nM Ki J Med Chem (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane B 8.11 pKi 7.8 nM Ki J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Binding affinity to human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 8.17 pKi 6.8 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method B 8.17 pKi 6.8 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer B 8.17 pKi 6.8 nM Ki J Med Chem (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells B 8.17 pKi 6.8 nM Ki J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells B 8.3 pKi 5 nM Ki J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method B 8.34 pKi 4.6 nM Ki J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL Displacement of [3H]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 8.34 pKi 4.6 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
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 8.52 pKi 3 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of 3[H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 mins by Liquid scintillation analysis B 8.52 pKi 3 nM Ki J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells B 8.98 pKi 1.04 nM Ki Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Antagonist activity at wild type A1R (unknown origin) expressed in CHO-K1 cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins F 8.95 pIC50 1.12 nM IC50 J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry F 9.1 pIC50 0.79 nM IC50 Medchemcomm (2012) 3: 333-338
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 9.68 pIC50 0.21 nM IC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gs-mediated activation of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry F 5.83 pEC50 1479.11 nM EC50 Medchemcomm (2012) 3: 333-338
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 pEC50 1000 nM EC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL Binding against human adenosine A1 receptor B 7.23 pEC50 59 nM EC50 Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells B 7.5 pEC50 31.62 nM EC50 Med Chem Res (2004) 13: 88-98
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay B 7.52 pEC50 30 nM EC50 Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay F 7.99 pEC50 10.2 nM EC50 ACS Med Chem Lett (2011) 2: 626-631 [PMID:21858244]
ChEMBL Agonist activity at human A1A adenosine receptor expressed in CHOKI cells assessed as induction of beta-arrestin2 recruitment after 60 mins B 8.3 pEC50 5.03 nM EC50 J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of calcium mobilization by calcium mobilization assay F 8.31 pEC50 4.9 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay F 8.74 pEC50 1.82 nM EC50 ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
ChEMBL Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay F 8.79 pEC50 1.62 nM EC50 J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL Agonist activity at human A1 receptor expressed in Flp-In-CHO cells assessed as inhibition of forskolin stimulated cAMP accumulation incubated for 30 mins by LANCE cAMP assay F 8.86 pEC50 1.38 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
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 8.9 pEC50 1.26 nM EC50 Medchemcomm (2014) 5: 192-196
ChEMBL Agonist activity at human adenosine A1 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 8.96 pEC50 1.1 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay F 9.12 pEC50 0.76 nM EC50 J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
ChEMBL Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of ERK1/2 phosphorylation incubated for 5 mins B 9.3 pEC50 0.5 nM EC50 J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL Activity at human adenosine A1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells F 9.44 pEC50 0.36 nM EC50 J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL Agonist activity at adenosine A1 receptor assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation in CHO cells F 9.44 pEC50 0.36 nM EC50 J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL Agonist activity at human A1A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay F 9.92 pEC50 0.12 nM EC50 J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. B 7.85 pKi 14 nM Ki J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes B 7.85 pKi 14 nM Ki J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes B 7.85 pKi 14 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes B 7.85 pKi 14 nM Ki J Med Chem (2005) 48: 1550-1562 [PMID:15743197]
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 9.35 pKi 0.45 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells assessed as kinetic dissociation constant by NanoBRET competition binding assay B 6.53 pKd 295.12 nM Kd J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
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 5.9 pKi 1257 nM Ki J Med Chem (1990) 33: 1919-1924 [PMID:2362269]
ChEMBL Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX B 6.19 pKi 650 nM Ki J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the presence of 1 mM of GTP B 6.28 pKi 530 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Inhibition of CA200645 binding to NanoLuc-fused rat adenosine A1 receptor expressed in HEK293 cells measured for 10 mins by NanoBRET competition binding assay B 6.38 pKi 416.87 nM Ki J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. B 7.2 pKi 63 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the absence of GTP B 7.2 pKi 63 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [3H]N6-R-phenylisopropyladenosine from rat A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 7.2 pKi 63 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of 3[H]R-PIA from rat A1 adenosine receptor expressed in CHO cells after 60 min by Liquid scintillation analysis B 7.2 pKi 63 nM Ki J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL Ability to displace [3H]DPCPX from Adenosine A1 receptor in rat cortical membrane B 7.2 pKi 63 nM Ki J Med Chem (2002) 45: 420-429 [PMID:11784146]
ChEMBL Binding affinity towards adenosine A1 receptor in rat brain cortex B 7.88 pKi 13.3 nM Ki J Med Chem (2001) 44: 531-539 [PMID:11170643]
ChEMBL Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand B 7.88 pKi 13.3 nM Ki J Med Chem (1992) 35: 241-252 [PMID:1732541]
ChEMBL Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX B 7.96 pKi 11 nM Ki J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor of rat brain B 7.98 pKi 10.4 nM Ki J Med Chem (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor of rat brain B 7.98 pKi 10.4 nM Ki J Med Chem (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. B 7.98 pKi 10.4 nM Ki J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand B 7.98 pKi 10.4 nM Ki J Med Chem (1994) 37: 1720-1726 [PMID:8201607]
ChEMBL Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor B 7.99 pKi 10.3 nM Ki J Med Chem (1992) 35: 4143-4149 [PMID:1433217]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. B 8.08 pKi 8.3 nM Ki J Med Chem (1992) 35: 2881-2890 [PMID:1495019]
ChEMBL Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes B 8.09 pKi 8.2 nM Ki J Med Chem (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA B 8.09 pKi 8.2 nM Ki J Med Chem (1992) 35: 2363-2368 [PMID:1619615]
ChEMBL Binding activity against Adenosine A1 receptor from rat brain membranes using [3H]8-cyclopentyl-1,3-dipropylxanthine (DPCPX) B 8.11 pKi 7.7 nM Ki J Med Chem (2001) 44: 208-214 [PMID:11170630]
ChEMBL Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. B 8.2 pKi 6.3 nM Ki J Med Chem (1988) 31: 1282-1285 [PMID:3385722]
ChEMBL Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand B 8.2 pKi 6.3 nM Ki J Med Chem (1992) 35: 407-422 [PMID:1738138]
ChEMBL Inhibition of [3H]- DPCPX binding to Adenosine A1 receptor ofrat brain membranes B 8.2 pKi 6.3 nM Ki J Med Chem (1998) 41: 2676-2678 [PMID:9667957]
ChEMBL Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA. B 8.2 pKi 6.3 nM Ki J Med Chem (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine B 8.2 pKi 6.3 nM Ki J Med Chem (1988) 31: 271-273 [PMID:3336027]
ChEMBL Binding affinity for A1-adenosine receptor by the displacement of specific [3H]-PIA binding in rat brain was determined B 8.2 pKi 6.3 nM Ki J Med Chem (1994) 37: 636-646 [PMID:8126704]
ChEMBL Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain B 8.2 pKi 6.24 nM Ki J Med Chem (1985) 28: 1383-1384 [PMID:2995663]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis B 8.29 pKi 5.1 nM Ki Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex B 8.29 pKi 5.1 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor B 4.05 pIC50 90000 nM IC50 J Med Chem (1988) 31: 752-756 [PMID:3351851]
ChEMBL Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor B 4.28 pIC50 52000 nM IC50 J Med Chem (1988) 31: 752-756 [PMID:3351851]
ChEMBL Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding B 5.61 pIC50 2460 nM IC50 J Med Chem (1988) 31: 745-751 [PMID:3351850]
ChEMBL Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor B 6.7 pIC50 200 nM IC50 J Med Chem (1988) 31: 1179-1183 [PMID:3373486]
ChEMBL Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor B 7.8 pIC50 16 nM IC50 J Med Chem (1991) 34: 2570-2579 [PMID:1875349]
ChEMBL Potency against rat brain adenosine A1 receptor B 7.99 pIC50 10.2 nM IC50 J Med Chem (1986) 29: 1683-1689 [PMID:3018244]
ChEMBL Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. B 8 pIC50 10 nM IC50 J Med Chem (1990) 33: 2240-2254 [PMID:2374150]
ChEMBL Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding B 8.62 pIC50 2.4 nM IC50 J Med Chem (1988) 31: 745-751 [PMID:3351850]
ChEMBL Functional activity against adenosine A1 receptor from rat atria. F 4.26 pEC50 54800 nM EC50 J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL [S]GTP gamma-S binding against adenosine A1 receptor in rat brain B 7.06 pEC50 87.2 nM EC50 Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584]
ChEMBL Activity at Adenosine A1 receptor of rat atria F 7.26 pEC50 55 nM EC50 J Med Chem (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria F 7.26 pEC50 54.8 nM EC50 J Med Chem (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria F 7.26 pEC50 54.8 nM EC50 J Med Chem (1994) 37: 1720-1726 [PMID:8201607]
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]
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 7.2 pEC50 63.1 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]
GtoPdb - - 7.7 pKd - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]
ChEMBL Inhibitory constant against human adenosine A2a receptor B 6.17 pKi 680 nM Ki J Med Chem (2007) 50: 65-73 [PMID:17201410]
ChEMBL Displacement of MRS5346 from C-terminal 10xHis and 1D4-tagged C-terminal-truncated human A2A adenosine receptor (1 to 316 residues) expressed in Pichia pastoris expression system after 1 hr by fluorescence polarization assay B 6.32 pKi 481 nM Ki ACS Med Chem Lett (2017) 8: 660-665 [PMID:28626529]
ChEMBL Inhibition of [3H]ZM-241385 binding to human adenosine A2A receptor expressed in HeLa cells B 6.89 pKi 130 nM Ki J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [125I]ZM241385 from human adenosine A2A receptor in HEK cells B 6.91 pKi 124 nM Ki Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane B 6.96 pKi 110 nM Ki Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536]
ChEMBL Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand B 7.22 pKi 60 nM Ki J Med Chem (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Binding affinity against human adenosine A2A receptor expressed in HEK293 cells using [3H]ZM-241385 B 7.22 pKi 60 nM Ki J Med Chem (2004) 47: 3707-3709 [PMID:15239649]
ChEMBL Displacement of radiolabeled NECA from human adenosine A2A receptor B 7.28 pKi 52 nM Ki J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
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 7.46 pKi 35 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of 3[H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cells after 60 mins by Liquid scintillation analysis B 7.46 pKi 35 nM Ki J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL Binding affinity against S277E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 7.53 pKi 29.2 nM Ki J Med Chem (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in Sf21 cells co-expressing GalphaS2, beta4, gamma2 B 7.6 pKi 25 nM Ki Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Binding affinity against H278E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 7.61 pKi 24.6 nM Ki J Med Chem (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Binding affinity for HA-tagged wild type human Adenosine A2A receptor (WT) using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 7.67 pKi 21.6 nM Ki J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells B 7.67 pKi 21.5 nM Ki J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Binding affinity against WT human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 7.67 pKi 21.4 nM Ki J Med Chem (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346 B 7.67 pKi 21.2 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL [3H]NECA saturation binding in CHO cells expressing human recombinant A2A adenosine receptor B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells B 7.7 pKi 20 nM Ki Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 7.7 pKi 20 nM Ki J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL Binding affinity to human recombinant adenosine receptor A2a B 7.7 pKi 20 nM Ki J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis B 7.7 pKi 20 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Agonist activity at human adenosine receptor A2A B 7.7 pKi 20 nM Ki Eur J Med Chem (2019) 179: 310-324 [PMID:31255928]
ChEMBL Displacement of [3H]DPCPX from human A2AAR expressed in human HeLa cell membrane assessed as inhibition constant incubated for 30 mins by competitive binding assay B 7.7 pKi 20 nM Ki J Med Chem (2023) 66: 890-912 [PMID:36517209]
ChEMBL Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer B 7.7 pKi 20 nM Ki J Med Chem (2012) 55: 8075-8090 [PMID:22921089]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor B 7.7 pKi 20 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity against H278D human adenosine A2A receptor stably transfected in CHO cells using [3H]- ZM-241385 as radioligand. B 7.72 pKi 19.1 nM Ki J Med Chem (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL Displacement of [3H]NECA from human adenosine receptor A2A expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method B 7.8 pKi 16 nM Ki J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 7.8 pKi 16 nM Ki J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane B 7.8 pKi 16 nM Ki J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes B 7.8 pKi 16 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
ChEMBL Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 1550-1562 [PMID:15743197]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 7.8 pKi 16 nM Ki J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 7.8 pKi 16 nM Ki J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 7.8 pKi 16 nM Ki J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane B 7.8 pKi 16 nM Ki J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins B 7.8 pKi 16 nM Ki Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [3H]-NECA from human A2A receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 7.8 pKi 16 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
ChEMBL Affinity for A2a receptor by displacement of [3H]-CGS- 21680 from human striatum B 7.82 pKi 15.1 nM Ki Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells B 7.9 pKi 12.5 nM Ki J Med Chem (2007) 50: 374-380 [PMID:17228880]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells B 7.91 pKi 12.4 nM Ki Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548]
ChEMBL Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells B 7.91 pKi 12.2 nM Ki J Med Chem (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Binding affinity to human adenosine A2A receptor by radioligand displacement assay B 7.92 pKi 12 nM Ki Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method B 8.08 pKi 8.41 nM Ki J Med Chem (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Binding affinity for HA-tagged mutant human Adenosine A2A receptor (H250N) using [3H]-CGS-21,680 as radioligand expressed in COS-7 cells B 8.28 pKi 5.24 nM Ki J Med Chem (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells B 8.66 pKi 2.2 nM Ki J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Binding affinity to human A2A adenosine receptor expressed in HEK293 cell membranes B 8.66 pKi 2.2 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Binding affinity to A2A adenosine receptor B 8.66 pKi 2.2 nM Ki J Med Chem (2012) 55: 538-552 [PMID:22104008]
ChEMBL Binding affinity against Q89D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 B 8.82 pKi 1.5 nM Ki J Med Chem (2003) 46: 4847-4859 [PMID:14584936]
ChEMBL In vitro inhibition of human neutrophil activation via Adenosine A2A receptor. B 9 pKi 1 nM Ki Bioorg Med Chem Lett (2000) 10: 403-406 [PMID:10714510]
ChEMBL Inhibition of human adenosine A2A receptor B 7.17 pIC50 67 nM IC50 Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743]
ChEMBL Displacement of radiolabeled NECA from human adenosine A2A receptor B 7.19 pIC50 64 nM IC50 J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Displacement of [3H]CGS 21680 from human recombinant adenosine receptor A2A expressed in HEK293 cells measured after 120 mins by scintillation counting method B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [3H]CGS 21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells B 7.43 pIC50 37 nM IC50 Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Inhibition of human adenosine A2A receptor B 7.64 pIC50 23 nM IC50 J Med Chem (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay F 7.8 pIC50 16 nM IC50 Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Binding affinity to human adenosine A2A receptor by radioligand displacement assay B 7.82 pIC50 15 nM IC50 Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL Binding affinity to human adenosine A2A receptor by radioligand displacement assay B 8 pIC50 10 nM IC50 Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
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 6.47 pEC50 338.84 nM EC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells F 6.6 pEC50 251.19 nM EC50 Med Chem Res (2004) 13: 88-98
ChEMBL Potency against cAMP formation in CHO cells expressing recombinant human A2A receptor F 7.3 pEC50 50 nM EC50 J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay F 7.35 pEC50 45 nM EC50 Medchemcomm (2015) 6: 1178-1185
ChEMBL G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay F 7.4 pEC50 40 nM EC50 J Med Chem (2002) 45: 420-429 [PMID:11784146]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production F 7.66 pEC50 21.9 nM EC50 J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting F 7.74 pEC50 18 nM EC50 Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay F 7.75 pEC50 17.6 nM EC50 ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells F 7.76 pEC50 17.38 nM EC50 J Med Chem (2007) 50: 782-793 [PMID:17249651]
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 [3H]cAMP levels by scintillation counting method F 7.9 pEC50 12.58 nM EC50 J Med Chem (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.95 pEC50 11.22 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Agonist activity at human A2A receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay F 8.32 pEC50 4.79 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL Agonist activity at human A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay F 8.48 pEC50 3.31 nM EC50 J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
ChEMBL Irreversible agonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay F 8.6 pEC50 2.51 nM EC50 J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity at Adenosine A2A receptor in rat striatal membrane by [3H]ZM-241385 displacement. B 7.8 pKi 16 nM Ki J Med Chem (2002) 45: 420-429 [PMID:11784146]
ChEMBL Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane B 7.8 pKi 16 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis B 7.82 pKi 15 nM Ki Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803]
ChEMBL Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatum B 7.82 pKi 15 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity towards adenosine A2A receptor in rat brain striatum B 7.91 pKi 12.4 nM Ki J Med Chem (2001) 44: 531-539 [PMID:11170643]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from rat A2A adenosine receptor expressed in HEK293 cell membranes at 10 uM after 60 mins by scintillation proximity assay relative to adenosine 5-N-ethyluronamide B 7.92 pKi 12 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Displacement of 3[H]CGS21680 from rat A2A adenosine receptor expressed in HEK293 cells after 60 min by Liquid scintillation analysis B 7.92 pKi 12 nM Ki J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand B 7.99 pKi 10.3 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from rat adenosine receptor A2A after 60 mins by liquid scintillation counting method B 7.99 pKi 10.3 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680. B 7.99 pKi 10.3 nM Ki J Med Chem (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Inhibition of [3H]- CGS 21680 binding to Adenosine A2A receptor of rat brain membranes B 8 pKi 10 nM Ki J Med Chem (1998) 41: 2676-2678 [PMID:9667957]
ChEMBL Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. B 8.11 pKi 7.8 nM Ki J Med Chem (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum B 8.11 pKi 7.8 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 8.11 pKi 7.8 nM Ki J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Binding affinity for Adenosine A2A receptor in rat brain membranes using [3H]CGS-21680 B 8.38 pKi 4.13 nM Ki J Med Chem (2001) 44: 208-214 [PMID:11170630]
ChEMBL Displacement of [3H]MSX-2 from rat adenosine A2A receptor in presence of 100 mM NaCl B 6.44 pIC50 366 nM IC50 Eur J Med Chem (2011) 46: 3590-3607 [PMID:21664729]
ChEMBL Displacement of [3H]MSX-2 from rat adenosine A2A receptor B 8.15 pIC50 7.05 nM IC50 Eur J Med Chem (2011) 46: 3590-3607 [PMID:21664729]
ChEMBL Vasorelaxation as Adenosine A2A receptor activity in rat aorta F 6.4 pEC50 394 nM EC50 J Med Chem (1996) 39: 4211-4217 [PMID:8863798]
ChEMBL Functional activity against adenosine A2a receptor from rat aorta. F 6.4 pEC50 394 nM EC50 J Med Chem (1995) 38: 1462-1472 [PMID:7739005]
ChEMBL Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta F 6.4 pEC50 394 nM EC50 J Med Chem (1995) 38: 3581-3585 [PMID:7658444]
ChEMBL Efficacy against phenylephrine precontracted tissue relaxation in rat aorta F 7.47 pEC50 34 nM EC50 J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
ChEMBL Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane assessed as inhibition constant incubated for 30 mins by competitive binding assay B 5.62 pKi 2400 nM Ki J Med Chem (2023) 66: 890-912 [PMID:36517209]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay B 5.72 pKi 1890 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells B 5.72 pKi 1890 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method B 5.72 pKi 1890 nM Ki J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane B 5.9 pKi 1270 nM Ki J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells B 6.05 pKi 884 nM Ki Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells B 6.12 pKi 760 nM Ki J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 6.24 pKi 570 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells B 6.58 pKi 262 nM Ki J Med Chem (2009) 52: 3994-4006 [PMID:19569717]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase F 2.15 pEC50 -2.15 - logEC50 J Med Chem (2008) 51: 2088-2099 [PMID:18321038]
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 4.83 pEC50 14791.08 nM EC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
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 Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells F 5.44 pEC50 3630.78 nM EC50 J Med Chem (2007) 50: 782-793 [PMID:17249651]
ChEMBL Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA F 5.51 pEC50 3100 nM EC50 J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor F 5.62 pEC50 2400 nM EC50 Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663]
ChEMBL Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method F 5.82 pEC50 1510 nM EC50 J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL Potency against cAMP formation in CHO cells expressing recombinant human A2B receptor F 6.36 pEC50 440 nM EC50 J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins in presence of PSB603 by LANCE cAMP assay F 6.48 pEC50 331.13 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL Agonist activity at human recombinant adenosine receptor A2b by cAMP assay F 6.48 pEC50 330 nM EC50 J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells B 6.5 pEC50 316.23 nM EC50 Med Chem Res (2004) 13: 88-98
ChEMBL Agonist activity at human A2BAR expressed in HEK293T cells assessed as increase in cAMP accumulation incubated for 30 mins by TR-FRET assay F 6.59 pEC50 257 nM EC50 J Med Chem (2023) 66: 890-912 [PMID:36517209]
ChEMBL Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta F 6.6 pEC50 250 nM EC50 J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels F 6.8 pEC50 160 nM EC50 J Med Chem (2007) 50: 374-380 [PMID:17228880]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production F 6.81 pEC50 155 nM EC50 Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production F 6.85 pEC50 140 nM EC50 J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Agonist activity at human A2B adenosine receptor by cell based assay B 6.85 pEC50 140 nM EC50 J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production F 6.96 pEC50 110 nM EC50 J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Agonistic activity against human adenosine A2B receptor expressed in CHO cells F 6.98 pEC50 104 nM EC50 J Med Chem (2004) 47: 3707-3709 [PMID:15239649]
ChEMBL Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay F 7.02 pEC50 94.8 nM EC50 ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.2 pEC50 63.1 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay F 7.37 pEC50 42.66 nM EC50 J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay F 7.42 pEC50 38 nM EC50 Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay F 7.8 pEC50 15.85 nM EC50 J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
ChEMBL Agonist activity at A2BR in human NHVCF cells assessed as cAMP accumulation incubated for 30 mins by LANCE cAMP assay F 7.91 pEC50 12.3 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL Agonist activity at human A2B receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 10 mins in presence of forskolin by LANCE cAMP assay F 8.32 pEC50 4.79 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
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 8.5 pEC50 3.16 nM EC50 Medchemcomm (2014) 5: 192-196
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
ChEMBL Activity against Adenosine A2B receptor as cAMP production in VA-13 cells F 5.59 pKi 2600 nM Ki J Med Chem (1998) 41: 2676-2678 [PMID:9667957]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
GtoPdb - - 8.2 pKd - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Biochem Pharmacol (2001) 62: 1163-73 [PMID:11705449]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells B 4.75 pKi 17700 nM Ki Bioorg Med Chem (2008) 16: 3825-3830 [PMID:18262425]
ChEMBL Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells B 5.49 pKi 3200 nM Ki J Med Chem (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity to wild type A3R (unknown origin) expressed in CHO-K1 cells assessed as equilibrium binding affinity constant by nanoBRET assay B 6.72 pKi 190.55 nM Ki J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells B 6.77 pKi 169 nM Ki J Med Chem (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Competitive binding affinity to human adenosine A3 receptor expressed in CHO cells after 90 mins by flow cytometric analysis in presence of MRS5449 B 6.83 pKi 149 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of CA200645 from NLuc human A3 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay B 7.05 pKi 89.13 nM Ki ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
ChEMBL Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins B 7.12 pKi 75.5 nM Ki Medchemcomm (2018) 9: 81-86 [PMID:30108902]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 7.14 pKi 73 nM Ki J Med Chem (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX B 7.14 pKi 73 nM Ki J Med Chem (2001) 44: 316-327 [PMID:11462973]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins B 7.14 pKi 73 nM Ki Eur J Med Chem (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane B 7.14 pKi 73 nM Ki J Med Chem (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes B 7.14 pKi 73 nM Ki J Med Chem (2005) 48: 1550-1562 [PMID:15743197]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 7.14 pKi 73 nM Ki J Med Chem (2005) 48: 8253-8260 [PMID:16366607]
ChEMBL Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 7.14 pKi 73 nM Ki J Med Chem (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay B 7.36 pKi 44.1 nM Ki ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351]
ChEMBL Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells B 7.45 pKi 35.7 nM Ki Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548]
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 7.46 pKi 35 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 7.46 pKi 35 nM Ki J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells B 7.46 pKi 34.8 nM Ki J Med Chem (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 7.46 pKi 34.6 nM Ki J Med Chem (2007) 50: 374-380 [PMID:17228880]
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 7.52 pKi 30 nM Ki J Med Chem (2015) 58: 3253-3267 [PMID:25780876]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 7.6 pKi 25 nM Ki Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells by scintillation counting B 7.7 pKi 20 nM Ki Bioorg Med Chem (2009) 17: 4280-4284 [PMID:19481943]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells B 7.7 pKi 20 nM Ki Bioorg Med Chem (2007) 15: 3235-3240 [PMID:17350268]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay B 7.71 pKi 19.6 nM Ki ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells B 7.8 pKi 16 nM Ki J Med Chem (2007) 50: 1810-1827 [PMID:17378544]
ChEMBL Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 mins gamma counter B 7.8 pKi 16 nM Ki J Med Chem (2012) 55: 4297-4308 [PMID:22486652]
ChEMBL Displacement of [3H]HEMADO from human adenosine receptor A3 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method B 7.89 pKi 12.8 nM Ki J Med Chem (2017) 60: 5772-5790 [PMID:28590753]
ChEMBL Displacement of [3H]-HEMADO from human A3 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay B 7.89 pKi 12.8 nM Ki Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606]
ChEMBL Binding affinity against human adenosine A3 receptor expressed on HEK293 cells using [125I]I-AB-MECA B 7.96 pKi 11 nM Ki J Med Chem (2004) 47: 3707-3709 [PMID:15239649]
ChEMBL Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor B 7.96 pKi 11 nM Ki J Med Chem (2003) 46: 1492-1503 [PMID:12672250]
ChEMBL Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cell membrane B 7.96 pKi 11 nM Ki J Med Chem (2008) 51: 4449-4455 [PMID:18637670]
ChEMBL Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]-AB MECA displacement. B 7.96 pKi 11 nM Ki J Med Chem (2002) 45: 420-429 [PMID:11784146]
ChEMBL Ability to displace radioligand [125I]AB-MECA from membrane of HEK 293 cells stably transfected with human adenosine A3 receptor cDNA B 7.97 pKi 10.6 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells B 7.99 pKi 10.2 nM Ki Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in CHO cells B 8.09 pKi 8.22 nM Ki Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602]
ChEMBL Displacement of [3H]NECA from human A3AR expressed in human HeLa cell membrane assessed as inhibition constant incubated for 180 mins by competitive binding assay B 8.21 pKi 6.2 nM Ki J Med Chem (2023) 66: 890-912 [PMID:36517209]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.21 pKi 6.2 nM Ki J Med Chem (2010) 53: 3954-3963 [PMID:20408530]
ChEMBL Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells B 8.21 pKi 6.2 nM Ki ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277]
ChEMBL Binding affinity to human recombinant adenosine A3 receptor B 8.21 pKi 6.2 nM Ki J Med Chem (2014) 57: 3623-3650 [PMID:24164628]
ChEMBL [3H]NECA saturation binding in CHO cells expressing human Adenosine A3 receptor B 8.22 pKi 6 nM Ki Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663]
ChEMBL Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells B 8.4 pKi 4 nM Ki J Med Chem (2004) 47: 4041-4053 [PMID:15267242]
ChEMBL Binding affinity towards Adenosine A3 receptor (W243 A mutant receptor) B 9.05 pKi 0.9 nM Ki J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity towards human Adenosine A3 receptor wild type B 9.1 pKi 0.8 nM Ki J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor F 4.18 pIC50 65600 nM IC50 J Med Chem (2004) 47: 2243-2255 [PMID:15084123]
ChEMBL Agonist activity at wild type human A3 receptor M177'5.38A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 6.96 pIC50 109.65 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor L90'3.32A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 7.81 pIC50 15.49 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor M174'5.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 8.42 pIC50 3.8 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 8.92 pIC50 1.2 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 8.94 pIC50 1.15 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Antagonist activity at wild type A3R (unknown origin) expressed in Flp-In-CHO cells assessed as inhibition of NECA reduced forskolin stimulated cAMP accumulation incubated for 30 mins F 9.03 pIC50 0.93 nM IC50 J Med Chem (2022) 65: 13305-13327 [PMID:36173355]
ChEMBL Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.11 pIC50 0.78 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.21 pIC50 0.62 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.23 pIC50 0.59 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.31 pIC50 0.49 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
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 9.31 pIC50 0.49 nM IC50 J Med Chem (2016) 59: 947-964 [PMID:26756468]
ChEMBL Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.53 pIC50 0.3 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.59 pIC50 0.26 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay F 9.68 pIC50 0.21 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay F 4.98 pEC50 10400 nM EC50 J Med Chem (2006) 49: 2689-2702 [PMID:16640329]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay F 6.46 pEC50 346.74 nM EC50 Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as beta arrestin 2 recruitment potency by luciferase based NanoBiT assay F 6.75 pEC50 177 nM EC50 Eur J Med Chem (2022) 228: 113983-113983 [PMID:34844790]
ChEMBL Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor F 6.81 pEC50 155 nM EC50 J Med Chem (2000) 43: 2196-2203 [PMID:10841798]
ChEMBL Agonist activity at human adenosine A3A receptor stably expressed in HEK293 cells assessed as mini G-alpha recruitment potency by luciferase based NanoBiT assay F 6.81 pEC50 154 nM EC50 Eur J Med Chem (2022) 228: 113983-113983 [PMID:34844790]
ChEMBL Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor F 7.05 pEC50 89 nM EC50 J Med Chem (1999) 42: 1393-1400 [PMID:10212125]
ChEMBL Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells F 7.07 pEC50 84.8 nM EC50 J Med Chem (2004) 47: 3580-3590 [PMID:15214785]
ChEMBL Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay F 7.11 pEC50 78 nM EC50 J Med Chem (2006) 49: 2689-2702 [PMID:16640329]
ChEMBL Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells B 7.2 pEC50 63.1 nM EC50 Med Chem Res (2004) 13: 88-98
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay B 7.2 pEC50 63 nM EC50 Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406]
ChEMBL Agonist activity at human A3 receptor expressed in Flp-In-CHO cells assessed as cAMP accumulation incubated for 30 mins in presence of forskolin by LANCE cAMP assay F 7.32 pEC50 47.86 nM EC50 J Med Chem (2022) 65: 9076-9095 [PMID:35729775]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 7.59 pEC50 26 nM EC50 J Med Chem (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay F 7.8 pEC50 15.85 nM EC50 J Med Chem (2016) 59: 11182-11194 [PMID:27958734]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 30 mins by LANCE ultra assay F 7.83 pEC50 14.79 nM EC50 J Med Chem (2022) 65: 14864-14890 [PMID:36270633]
ChEMBL Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay F 7.85 pEC50 14.13 nM EC50 J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
ChEMBL Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells F 8.34 pEC50 4.57 nM EC50 J Med Chem (2007) 50: 782-793 [PMID:17249651]
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 8.5 pEC50 3.16 nM EC50 Medchemcomm (2014) 5: 192-196
ChEMBL Antagonist activity at human wild type A3R expressed in Flp-In-CHO cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay F 9.93 pEC50 0.12 nM EC50 ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146]
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 7.85 pKi 14.1 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis F 6.73 pEC50 188 nM EC50 J Med Chem (2020) 63: 4334-4348 [PMID:32271569]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Binding affinity for adenosine A3 receptor in CHO cell membranes using [125I]IB-MECA B 6.39 pKi 412 nM Ki J Med Chem (2001) 44: 208-214 [PMID:11170630]
ChEMBL Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-. B 6.95 pKi 113 nM Ki J Med Chem (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from rat A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay B 6.95 pKi 113 nM Ki J Med Chem (2019) 62: 1502-1522 [PMID:30605331]
ChEMBL Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor B 6.95 pKi 113 nM Ki J Med Chem (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Binding affinity for rat adenosine A3 receptor B 6.95 pKi 113 nM Ki J Med Chem (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Binding affinity for recombinant rat A3-adenosine receptor by the displacement of specific [125I]APNEA or [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5'-N-methyluronamide B 6.95 pKi 113 nM Ki J Med Chem (1994) 37: 636-646 [PMID:8126704]
ChEMBL Inhibition of [125I]AB-MECA (0.15 nM) binding to Adenosine A3 receptor of RBL-2H3 cell membranes B 6.96 pKi 110 nM Ki J Med Chem (1998) 41: 2676-2678 [PMID:9667957]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 7.31 pKi 49 nM Ki J Med Chem (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes B 7.31 pKi 49 nM Ki J Med Chem (2000) 43: 2814-2823 [PMID:10956189]
heat shock protein 90 beta family member 1/Endoplasmin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625]
ChEMBL Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay B 6.28 pKd 530 nM Kd ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064]
ChEMBL Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay B 6.96 pKi 110 nM Ki ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064]
ChEMBL Inhibition of Grp94 (unknown origin) B 6.96 pKi 110 nM Ki RSC Med Chem (2021) 12: 1808-1825 [PMID:34825182]
Endoplasmin in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3425397] [UniProtKB: Q29092]
ChEMBL Binding affinity to porcine pancreas rough microsomal GRP94 after 1 hr B 6.7 pKd 200 nM Kd J Med Chem (2015) 58: 3922-3943 [PMID:25901531]
ChEMBL Displacement of [3H]NECA from GRP94 in porcine pancreas rough microsomes by liquid scintillation spectrometry B 6.7 pKd 200 nM Kd J Med Chem (2018) 61: 9513-9533 [PMID:30351001]
oxoglutarate receptor/G protein-coupled receptor 80 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2325] [GtoPdb: 162] [UniProtKB: Q6Y1R5]
ChEMBL Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes B 7.43 pKi 37 nM Ki J Med Chem (2001) 44: 208-214 [PMID:11170630]
ChEMBL Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes B 7.57 pKi 27 nM Ki J Med Chem (2001) 44: 208-214 [PMID:11170630]
Heat shock protein 90 beta in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4748] [UniProtKB: P41148]
ChEMBL Inhibition of N-terminal full length dog GRP94 (73 to 754 residues) expressed in Escherichia coli BL21(DE3) measured after 24 hrs by fluorescence polarization assay B 5.55 pKd 2800 nM Kd Eur J Med Chem (2022) 238: 114516-114516 [PMID:35691175]
heat shock protein 90 alpha family class A member 1/Heat shock protein HSP 90-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3880] [GtoPdb: 2905] [UniProtKB: P07900]
ChEMBL Inhibition of human N-terminal His-tagged Hsp90alpha (1 to 236 residues) expressed in Escherichia coli BL21(DE3) measured after 24 hrs by fluorescence polarization assay B 4.85 pKd 14000 nM Kd Eur J Med Chem (2022) 238: 114516-114516 [PMID:35691175]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
Transmembrane domain-containing protein TMIGD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9]
ChEMBL Displacement of [125l]N 6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from recombinant human A3AR expressed in CHO cell membranes after 60 mins by gamma counting method B 7.8 pKi 16 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]

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]