NECA [Ligand Id: 377] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL464859 (5'-N-Ethylcarboxamidoadenosine, NECA)
1 CHEMBL464859_lig_chart_1 Adenosine A1 receptor ChickenHumanBovineRatGuinea pig
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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]
2 CHEMBL464859_lig_chart_2 Adenosine A2a receptor HumanRat
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614]
  • A2B receptor/Adenosine A2b receptor in Rat [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276]
3 CHEMBL464859_lig_chart_3 Adenosine A2b receptor HumanMouseRat
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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]
4 CHEMBL464859_lig_chart_4 Adenosine A3 receptor HumanRat
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  • Endoplasmin in Pig [ChEMBL: CHEMBL3425397] [UniProtKB: Q29092]
  • This target only has 0 pki data point
5 CHEMBL464859_lig_chart_5 Endoplasmin Pig
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  • oxoglutarate receptor/G protein-coupled receptor 80 in Rat [ChEMBL: CHEMBL2325] [GtoPdb: 162] [UniProtKB: Q6Y1R5]
6 CHEMBL464859_lig_chart_6 G protein-coupled receptor 80 Rat
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
7 CHEMBL464859_lig_chart_7 Serotonin 2a (5-HT2a) receptor Human
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  • Transmembrane domain-containing protein TMIGD3 in Human [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9]
  • This target only has 1 pki data point
8 CHEMBL464859_lig_chart_8 Transmembrane domain-containing protein TMIGD3 Human
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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 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 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 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 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 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]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 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 ACS Med. Chem. Lett. (2011) 2: 890-895 [PMID:24900277]
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 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]
GtoPdb - - 8.2 pKi - - - J. Biol. Chem. (1994) 269: 32077-84 [PMID:7798201];
J. Biol. Chem. (1999) 274: 3617-21 [PMID:9920910];
J. Biol. Chem. (1994) 269: 2373-6 [PMID:8300561];
Biochem. Pharmacol. (2004) 68: 1985-93 [PMID:15476669];
Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005]
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 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 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 B 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 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 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 B 9.12 pEC50 0.76 nM EC50 J Med Chem (2018) 61: 2087-2103 [PMID:29446948]
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]
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 Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
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 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 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 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 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 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 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 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 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 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 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 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 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 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]
GtoPdb - - 8.29 pKi 5.1 nM Ki Curr Pharm Des (1996) 2: 501-530
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 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 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]
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 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 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 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 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]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 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 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 expressed in HEK cells B 7.7 pKi 20 nM Ki Bioorg. Med. Chem. (2013) 21: 436-447 [PMID:23245803]
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 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 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 A2A receptor expressed in CHO cells B 7.8 pKi 16 nM Ki J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
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]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]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]-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]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 adenosine A2A receptor expressed in CHO cells B 7.8 pKi 16 nM