piclidenoson [Ligand Id: 422] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL119709 (IB-MECA)
  • 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]
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  • A2A receptor/Adenosine A2a receptor in Human [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
  • A2A receptor/Adenosine A2a receptor in Mouse [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
  • A2A receptor/Adenosine A2a receptor in Rat [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
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  • A2B receptor/Adenosine A2b receptor in Human [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
  • A2B receptor/Adenosine A2b receptor in Mouse [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
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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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  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542]
ChEMBL Displacement of [3H]R-PLA from human adenosine A1 receptor expressed in CHO cells after 60 mins by liquid scintillation analyzer B 5.79 pKi 1620 nM Ki J Med Chem (2017) 60: 3422-3437 [PMID:28380296]
ChEMBL Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method B 6.15 pKi 700 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells B 7.27 pKi 54 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells B 7.27 pKi 54 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
GtoPdb - - 7.29 pKi 51 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]CCPA from human A1 receptor expressed in CHO cell membranes after 60 mins by gamma counting method B 7.29 pKi 51.2 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Binding affinity towards recombinant human Adenosine A1 receptor was determined using [3H]R-PIA (2.0 nM) as radioligand B 7.29 pKi 51.2 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Binding affinity to adenosine A1 receptor (unknown origin) B 7.29 pKi 51 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method B 7.29 pKi 51 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Inhibition of [3H]R-PIA binding to human Adenosine A1 receptor expressed in CHO cells B 7.29 pKi 51 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells B 7.29 pKi 51 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells B 7.29 pKi 51 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Displacement of radioligand from human adenosine A1 receptor expressed in CHO cells B 7.31 pKi 49.3 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Binding affinity using [125I]ABA against human Adenosine A1 receptor B 7.7 pKi 20 nM Ki J. Med. Chem. (2003) 46: 353-355 [PMID:12540233]
ChEMBL Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells B 8.4 pKi 3.98 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Binding affinity for human adenosine A1 receptor B 8.43 pKi 3.73 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
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 7.5 pEC50 31.62 nM EC50 MedChemComm (2014) 5: 192-196
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 7.48 pKi 33.1 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes B 7.92 pKi 12 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 [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A1 receptor expressed in HEK293 cells B 8.23 pKi 5.9 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099]
ChEMBL Binding affinity for adenosine A1 receptor as displacement of [3H]R-PIA from rat brain membranes at 10e-4 M B 7.27 pKi 54 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Binding affinity for A1-adenosine receptor by the displacement of specific [3H]-PIA binding in rat brain was determined B 7.27 pKi 54 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 7.27 pKi 54 nM Ki J. Med. Chem. (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Displacement of [3H]CHA from Adenosine A1 receptor in rat brain homogenates B 7.27 pKi 54 nM Ki J. Med. Chem. (1996) 39: 802-806 [PMID:8576924]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 7.27 pKi 54 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A1 receptor from rat brain. B 7.27 pKi 54 nM Ki J. Med. Chem. (1995) 38: 1720-1735 [PMID:7752196]
ChEMBL Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. B 7.27 pKi 54 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 7.27 pKi 54 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of radioligand from rat adenosine A1 receptor B 7.27 pKi 54 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [3H]CCPA from rat adenosine A1 receptor expressed in CHO cells after 60 mins by gamma counter B 7.27 pKi 54 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from recombinant human adenosine receptor A2A expressed in HEK293 cell membranes after 60 mins by liquid scintillation counting method B 5.21 pKi 6200 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Binding affinity towards recombinant human Adenosine A2a receptor was determined using [3H]CGS-21680 (10 nM) as radioligand B 5.54 pKi 2910 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Displacement of [3H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by gamma counting method B 5.54 pKi 2910 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation analyzer B 5.54 pKi 2910 nM Ki J Med Chem (2017) 60: 3422-3437 [PMID:28380296]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method B 5.54 pKi 2900 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells B 5.54 pKi 2900 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in HEK293 cells B 5.54 pKi 2900 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells B 5.54 pKi 2900 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Binding affinity for human adenosine A2A receptor B 5.6 pKi 2520 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [125I]ZM241385 from human adenosine A2A receptor in HEK cells B 6.29 pKi 510 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
GtoPdb - - 6.3 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
J Biol Chem (1995) 270: 13987-97 [PMID:7775460];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
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 6.43 pKi 370 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 6.84 pKi 143 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
ChEMBL Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. B 6.94 pKi 116 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Displacement of radioligand from human adenosine A2A receptor expressed in HEK293 cells B 7.03 pKi 93.1 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells B 7.25 pKi 56 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells B 7.25 pKi 56 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes B 7.4 pKi 40 nM Ki J. Med. Chem. (2005) 48: 1550-1562 [PMID:15743197]
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 7.49 pKi 32 nM Ki J. Med. Chem. (1997) 40: 2588-2595 [PMID:9258366]
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 7.1 pEC50 79.43 nM EC50 MedChemComm (2014) 5: 192-196
A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from mouse recombinant adenosine A2A receptor expressed in HEK293 cells B 6 pKi 1000 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543]
ChEMBL Binding affinity for adenosine A2A receptor as displacement of [3H]-CGS- 21680 from rat striatal membranes at 10e-4 M B 7.25 pKi 56 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680. B 7.25 pKi 56 nM Ki J. Med. Chem. (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor in rat striatal homogenates B 7.25 pKi 56 nM Ki J. Med. Chem. (1996) 39: 802-806 [PMID:8576924]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 7.25 pKi 56 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A2A receptor from rat brain. B 7.25 pKi 56 nM Ki J. Med. Chem. (1995) 38: 1720-1735 [PMID:7752196]
ChEMBL Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand B 7.25 pKi 56 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane B 7.25 pKi 56 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of radioligand from rat adenosine A2A receptor B 7.25 pKi 56 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [3H]CGS21680 from rat adenosine A2A receptor expressed in CHO cells after 60 mins by gamma counter B 7.25 pKi 56 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 4.9 pKi - - - Mol Pharmacol (1999) 56: 705-13 [PMID:10496952];
Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Antagonist activity at human adenosine A2B receptor expressed in CHO cell membranes assessed as inhibition of NECA-stimulated adenylyl cyclase activity by [alpha-32P]ATP based assay F 4.96 pKi 11000 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells B 5.69 pKi 2040 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA F 4.96 pEC50 11000 nM EC50 J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay F 7.5 pEC50 31.62 nM EC50 MedChemComm (2014) 5: 192-196
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
ChEMBL Activation of mouse adenosine A2B receptor B 5 pEC50 >=10000 nM EC50 Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8]
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 7.96 pKi 10.9 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes B 8.06 pKi 8.8 nM Ki J. Med. Chem. (2005) 48: 1550-1562 [PMID:15743197]
ChEMBL Binding affinity to human adenosine A3 receptor B 8.36 pKi 4.4 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2525-2527 [PMID:16464581]
ChEMBL Binding affinity using [125I]ABA against human Adenosine A3 receptor B 8.36 pKi 4.4 nM Ki J. Med. Chem. (2003) 46: 353-355 [PMID:12540233]
ChEMBL Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter B 8.39 pKi 4.1 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL Inhibitory constant against human adenosine A3 receptor B 8.7 pKi 2 nM Ki J. Med. Chem. (2007) 50: 65-73 [PMID:17201410]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 8.74 pKi 1.8 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins by gamma counting method B 8.74 pKi 1.8 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis B 8.74 pKi 1.8 nM Ki J Med Chem (2017) 60: 3422-3437 [PMID:28380296]
ChEMBL Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of [3H]HEMADO from human adenosine A3 receptor expressed in CHO cell membranes after 3 hrs by micro beta scintillation counting method B 8.74 pKi 1.8 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Binding affinity towards human Adenosine A3 receptor stably transfected in CHO cells was determined using [125I]I-AB-MECA (1.0 nM) as radioligand B 8.74 pKi 1.8 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity to Adenosine receptor A3 (unknown origin) B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
ChEMBL Binding affinity to adenosine A3 receptor (unknown origin) B 8.74 pKi 1.8 nM Ki J. Med. Chem. (2016) 59: 788-809 [PMID:26356532]
ChEMBL Displacement of radioligand from human adenosine A3 receptor expressed in CHO cells B 8.76 pKi 1.74 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Binding affinity towards human Adenosine A3 receptor wild type B 8.8 pKi 1.6 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity to human adenosine A3 receptor B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Displacement of [125I]AB-MECA from membranes of HEK 293 cells expressing human Adenosine A3 receptor B 8.92 pKi 1.2 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells B 9 pKi 1 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Binding affinity to human adenosine A3 receptor B 9 pKi 1 nM Ki Eur. J. Med. Chem. (2016) 118: 121-142 [PMID:27128178]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 9 pKi 1 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Binding affinity to A3AR (unknown origin) B 9 pKi 1 nM Ki Bioorg. Med. Chem. (2014) 22: 4257-4268 [PMID:24931275]
ChEMBL Binding affinity towards Adenosine A3 receptor (W243A) 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 expressed in HEK293 cells using 0.1 nM [3H]AB-MECA B 9.08 pKi 0.84 nM Ki J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins B 9.14 pKi 0.72 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of radiolabeled IB-MECA from human adenosine A3 receptor B 9.15 pKi 0.7 nM Ki J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
GtoPdb - - 9.2 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566];
Mol Pharmacol (2000) 57: 968-75 [PMID:10779381];
Biochem Pharmacol (2001) 62: 1163-73 [PMID:11705449];
J Med Chem (1994) 37: 636-46 [PMID:8126704]
ChEMBL Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells B 9.67 pKi 0.21 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Binding affinity to human adenosine A3 receptor by radioligand displacement assay B 10.1 pKi 0.08 nM Ki Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
ChEMBL Inhibition of human adenosine A3 receptor B 8.6 pIC50 2.5 nM IC50 J. Med. Chem. (2008) 51: 4150-4169 [PMID:18588282]
ChEMBL Displacement of radiolabeled IB-MECA from human adenosine A3 receptor B 8.92 pIC50 1.2 nM IC50 J. Med. Chem. (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL Inhibitory concentration against human Adenosine A3 receptor expressed in HEK293 cells using 0.1 nM [3H]AB-MECA B 8.92 pIC50 1.2 nM IC50 J. Med. Chem. (2005) 48: 6887-6896 [PMID:16250647]
ChEMBL Displacement of [3H]ABMECA from human recombinant adenosine receptor A3 expressed in CHOK1 cells after 60 mins B 9.11 pIC50 0.78 nM IC50 Bioorg. Med. Chem. Lett. (2013) 23: 1834-1838 [PMID:23403082]
ChEMBL Displacement of [125I]AB-MECA from human recombinant adenosine receptor A3 expressed in HEK293 cells measured after 120 mins by scintillation counting method B 9.22 pIC50 0.6 nM IC50 Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
ChEMBL Displacement of [125I]ABMECA from human recombinant adenosine A3 receptor expressed in HEK293 cells B 9.22 pIC50 0.6 nM IC50 Bioorg. Med. Chem. (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL Binding affinity to human adenosine A3 receptor by radioligand displacement assay B 9.89 pIC50 0.13 nM IC50 Eur. J. Med. Chem. (2013) 63: 85-94 [PMID:23466604]
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 B 10.64 pIC50 0.02 nM IC50 J Med Chem (2019) 62: 8831-8846 [PMID:31502843]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 8.44 pEC50 3.6 nM EC50 J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Inhibition of isoproterenol-stimulated cAMP accumulation in HEK 293 cells expressing human Adenosine A3 receptor F 9 pEC50 1 nM EC50 J. Med. Chem. (2003) 46: 353-355 [PMID:12540233]
ChEMBL Agonist activity at adenosine A3 receptor (unknown origin) expressed in serum starved CHO cells assessed as increase in cell survival after 24 hrs by propidium iodide staining-based assay B 9.2 pEC50 0.63 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
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 9.3 pEC50 0.5 nM EC50 MedChemComm (2014) 5: 192-196
ChEMBL Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-mediated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by alphascreen assay B 9.4 pEC50 0.4 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay B 9.6 pEC50 0.25 nM EC50 J Med Chem (2018) 61: 9841-9878 [PMID:29939744]
A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618]
ChEMBL Displacement of [125I]N6-(-amino-3-iodobenzyl)adenosine-5'-N-methyl-uronamide from mouse recombinant adenosine A3 receptor expressed in HEK293 cells B 10.06 pKi 0.09 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647]
ChEMBL Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes B 7.52 pKi 30 nM Ki J. Med. Chem. (1998) 41: 1708-1715 [PMID:9572897]
ChEMBL Binding affinity for rat Adenosine A3 receptor in CHO cells using [125I]iodo-AB-MECA B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
ChEMBL Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-. B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1998) 41: 3174-3185 [PMID:9703463]
ChEMBL Displacement of [125I]AB-MECA from cloned rat Adenosine A3 receptor in stably transfected CHO cells B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1996) 39: 802-806 [PMID:8576924]
ChEMBL Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Binding affinity against adenosine A3 receptor from rat brain. B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1995) 38: 1720-1735 [PMID:7752196]
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 8.96 pKi 1.1 nM Ki J. Med. Chem. (1995) 38: 1174-1188 [PMID:7707320]
ChEMBL Binding affinity for rat adenosine A3 receptor B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1999) 42: 1384-1392 [PMID:10212124]