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

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

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]
1 CHEMBL119709_lig_chart_1 Adenosine A1 receptor HumanBovineMouseRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
2 CHEMBL119709_lig_chart_2 Adenosine A2a receptor HumanMouseRat
There should be some charts here, you may need to enable JavaScript!
  • 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]
3 CHEMBL119709_lig_chart_3 Adenosine A2b receptor HumanMouse
There should be some charts here, you may need to enable JavaScript!
  • 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]
4 CHEMBL119709_lig_chart_4 Adenosine A3 receptor HumanMouseRat
There should be some charts here, you may need to enable JavaScript!
  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
  • This target only has 1 pki data point
5 CHEMBL119709_lig_chart_5 Equilibrative nucleoside transporter 1 Rat
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • This target only has 1 pki data point
6 CHEMBL119709_lig_chart_6 Serotonin 2a (5-HT2a) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
7 CHEMBL119709_lig_chart_7 Serotonin 2b (5-HT2b) receptor Human
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
8 CHEMBL119709_lig_chart_8 Serotonin 2c (5-HT2c) receptor Human
There should be some charts here, you may need to enable JavaScript!
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 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 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 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]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 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 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 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 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
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]
ChEMBL Inhibition of [125I]AB-MECA binding to rat Adenosine A3 receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of radioligand from rat A3 adenosine receptor B 8.96 pKi 1.1 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [125I]I-AB-MECA from rat adenosine A3 receptor expressed in CHO cells B 8.96 pKi 1.1 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Binding affinity for rat A3-adenosine receptor expressed in chinese hamster ovarian cells (assayed by the displacement of specific [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5''-N-methyluronamide) B 8.96 pKi 1.1 nM Ki J. Med. Chem. (1994) 37: 636-646 [PMID:8126704]
ChEMBL