Cl-IB-MECA [Ligand Id: 457] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL431733 (CL-IB-MECA, Chloro-IB-MECA, CI-IB-MECA, CF-102, Namodenoson)
  • 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 CHEMBL431733_lig_chart_1 Adenosine A1 receptor HumanBovineMouseRat
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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]
2 CHEMBL431733_lig_chart_2 Adenosine A2a receptor HumanMouseRat
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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]
3 CHEMBL431733_lig_chart_3 Adenosine A2b receptor HumanMouse
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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]
4 CHEMBL431733_lig_chart_4 Adenosine A3 receptor HumanMouseRat
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  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
  • This target only has 1 pki data point
5 CHEMBL431733_lig_chart_5 Equilibrative nucleoside transporter 1 Rat
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • This target only has 1 pki data point
6 CHEMBL431733_lig_chart_6 Peroxisome proliferator-activated receptor delta Human
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • This target only has 1 pki data point
7 CHEMBL431733_lig_chart_7 Peroxisome proliferator-activated receptor gamma Human
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  • Plasmodium falciparum [ChEMBL: CHEMBL364]
  • This target only has 0 pki data point
8 CHEMBL431733_lig_chart_8 Plasmodium falciparum Plasmodium falciparum
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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
9 CHEMBL431733_lig_chart_9 Serotonin 2a (5-HT2a) receptor Human
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
  • This target only has 1 pki data point
10 CHEMBL431733_lig_chart_10 Serotonin 2b (5-HT2b) receptor Human
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • This target only has 1 pki data point
11 CHEMBL431733_lig_chart_11 Serotonin 2c (5-HT2c) receptor Human
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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 5.91 pKi 1240 nM Ki J Med Chem (2017) 60: 3422-3437 [PMID:28380296]
ChEMBL Binding affinity for human Adenosine A1 receptor in CHO cells using [3H]N6-(R)-phenylisopropyladenosine B 5.91 pKi 1240 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
ChEMBL Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells B 5.91 pKi 1240 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins B 6.05 pKi 890 nM Ki Eur. J. Med. Chem. (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells B 6.05 pKi 890 nM Ki J. Med. Chem. (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane B 6.05 pKi 890 nM Ki J. Med. Chem. (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells B 6.05 pKi 890 nM Ki J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells B 6.08 pKi 823 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor in CHO cells B 6.65 pKi 222 nM Ki J. Med. Chem. (2007) 50: 3159-3162 [PMID:17555308]
ChEMBL Displacement of [3H]CCPA from human A1 receptor expressed in CHO cell membranes after 60 mins by gamma counting method B 6.65 pKi 222 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells B 6.65 pKi 222 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells B 6.65 pKi 222 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 1612-1616 [PMID:18255292]
ChEMBL Binding affinity towards recombinant human Adenosine A1 receptor was determined using [3H]R-PIA (2.0 nM) as radioligand B 6.65 pKi 222 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells B 6.65 pKi 222 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Displacement of [3H]CCPA form human adenosine A1 receptor expressed in CHO cells B 6.65 pKi 222 nM Ki Bioorg. Med. Chem. (2008) 16: 8546-8556 [PMID:18752961]
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 6.66 pKi 220 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 6.66 pKi 220 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of radioligand from human adenosine A1 receptor expressed in CHO cells B 6.66 pKi 220 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [3H]NECA from human recombinant adenosine A1 receptor expressed in CHO cells by liquid scintillation counting B 6.66 pKi 220 nM Ki Bioorg. Med. Chem. (2009) 17: 3733-3738 [PMID:19375920]
ChEMBL Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method B 6.66 pKi 220 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
GtoPdb - - 6.66 pKi 220 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Binding affinity using [125I]ABA against human Adenosine A1 receptor B 7 pKi 99 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 8.28 pKi 5.26 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190]
ChEMBL Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes B 6.05 pKi 890 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 7.46 pKi 35 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
GtoPdb - - 7.46 pKi 35 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
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 6.09 pKi 820 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Binding affinity for rat Adenosine A1 receptor in CHO cells using [3H]N6-(R)-phenylisopropyladenosine B 6.09 pKi 820 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
ChEMBL Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes B 6.09 pKi 820 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Displacement of radioligand from rat adenosine A1 receptor B 6.09 pKi 820 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 6.09 pKi 820 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
GtoPdb - - 6.55 pKi 280 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
ChEMBL Binding affinity for adenosine A1 receptor as inhibition of 3[H]-R-PIA binding in rat brain B 7.27 pKi 54 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1767-1770 [PMID:9873431]
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274]
ChEMBL Inhibition of [3H]-CGS- 21680 binding to human Adenosine A2A receptor expressed in CHO cells B 5.27 pKi 5400 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of [3H]CGS21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells by liquid scintillation counting B 5.27 pKi 5400 nM Ki Bioorg. Med. Chem. (2009) 17: 3733-3738 [PMID:19375920]
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 5.27 pKi 5400 nM Ki J Med Chem (2016) 59: 11006-11026 [PMID:27933810]
ChEMBL Displacement of radioligand from human adenosine A2A receptor expressed in HEK293 cells B 5.27 pKi 5400 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
GtoPdb - - 5.27 pKi 5360 nM Ki Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation analyzer B 5.27 pKi 5370 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 5.27 pKi 5360 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Binding affinity towards recombinant human Adenosine A2a receptor was determined using [3H]CGS-21680 (10 nM) as radioligand B 5.27 pKi 5360 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Displacement of [3H]CGS-21680 from recombinant human adenosine A2a receptor expressed in HEK cells B 5.27 pKi 5360 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells B 5.27 pKi 5360 nM Ki J. Med. Chem. (2007) 50: 3159-3162 [PMID:17555308]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells B 5.27 pKi 5360 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 1612-1616 [PMID:18255292]
ChEMBL Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in HEK293 cells B 5.27 pKi 5360 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Displacement of [3H]R-PIA form human adenosine A2A receptor expressed in HEK cells B 5.27 pKi 5360 nM Ki Bioorg. Med. Chem. (2008) 16: 8546-8556 [PMID:18752961]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cells B 5.27 pKi 5360 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis B 5.27 pKi 5360 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [3H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by gamma counting method B 5.27 pKi 5360 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Binding affinity for human adenosine A2A receptor in CHO cells using [3H]CGS-21680 B 5.27 pKi 5360 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
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 5.43 pKi 3720 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells B 6.35 pKi 448 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells B 6.4 pKi 401 nM Ki J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes B 6.4 pKi 401 nM Ki J. Med. Chem. (2005) 48: 1550-1562 [PMID:15743197]
ChEMBL Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane B 6.4 pKi 401 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 6.4 pKi 401 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 6.4 pKi 401 nM Ki J. Med. Chem. (2008) 51: 1764-1770 [PMID:18269230]
A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613]
GtoPdb - - 5 pKi ~10000 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
ChEMBL Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from mouse recombinant adenosine A2A receptor expressed in HEK293 cells B 5 pKi 10000 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 6.33 pKi 470 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Binding affinity for rat adenosine A2A receptor of CHO cells using [3H]CGS-21680 B 6.33 pKi 470 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
ChEMBL Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes B 6.33 pKi 470 nM Ki J. Med. Chem. (1994) 37: 3614-3621 [PMID:7932588]
ChEMBL Displacement of radioligand from rat adenosine A2A receptor B 6.33 pKi 470 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 6.33 pKi 470 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
GtoPdb - - 6.33 pKi 470 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
ChEMBL Binding affinity for adenosine A2a receptor as inhibition of 3[H]-CGS 21680 binding in rat striatum B 7.25 pKi 56 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1767-1770 [PMID:9873431]
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275]
GtoPdb - - 5 pKi >10000 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
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 5 pKi >10000 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
A2B receptor/Adenosine A2b receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2237] [GtoPdb: 20] [UniProtKB: Q60614]
GtoPdb - - 5 pKi >10000 nM Ki Adenosine A3 receptors in muscle protection.. Adenosine Receptors from Cell Biology to Pharmacology (2010)
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 Binding affinity towards Adenosine A3 receptor (H95A mutant receptor) B 7.22 pKi 60 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
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 7.56 pKi 27.7 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells B 7.7 pKi 20.1 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity using [125I]ABA against human Adenosine A3 receptor B 7.85 pKi 14 nM Ki J. Med. Chem. (2003) 46: 353-355 [PMID:12540233]
ChEMBL Binding affinity for CHO cell membrane expressing human A3AR with GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one B 8.2 pKi 6.3 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells B 8.37 pKi 4.3 nM Ki J. Med. Chem. (2001) 44: 4125-4136 [PMID:11708915]
ChEMBL Binding affinity towards Adenosine A3 receptor (W243 mutant) receptor B 8.54 pKi 2.9 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Binding affinity towards human Adenosine A3 receptor wild type B 8.64 pKi 2.3 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counter B 8.66 pKi 2.2 nM Ki J. Med. Chem. (2012) 55: 5676-5703 [PMID:22468757]
ChEMBL Binding affinity for CHO cell membrane expressing human Adenosine A3 receptor using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one B 8.82 pKi 1.5 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
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 8.85 pKi 1.4 nM Ki Eur J Med Chem (2018) 157: 837-851 [PMID:30144700]
ChEMBL Affinity for human Adenosine A3 receptor expressed in CHO cell B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
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 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4851-4854 [PMID:15341938]
ChEMBL Displacement of [125I]-AB MECA from recombinant human adenosine A3 receptor expressed in HEK cells B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2004) 47: 4766-4773 [PMID:15341491]
ChEMBL Inhibition of [125I]-AB-MECA binding to human Adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2005) 48: 1745-1758 [PMID:15771421]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2007) 50: 3159-3162 [PMID:17555308]
ChEMBL Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 1612-1616 [PMID:18255292]
ChEMBL Displacement of radioligand from human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2008) 18: 2813-2819 [PMID:18424135]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2008) 51: 6609-6613 [PMID:18811138]
ChEMBL Displacement of [3H]CGS21680 form human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2008) 16: 8546-8556 [PMID:18752961]
ChEMBL Displacement of [3H]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells by liquid scintillation counting B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2009) 17: 3733-3738 [PMID:19375920]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. (2009) 17: 8003-8011 [PMID:19879151]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis B 8.85 pKi 1.4 nM Ki Bioorg. Med. Chem. Lett. (2013) 23: 26-36 [PMID:23200243]
ChEMBL Binding affinity to Adenosine receptor A3 (unknown origin) B 8.85 pKi 1.4 nM Ki J. Med. Chem. (2016) 59: 810-840 [PMID:26390077]
ChEMBL Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis B 8.85 pKi 1.4 nM Ki J Med Chem (2017) 60: 3422-3437 [PMID:28380296]
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 8.85 pKi 1.4 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
GtoPdb - - 8.9 pKi - - - Naunyn Schmiedebergs Arch. Pharmacol. (2000) 361: 225-34 [PMID:10731034];
Neuropharmacology (1997) 36: 1157-65 [PMID:9364471];
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ChEMBL Binding affinity for adenosine A3 receptor as inhibition of [125I]AB-MECA binding to human receptor expressed in HEK 293 cells B 8.96 pKi 1.1 nM Ki Bioorg. Med. Chem. Lett. (1998) 8: 1767-1770 [PMID:9873431]
ChEMBL Binding affinity to human adenosine A3 receptor 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 for human Adenosine A3 receptor in CHO cells using [125I]-iodo-AB-MECA B 9 pKi 1 nM Ki J. Med. Chem. (2003) 46: 3775-3777 [PMID:12930138]
ChEMBL Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells B 9.2 pKi 0.64 nM Ki Bioorg. Med. Chem. Lett. (2006) 16: 2416-2418 [PMID:16487705]
ChEMBL Displacement of [125I]I-AB-MEAC from human adenosine A3 receptor expressed in CHO cells B 9.42 pKi 0.38 nM Ki Eur. J. Med. Chem. (2009) 44: 1377-1382 [PMID:18973967]
ChEMBL Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells B 9.48 pKi 0.33 nM Ki J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptor from HEK293 cell membranes B 9.48 pKi 0.33 nM Ki J. Med. Chem. (1998) 41: 3186-3201 [PMID:9703464]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins B 9.66 pKi 0.22 nM Ki Eur. J. Med. Chem. (2013) 69: 331-337 [PMID:24077183]
ChEMBL Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2005) 48: 1550-1562 [PMID:15743197]
ChEMBL Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2012) 55: 1490-1499 [PMID:22257095]
ChEMBL Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2007) 50: 5676-5684 [PMID:17927167]
ChEMBL Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells B 9.66 pKi 0.22 nM Ki J. Med. Chem. (2008) 51: 1764-1770 [PMID:18269230]
ChEMBL Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins B 9.7 pKi 0.2 nM Ki MedChemComm (2018) 9: 81-86
ChEMBL Inhibition of (10 uM) forskolin-mediated cAMP production in CHO cells expressing human Adenosine A3 receptor F 8.66 pIC50 2.2 nM IC50 J. Med. Chem. (2004) 47: 5535-5540 [PMID:15481989]
ChEMBL Agonist activity at human recombinant A3AR expressed in CHO cells assessed as inhibition of forskolin-induced stimulation of cAMP production F 8.92 pIC50 1.21 nM IC50 Bioorg. Med. Chem. (2014) 22: 4257-4268 [PMID:24931275]
ChEMBL Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor F 8.55 pEC50 2.8 nM EC50 J. Med. Chem. (2002) 45: 4471-4484 [PMID:12238926]
ChEMBL Agonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP F