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

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ChEMBL ligand: CHEMBL431733 (Cf102, CF-102, CF102, Chloro-ib-meca, CI-IB-MECA, CL-IB-MECA, 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]
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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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  • ABCG2/ATP-binding cassette sub-family G member 2 in Human [ChEMBL: CHEMBL5393] [GtoPdb: 792] [UniProtKB: Q9UNQ0]
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  • Equilibrative nucleoside transporter 1 in Rat [ChEMBL: CHEMBL4604] [GtoPdb: 1117] [UniProtKB: O54698]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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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 5.91 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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (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 to human adenosine A3 receptor measured by radioligand binding assay B 5.85 pKi 1400 nM Ki ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351]
ChEMBL Binding affinity towards human adenosine A3 receptor B 7 pKi >=99 nM Ki Eur J Med Chem (2022) 231: 114103-114103 [PMID:35152062]
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]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 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]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]
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 Binding affinity to human A3AR assessed as inhibitor constant B 8.85 pKi 1.4 nM Ki ACS Med Chem Lett (2020) 11: 1935-1941 [PMID:33062176]
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]
GtoPdb - - 8.9 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2000) 361: 225-34 [PMID:10731034];
Neuropharmacology (1997) 36: 1157-65 [PMID:9364471];
J Med Chem (1994) 37: 3614-21 [PMID:7932588]
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 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 Binding affinity to A3AR (unknown origin) B 9 pKi 1 nM Ki Bioorg Med Chem (2014) 22: 4257-4268 [PMID:24931275]
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 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 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 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 [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 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