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ChEMBL ligand: CHEMBL183 (GNF-Pf-2224) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | pA2 against human brain adenosine A1 receptor | B | 8.43 | pKd | 3.71 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
ChEMBL | The A1-StaR receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. | B | 8.57 | pKd | 2.7 | nM | Kd | K4DD drug target binding kinetics data |
ChEMBL | Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHOK1 cells by scintillation counting | B | 7.02 | pKi | 95 | nM | Ki | Eur J Med Chem (2009) 44: 2122-2127 [PMID:19036477] |
ChEMBL | Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay | B | 7.4 | pKi | 39.81 | nM | Ki | J Med Chem (2021) 64: 6670-6695 [PMID:33724031] |
ChEMBL | Binding affinity to adenosine receptor A1 | B | 7.89 | pKi | 12.9 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 2 hrs by scintillation counting analysis relative to control | B | 7.92 | pKi | 12.02 | nM | Ki | Medchemcomm (2012) 3: 333-338 |
ChEMBL | Binding affinity for human Adenosine A1 receptor | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2004) 47: 663-672 [PMID:14736246] |
ChEMBL | Binding affinity towards human A1 receptor (hA1) was measured through displacement of [3H]-DPCPX using mammalian cell membranes | B | 8.15 | pKi | 7 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
ChEMBL | Binding affinity against adenosine A1 receptor in human cortical membranes using [3H]CHA as radioligand | B | 8.17 | pKi | 6.7 | nM | Ki | J Med Chem (2004) 47: 3019-3031 [PMID:15163184] |
ChEMBL | Binding affinity towards human Adenosine A1 receptor expressed in CHO cells using 1 nM [3H]DPCPX | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
ChEMBL | Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2005) 48: 2045-2053 [PMID:15771447] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 8.21 | pKi | 6.1 | nM | Ki | Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane | B | 8.21 | pKi | 6.1 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
ChEMBL | Displacement of radiolabeled DPCPX from human adenosine A1 receptor | B | 8.38 | pKi | 4.2 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 8.4 | pKi | 4 | nM | Ki | Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 8.41 | pKi | 3.9 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO-A1 cells after 60 mins | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells after 120 mins | B | 8.49 | pKi | 3.2 | nM | Ki | Eur J Med Chem (2015) 89: 32-41 [PMID:25462223] |
ChEMBL | Displacement of [3H]CHA from cloned human adenosine A1 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2007) 50: 4061-4074 [PMID:17665891] |
ChEMBL | Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]CHA | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Displacement of [125I]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Displacement of [3H]DPCPX from human cloned adenosine A1 receptor expressed in CHO cells | B | 8.49 | pKi | 3.2 | nM | Ki | J Med Chem (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Inhibitory constant aganist human adenosine A1 receptor | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2007) 50: 65-73 [PMID:17201410] |
ChEMBL | Inhibition of binding to membranes from HEK293 cells expressing human Adenosine A1 receptor | B | 8.6 | pKi | 2.52 | nM | Ki | J Med Chem (1997) 40: 1773-1778 [PMID:9191953] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2021) 64: 458-480 [PMID:33372800] |
ChEMBL | Displacement of [3H]DPCPX from human Adenosine A1 receptor expressed in CHO cells after 60 mins | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2016) 59: 1967-1983 [PMID:26824742] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes after 60 mins | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2017) 60: 3372-3382 [PMID:28368607] |
ChEMBL | Displacement [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes incubated for 60 mins by scintillation counting method | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2020) 63: 7721-7739 [PMID:32573250] |
ChEMBL | Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membrane incubated for 60 mins by microbeta trilux scintillation counter analysis | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2022) 65: 2091-2106 [PMID:35068155] |
ChEMBL | Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membrane assessed as inhibition constant incubated for 60 mins by competitive binding assay | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2023) 66: 890-912 [PMID:36517209] |
ChEMBL | Binding affinity at human Adenosine A1 receptor expressed in CHO cells | B | 8.67 | pKi | 2.13 | nM | Ki | J Med Chem (2002) 45: 1845-1852 [PMID:11960496] |
ChEMBL | Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in HEK293 cells | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2008) 51: 400-406 [PMID:18189346] |
ChEMBL | Displacement of [3H]DPCPX from human A1AR expressed in CHO cell membranes measured after 90 mins by scintillation counting method | B | 8.96 | pKi | 1.09 | nM | Ki | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
ChEMBL | Displacement of [3H]CPX from human adenosine A3 receptor expressed in CHO cells | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2006) 49: 3682-3692 [PMID:16759111] |
ChEMBL | Antagonist activity against human adenosine A1 receptor | F | 9.05 | pKi | 0.9 | nM | Ki | Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438] |
ChEMBL | Binding affinity to human A1R expressed in Flp-In-CHO cells incubated for 12 hrs by microbeta plate counter analysis | B | 9.08 | pKi | 0.83 | nM | Ki | Eur J Med Chem (2023) 257: 115419-115419 [PMID:37301076] |
GtoPdb | - | - | 9.2 | pKi | 0.63 | nM | Ki |
J Biol Chem (1999) 274: 3617-21 [PMID:9920910]; J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]; Eur J Pharmacol (2005) 510: 1-8 [PMID:15740718]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; Br J Pharmacol (1994) 111: 1252-6 [PMID:8032613] |
ChEMBL | Displacement of CA200645 from NLuc human A1 receptor expressed in HEK293 cells assessed as inhibition constant by NanoBRET binding assay | B | 9.23 | pKi | 0.59 | nM | Ki | ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146] |
ChEMBL | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | B | 9.25 | pKi | 0.56 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2005) 48: 8253-8260 [PMID:16366607] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
ChEMBL | Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
ChEMBL | Antagonist activity against adenosine A1 receptor in human platelets | F | 9.33 | pKi | 0.47 | nM | Ki | J Med Chem (1990) 33: 1906-1910 [PMID:1694546] |
ChEMBL | Inhibition of human adenosine A1 receptor | B | 7.6 | pIC50 | 25 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
ChEMBL | Binding affinity against human A1 receptor (hA1) was measured through displacement of [3H]DPCPX using yeast cell membranes | B | 7.85 | pIC50 | 14 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
ChEMBL | Inhibitory activity against human A1 receptor (hA1) on membranes from yeast cells | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
ChEMBL | Inhibition of human adenosine A1 receptor | B | 7.89 | pIC50 | 13 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
ChEMBL | Displacement of radiolabeled DPCPX from human adenosine A1 receptor | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
ChEMBL | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | B | 9.05 | pIC50 | 0.89 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
ChEMBL | Binding affinity to human adenosine A1 receptor by radioligand displacement assay | B | 9.06 | pIC50 | 0.87 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
ChEMBL | Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
ChEMBL | Displacement of [3H]DPCPX from human recombinant adenosine receptor A1 expressed in CHO cells measured after 60 mins by scintillation counting method | B | 9.3 | pIC50 | 0.5 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
ChEMBL | Antagonist activity at human wild type A1R expressed in CHO-K1 cells assessed as inhibition of forskolin/ NECA-stimulated cAMP accumulation by measuring NECA-mediated cAMP stimulation at 1 uM incubated with NECA for 30 mins by LANCE cAMP detection assay | F | 6.03 | pEC50 | 933.25 | nM | EC50 | ACS Med Chem Lett (2022) 13: 923-934 [PMID:35707146] |
ChEMBL | Inverse agonist activity at human A1AR expressed in CHO cells assessed as increase in forskolin-stimulated cAMP production by alphascreen assay | F | 8.82 | pEC50 | 1.52 | nM | EC50 | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
ChEMBL | Displacement of [125I]DPCPX from adenosine A1 receptor in bovine brain membrane | B | 9.3 | pKi | 0.5 | nM | Ki | Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Binding affinity against adenosine A1 receptor in bovine brain membranes by [3H]CHA displacement. | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in bovine brain membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2000) 43: 3118-3124 [PMID:10956220] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in bovine cerebral cortical membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in bovine brain membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]DPCPX from bovine brain cortical membrane adenosine A1 receptor | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2001) 44: 316-327 [PMID:11462973] |
ChEMBL | Binding affinity at bovine Adenosine A1 receptor. | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2002) 45: 4875-4887 [PMID:12383013] |
ChEMBL | Affinity to A1 adenosine receptor was measured by the displacement of [3H]PIA in bovine brain cortical membrane | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1994) 37: 2970-2975 [PMID:8071944] |
ChEMBL | Binding affinity against adenosine A1 receptor in bovine cortical membranes using [3H]CHA as radioligand | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2004) 47: 3019-3031 [PMID:15163184] |
ChEMBL | Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes | B | 9.77 | pKi | 0.17 | nM | Ki | J Med Chem (1998) 41: 555-563 [PMID:9484505] |
ChEMBL | Displacement of [3H]CPX from Adenosine A1 receptor of bovine brain cerebral cortex membranes | B | 9.81 | pKi | 0.15 | nM | Ki | J Med Chem (1998) 41: 555-563 [PMID:9484505] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | pA2 against rat brain adenosine A1 receptor | B | 8.24 | pKd | 5.75 | nM | Kd | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
ChEMBL | Binding affinity for Adenosine A1 receptor of rat forebrain | B | 8.42 | pKi | 3.77 | nM | Ki | J Med Chem (1997) 40: 1773-1778 [PMID:9191953] |
ChEMBL | Inhibition of [3H]-CHA binding to Adenosine A1 receptor in rat whole brain homogenates. | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (1996) 39: 1164-1171 [PMID:8676354] |
ChEMBL | Binding affinity at rat Adenosine A1 receptor in the absence of GTP | B | 8.84 | pKi | 1.46 | nM | Ki | J Med Chem (2002) 45: 1845-1852 [PMID:11960496] |
ChEMBL | Binding affinity at rat Adenosine A1 receptor in the presence of GTP | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2002) 45: 1845-1852 [PMID:11960496] |
ChEMBL | Binding affinity of specific [3H]R-PIA binding to rat Adenosine A1 receptor in HEK293 cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
ChEMBL | Inhibition of (R)-N6-([3H]-phenylisopropyl) adenosine binding to adenosine A1 receptor from rat cortical membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat cortical membranes using N6-[3H]cyclohexyladenosine as radioligand | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Inhibition of 1 nM [3H]- N6-(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat cerebral cortical membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1989) 32: 1231-1237 [PMID:2724296] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex membrane | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Inhibition of [3H]CCPA binding to rat adenosine A1 receptor | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
ChEMBL | Inhibition of [3H]CCPA binding to adenosine A1 receptor | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2005) 48: 2108-2114 [PMID:15771453] |
ChEMBL | Inhibition of binding of 1 nM [3H]N-6-(phenylisopropyl)adenosine to adenosine A1 receptor in rat cortical membranes | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (1989) 32: 1873-1879 [PMID:2754711] |
ChEMBL | GTP-induced shift at rat Adenosine A1 receptor (A1AR) | B | 9.11 | pKi | 0.77 | nM | Ki | J Med Chem (2002) 45: 1845-1852 [PMID:11960496] |
ChEMBL | Evaluated for binding affinity against Adenosine A1 receptor | B | 9.21 | pKi | 0.62 | nM | Ki | J Med Chem (1992) 35: 629-635 [PMID:1542091] |
ChEMBL | Inhibition of 1 nM [3H]- N6 -(phenylisopropyl) adenosine binding to Adenosine A1 receptor in rat fat cell membrane | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1989) 32: 1231-1237 [PMID:2724296] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat whole brain membranes | B | 9.25 | pKi | 0.56 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes | B | 9.26 | pKi | 0.55 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in absence of GTP | B | 9.26 | pKi | 0.55 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by scintillation counting | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2010) 45: 1739-1745 [PMID:20116907] |
ChEMBL | Displacement of [3H]CCPA from rat adenosine A1 receptor | B | 9.3 | pKi | 0.5 | nM | Ki | Eur J Med Chem (2008) 43: 614-620 [PMID:17602796] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat forebrain membranes using N6-[3H]cyclohexyladenosine | B | 9.31 | pKi | 0.49 | nM | Ki | J Med Chem (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in presence of 0.1 mM GTP | B | 9.32 | pKi | 0.48 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from whole brain membranes | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Tested for binding affinity against Adenosine A1 receptor from rat forebrain membranes, using N6-[3H]- cyclohexyladenosine as radioligand | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1993) 36: 2508-2518 [PMID:8355252] |
ChEMBL | Binding affinity against adenosine A1 receptor using N6-[3H]-cyclohexyladenosinene in rat whole brain membranes | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Displacement of [3H]PIA from adenosine A1 receptors of rat brain membrane | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor derived from rat brain membrane assessed as inhibition constant | B | 9.34 | pKi | 0.46 | nM | Ki | J Med Chem (2021) 64: 7156-7178 [PMID:34019396] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes in presence of GTP by radioligand competition assay | B | 9.4 | pKi | 0.4 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay | B | 9.4 | pKi | 0.4 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes | B | 9.52 | pKi | 0.3 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]-PIA from Adenosine A1 receptor in Wistar rat brain membranes | B | 9.52 | pKi | 0.3 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Adenosine A1 receptor binding using [3H]DPCPX in rat cortical membranes | B | 9.55 | pKi | 0.28 | nM | Ki | J Med Chem (1999) 42: 779-783 [PMID:10072675] |
ChEMBL | Inhibition of N6-[3H]cyclohexyladenosine binding to adenosine A1 receptor from rat cortical membranes | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Binding affinity against adenosine A1 receptor in rat cortex by the displacement of [3H]cyclohexyladenosine (CHA). | B | 9.64 | pKi | 0.23 | nM | Ki | J Med Chem (1991) 34: 1431-1435 [PMID:2016719] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in absence of GTP | B | 9.64 | pKi | 0.23 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in presence of 0.1 mM GTP | B | 9.68 | pKi | 0.21 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
GtoPdb | - | - | 9.74 | pKi | 0.18 | nM | Ki |
ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Naunyn Schmiedebergs Arch Pharmacol (1991) 343: 196-201 [PMID:2067592] |
ChEMBL | Antagonist activity at adenosine A1 receptor in rat cortical membrane assessed as reduction of [35S]GTPgammaS binding | F | 8.22 | pIC50 | 6 | nM | IC50 | J Nat Prod (2002) 65: 1479-1485 [PMID:12398547] |
ChEMBL | Inhibitory activity against Adenosine A1 Receptor using [3H]CHA in rat cortical membranes | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1979-1984 [PMID:10450966] |
ChEMBL | Inhibition of [3H]-CHA binding against Adenosine A1 receptors of rat cortical membranes; Not tested | B | 8.33 | pIC50 | 4.7 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2059-2062 |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | Displacement of N6-[3H]cyclohexyladenosine from adenosine receptor A1 in guinea pig forebrain membranes by liquid scintillation counting method | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (2020) 63: 13291-13315 [PMID:32805118] |
ChEMBL | Binding affinity towards adenosine A1 receptor using N6-[3H]cyclohexyladenosine in guinea pig forebrain membranes | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1992) 35: 3578-3581 [PMID:1404238] |
ChEMBL | Inhibition of [3H]cyclohexyladenosine binding to guinea pig forebrain membranes Adenosine A1 receptor | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1991) 34: 466-469 [PMID:1992150] |
ChEMBL | Binding affinity against adenosine A1 receptor in guinea pig forebrain membranes using N6-[3H]cyclohexyladenosine as radioligand | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1992) 35: 3066-3075 [PMID:1501234] |
ChEMBL | Binding affinity against adenosine A1 receptor using N6-[3H]cyclohexyladenosine as radioligand in guinea pig forebrain membranes | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Binding affinity against Adenosine A1 receptor from guinea pig forebrain membranes by N6-[3H]- cyclohexyladenosine displacement. | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1993) 36: 2508-2518 [PMID:8355252] |
ChEMBL | Binding affinity against adenosine A1 receptor from guinea pig forebrain membranes, using N6-[3H]cyclohexyladenosine as radioligand. | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (1992) 35: 2342-2345 [PMID:1613758] |
ChEMBL | Binding affinity for Adenosine A1 receptor from Guinea pig membranes | B | 8.53 | pKi | 2.93 | nM | Ki | J Med Chem (1997) 40: 1773-1778 [PMID:9191953] |
ChEMBL | Inhibition of adenosine induced negative inotropic activity against guinea-pig atria (Adenosine A1 receptor) | F | 8.88 | pIC50 | 1.31 | nM | IC50 | Bioorg Med Chem Lett (1996) 6: 2059-2062 |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Then it has been reconstituted into rHDLs membrane discs.Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. | B | 6.97 | pKd | 106.44 | nM | Kd | K4DD drug target binding kinetics data |
ChEMBL | The A2A-StaR2 receptor has been purified from membranes in n-decyl-beta-D-maltoside as detergent. Ligands were prepared over a five-fold concentration series and injected in either a multi- or a single-cycle format depending on the kinetic parameters of the ligand. The actual concentrations as well as contact and dissociation times varied between the ligands depended on the kinetics and affinity of the interaction. The data were fitted to a 1:1 interaction model using the kinetics evaluation software from Biacore. A minimum of three measurements were recorded for each interaction. | B | 7.12 | pKd | 76.29 | nM | Kd | K4DD drug target binding kinetics data |
ChEMBL | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells | B | 6.1 | pKi | 788 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
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 | 6.2 | pKi | 630 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Affinity to A2 adenosine receptor was measured by the displacement of [3H]-CGS- 21680 in bovine brain striatal membrane | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (1994) 37: 2970-2975 [PMID:8071944] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2005) 48: 8253-8260 [PMID:16366607] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
ChEMBL | Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
ChEMBL | Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2001) 44: 316-327 [PMID:11462973] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membranes | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2A receptor in bovine striatal membranes. | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2000) 43: 3118-3124 [PMID:10956220] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins | B | 6.47 | pKi | 337 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
ChEMBL | Displacement of [3H]CGS 21680 from adenosine A2A receptor in bovine striatal membranes | B | 6.47 | pKi | 337 | nM | Ki | J Med Chem (2005) 48: 7932-7945 [PMID:16335918] |
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 | 6.54 | pKi | 291 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells after 120 mins | B | 6.58 | pKi | 260.3 | nM | Ki | Eur J Med Chem (2015) 89: 32-41 [PMID:25462223] |
ChEMBL | Displacement of [3H]NECA from human cloned adenosine A2A receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Displacement of [3H]NECA from cloned human adenosine A2A receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | J Med Chem (2007) 50: 4061-4074 [PMID:17665891] |
ChEMBL | Displacement of [3H]ZM241385 from human adenosine A2a receptor expressed in HeLa cells after 30 mins | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560] |
ChEMBL | Displacement of [125I]NECA from human cloned adenosine A2A receptor expressed in CHO cells | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446] |
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 | 6.65 | pKi | 226 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Binding affinity against adenosine A2 receptor in bovine striatal membranes using [3H]-CGS-21,680 as radioligand | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (2004) 47: 3019-3031 [PMID:15163184] |
ChEMBL | Displacement of [3H]DPCPX from human A2AAR expressed in human HeLa cell membrane assessed as inhibition constant incubated for 30 mins by competitive binding assay | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2023) 66: 890-912 [PMID:36517209] |
ChEMBL | Displacement of [3H]ZM241385 from human Adenosine A2A receptor expressed in HeLa cells after 30 mins | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2016) 59: 1967-1983 [PMID:26824742] |
ChEMBL | Displacement of [3H]4-(2-[7-amino-2-(2-furyl)[1,2,4]triazolo[2,3-a][1,3,5]triazin-5-ylamino]ethyl)phenol from human adenosine A2A receptor expressed in human Hela cell membranes after 30 mins | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2017) 60: 3372-3382 [PMID:28368607] |
ChEMBL | Displacement [3H]ZM241385 from adenosine A2A receptor in human HeLa cell membranes incubated for 30 mins by scintillation counting method | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2020) 63: 7721-7739 [PMID:32573250] |
ChEMBL | Displacement of [3H]ZM2421385 from adenosine A2A receptor expressed in human HeLa cell membranes incubated for 30 mins by scintillation counting method | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2021) 64: 458-480 [PMID:33372800] |
ChEMBL | Displacement of [3H]HZ241385 from human A2AAR expressed in HeLa cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis | B | 6.8 | pKi | 157 | nM | Ki | J Med Chem (2022) 65: 2091-2106 [PMID:35068155] |
ChEMBL | Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand | B | 6.84 | pKi | 144 | nM | Ki | J Med Chem (2004) 47: 3019-3031 [PMID:15163184] |
ChEMBL | Displacement of [3H]ZM-241385 from human cloned adenosine A2A receptor expressed in HEK293 cells by scintillation counting | B | 6.89 | pKi | 130 | nM | Ki | Eur J Med Chem (2009) 44: 2122-2127 [PMID:19036477] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.89 | pKi | 130 | nM | Ki | Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
ChEMBL | Displacement of [3H]ZM241385 from human adenosine A2A receptor expressed in HEK293 cell membrane | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
ChEMBL | Displacement of [3H]ZM-241385 from human adenosine A2A receptor expressed in HEK293 cells | B | 6.89 | pKi | 129 | nM | Ki | Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439] |
ChEMBL | Displacement of [3H]-ZM 241385 binding to human adenosine A2A receptor expressed in CHO cells | B | 6.89 | pKi | 129 | nM | Ki | J Med Chem (2005) 48: 2045-2053 [PMID:15771447] |
ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | B | 6.89 | pKi | 129 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Displacement of [3H]ZM241385 from human A2AR expressed in CHO cell membranes measured after 60 mins by scintillation counting method | B | 7.01 | pKi | 97 | nM | Ki | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
ChEMBL | Binding affinity towards human A2 receptor (hA2) was measured through displacement of [3H]-CGS-21,680 using yeast cell membranes | B | 7.15 | pKi | 70 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
GtoPdb | - | - | 7.2 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 7-10 [PMID:9933143]; Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]; ChemMedChem (2006) 1: 891-902 [PMID:16902942] |
ChEMBL | Binding affinity towards human Adenosine A2a receptor expressed in HEK293 cells using 6 nM [3H]CGS-21680 | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2005) 48: 6887-6896 [PMID:16250647] |
ChEMBL | Inhibitory activity against membranes from HEK293 cells stably expressing the human A2a receptor (hA2a) | B | 6.58 | pIC50 | 261 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
ChEMBL | Binding affinity against human A2 receptor (hA2) was measured through displacement of [3H]CGS-21680 using yeast cell membranes | B | 6.66 | pIC50 | 217 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 2413-2418 [PMID:10476879] |
ChEMBL | Antagonist activity at human A2AR expressed in CHO cells assessed as inhibition of CGS21680-stimulated cAMP production by alphascreen assay | F | 6.88 | pIC50 | 132 | nM | IC50 | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Inhibition of [3H]-CGS- 21680 binding to Adenosine A2A receptor in rat striatal homogenates. | B | 6.15 | pKi | 706 | nM | Ki | J Med Chem (1996) 39: 1164-1171 [PMID:8676354] |
ChEMBL | Displacement of [3H]NECA from adenosine A2A receptor in rat striatal membranes by radioligand competition assay | B | 6.26 | pKi | 545 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]-NECA from Adenosine A2A receptor in Sprague-Dawley rat striatal membranes | B | 6.28 | pKi | 530 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Binding affinity at rat Adenosine A2A receptor by [3H]-CGS- 21680 displacement. | B | 6.3 | pKi | 500 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
ChEMBL | Inhibition of [3H]MSX-2 binding to rat adenosine A2A receptor | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
ChEMBL | Inhibition of [3H]MSX-2 binding to adenosine A2a receptor | B | 6.33 | pKi | 470 | nM | Ki | J Med Chem (2005) 48: 2108-2114 [PMID:15771453] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A2A receptor in rat striatal membranes | B | 6.47 | pKi | 340 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptors of rat striatal membrane | B | 6.47 | pKi | 340 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
ChEMBL | Displacement of [3H]-NECA from Adenosine A2A receptor in rat striatal membranes | B | 6.47 | pKi | 340 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]-NECA from Adenosine A2A receptor in Wistar rat striatal membranes | B | 6.47 | pKi | 340 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
GtoPdb | - | - | 6.8 | pKi | 157 | nM | Ki |
J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Eur J Pharm Sci (2000) 10: 259-65 [PMID:10838015] |
ChEMBL | Displacement of [3H]MSX2 from rat adenosine A2A receptor | B | 6.8 | pKi | 157 | nM | Ki | Eur J Med Chem (2008) 43: 614-620 [PMID:17602796] |
ChEMBL | Displacement of [3H]MSX-2 from adenosine A2A receptor in rat brain striatal membrane after 30 mins by scintillation counting | B | 6.8 | pKi | 157 | nM | Ki | Eur J Med Chem (2010) 45: 1739-1745 [PMID:20116907] |
ChEMBL | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatum membrane | B | 6.8 | pKi | 157 | nM | Ki | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Inhibitory activity against Adenosine A2a receptor using [3H]NECA in rat striatal membranes | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem Lett (1999) 9: 1979-1984 [PMID:10450966] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method | B | 5.14 | pKi | 7324 | nM | Ki | J Med Chem (2021) 64: 458-480 [PMID:33372800] |
ChEMBL | Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity | F | 6 | pKi | 1000 | nM | Ki | Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184] |
ChEMBL | Displacement [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes incubated for 60 mins by scintillation counting method | B | 7.14 | pKi | 73.24 | nM | Ki | J Med Chem (2020) 63: 7721-7739 [PMID:32573250] |
ChEMBL | Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane incubated for 30 mins by microbeta trilux scintillation counter analysis | B | 7.14 | pKi | 73.24 | nM | Ki | J Med Chem (2022) 65: 2091-2106 [PMID:35068155] |
ChEMBL | Displacement of [3H]DPCPX from human Adenosine A2B receptor expressed in HEK293 cells after 30 mins | B | 7.14 | pKi | 73.24 | nM | Ki | J Med Chem (2016) 59: 1967-1983 [PMID:26824742] |
ChEMBL | Displacement of [3H]DPCPX from human A2BAR expressed in HEK293 cell membrane assessed as inhibition constant incubated for 30 mins by competitive binding assay | B | 7.14 | pKi | 73.2 | nM | Ki | J Med Chem (2023) 66: 890-912 [PMID:36517209] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A2B receptor expressed in HEK293 cell membranes after 30 mins | B | 7.14 | pKi | 73.2 | nM | Ki | J Med Chem (2017) 60: 3372-3382 [PMID:28368607] |
ChEMBL | Binding affinity at human Adenosine A2B receptor expressed in HEK293 cells, using [125I]ABOPX as radioligand | B | 7.2 | pKi | 63.8 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
ChEMBL | Antagonist activity against human adenosine A2B receptor | F | 7.25 | pKi | 56 | nM | Ki | Eur J Med Chem (2010) 45: 3459-3471 [PMID:20537438] |
ChEMBL | Displacement of [3H]ZM241385 from human adenosine A2b receptor expressed in HEK cells | B | 7.25 | pKi | 56 | nM | Ki | J Med Chem (2006) 49: 3682-3692 [PMID:16759111] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A2b receptor expressed in HEK293 cells after 30 mins | B | 7.29 | pKi | 51 | nM | Ki | Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560] |
ChEMBL | Inhibition of [3H]ZM-241,385 binding to adenosine A2b receptor | B | 7.29 | pKi | 51 | nM | Ki | J Med Chem (2005) 48: 2108-2114 [PMID:15771453] |
ChEMBL | Inhibition of [3H]ZM-241385 binding to human adenosine A2B receptor | B | 7.29 | pKi | 51 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
GtoPdb | - | - | 7.3 | pKi | - | - | - |
J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]; Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 2131-8 [PMID:12014951] |
ChEMBL | Antagonist activity at human A2BR expressed in CHO cells assessed as inhibition of NECA-stimulated cAMP production by alphascreen assay | F | 7.37 | pIC50 | 43 | nM | IC50 | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
ChEMBL | Displacement of PSB-12105 from recombinant human adenosine A2B receptor expressed in CHO cell membranes preincubated for 30 mins followed by PSB-12105 addition measured after 20 mins by flow cytometric method | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2018) 61: 4301-4316 [PMID:29681156] |
ChEMBL | Agonist activity at human A2B expressed in CHO cells assessed as stimulation of cAMP production by alphascreen assay | F | 6 | pEC50 | >1000 | nM | EC50 | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
GtoPdb | - | - | 7.06 | pKi | 86.2 | nM | Ki | J Pharmacol Exp Ther (2009) 329: 2-13 [PMID:19141710] |
A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
GtoPdb | - | - | 6.73 | pKi | 186 | nM | Ki |
J Med Chem (2002) 45: 2131-8 [PMID:12014951]; Eur J Pharmacol (2003) 475: 79-84 [PMID:12954362] |
ChEMBL | Inhibition of [125I]-APOBX binding to rat Adenosine A2B receptor expressed in HEK cells | B | 6.73 | pKi | 186 | nM | Ki | J Med Chem (2002) 45: 2131-2138 [PMID:12014951] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
ChEMBL | Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2001) 44: 316-327 [PMID:11462973] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
ChEMBL | Displacement of [3H]NECA from human adenosine A3 receptor expressed in CHO cells | B | 5.4 | pKi | 4000 | nM | Ki | Bioorg Med Chem (2009) 17: 2812-2822 [PMID:19282184] |
ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis | B | 5.4 | pKi | 3980 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Displacement of [3H]NECA from human Adenosine A3 receptor expressed in HeLa cells after 30 mins | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2016) 59: 1967-1983 [PMID:26824742] |
ChEMBL | Displacement of [3H]NECA from adenosine A3 receptor expressed in human HeLa cell membranes incubated for 180 mins by scintillation counting method | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2021) 64: 458-480 [PMID:33372800] |
ChEMBL | Displacement of [3H]NECA from human adenosine A3 receptor expressed in human Hela cell membranes after 180 mins | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2017) 60: 3372-3382 [PMID:28368607] |
ChEMBL | Displacement of [3H]NECA from human A3AR expressed in human HeLa cell membrane assessed as inhibition constant incubated for 180 mins by competitive binding assay | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2023) 66: 890-912 [PMID:36517209] |
ChEMBL | Displacement of [3H]NECA from human A3AR expressed in HeLa cell membrane incubated for 180 mins by microbeta trilux scintillation counter analysis | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2022) 65: 2091-2106 [PMID:35068155] |
ChEMBL | Displacement [3H]NECA from adenosine A3 receptor in human HeLa cell membranes incubated for 180 mins by scintillation counting method | B | 5.76 | pKi | 1722 | nM | Ki | J Med Chem (2020) 63: 7721-7739 [PMID:32573250] |
ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cells | B | 5.77 | pKi | 1700 | nM | Ki | Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439] |
ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cell membrane | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
ChEMBL | Displacement of [125I]-AB-MECA binding to human adenosine A3 receptor expressed in HEK 293 cells | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2005) 48: 2045-2053 [PMID:15771447] |
ChEMBL | Displacement of specific [125I]AB-MECA binding at human adenosine A3 receptor expressed in HEK 293 cells. | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (1998) 41: 3987-3993 [PMID:9767636] |
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 | 5.88 | pKi | 1320 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2009) 52: 2407-2419 [PMID:19301821] |
ChEMBL | Binding affinity against human adenosine A3 receptor expressed in CHO cells by [125I]AB-MECA displacement. | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2004) 47: 3580-3590 [PMID:15214785] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells. | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2000) 43: 3118-3124 [PMID:10956220] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2005) 48: 7932-7945 [PMID:16335918] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2006) 49: 3916-3925 [PMID:16789747] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | J Med Chem (2007) 50: 4061-4074 [PMID:17665891] |
ChEMBL | Displacement of [125I]AB-MECA from human cloned adenosine A3 receptor expressed in CHO cells | B | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem (2008) 16: 6086-6102 [PMID:18468446] |
ChEMBL | Displacement of [3H]NECA from human adenosine A3 receptor expressed in HeLa cells after 180 mins | B | 5.89 | pKi | 1300 | nM | Ki | Bioorg Med Chem (2010) 18: 7890-7899 [PMID:20937560] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
ChEMBL | Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins | B | 6 | pKi | >1000 | nM | Ki | Medchemcomm (2018) 9: 81-86 [PMID:30108902] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins | B | 6 | pKi | >1000 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 6 | pKi | >1000 | nM | Ki | J Med Chem (2005) 48: 8253-8260 [PMID:16366607] |
ChEMBL | Displacement of [125I]ABMECA from human A3R expressed in CHO cell membranes measured after 120 mins by scintillation counting method | B | 6.01 | pKi | 985 | nM | Ki | J Med Chem (2019) 62: 6894-6912 [PMID:31306001] |
ChEMBL | Inhibition of [3H]PSB-11 binding to human Adenosine A3 receptor | B | 6.1 | pKi | 795 | nM | Ki | J Med Chem (2002) 45: 1500-1510 [PMID:11906291] |
ChEMBL | Displacement of [125I]ABA from human adenosine A3 receptor expressed in CHO cells | B | 6.12 | pKi | 759 | nM | Ki | J Med Chem (1998) 41: 3987-3993 [PMID:9767636] |
ChEMBL | Inhibition of [3H]PSB-11 binding to adenosine A3 receptor | B | 6.12 | pKi | 759 | nM | Ki | J Med Chem (2005) 48: 2108-2114 [PMID:15771453] |
GtoPdb | - | - | 6.61 | pKi | 243 | nM | Ki |
Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Mol Pharmacol (2000) 57: 968-75 [PMID:10779381]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; J Med Chem (2002) 45: 1500-10 [PMID:11906291]; Mol Pharmacol (1997) 52: 846-60 [PMID:9351976] |
ChEMBL | Displacement of [3H]PSB-11 from human adenosine A3 receptor expressed in CHO cells | B | 6.61 | pKi | 243 | nM | Ki | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 6.7 | pKi | 200 | nM | Ki | J Med Chem (1998) 41: 3987-3993 [PMID:9767636] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Displacement of [125I]AB-MECA from membranes of CHO cells stably transfected with the rat adenosine A3 receptor cDNA | B | 5.28 | pKi | 5290 | nM | Ki | J Med Chem (1994) 37: 3373-3382 [PMID:7932565] |
GtoPdb | - | - | 7.6 | pKi | - | - | Ki |
J Biol Chem (1994) 269: 24692-8 [PMID:7929142]; ChemMedChem (2006) 1: 891-902 [PMID:16902942]; Mol Pharmacol (1997) 52: 846-60 [PMID:9351976] |
μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
ChEMBL | Binding affinity to mu opioid receptor | B | 4 | pKi | >100000 | nM | Ki | Bioorg Med Chem Lett (2009) 19: 6736-6739 [PMID:19836950] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.1 | pIC50 | 7943.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum 3D7 (drug-susceptible) proliferation in erythrocyte-based infection assay | F | 6.12 | pEC50 | 764 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
ChEMBL | NOVARTIS: Inhibition of Plasmodium falciparum W2 (drug-resistant) proliferation in erythrocyte-based infection assay | F | 6.46 | pEC50 | 346 | nM | EC50 | Proc Natl Acad Sci U S A (2008) 105: 9059-9064 [PMID:18579783] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]