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ChEMBL ligand: CHEMBL68738 (CCPA, Cyclopentyladenosine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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23S rRNA methylase leader peptide in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5291611] [UniProtKB: P10739] | ||||||||
ChEMBL | Inhibition of Escherichia coli ErmC methyltransferase | B | 4.2 | pIC50 | 63000 | nM | IC50 | RSC Med Chem (2023) 14: 624-643 [PMID:37122541] |
A1 adenosine receptor in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075029] [UniProtKB: Q4VQ11] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in pig striatum membrane | B | 6.09 | pKi | 810 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in pig cortical membrane | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Agonist activity at adenosine A1 receptor in pig cortical membrane assessed as stimulation of GTPgammaS binding | F | 8.1 | pEC50 | 7.9 | nM | EC50 | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Displacement of [3H]CPX from adenosine A1 receptor in DDT1MF-2 cells | B | 7.67 | pKi | 21.5 | nM | Ki | Bioorg Med Chem (2008) 16: 1861-1873 [PMID:18042389] |
ChEMBL | Displacement of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells | B | 8 | pKi | 10 | 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 | pKi | 10 | 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 | pKi | 10 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
ChEMBL | Binding affinity to adenosine A1 receptor (unknown origin) | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (2016) 59: 788-809 [PMID:26356532] |
ChEMBL | Displacement of [3H]N6-R-phenylisopropyladenosine from human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 8.64 | pKi | 2.3 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Displacement of [3H]DPCPX from recombinant human A1 receptor expressed in CHO cell membranes | B | 8.64 | pKi | 2.3 | nM | Ki | Medchemcomm (2018) 9: 1920-1932 [PMID:30568760] |
ChEMBL | Radioligand Binding Assay: Membranes for radioligand binding experiments are prepared from fresh or frozen cells as described in Klotz et al., Naunyn-Schmiedeberg's Arch. Pharmacol, 357:1-9 (1998). The cell suspension is then homogenized in ice-cold hypotonic buffer (5 mM Tris/HCl, 2 mM EDTA, pH 7.4) and the homogenate is spun for 10 minutes (4° C.) at 1,000 g. The membranes are then sedimented from the supernatant for 30 minutes at 100,000 g and resuspended in 50 mM Tris/HCl buffer pH 7.4 (for A3 adenosine receptors: 50 mM Tris/HCl, 10 mM MgCl2, 1 mM EDTA, pH 8.25), frozen in liquid nitrogen at a protein concentration of 1-3 mg/mL and stored at −80° C. Dissociation constants of unlabeled compounds (Ki-values) are determined in competition experiments in 96-well microplates using the A1 selective agonist 2-chloro-N6-[3H]cyclopentyladenosine ([3H]CCPA, 1 nM) for the characterization of A1 receptor binding. Nonspecific binding is determined in the presence of 100 μM R-PM and 1 mM theophylline, respectively. | B | 8.64 | pKi | 2.3 | nM | Ki | US-8470800-B2. Method of reducing intraocular pressure in humans (2013) |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 8.65 | pKi | 2.25 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer | B | 8.74 | pKi | 1.8 | nM | Ki | J Med Chem (2012) 55: 8075-8090 [PMID:22921089] |
ChEMBL | Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A1 receptor in CHO cells | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
GtoPdb | - | - | 9.4 | pKi | - | - | - |
J Biol Chem (1994) 269: 32077-84 [PMID:7798201]; J Biol Chem (1999) 274: 3617-21 [PMID:9920910]; Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Br J Pharmacol (2006) 147: 533-41 [PMID:16444290]; Eur J Pharmacol (2005) 510: 1-8 [PMID:15740718]; Biochem Pharmacol (1998) 56: 1437-45 [PMID:9827575]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Agonist activity at adenosine A1 receptor assessed as inhibition of isoproterenol-stimulated cAMP accumulation in DDT1MF-2 cells | F | 8.57 | pIC50 | 2.7 | nM | IC50 | Bioorg Med Chem (2008) 16: 1861-1873 [PMID:18042389] |
ChEMBL | Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay | F | 8.2 | pEC50 | 6.3 | nM | EC50 | J Med Chem (2012) 55: 6467-6477 [PMID:22738238] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to human adenosine A1 receptor | F | 8.38 | pEC50 | 4.15 | nM | EC50 | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Compound was evaluated for the Adenosine A1 receptor agonist potency. | F | 9.72 | pEC50 | 0.19 | nM | EC50 | Bioorg Med Chem Lett (1996) 6: 811-814 |
Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from adenosine A1 receptor in bovine striatum membrane | B | 5.91 | pKi | 1220 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL | Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2000) 43: 2814-2823 [PMID:10956189] |
A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612] | ||||||||
ChEMBL | Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 9.66 | pKi | 0.22 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]DPCPX from Sprague-Dawley rat whole brain membrane A1AR in presence of GTP by radioligand binding assay | B | 4.53 | pKi | 29500 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127274-127274 [PMID:32631506] |
ChEMBL | Binding affinity for Adenosine A1 receptor in corpora striata of rats using [3H]NECA | B | 6.34 | pKi | 462 | nM | Ki | J Med Chem (1990) 33: 2240-2254 [PMID:2374150] |
ChEMBL | Binding affinity towards rat Adenosine A1 receptor using [3H]-DPCPX | B | 6.64 | pKi | 230 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 815-818 [PMID:11277527] |
ChEMBL | Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes in presence of 0.1 mM GTP | B | 7 | pKi | 99.21 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes in presence of GTP by radioligand competition assay | B | 7 | pKi | 99 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in presence of 0.1 mM GTP | B | 7.2 | pKi | 63.08 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat brain cortical membranes in presence of GTP | B | 7.45 | pKi | 35.2 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Affinity for the Adenosine A1 receptor in the presence of GTP (A1+GTP) by using [3H]-DPCPX as radioligand | B | 7.45 | pKi | 35.2 | nM | Ki | J Med Chem (1995) 38: 4000-4006 [PMID:7562934] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the presence of GTP. | B | 7.45 | pKi | 35.2 | nM | Ki | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the presence of GTP. | B | 7.45 | pKi | 35.2 | nM | Ki | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Displacement of [3H]DPCPX (with GTP) from Adenosine A1 receptor of rat cortical membrane | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (1996) 39: 1463-1471 [PMID:8691477] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat whole brain membranes | B | 7.82 | pKi | 15.3 | 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 | 7.82 | pKi | 15.3 | 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 after 1 hr by scintillation counting analysis | B | 7.98 | pKi | 10.4 | nM | Ki | Eur J Med Chem (2015) 104: 177-188 [PMID:26462195] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in Sprague-Dawley rat whole brain after 1 hr by scintillation counting | B | 8.07 | pKi | 8.48 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 734-738 [PMID:26776359] |
ChEMBL | Displacement of [3H]PD116948 from Long-Evans rat whole brain membrane A1AR incubated for 60 mins by liquid scintillation counting analysis | B | 8.1 | pKi | 7.9 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127274-127274 [PMID:32631506] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat whole brain membranes | B | 8.1 | pKi | 7.9 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor in rat brain membranes | B | 8.1 | pKi | 7.9 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Affinity towards adenosine A1 receptor from rat cortical membranes using [3H]DPCPX | B | 8.15 | pKi | 7.14 | nM | Ki | J Med Chem (2001) 44: 2966-2975 [PMID:11520205] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain membranes by radioligand competition assay | B | 8.17 | pKi | 6.8 | nM | Ki | Medchemcomm (2019) 10: 300-309 [PMID:30881617] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in rat brain cortical membranes in absence of GTP | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]DPCPX from rat cortical membranes Adenosine A1 receptor | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1999) 42: 1393-1400 [PMID:10212125] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the absence of GTP | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]DPCPX in rat cortical membranes in the absence of GTP | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Displacement of [3H]DPCPX (without GTP) from Adenosine A1 receptor of rat cortical membrane | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1996) 39: 1463-1471 [PMID:8691477] |
ChEMBL | Affinity for the Adenosine A1 receptor in the absence of GTP (A1-GTP) by using [3H]DPCPX as radioligand | B | 8.23 | pKi | 5.9 | nM | Ki | J Med Chem (1995) 38: 4000-4006 [PMID:7562934] |
ChEMBL | Binding affinity for Adenosine A1 receptor of rat cortical membrane by displacing [3H]DPCPX | B | 8.23 | pKi | 5.9 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2141-2144 [PMID:10999489] |
ChEMBL | Displacement of [3H]DPCPX from Sprague-Dawley rat whole brain membrane A1AR by scintillation counting analysis | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 127274-127274 [PMID:32631506] |
ChEMBL | Binding affinity for adenosine A1 receptor was assayed by displacement of [3H]DPCPX from rat cortical membranes. | B | 8.29 | pKi | 5.07 | nM | Ki | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
ChEMBL | Displacement of [3H]-DPCPX from Adenosine A1 receptor in Sprague-Dawley rat brain cortical membranes in absence of GTP | B | 8.35 | pKi | 4.43 | nM | Ki | Bioorg Med Chem (2015) 23: 6641-6649 [PMID:26392370] |
ChEMBL | Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand | B | 8.92 | pKi | 1.21 | nM | Ki | J Med Chem (1992) 35: 241-252 [PMID:1732541] |
ChEMBL | Tested for inhibition of adenosine A1 receptor binding to rat brain | B | 8.92 | pKi | 1.2 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2661-2666 |
ChEMBL | Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (1999) 42: 3463-3477 [PMID:10479279] |
ChEMBL | Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1988) 31: 1179-1183 [PMID:3373486] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex membrane | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
ChEMBL | Affinity for Adenosine A1 receptor determined by [3H]N6-cyclohexyladenosine binding to rat brain membranes | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (1991) 1: 481-486 |
ChEMBL | Binding affinity against Adenosine A1 receptor using [3H]CHA in rat brain membranes | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1989) 32: 8-11 [PMID:2909748] |
ChEMBL | Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1992) 35: 4143-4149 [PMID:1433217] |
ChEMBL | Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1988) 31: 1282-1285 [PMID:3385722] |
ChEMBL | Binding affinity towards adenosine A1 receptor on rat whole brain membrane using [3H]N6-cyclohexyladenosine | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1988) 31: 271-273 [PMID:3336027] |
ChEMBL | Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Binding affinity against Adenosine A1 receptor using N6-[3H]cyclohexyladenosine in rat brain membranes | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Inhibition of binding of [3H]N6-cyclohexyladenosine to adenosine A1 receptor of rat whole brain membranes. | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1989) 32: 1667-1673 [PMID:2754691] |
ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1985) 28: 1383-1384 [PMID:2995663] |
ChEMBL | Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand. | B | 9.23 | pKi | 0.59 | nM | Ki | J Med Chem (1990) 33: 2240-2254 [PMID:2374150] |
ChEMBL | Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor | B | 9.35 | pKi | 0.45 | nM | Ki | J Med Chem (1991) 34: 3388-3390 [PMID:1766003] |
ChEMBL | Inhibition of [3H]-CHA binding to rat brain membrane Adenosine A1 receptor | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (1990) 33: 3127-3130 [PMID:2258897] |
ChEMBL | Inhibition of [3H]CHA (N6-cyclohexyl adenosine) to rat brain membrane Adenosine A1 receptor | B | 9.52 | pKi | 0.3 | nM | Ki | J Med Chem (2002) 45: 1196-1202 [PMID:11881988] |
ChEMBL | Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (1988) 31: 752-756 [PMID:3351851] |
ChEMBL | Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor | B | 4.96 | pIC50 | 11000 | nM | IC50 | J Med Chem (1988) 31: 752-756 [PMID:3351851] |
ChEMBL | Binding affinity towards adenosine A1 receptor rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
ChEMBL | Evaluated for the binding affinity towards the Adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. | B | 6.19 | pIC50 | 640 | nM | IC50 | J Med Chem (1990) 33: 2240-2254 [PMID:2374150] |
ChEMBL | Displacement of [3H]DPCPX from rat brain cortical membrane A1AR in presence of 100 uM of GTP by scintillation counting analysis | B | 6.27 | pIC50 | 537.6 | nM | IC50 | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain cortical membrane in presence of 100 uM GTP | B | 6.81 | pIC50 | 154 | nM | IC50 | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Displacement of [3H]DPCPX from rat brain cortical membrane A1AR in absence of GTP by scintillation counting analysis | B | 7.19 | pIC50 | 64.7 | nM | IC50 | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (1988) 31: 1179-1183 [PMID:3373486] |
ChEMBL | Displacement of [3H]DPCPX from rat brain cortical membrane A1AR assessed as GTP shift | B | 8.08 | pIC50 | 8.3 | nM | IC50 | Eur J Med Chem (2020) 186: 111879-111879 [PMID:31780082] |
ChEMBL | Displacement of [3H]DPCPX from adenosine A1 receptor in rat brain cortical membrane in absence of 100 uM GTP | B | 8.15 | pIC50 | 7.09 | nM | IC50 | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
ChEMBL | Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor | B | 9 | pIC50 | 1 | nM | IC50 | J Med Chem (1991) 34: 2570-2579 [PMID:1875349] |
ChEMBL | Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
ChEMBL | Evaluated for binding affinity against Adenosine A1 receptor | B | 9.49 | pIC50 | 0.32 | nM | IC50 | J Med Chem (1992) 35: 629-635 [PMID:1542091] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to adenosine A1 receptor of rat cerebral cortical membrane | F | 7.69 | pEC50 | 20.3 | nM | EC50 | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Agonist activity at adenosine A1 receptor in rat cortical membrane by [35S]GTPgammaS binding assay | F | 7.77 | pEC50 | 16.9 | nM | EC50 | J Nat Prod (2002) 65: 1479-1485 [PMID:12398547] |
ChEMBL | Effective concentration for [35S]GTP-gamma-S, binding to adenosine A1 receptor in rat brain membranes | F | 7.84 | pEC50 | 14.3 | nM | EC50 | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Effective concentration for [35S]GTP-gamma-S, binding to adenosine A1 receptor in rat brain membranes | F | 7.84 | pEC50 | 14.3 | nM | EC50 | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to rat brain membranes by adenosine A1 receptor activation | F | 7.88 | pEC50 | 13.3 | nM | EC50 | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CPX in guinea pig DDT membrane; 19.5+/-12.0 | B | 7.71 | pKi | 19.5 | nM | Ki low | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]CCPA in guinea pig DDT membrane | B | 9.1 | pKi | 0.8 | nM | Ki high | Bioorg Med Chem Lett (2004) 14: 3793-3797 [PMID:15203164] |
ChEMBL | Inhibition of N6-[3H]cyclohexyladenosine binding to guinea pig forebrain membrane Adenosine A1 receptor | B | 9.49 | pKi | 0.32 | nM | Ki | J Med Chem (1992) 35: 924-930 [PMID:1548682] |
ChEMBL | Prolongation of the stimulus-QRS interval by 50% of the maximum response at the adenosine A1 receptor in langendorff guinea pig heart preparation | F | 7.9 | pEC50 | 12.59 | nM | EC50 | J Med Chem (1991) 34: 1334-1339 [PMID:2016707] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
ChEMBL | Displacement of [3H]ZM241385 from human adenosine A2A 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 [3H]ZM-241385 from human adenosine A2A receptor expressed in HEK293 cells | B | 5.78 | pKi | 1652 | nM | Ki | Bioorg Med Chem (2008) 16: 2741-2752 [PMID:18258439] |
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 | 6.09 | pKi | 814 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
GtoPdb | - | - | 6.1 | pKi | - | - | - |
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay | B | 6.1 | pKi | 794 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 6.1 | pKi | 794 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer | B | 6.1 | pKi | 794 | nM | Ki | J Med Chem (2012) 55: 8075-8090 [PMID:22921089] |
ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | B | 6.1 | pKi | 794 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
ChEMBL | Displacement of [3H]-ZM 241385 binding to human adenosine A2A receptor expressed in CHO cells | B | 6.1 | pKi | 790 | nM | Ki | J Med Chem (2005) 48: 2045-2053 [PMID:15771447] |
ChEMBL | Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A2A receptor in CHO cells | B | 6.34 | pKi | 462 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
ChEMBL | Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes | B | 6.41 | pKi | 390 | nM | Ki | J Med Chem (2000) 43: 2814-2823 [PMID:10956189] |
ChEMBL | Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. | B | 6.41 | pKi | 385 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
A2A receptor/Adenosine A2a receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2115] [GtoPdb: 19] [UniProtKB: Q60613] | ||||||||
ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from mouse A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins by scintillation proximity assay | B | 6.09 | pKi | 808 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes. | B | 5.47 | pKi | 3370 | nM | Ki | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
ChEMBL | Displacement of [3H]MSX2 from adenosine A2A receptor in rat brain striatum membrane | B | 5.61 | pKi | 2470 | nM | Ki | Bioorg Med Chem (2010) 18: 2195-2203 [PMID:20188574] |
GtoPdb | - | - | 6.02 | pKi | 950 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes | B | 6.07 | pKi | 857 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Binding affinity against Adenosine A2A receptor using [3H]-CGS- 21680 as the radioligand in rat striatal membranes | B | 6.24 | pKi | 580 | nM | Ki | J Med Chem (1998) 41: 102-108 [PMID:9438026] |
ChEMBL | Binding affinity for adenosine A2A receptor of rat striatal membrane by displacing [3H]-ZM 241385 | B | 6.24 | pKi | 580 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 2141-2144 [PMID:10999489] |
ChEMBL | Binding affinity against Adenosine A2A receptor by using [3H]CGS-21680 as radioligand |