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ChEMBL ligand: CHEMBL284969 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
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 | 6.19 | pKi | 650 | 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 | 9.52 | pKi | 0.3 | nM | Ki | 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]DPCPX from human adenosine A1 receptor expressed in CHO cells after 90 mins | B | 7.82 | pKi | 15.3 | nM | Ki | J Med Chem (2012) 55: 7719-7735 [PMID:22889387] |
ChEMBL | Binding affinity to human adenosine A1 receptor expressed in CHO cells | B | 7.82 | pKi | 15.1 | nM | Ki | J Med Chem (2008) 51: 5875-5879 [PMID:18729349] |
ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membranes | B | 7.83 | pKi | 14.9 | nM | Ki | J Med Chem (2014) 57: 7673-7686 [PMID:25181013] |
GtoPdb | - | - | 8.1 | pKi | - | - | - |
J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. | B | 8.19 | pKi | 6.4 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
ChEMBL | Displacement of [3H]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 8.92 | pKi | 1.2 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
ChEMBL | Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A1 receptor in CHO cells | B | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cells | B | 9.08 | pKi | 0.83 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1495-1498 [PMID:15006389] |
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 | 9.08 | pKi | 0.83 | nM | Ki | US-8470800-B2. Method of reducing intraocular pressure in humans (2013) |
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 | 9.08 | pKi | 0.83 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor expressed in CHO cells | B | 9.1 | pKi | 0.8 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Inhibition of cAMP formation in CHO cells expressing adenosine A1 receptor | B | 8.89 | pIC50 | 1.3 | nM | IC50 | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
ChEMBL | Agonist activity at human Adenosine A1 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis | F | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
ChEMBL | Agonist activity at human Adenosine A1 receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphai1 after 16 hrs by beta galactosidase reporter gene assay | B | 6.7 | pEC50 | 199.53 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
ChEMBL | Agonist activity at human A1AR expressed in HEK293T/17 cells assessed as inhibition of isoproterenol-induced cAMP accumulation incubated for 10 mins by luciferase reporter assay | F | 7.85 | pEC50 | 14 | nM | EC50 | J Med Chem (2012) 55: 6467-6477 [PMID:22738238] |
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 | 8.34 | pEC50 | 4.6 | nM | EC50 | J Med Chem (2012) 55: 6467-6477 [PMID:22738238] |
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 | 6.14 | pKi | 730 | 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 | 9.46 | pKi | 0.35 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in bovine cortical membrane | B | 9.47 | pKi | 0.34 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
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 | 9.68 | pKi | 0.21 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Agonist activity at mouse adenosine A1 receptor expressed in HEK293 cell membranes assessed as inhibition of forskolin-stimulated cAMP production preincubated for 30 mins prior to forskolin-treatment measured after 15 mins by ELISA | F | 7.75 | pEC50 | 17.7 | nM | EC50 | J Med Chem (2013) 56: 5949-5963 [PMID:23789857] |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Affinity towards adenosine A1 receptor from rat cortical membranes using [3H]DPCPX | B | 8.02 | pKi | 9.47 | nM | Ki | J Med Chem (2001) 44: 2966-2975 [PMID:11520205] |
ChEMBL | Binding affinity for adenosine A1 receptor was assayed by displacement of [3H]DPCPX from rat cortical membranes. | B | 8.13 | pKi | 7.43 | nM | Ki | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
ChEMBL | Tested for inhibition of adenosine A1 receptor binding to rat brain | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem Lett (1993) 3: 2661-2666 |
ChEMBL | Displacement of [3H]R-PIA from rat brain membrane Adenosine A1 receptor | B | 8.88 | pKi | 1.33 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. | B | 8.89 | pKi | 1.3 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
GtoPdb | - | - | 8.89 | pKi | 1.3 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Inhibition of [3H]- (R)-P1A binding to adenosine A1 receptor | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1991) 34: 3388-3390 [PMID:1766003] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes | B | 9.22 | pKi | 0.6 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Functional activity against adenosine A1 receptor from rat atria. | F | 5.09 | pEC50 | 8200 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Stimulation of [35S]GTP-gamma-S, binding to rat brain membranes by adenosine A1 receptor activation | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
ChEMBL | Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria | F | 8.09 | pEC50 | 8.2 | nM | EC50 | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
ChEMBL | Activity at Adenosine A1 receptor of rat atria | F | 8.09 | pEC50 | 8.2 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | Agonist activity at rat A1A adenosine receptor expressed in CHO-K1 cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | F | 8.78 | pEC50 | 1.65 | nM | EC50 | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
ChEMBL | Ex vivo inhibition of guinea pig ileum twitch via Adenosine A1 receptor. | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 403-406 [PMID:10714510] |
A2A receptor/Adenosine A2a receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL251] [GtoPdb: 19] [UniProtKB: P29274] | ||||||||
GtoPdb | - | - | 5.6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells | B | 5.64 | pKi | 2300 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
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 | 5.64 | pKi | 2270 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor in stably transfected CHO cells | B | 5.64 | pKi | 2270 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1495-1498 [PMID:15006389] |
ChEMBL | Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer | B | 5.64 | pKi | 2270 | nM | Ki | J Med Chem (2012) 55: 8075-8090 [PMID:22921089] |
ChEMBL | Displacement of [3H]R-PIA or [3H]CGS 21680 from human adenosine A2A receptor in CHO cells | B | 5.64 | pKi | 2270 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
ChEMBL | Displacement of [3H]-NECA from human A2A receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 5.69 | pKi | 2050 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
ChEMBL | Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand | B | 6.19 | pKi | 639 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
ChEMBL | Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. | B | 6.24 | pKi | 580 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL | In vitro inhibition of human neutrophil activation via Adenosine A2A receptor. | B | 7.77 | pKi | 17 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 403-406 [PMID:10714510] |
ChEMBL | Agonist activity at human Adenosine A2A receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay | B | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
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 | 6.01 | pKi | 988 | 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] | ||||||||
GtoPdb | - | - | 6.02 | pKi | 950 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes | B | 6.02 | pKi | 950 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. | B | 6.19 | pKi | 650 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum | B | 6.19 | pKi | 650 | nM | Ki | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | Binding affinity for adenosine A2A receptor was determined by displacement of [3H]-DPCPX from rat striatal membranes. | B | 6.19 | pKi | 640 | nM | Ki | J Med Chem (2000) 43: 250-260 [PMID:10649980] |
ChEMBL | Displacement of specific [3H]-CGS- 21680 binding to adenosine A2A receptor in rat striatal membranes | B | 6.22 | pKi | 605 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | Functional activity against adenosine A2a receptor from rat aorta. | F | 8 | pEC50 | >10 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
ChEMBL | Displacement of [3H]- ZM-241385 from human adenosine A2B receptor expressed in HEK cells | B | 4.69 | pKi | 20400 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
GtoPdb | - | - | 4.7 | pKi | - | - | - |
Mol Pharmacol (1999) 56: 705-13 [PMID:10496952]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Agonist activity at human recombinant adenosine A2B receptor expressed in CHO cells assessed as activation of adenylyl cyclase activity | F | 7.38 | pKi | 42 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Agonist activity at human Adenosine A2B receptor expressed in yeast cells coexpressed with chimeric GPA1/Galphas after 16 hrs by beta-galactosidase reporter gene assay | B | 4.14 | pEC50 | 72443.6 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in CHO cells | B | 4.73 | pKi | 18800 | nM | Ki | Bioorg Med Chem (2008) 16: 336-353 [PMID:17933541] |
ChEMBL | Binding affinity towards Adenosine A3 receptor (H95A mutant receptor) | B | 6.1 | pKi | 796 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor | B | 6.55 | pKi | 281 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
ChEMBL | Affinity towards Adenosine A3 receptor expressed in HEK 293 cells using [125I]AB-MECA radioligand | B | 6.69 | pKi | 204 | nM | Ki | J Med Chem (2001) 44: 2966-2975 [PMID:11520205] |
ChEMBL | Binding affinity towards human Adenosine A3 receptor wild type | B | 6.94 | pKi | 114 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Binding affinity towards Adenosine A3 receptor (W243 mutant receptor) | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Displacement of [3H]NECA from human adenosine A3 receptor in stably transfected HEK cells | B | 7.37 | pKi | 42.3 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 1495-1498 [PMID:15006389] |
GtoPdb | - | - | 7.4 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from human A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
ChEMBL | Bnding affinity in membrane of CHO cell stably expressing recombinant 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 as radioligand | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Affinity for human Adenosine A3 receptor expressed in CHO cell | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Binding affinity to human adenosine A3 receptor in CHO cells | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
ChEMBL | Binding affinity to Adenosine receptor A3 (unknown origin) | B | 7.42 | pKi | 38 | nM | Ki | J Med Chem (2016) 59: 810-840 [PMID:26390077] |
ChEMBL | Binding affinity in membrane of CHO cell stably expressing recombinant human Adenosine A3 receptor in the presence of GTPgammaS using [3H]8-ethyl-4-methyl-2-phenyl-(8R)-4,5,7,8-tetrahydro-1H-imidazo[2,1-i]-purin-5-one as radioligand | B | 7.47 | pKi | 34 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
ChEMBL | Displacement of [3H]-HEMADO from human A3 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 7.59 | pKi | 26 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
ChEMBL | Agonist activity at human Adenosine A3 receptor transfected in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production after 30 mins by multimode microplate reader analysis | F | 7.95 | pIC50 | 11.22 | nM | IC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
A3 receptor/Adenosine A3 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075269] [GtoPdb: 21] [UniProtKB: Q61618] | ||||||||
ChEMBL | Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from mouse A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
ChEMBL | Tested for the binding affinity of A3 receptor by displacing N6-[[125I]-4-amino-3-iodobenzyl]-adenosine-5''-N-methyluronamide from membranes of CHO cells transfected with rat A3-cDNA | B | 6.63 | pKi | 237 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Displacement of [125I]- AB-MECA from rat adenosine A3 receptor expressed in HEK cells | B | 6.63 | pKi | 237 | nM | Ki | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
ChEMBL | Binding affinity to rat adenosine A3 receptor in CHO cells | B | 6.63 | pKi | 237 | nM | Ki | J Med Chem (2005) 48: 8103-8107 [PMID:16366590] |
GtoPdb | - | - | 6.63 | pKi | 237 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
ChEMBL data shown on this page come from version 32:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]