NECA [Ligand Id: 377] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL464859 (5'-N-Ethylcarboxamidoadenosine, NECA) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Adenosine A1 receptor in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2114] [UniProtKB: P49892] | ||||||||
| ChEMBL | Displacement of [125I]ABA from adenosine A1 receptor of chick cerebellar membrane | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (1987) 30: 954-956 [PMID:3572985] |
| 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 in CHO cells | B | 6.24 | pKd | 575.44 | nM | Kd | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Dissociation constant against Adenosine A1 receptor | B | 8.07 | pKd | 8.6 | nM | Kd | J Med Chem (2005) 48: 2026-2035 [PMID:15771445] |
| ChEMBL | Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO-K1 cells by radioligand binding assay | B | 5.3 | pKi | 5011.87 | nM | Ki | J Med Chem (2021) 64: 6670-6695 [PMID:33724031] |
| 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 | 5.95 | pKi | 1122.02 | nM | Ki | Medchemcomm (2012) 3: 333-338 |
| ChEMBL | Affinity for Adenosine A1 receptor by displacement of [3H]DPCPX from human cerebral cortex | B | 6.7 | pKi | >200 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602] |
| ChEMBL | Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells | B | 7.74 | pKi | 18.3 | nM | Ki | J Med Chem (2007) 50: 374-380 [PMID:17228880] |
| ChEMBL | Displacement of [3H]CHA binding to Adenosine A1 receptor expressed in CHO cells | B | 7.74 | pKi | 18.2 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Displacement of [3H]CHA from human adenosine A1 receptor expressed in CHO cells | B | 7.74 | pKi | 18.2 | nM | Ki | Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 8253-8260 [PMID:16366607] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [3H]DPDPX from human adenosine A1 receptor expressed in CHO cells | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| ChEMBL | Displacement of [3H]-CCPA from CHO cells expressing human recombinant Adenosine A1 receptor | B | 7.85 | pKi | 14 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663] |
| ChEMBL | Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane after 180 mins | B | 7.85 | pKi | 14 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Binding affinity to human recombinant adenosine A1 receptor | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
| ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor | B | 7.87 | pKi | 13.6 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
| ChEMBL | Binding affinity for human adenosine A1 receptor | B | 7.87 | pKi | 13.6 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor | B | 7.87 | pKi | 13.6 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | In vitro binding affinity towards human adenosine A1 receptor by [3H]DPCPX displacement. | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
| ChEMBL | Binding affinity against human adenosine A1 receptor expressed in CHO cells using [3H]DPCPX; Range = 9.6-15 nM | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2004) 47: 3707-3709 [PMID:15239649] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 8.06 | pKi | 8.62 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
| ChEMBL | Displacement of [3H]DPCPX from human adenosine A1 receptor expressed in CHO cell membrane | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
| 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 | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2012) 55: 8075-8090 [PMID:22921089] |
| ChEMBL | Displacement of [3H]N6-phenylisopropyladenosine from recombinant human A1AR expressed in CHO cell membranes after 60 mins by liquid scintillation counting method | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Binding affinity to human A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of [3H]CPPA from human adenosine A1 receptor expressed in CHO cells | B | 8.17 | pKi | 6.8 | nM | Ki | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Biol Chem (1994) 269: 32077-84 [PMID:7798201]; J Biol Chem (1999) 274: 3617-21 [PMID:9920910]; J Biol Chem (1994) 269: 2373-6 [PMID:8300561]; Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005] |
| ChEMBL | Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Displacement of [3H]CCPA from human adenosine receptor A1 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method | B | 8.34 | pKi | 4.6 | nM | Ki | J Med Chem (2017) 60: 5772-5790 [PMID:28590753] |
| ChEMBL | Displacement of [3H]-CCPA from human A1 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 8.34 | pKi | 4.6 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
| 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 | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of 3[H]R-PIA from human A1 adenosine receptor expressed in CHO cells after 60 mins by Liquid scintillation analysis | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2012) 55: 4297-4308 [PMID:22486652] |
| ChEMBL | Displacement of [125I]ABA from human adenosine A1 receptor expressed in HEK cells | B | 8.98 | pKi | 1.04 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| ChEMBL | Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gi-mediated inhibition of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry | F | 9.1 | pIC50 | 0.79 | nM | IC50 | Medchemcomm (2012) 3: 333-338 |
| 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 | 9.68 | pIC50 | 0.21 | nM | IC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
| ChEMBL | Agonist activity at human adenosine A1 receptor expressed in CHO cells assessed as Gs-mediated activation of forskolin-stimulated SPAP secretion incubated for 10 mins prior to forskolin challenge measured after 5 hrs by spectrophotometry | F | 5.83 | pEC50 | 1479.11 | nM | EC50 | Medchemcomm (2012) 3: 333-338 |
| 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 | pEC50 | 1000 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
| ChEMBL | Binding against human adenosine A1 receptor | B | 7.23 | pEC50 | 59 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A1 receptor expressed in CHO cells | B | 7.5 | pEC50 | 31.62 | nM | EC50 | Med Chem Res (2004) 13: 88-98 |
| ChEMBL | Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
| ChEMBL | Agonist activity at human recombinant adenosine receptor-1 expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP production preincubated for 45 mins prior forskolin-induction measured after 15 mins by immunoassay | F | 7.99 | pEC50 | 10.2 | nM | EC50 | ACS Med Chem Lett (2011) 2: 626-631 [PMID:21858244] |
| ChEMBL | Agonist activity at human A1A adenosine receptor expressed in CHOKI cells assessed as induction of beta-arrestin2 recruitment after 60 mins | B | 8.3 | pEC50 | 5.03 | nM | EC50 | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay | F | 8.79 | pEC50 | 1.62 | nM | EC50 | J Med Chem (2016) 59: 11182-11194 [PMID:27958734] |
| ChEMBL | Agonist activity at human adenosine A1 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay | F | 8.9 | pEC50 | 1.26 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
| ChEMBL | Agonist activity at human A1AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay | F | 9.12 | pEC50 | 0.76 | nM | EC50 | J Med Chem (2018) 61: 2087-2103 [PMID:29446948] |
| ChEMBL | Irreversible agonist activity at human adenosine A1 receptor expressed in Flp-In-CHO cells assessed as stimulation of ERK1/2 phosphorylation incubated for 5 mins | B | 9.3 | pEC50 | 0.5 | nM | EC50 | J Med Chem (2016) 59: 11182-11194 [PMID:27958734] |
| ChEMBL | Agonist activity at adenosine A1 receptor assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation in CHO cells | F | 9.44 | pEC50 | 0.36 | nM | EC50 | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Activity at human adenosine A1 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells | F | 9.44 | pEC50 | 0.36 | nM | EC50 | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Agonist activity at human A1A adenosine receptor expressed in HEK cell membranes incubated for 60 mins by [35S]GTPgammaS binding assay | F | 9.92 | pEC50 | 0.12 | nM | EC50 | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| Adenosine A1 receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4975] [UniProtKB: P28190] | ||||||||
| ChEMBL | Inhibitory activity at Adenosine A1 receptor by inhibition of [3H]CHA binding to bovine brain cortical membranes. | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
| ChEMBL | Displacement of [3H]CHA from adenosine A1 receptors was determined in bovine cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2001) 44: 316-327 [PMID:11462973] |
| ChEMBL | Ability to displace the specific binding of [3H]CHA to adenosine A1 receptor from bovine brain cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2000) 43: 2814-2823 [PMID:10956189] |
| ChEMBL | Displacement of [3H]DPCPX binding to adenosine A1 receptors of bovine cortical membranes | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| A1 receptor/Adenosine A1 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3688] [GtoPdb: 18] [UniProtKB: Q60612] | ||||||||
| ChEMBL | Displacement of [3H]N6-R-phenylisopropyladenosine from mouse A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 9.35 | pKi | 0.45 | 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 | Adenosine A1 receptor binding was measured in adenosine deaminase (ADA) pretreated rat cortical membranes using [3H]cyclohexyladenosine in the presence of 2-chloroadenosine | B | 5.9 | pKi | 1257 | nM | Ki | J Med Chem (1990) 33: 1919-1924 [PMID:2362269] |
| ChEMBL | Binding affinity against low affinity component of adenosine A1 receptors from rat brain membranes using [3H]-DPCPX | B | 6.19 | pKi | 650 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
| ChEMBL | Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the presence of 1 mM of GTP | B | 6.28 | pKi | 530 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Displacement of [3H]N6-R-phenylisopropyladenosine from rat A1A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Ability to displace [3H]DPCPX from Adenosine A1 receptor in rat cortical membrane | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
| ChEMBL | Ability to displace radioligand [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane in the absence of GTP | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Binding affinity to adenosine A1 receptor in rat brain membranes by measuring displacement of specific [3H]PIA as radioligand. | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
| ChEMBL | Displacement of 3[H]R-PIA from rat A1 adenosine receptor expressed in CHO cells after 60 min by Liquid scintillation analysis | B | 7.2 | pKi | 63 | nM | Ki | J Med Chem (2012) 55: 4297-4308 [PMID:22486652] |
| ChEMBL | Binding affinity towards adenosine A1 receptor in rat brain cortex | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
| ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand | B | 7.88 | pKi | 13.3 | nM | Ki | J Med Chem (1992) 35: 241-252 [PMID:1732541] |
| ChEMBL | Binding affinity against high affinity component of adenosine A1 receptors from rat brain membranes using [3H]DPCPX | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
| ChEMBL | Affinity for adenosine A1 receptor assayed in a competition assay in rat brain using [3H]-CHA as radioligand | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
| ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
| ChEMBL | Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
| ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 7.98 | pKi | 10.4 | nM | Ki | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
| ChEMBL | Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (1992) 35: 4143-4149 [PMID:1433217] |
| ChEMBL | Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. | B | 8.08 | pKi | 8.3 | nM | Ki | J Med Chem (1992) 35: 2881-2890 [PMID:1495019] |
| ChEMBL | Binding affinity against adenosine A1 receptors from rat brain membranes using [3H]CCPA | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (1992) 35: 2363-2368 [PMID:1619615] |
| ChEMBL | Displacement of [3H]PIA from adenosine A1 receptor of rat brain membranes | B | 8.09 | pKi | 8.2 | nM | Ki | J Med Chem (1988) 31: 1179-1183 [PMID:3373486] |
| ChEMBL | Binding activity against Adenosine A1 receptor from rat brain membranes using [3H]8-cyclopentyl-1,3-dipropylxanthine (DPCPX) | B | 8.11 | pKi | 7.7 | nM | Ki | J Med Chem (2001) 44: 208-214 [PMID:11170630] |
| ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]R-PIA. | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (1998) 41: 3174-3185 [PMID:9703463] |
| ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
| ChEMBL | Inhibition of [3H]- DPCPX binding to Adenosine A1 receptor ofrat brain membranes | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (1998) 41: 2676-2678 [PMID:9667957] |
| ChEMBL | Binding affinity at adenosine A1 receptor from rat brain membranes by [3H]N6-cyclohexyladenosine displacement. | B | 8.2 | pKi | 6.3 | 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 | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (1988) 31: 271-273 [PMID:3336027] |
| ChEMBL | Binding affinity for A1-adenosine receptor by the displacement of specific [3H]-PIA binding in rat brain was determined | B | 8.2 | pKi | 6.3 | nM | Ki | J Med Chem (1994) 37: 636-646 [PMID:8126704] |
| ChEMBL | Displacement of [3H]CHA from adenosine A1 receptor of rat whole brain | B | 8.2 | pKi | 6.24 | nM | Ki | J Med Chem (1985) 28: 1383-1384 [PMID:2995663] |
| GtoPdb | - | - | 8.29 | pKi | 5.1 | nM | Ki | Curr Pharm Des (1996) 2: 501-530 |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis | B | 8.29 | pKi | 5.1 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
| ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex | B | 8.29 | pKi | 5.1 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | Inhibition of photolabeling of 24 kDa polypeptide in adenosine A1 receptor | B | 4.05 | pIC50 | 90000 | nM | IC50 | J Med Chem (1988) 31: 752-756 [PMID:3351851] |
| ChEMBL | Inhibition of photolabeling of 34 kDa polypeptide in adenosine A1 receptor | B | 4.28 | pIC50 | 52000 | nM | IC50 | J Med Chem (1988) 31: 752-756 [PMID:3351851] |
| ChEMBL | Binding affinity towards adenosine A1 receptor of rat brain membranes with 1 M NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 5.61 | pIC50 | 2460 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
| ChEMBL | Inhibition of Adenylate cyclase activity in rat fat cell membrane at adenosine A1 receptor | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1988) 31: 1179-1183 [PMID:3373486] |
| ChEMBL | Concentration required for 50% inhibition of [3H]-CHA binding on rat brain adenosine A1 receptor | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (1991) 34: 2570-2579 [PMID:1875349] |
| ChEMBL | Potency against rat brain adenosine A1 receptor | B | 7.99 | pIC50 | 10.2 | nM | IC50 | J Med Chem (1986) 29: 1683-1689 [PMID:3018244] |
| ChEMBL | Binding affinity towards the adenosine A1 receptor in cerebral cortices of Sprague-Dawley male rats using [3H]CHA as radioligand. | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (1990) 33: 2240-2254 [PMID:2374150] |
| ChEMBL | Binding affinity to adenosine A1 receptor of rat brain membranes without NaCl by inhibition of [125-I]-labeled aminobenzyl adenosine binding | B | 8.62 | pIC50 | 2.4 | nM | IC50 | J Med Chem (1988) 31: 745-751 [PMID:3351850] |
| ChEMBL | Functional activity against adenosine A1 receptor from rat atria. | F | 4.26 | pEC50 | 54800 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
| ChEMBL | [S]GTP gamma-S binding against adenosine A1 receptor in rat brain | B | 7.06 | pEC50 | 87.2 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
| ChEMBL | Activity at Adenosine A1 receptor of rat atria | F | 7.26 | pEC50 | 55 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
| ChEMBL | Adenosine A1 receptor mediated negative chronotropic activity in spontaneously beating rat atria | F | 7.26 | pEC50 | 54.8 | nM | EC50 | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
| ChEMBL | Negative chronotropic activity via A1 Adenosine receptor was tested in spontaneously beating rat atria | F | 7.26 | pEC50 | 54.8 | nM | EC50 | J Med Chem (1994) 37: 1720-1726 [PMID:8201607] |
| 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] |
| 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 | 7.2 | pEC50 | 63.1 | 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 | Inhibitory constant against human adenosine A2a receptor | B | 6.17 | pKi | 680 | nM | Ki | J Med Chem (2007) 50: 65-73 [PMID:17201410] |
| ChEMBL | Displacement of MRS5346 from C-terminal 10xHis and 1D4-tagged C-terminal-truncated human A2A adenosine receptor (1 to 316 residues) expressed in Pichia pastoris expression system after 1 hr by fluorescence polarization assay | B | 6.32 | pKi | 481 | nM | Ki | ACS Med Chem Lett (2017) 8: 660-665 [PMID:28626529] |
| ChEMBL | Inhibition of [3H]ZM-241385 binding to human adenosine A2A receptor expressed in HeLa cells | B | 6.89 | pKi | 130 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Displacement of [125I]ZM241385 from human adenosine A2A receptor in HEK cells | B | 6.91 | pKi | 124 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| ChEMBL | Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane | B | 6.96 | pKi | 110 | nM | Ki | Bioorg Med Chem Lett (2007) 17: 6779-6784 [PMID:17967536] |
| ChEMBL | Tested for binding affinity towards human adenosine A2A receptor using [3H]ZM-241385 as radioligand | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
| ChEMBL | Binding affinity against human adenosine A2A receptor expressed in HEK293 cells using [3H]ZM-241385 | B | 7.22 | pKi | 60 | nM | Ki | J Med Chem (2004) 47: 3707-3709 [PMID:15239649] |
| ChEMBL | Displacement of radiolabeled NECA from human adenosine A2A receptor | B | 7.28 | pKi | 52 | nM | Ki | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| 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 | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of 3[H]CGS21680 from human A2A adenosine receptor expressed in HEK293 cells after 60 mins by Liquid scintillation analysis | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2012) 55: 4297-4308 [PMID:22486652] |
| ChEMBL | Binding affinity against S277E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 | B | 7.53 | pKi | 29.2 | nM | Ki | J Med Chem (2003) 46: 4847-4859 [PMID:14584936] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in Sf21 cells co-expressing GalphaS2, beta4, gamma2 | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
| ChEMBL | Binding affinity against H278E human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 | B | 7.61 | pKi | 24.6 | nM | Ki | J Med Chem (2003) 46: 4847-4859 [PMID:14584936] |
| 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 | 7.67 | pKi | 21.6 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| ChEMBL | Binding affinity for HA-tagged mutant human Adenosine A2A receptor (V84L), using [3H]CGS-21680 as radioligand expressed in COS-7 cells | B | 7.67 | pKi | 21.5 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| ChEMBL | Binding affinity against WT human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 | B | 7.67 | pKi | 21.4 | nM | Ki | J Med Chem (2003) 46: 4847-4859 [PMID:14584936] |
| 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 | 7.67 | pKi | 21.2 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
| ChEMBL | Agonist activity at human adenosine receptor A2A | B | 7.7 | pKi | 20 | nM | Ki | Eur J Med Chem (2019) 179: 310-324 [PMID:31255928] |
| ChEMBL | [3H]NECA saturation binding in CHO cells expressing human recombinant A2A adenosine receptor | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663] |
| ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor | B | 7.7 | pKi | 20 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | Displacement of [3H]CGS21680 from human A2a adenosine receptor expressed in HEK293 cells after 60 min by Perkin Elmer Liquid Scintillation Analyzer | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2012) 55: 8075-8090 [PMID:22921089] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
| ChEMBL | Binding affinity to human recombinant adenosine receptor A2a | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting analysis | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Binding affinity against H278D human adenosine A2A receptor stably transfected in CHO cells using [3H]- ZM-241385 as radioligand. | B | 7.72 | pKi | 19.1 | nM | Ki | J Med Chem (2003) 46: 4847-4859 [PMID:14584936] |
| ChEMBL | Displacement of [3H]-NECA from human A2A receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
| ChEMBL | Inhibitory activity at Adenosine A2A receptor by inhibition of [3H]-CGS- 21680 binding to bovine striatal membranes. | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
| ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2a receptor of bovine striatal membrane | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2001) 44: 316-327 [PMID:11462973] |
| ChEMBL | Ability to displace the specific binding of [3H]-CGS- to adenosine A2A receptor form bovine brain striatal membranes | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2000) 43: 2814-2823 [PMID:10956189] |
| ChEMBL | Displacement of [3H]CGS-21680 binding to adenosine A2A receptors of bovine striatal membranes | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 7.8 | pKi | 16 | 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 | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| ChEMBL | Displacement of [3H]NECA from human A2A adenosine receptor expressed in CHO cell membrane | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cell membrane after 90 mins | B | 7.8 | pKi | 16 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Displacement of [3H]NECA from human adenosine receptor A2A expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2017) 60: 5772-5790 [PMID:28590753] |
| ChEMBL | Affinity for A2a receptor by displacement of [3H]-CGS- 21680 from human striatum | B | 7.82 | pKi | 15.1 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602] |
| ChEMBL | Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells | B | 7.9 | pKi | 12.5 | nM | Ki | J Med Chem (2007) 50: 374-380 [PMID:17228880] |
| ChEMBL | Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells | B | 7.91 | pKi | 12.4 | nM | Ki | Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548] |
| ChEMBL | Displacement of [3H]CGS-21680 binding to Adenosine A2 receptor expressed in CHO cells | B | 7.91 | pKi | 12.2 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | B | 7.92 | pKi | 12 | nM | Ki | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 8.08 | pKi | 8.41 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
| 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 | 8.28 | pKi | 5.24 | nM | Ki | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
| ChEMBL | Binding affinity to human A2A adenosine receptor expressed in HEK293 cell membranes | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of [3H]CGS-21680 from human adenosine A2A receptor expressed in CHO cells | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| ChEMBL | Binding affinity to A2A adenosine receptor | B | 8.66 | pKi | 2.2 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; J Med Chem (2004) 47: 4041-53 [PMID:15267242]; J Biol Chem (1995) 270: 13987-97 [PMID:7775460]; Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]; Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005] |
| ChEMBL | Binding affinity against Q89D human adenosine A2A receptor expressed in CHO cells using [3H]- ZM-241385 | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2003) 46: 4847-4859 [PMID:14584936] |
| ChEMBL | In vitro inhibition of human neutrophil activation via Adenosine A2A receptor. | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 403-406 [PMID:10714510] |
| ChEMBL | Inhibition of human adenosine A2A receptor | B | 7.17 | pIC50 | 67 | nM | IC50 | Bioorg Med Chem (2010) 18: 7675-7699 [PMID:20875743] |
| ChEMBL | Displacement of radiolabeled NECA from human adenosine A2A receptor | B | 7.19 | pIC50 | 64 | nM | IC50 | J Med Chem (2008) 51: 7094-7098 [PMID:18983139] |
| ChEMBL | Displacement of [3H]CGS 21680 from human recombinant adenosine receptor A2A expressed in HEK293 cells measured after 120 mins by scintillation counting method | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250] |
| ChEMBL | Displacement of [3H]CGS 21680 from human recombinant adenosine A2a receptor expressed in HEK293 cells | B | 7.43 | pIC50 | 37 | nM | IC50 | Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801] |
| ChEMBL | Inhibition of human adenosine A2A receptor | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2008) 51: 4150-4169 [PMID:18588282] |
| ChEMBL | Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay | F | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
| ChEMBL | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2013) 63: 85-94 [PMID:23466604] |
| ChEMBL | Binding affinity to human adenosine A2A receptor by radioligand displacement assay | B | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449] |
| 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 | 6.47 | pEC50 | 338.84 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A2a receptor expressed in CHO cells | F | 6.6 | pEC50 | 251.19 | nM | EC50 | Med Chem Res (2004) 13: 88-98 |
| ChEMBL | Potency against cAMP formation in CHO cells expressing recombinant human A2A receptor | F | 7.3 | pEC50 | 50 | nM | EC50 | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as stimulation of NECA-mediated cAMP accumulation preincubated for 15 mins followed by NECA addition measured after 15 mins by enzyme immunoassay | F | 7.35 | pEC50 | 45 | nM | EC50 | Medchemcomm (2015) 6: 1178-1185 |
| ChEMBL | G-protein activation in human Adenosine A2A receptor expressing CHO cells using cAMP assay | F | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
| ChEMBL | Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of cAMP production | F | 7.66 | pEC50 | 21.9 | nM | EC50 | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| ChEMBL | Agonist activity at human recombinant adenosine A2A receptor expressed in CHO cells assessed as [3H]cAMP accumulation after 15 mins by liquid scintillation counting | F | 7.74 | pEC50 | 18 | nM | EC50 | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
| ChEMBL | Agonist activity at human adenosine A2A receptor expressed in CHO-K1 cells by cAMP accumulation assay | F | 7.75 | pEC50 | 17.6 | nM | EC50 | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | Activity at human adenosine A2A receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells | F | 7.76 | pEC50 | 17.38 | nM | EC50 | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Agonist activity at human adenosine A2A receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay | F | 7.9 | pEC50 | 12.59 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
| ChEMBL | Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method | F | 7.9 | pEC50 | 12.58 | nM | EC50 | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
| ChEMBL | Agonist activity at human A2A-AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay | F | 8.48 | pEC50 | 3.31 | nM | EC50 | J Med Chem (2018) 61: 2087-2103 [PMID:29446948] |
| ChEMBL | Irreversible agonist activity at human adenosine A2A receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay | F | 8.6 | pEC50 | 2.51 | nM | EC50 | J Med Chem (2016) 59: 11182-11194 [PMID:27958734] |
| A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
| ChEMBL | Binding affinity at Adenosine A2A receptor in rat striatal membrane by [3H]ZM-241385 displacement. | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
| ChEMBL | Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
| ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatum | B | 7.82 | pKi | 15 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | Binding affinity towards adenosine A2A receptor in rat brain striatum | B | 7.91 | pKi | 12.4 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
| ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5-N-ethylcarboxamidoadenosine from rat A2A adenosine receptor expressed in HEK293 cell membranes at 10 uM after 60 mins by scintillation proximity assay relative to adenosine 5-N-ethyluronamide | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of 3[H]CGS21680 from rat A2A adenosine receptor expressed in HEK293 cells after 60 min by Liquid scintillation analysis | B | 7.92 | pKi | 12 | nM | Ki | J Med Chem (2012) 55: 4297-4308 [PMID:22486652] |
| ChEMBL | Binding affinity to adenosine A2A receptor in rat striatal membranes by measuring displacement of specific [3H]-CGS- 21680 as radioligand | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
| ChEMBL | Displacement of [3 H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from rat adenosine receptor A2A after 60 mins by liquid scintillation counting method | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| ChEMBL | Binding affinity against adenosine A2A receptor in rat striatal membranes using [3H]-CGS- 21680. | B | 7.99 | pKi | 10.3 | nM | Ki | J Med Chem (1998) 41: 3174-3185 [PMID:9703463] |
| ChEMBL | Inhibition of [3H]- CGS 21680 binding to Adenosine A2A receptor of rat brain membranes | B | 8 | pKi | 10 | nM | Ki | J Med Chem (1998) 41: 2676-2678 [PMID:9667957] |
| GtoPdb | - | - | 8.01 | pKi | 9.7 | nM | Ki | Curr Pharm Des (1996) 2: 501-530 |
| ChEMBL | Displacement of [3H]-CGS- 51680 from Adenosine A2A receptor of rat striatum. | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
| ChEMBL | Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
| ChEMBL | Binding affinity against adenosine A2a receptor from rat striatum using [3H]-CGS- 21680 as a radioligand. | B | 8.11 | pKi | 7.8 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
| ChEMBL | Binding affinity for Adenosine A2A receptor in rat brain membranes using [3H]CGS-21680 | B | 8.38 | pKi | 4.13 | nM | Ki | J Med Chem (2001) 44: 208-214 [PMID:11170630] |
| ChEMBL | Displacement of [3H]MSX-2 from rat adenosine A2A receptor in presence of 100 mM NaCl | B | 6.44 | pIC50 | 366 | nM | IC50 | Eur J Med Chem (2011) 46: 3590-3607 [PMID:21664729] |
| ChEMBL | Displacement of [3H]MSX-2 from rat adenosine A2A receptor | B | 8.15 | pIC50 | 7.05 | nM | IC50 | Eur J Med Chem (2011) 46: 3590-3607 [PMID:21664729] |
| ChEMBL | Vasorelaxation as Adenosine A2A receptor activity in rat aorta | F | 6.4 | pEC50 | 394 | nM | EC50 | J Med Chem (1996) 39: 4211-4217 [PMID:8863798] |
| ChEMBL | Functional activity against adenosine A2a receptor from rat aorta. | F | 6.4 | pEC50 | 394 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
| ChEMBL | Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta | F | 6.4 | pEC50 | 394 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
| ChEMBL | Efficacy against phenylephrine precontracted tissue relaxation in rat aorta | F | 7.47 | pEC50 | 34 | nM | EC50 | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
| ChEMBL | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells after 75 mins by liquid scintillation assay | B | 5.72 | pKi | 1890 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | Displacement of [3H]PSB-603 from human recombinant adenosine A2B receptor expressed in CHO cells | B | 5.72 | pKi | 1890 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
| ChEMBL | Displacement of [3H]PSB-603 from human adenosine receptor A2B in CHO cells after 75 mins by liquid scintillation method | B | 5.72 | pKi | 1890 | nM | Ki | J Med Chem (2017) 60: 5772-5790 [PMID:28590753] |
| ChEMBL | Displacement of [3H]MRS1754 from human adenosine A2B receptor expressed in CHO cell membrane | B | 5.9 | pKi | 1270 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
| ChEMBL | Displacement of [125I]ABOPX from human adenosine A2B receptor in HEK cells | B | 6.05 | pKi | 884 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| ChEMBL | Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells | B | 6.12 | pKi | 760 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Displacement of [3H]MRS-1754 from human recombinant adenosine A2B receptor expressed in HEK293 cells | B | 6.24 | pKi | 570 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
| ChEMBL | Displacement of [3H]MRE-2029F20 from human recombinant adenosine A2B receptor expressed in HEK293 cells | B | 6.58 | pKi | 262 | nM | Ki | J Med Chem (2009) 52: 3994-4006 [PMID:19569717] |
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
Mol Pharmacol (2000) 58: 1349-56 [PMID:11093773]; J Med Chem (2004) 47: 4041-53 [PMID:15267242]; Biochem Pharmacol (2001) 61: 657-63 [PMID:11266650]; Mol Pharmacol (1999) 56: 705-13 [PMID:10496952]; Biochem Pharmacol (2004) 68: 305-12 [PMID:15194002]; Biochem Pharmacol (2005) 70: 1601-12 [PMID:16219300]; Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of adenylate cyclase | F | 2.15 | pEC50 | -2.15 | - | logEC50 | J Med Chem (2008) 51: 2088-2099 [PMID:18321038] |
| 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 | 4.83 | pEC50 | 14791.08 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
| ChEMBL | Activity at human adenosine A2B receptor assessed as stimulation of [3H]cAMP accumulation in CHO cells | F | 5.44 | pEC50 | 3630.78 | nM | EC50 | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Effective concentration for cAMP production in CHO-KI cells stably transfected with human adenosine A2B receptor cDNA | F | 5.51 | pEC50 | 3100 | nM | EC50 | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Receptor stimulated adenylyl cyclase activity in CHO cells expressing human recombinant Adenosine A2B receptor | F | 5.62 | pEC50 | 2400 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663] |
| ChEMBL | Agonist activity at human adenosine receptor A2B expressed in CHO cell membranes assessed as forskolin-stimulated cAMP accumulation preincubated for 20 mins followed by forskolin addition measured after 10 mins by liquid scintillation counter method | F | 5.82 | pEC50 | 1510 | nM | EC50 | J Med Chem (2017) 60: 5772-5790 [PMID:28590753] |
| ChEMBL | Potency against cAMP formation in CHO cells expressing recombinant human A2B receptor | F | 6.36 | pEC50 | 440 | nM | EC50 | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Agonist activity at human recombinant adenosine receptor A2b by cAMP assay | F | 6.48 | pEC50 | 330 | nM | EC50 | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A2b receptor expressed in CHO cells | B | 6.5 | pEC50 | 316.23 | nM | EC50 | Med Chem Res (2004) 13: 88-98 |
| ChEMBL | Relative efficacy against phenylephrine precontracted tissue relaxation in Guinea pig aorta | F | 6.6 | pEC50 | 250 | nM | EC50 | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| ChEMBL | Activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP levels | F | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2007) 50: 374-380 [PMID:17228880] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production | F | 6.81 | pEC50 | 155 | nM | EC50 | Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548] |
| ChEMBL | Agonist activity at human A2B adenosine receptor by cell based assay | B | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production | F | 6.85 | pEC50 | 140 | nM | EC50 | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of cAMP production | F | 6.96 | pEC50 | 110 | nM | EC50 | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| ChEMBL | Agonistic activity against human adenosine A2B receptor expressed in CHO cells | F | 6.98 | pEC50 | 104 | nM | EC50 | J Med Chem (2004) 47: 3707-3709 [PMID:15239649] |
| ChEMBL | Agonist activity at recombinant human A2BAR expressed in CHO cells assessed as stimulation of cAMP formation preincubated for 30 mins in presence of rolipram and adenosine deaminase followed by compound addition and measured after 20 mins by alphascreen cAMP assay | F | 7.02 | pEC50 | 94.8 | nM | EC50 | ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064] |
| ChEMBL | Irreversible agonist activity at human adenosine A2B receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay | F | 7.37 | pEC50 | 42.66 | nM | EC50 | J Med Chem (2016) 59: 11182-11194 [PMID:27958734] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay | F | 7.42 | pEC50 | 38 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
| ChEMBL | Agonist activity at human A2BAR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 40 mins followed by forskolin addition measured after 30 mins by Alphascreen assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2018) 61: 2087-2103 [PMID:29446948] |
| ChEMBL | Agonist activity at human adenosine A2B receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
| A2B receptor in Mouse [GtoPdb: 20] [UniProtKB: Q60614] | ||||||||
| GtoPdb | - | - | 5.72 | pKi | 1900 | nM | Ki | Curr Pharm Des (1996) 2: 501-530 |
| A2B receptor/Adenosine A2b receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2592] [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
| ChEMBL | Activity against Adenosine A2B receptor as cAMP production in VA-13 cells | F | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1998) 41: 2676-2678 [PMID:9667957] |
| 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 HEK293T cells | B | 4.75 | pKi | 17700 | nM | Ki | Bioorg Med Chem (2008) 16: 3825-3830 [PMID:18262425] |
| ChEMBL | Binding affinity at Mutant (H272E) human adenosine A3 receptor expressed in COS-7 cells | B | 5.49 | pKi | 3200 | nM | Ki | J Med Chem (2001) 44: 4125-4136 [PMID:11708915] |
| ChEMBL | Binding affinity at wild-type Adenosine A3 receptor expressed in COS-7 cells | B | 6.77 | pKi | 169 | nM | Ki | J Med Chem (2001) 44: 4125-4136 [PMID:11708915] |
| 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 | 6.83 | pKi | 149 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Displacement of [3H]NECA from recombinant human adenosine A3 receptor expressed in CHO cell membranes measured after 180 mins | B | 7.12 | pKi | 75.5 | 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 | 7.14 | pKi | 73 | nM | Ki | Eur J Med Chem (2013) 69: 331-337 [PMID:24077183] |
| ChEMBL | Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX | B | 7.14 | pKi | 73 | 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 | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2008) 51: 1764-1770 [PMID:18269230] |
| ChEMBL | Displacement of [125I]AB-MECA from human A3 adenosine receptor expressed in CHO cell membrane | B | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2012) 55: 1490-1499 [PMID:22257095] |
| ChEMBL | Displacement of [125I]AB-MECA from adenosine A3 receptors in bovine cortical membranes | B | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2005) 48: 1550-1562 [PMID:15743197] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2005) 48: 8253-8260 [PMID:16366607] |
| ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 7.14 | pKi | 73 | nM | Ki | J Med Chem (2007) 50: 5676-5684 [PMID:17927167] |
| ChEMBL | Displacement of [3H]HMRS7799 from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay | B | 7.36 | pKi | 44.1 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| ChEMBL | Displacement of [3H]ABMECA from human adenosine A3 receptor expressed in CHO cells | B | 7.45 | pKi | 35.7 | nM | Ki | Bioorg Med Chem (2007) 15: 2514-2527 [PMID:17306548] |
| ChEMBL | Affinity for human Adenosine A3 receptor expressed in CHO cell | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| 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 | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Displacement of [125I]AB-MECA binding to Adenosine A3 receptor expressed in CHO cells | B | 7.46 | pKi | 34.8 | nM | Ki | J Med Chem (2004) 47: 5535-5540 [PMID:15481989] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 7.46 | pKi | 34.6 | nM | Ki | J Med Chem (2007) 50: 374-380 [PMID:17228880] |
| ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in CHO cell membranes incubated for 30 mins by scintillation counting method | B | 7.52 | pKi | 30 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells after 90 mins by gamma counting analysis | B | 7.6 | pKi | 25 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 26-36 [PMID:23200243] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells by scintillation counting | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2009) 17: 4280-4284 [PMID:19481943] |
| ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A3 receptor expressed in HEK293T cells | B | 7.7 | pKi | 20 | nM | Ki | Bioorg Med Chem (2007) 15: 3235-3240 [PMID:17350268] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in HEK293 cells by radioligand binding assay | B | 7.71 | pKi | 19.6 | nM | Ki | ACS Med Chem Lett (2022) 13: 623-631 [PMID:35450351] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2007) 50: 1810-1827 [PMID:17378544] |
| ChEMBL | Displacement of [125I]I-AB-MECA from human A3 adenosine receptor expressed in CHO cells after 60 mins gamma counter | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2012) 55: 4297-4308 [PMID:22486652] |
| ChEMBL | Displacement of [3H]-HEMADO from human A3 receptor stably expressed in CHO cell membranes by radioligand competitive binding assay | B | 7.89 | pKi | 12.8 | nM | Ki | Eur J Med Chem (2020) 201: 112478-112478 [PMID:32659606] |
| ChEMBL | Displacement of [3H]HEMADO from human adenosine receptor A3 expressed in CHO cell membranes after 3 hrs by microbeta scintillation counting method | B | 7.89 | pKi | 12.8 | nM | Ki | J Med Chem (2017) 60: 5772-5790 [PMID:28590753] |
| ChEMBL | Binding affinity against human adenosine A3 receptor expressed on HEK293 cells using [125I]I-AB-MECA | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2004) 47: 3707-3709 [PMID:15239649] |
| ChEMBL | Displacement of [3H]AB-MECA from human adenosine A3 receptor expressed in HEK293 cell membrane | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2008) 51: 4449-4455 [PMID:18637670] |
| ChEMBL | Binding affinity at human Adenosine A3 receptor expressed in HEK 293 cells by [125I]-AB MECA displacement. | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
| ChEMBL | Inhibition of [125 I]-IABMECA binding to human adenosine A3 receptor | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (2003) 46: 1492-1503 [PMID:12672250] |
| ChEMBL | Ability to displace radioligand [125I]AB-MECA from membrane of HEK 293 cells stably transfected with human adenosine A3 receptor cDNA | B | 7.97 | pKi | 10.6 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Displacement of [125I]ABA from human adenosine A3 receptor expressed in HEK cells | B | 7.99 | pKi | 10.2 | nM | Ki | Bioorg Med Chem Lett (2006) 16: 2416-2418 [PMID:16487705] |
| ChEMBL | Displacement of [125I]AB-MECA from human Adenosine A3 receptor expressed in CHO cells | B | 8.09 | pKi | 8.22 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3023-3026 [PMID:11714602] |
| ChEMBL | Binding affinity to human recombinant adenosine A3 receptor | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
| ChEMBL | Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 8.21 | pKi | 6.2 | nM | Ki | J Med Chem (2010) 53: 3954-3963 [PMID:20408530] |
| ChEMBL | Displacement of [3H]PSB-11 from human recombinant adenosine A3 receptor expressed in CHO cells | B | 8.21 | pKi | 6.2 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
| ChEMBL | [3H]NECA saturation binding in CHO cells expressing human Adenosine A3 receptor | B | 8.22 | pKi | 6 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 1931-1934 [PMID:11459663] |
| ChEMBL | Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells | B | 8.4 | pKi | 4 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
| GtoPdb | - | - | 8.4 | pKi | - | - | - |
Proc Natl Acad Sci USA (1993) 90: 10365-9 [PMID:8234299]; Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Mol Pharmacol (2000) 57: 968-75 [PMID:10779381]; J Med Chem (2004) 47: 4041-53 [PMID:15267242]; Neuropharmacology (1997) 36: 1157-65 [PMID:9364471]; Expert Opin Emerg Drugs (2003) 8: 537-76 [PMID:14662005] |
| ChEMBL | Binding affinity towards Adenosine A3 receptor (W243 A mutant receptor) | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Binding affinity towards human Adenosine A3 receptor wild type | B | 9.1 | pKi | 0.8 | nM | Ki | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Inhibition of forskolin-stimulated cAMP accumulation in chinese hamster ovary cell membranes expressing human adenosine A3 receptor | F | 4.18 | pIC50 | 65600 | nM | IC50 | J Med Chem (2004) 47: 2243-2255 [PMID:15084123] |
| ChEMBL | Agonist activity at wild type human A3 receptor M177'5.38A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 6.96 | pIC50 | 109.65 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor L90'3.32A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 7.81 | pIC50 | 15.49 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor M174'5.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor I253'6.58A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 8.92 | pIC50 | 1.2 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 8.94 | pIC50 | 1.15 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor L264'7.35A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.11 | pIC50 | 0.78 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor W185'5.46A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.21 | pIC50 | 0.62 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor I253'6.58E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.23 | pIC50 | 0.59 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| 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 | 9.31 | pIC50 | 0.49 | nM | IC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
| ChEMBL | Agonist activity at wild type human A3 receptor V169'5.30A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.31 | pIC50 | 0.49 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor I249'6.54A mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.53 | pIC50 | 0.3 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor V169'5.30A/W185'5.46A double mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.59 | pIC50 | 0.26 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay | F | 9.68 | pIC50 | 0.21 | nM | IC50 | J Med Chem (2019) 62: 8831-8846 [PMID:31502843] |
| ChEMBL | Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay | F | 4.98 | pEC50 | 10400 | nM | EC50 | J Med Chem (2006) 49: 2689-2702 [PMID:16640329] |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in CHO cells by [35S]GTPgammaS binding assay | F | 6.46 | pEC50 | 346.74 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2813-2819 [PMID:18424135] |
| ChEMBL | Stimulation of [35S]GTP-gamma-S, against human adenosine A3 receptor | F | 6.81 | pEC50 | 155 | nM | EC50 | J Med Chem (2000) 43: 2196-2203 [PMID:10841798] |
| ChEMBL | Effective concentration for stimulation of [35S]GTP-gamma-S, binding to human adenosine A3 receptor | F | 7.05 | pEC50 | 89 | nM | EC50 | J Med Chem (1999) 42: 1393-1400 [PMID:10212125] |
| ChEMBL | Effective concentration for stimulation of [35S]GTP-gamma-S, binding at human adenosine A3 receptor expressed in CHO cells | F | 7.07 | pEC50 | 84.8 | nM | EC50 | J Med Chem (2004) 47: 3580-3590 [PMID:15214785] |
| ChEMBL | Activity against human wild type adenosine A3 receptor expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay | F | 7.11 | pEC50 | 78 | nM | EC50 | J Med Chem (2006) 49: 2689-2702 [PMID:16640329] |
| ChEMBL | Agonist activity at Homo sapiens (human) adenosine A3 receptor expressed in CHO cells | B | 7.2 | pEC50 | 63.1 | nM | EC50 | Med Chem Res (2004) 13: 88-98 |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay | B | 7.2 | pEC50 | 63 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
| ChEMBL | Effect on forskolin-stimulated cyclic AMP production in intact chinese hamster ovary (CHO) cell expressing the human Adenosine A3 receptor | F | 7.59 | pEC50 | 26 | nM | EC50 | J Med Chem (2002) 45: 4471-4484 [PMID:12238926] |
| ChEMBL | Irreversible agonist activity at human adenosine A3 receptor expressed in Flp-In-CHO cells assessed as effect on forskolin-induced cAMP accumulation incubated for 30 mins by LANCE cAMP detection assay | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2016) 59: 11182-11194 [PMID:27958734] |
| ChEMBL | Agonist activity at human A3AR expressed in FlpIn-CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation preincubated for 10 mins followed by forskolin addition measured after 30 mins by Alphascreen assay | F | 7.85 | pEC50 | 14.13 | nM | EC50 | J Med Chem (2018) 61: 2087-2103 [PMID:29446948] |
| ChEMBL | Activity at human adenosine A3 receptor assessed as inhibition of forskolin-stimulated cAMP accumulation in CHO cells | F | 8.34 | pEC50 | 4.57 | nM | EC50 | J Med Chem (2007) 50: 782-793 [PMID:17249651] |
| ChEMBL | Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as inhibition of forskolin-induced cAMP accumulation after 30 mins by fluorescence assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
| 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 | 7.85 | pKi | 14.1 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Partial agonist activity at recombinant mouse A3AR expressed in HEK293 cell membranes assessed as stimulation of [35S]GTPgammaS binding measured after 2 hrs in presence of A2BAR blocker PSB-603 by liquid scintillation counting analysis | F | 6.73 | pEC50 | 188 | nM | EC50 | J Med Chem (2020) 63: 4334-4348 [PMID:32271569] |
| A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
| ChEMBL | Binding affinity for adenosine A3 receptor in CHO cell membranes using [125I]IB-MECA | B | 6.39 | pKi | 412 | nM | Ki | J Med Chem (2001) 44: 208-214 [PMID:11170630] |
| GtoPdb | - | - | 6.9 | pKi | - | - | - |
J Biol Chem (1994) 269: 24692-8 [PMID:7929142]; Curr Pharm Des (1996) 2: 501-530 |
| ChEMBL | Binding affinity against rat adenosine A3 receptor expressed in CHO cells using [125I]-. | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (1998) 41: 3174-3185 [PMID:9703463] |
| ChEMBL | Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5-N-methyluronamide from rat A3A adenosine receptor expressed in CHO cell membranes after 60 mins by scintillation proximity assay | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (2019) 62: 1502-1522 [PMID:30605331] |
| ChEMBL | Binding affinity determined by displacement of specific binding of [125I]N-(4-amino-3-iodophenethyl)-adenosine in membranes of CHO cells stably transfected with the rat adenosine A3 receptor | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (1995) 38: 1174-1188 [PMID:7707320] |
| ChEMBL | Binding affinity for rat adenosine A3 receptor | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
| ChEMBL | Binding affinity for recombinant rat A3-adenosine receptor by the displacement of specific [125I]APNEA or [125I]-N6-(4-amino-3-iodobenzyl)-adenosine-5'-N-methyluronamide | B | 6.95 | pKi | 113 | nM | Ki | J Med Chem (1994) 37: 636-646 [PMID:8126704] |
| ChEMBL | Inhibition of [125I]AB-MECA (0.15 nM) binding to Adenosine A3 receptor of RBL-2H3 cell membranes | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (1998) 41: 2676-2678 [PMID:9667957] |
| ChEMBL | Inhibitory activity against Adenosine A3 receptor by inhibiting specific [3H](R)-PIA binding to rat testis membranes | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (1998) 41: 1708-1715 [PMID:9572897] |
| ChEMBL | Ability to displace the specific binding of [3H](R)-PIA to adenosine A3 receptor from rat testis membranes | B | 7.31 | pKi | 49 | nM | Ki | J Med Chem (2000) 43: 2814-2823 [PMID:10956189] |
| heat shock protein 90 beta family member 1/Endoplasmin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075323] [GtoPdb: 2904] [UniProtKB: P14625] | ||||||||
| ChEMBL | Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay | B | 6.28 | pKd | 530 | nM | Kd | ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064] |
| ChEMBL | Displacement of FITC-geldanamycin from GRP94 (unknown origin) after 24 hrs by fluorescence polarization assay | B | 6.96 | pKi | 110 | nM | Ki | ACS Med Chem Lett (2021) 12: 373-379 [PMID:33738064] |
| Endoplasmin in Pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3425397] [UniProtKB: Q29092] | ||||||||
| ChEMBL | Binding affinity to porcine pancreas rough microsomal GRP94 after 1 hr | B | 6.7 | pKd | 200 | nM | Kd | J Med Chem (2015) 58: 3922-3943 [PMID:25901531] |
| ChEMBL | Displacement of [3H]NECA from GRP94 in porcine pancreas rough microsomes by liquid scintillation spectrometry | B | 6.7 | pKd | 200 | nM | Kd | J Med Chem (2018) 61: 9513-9533 [PMID:30351001] |
| oxoglutarate receptor/G protein-coupled receptor 80 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2325] [GtoPdb: 162] [UniProtKB: Q6Y1R5] | ||||||||
| ChEMBL | Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes | B | 7.43 | pKi | 37 | nM | Ki | J Med Chem (2001) 44: 208-214 [PMID:11170630] |
| ChEMBL | Binding activity of P3 purinoceptor-like protein (P3LP) using radioligand 40 nM [3H]NECA from rat brain membranes | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2001) 44: 208-214 [PMID:11170630] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5-HT2A receptor expressed in HEK-T cell membranes incubated for 90 mins under dark condition by microbeta scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
| Transmembrane domain-containing protein TMIGD3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3712907] [UniProtKB: P0DMS9] | ||||||||
| ChEMBL | Displacement of [125l]N 6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from recombinant human A3AR expressed in CHO cell membranes after 60 mins by gamma counting method | B | 7.8 | pKi | 16 | nM | Ki | J Med Chem (2016) 59: 11006-11026 [PMID:27933810] |
ChEMBL data shown on this page come from version 33:
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]
