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ChEMBL ligand: CHEMBL331372 (CGS-21680) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
A1 receptor/Adenosine A1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL226] [GtoPdb: 18] [UniProtKB: P30542] | ||||||||
ChEMBL | Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
GtoPdb | - | - | 6.4 | pKi | - | - | - |
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Displacement of [3H]R-PIA from human adenosine A1 receptor expressed in CHO cells | B | 6.42 | pKi | 380 | nM | Ki | ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664] |
ChEMBL | Displacement of [3H]N6-phenylisopropyladenosine from human A1 adenosine receptor expressed in CHO cell membranes after 60 mins | B | 6.42 | pKi | 380 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
ChEMBL | Inhibition of [3H]DPCPX binding to human adenosine A1 receptor expressed in CHO cells | B | 6.52 | pKi | 302 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
ChEMBL | Agonist activity at human adenosine receptor A1 | B | 6.54 | pKi | 290 | nM | Ki | Eur J Med Chem (2019) 179: 310-324 [PMID:31255928] |
ChEMBL | Binding affinity to human recombinant adenosine A1 receptor | B | 6.54 | pKi | 290 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor | B | 6.54 | pKi | 289 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Displacement of [3H]CCPA from human recombinant adenosine A1 receptor | B | 6.54 | pKi | 289 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
ChEMBL | Binding affinity for human adenosine A1 receptor | B | 6.54 | pKi | 289 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
ChEMBL | Agonist activity at human adenosine A1 receptor expressed in CHO cells by GTPPgammaS binding assay | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
ChEMBL | Binding against human adenosine A1 receptor | B | 5.19 | pEC50 | 6437 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
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 | 6.3 | pEC50 | 501.19 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
A1 receptor/Adenosine A1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL318] [GtoPdb: 18] [UniProtKB: P25099] | ||||||||
ChEMBL | Displacement of [3H]R-PIA from adenosine A1 receptor of Wistar rat forebrain | B | 5 | pKi | 9900 | nM | Ki | J Med Chem (1999) 42: 3463-3477 [PMID:10479279] |
ChEMBL | Binding affinity against adenosine A1 receptor using [3H]-CHA or [3H]PIA as radioligand | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1992) 35: 407-422 [PMID:1738138] |
ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor in rat cortical membrane | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
ChEMBL | Inhibition of [3H]PIA binding to rat cortical adenosine A1 receptor | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1992) 35: 4143-4149 [PMID:1433217] |
ChEMBL | Displacement of [3H]- DPCPX from adenosine A1 receptor on rat cortical membrane | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
ChEMBL | Tested for the binding affinity of A1 receptor by displacing the [3H]-PIA in rat brain membranes | B | 5.59 | pKi | 2600 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
GtoPdb | - | - | 5.74 | pKi | 1800 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortical membrane after 90 mins by liquid scintillation counting analysis | B | 5.74 | pKi | 1800 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Binding affinity towards adenosine A1 receptor in rat brain cortex | B | 5.74 | pKi | 1800 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
ChEMBL | Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex | B | 5.74 | pKi | 1800 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
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 | 5.85 | pKi | 1408 | nM | Ki | J Med Chem (1990) 33: 1919-1924 [PMID:2362269] |
ChEMBL | Binding affinity against adenosine A1 receptor in rat brain membranes using [3H]CHA as radioligand | B | 5.91 | pKi | 1232 | nM | Ki | J Med Chem (1992) 35: 241-252 [PMID:1732541] |
ChEMBL | Inhibition of [3H]CHA binding to adenosine A1 receptor from rat brain membranes | B | 5.91 | pKi | 1232 | nM | Ki | J Med Chem (1992) 35: 2253-2260 [PMID:1613750] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain membranes using [3H]cyclohexyladenosine as radioligand. | B | 5.94 | pKi | 1138 | nM | Ki | J Med Chem (1992) 35: 2881-2890 [PMID:1495019] |
ChEMBL | Binding affinity against adenosine A1 receptor from rat brain using [3H]CHA as a radioligand. | B | 6.24 | pKi | 569 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Displacement of [3H]CHA from Adenosine A1 receptor of rat brain | B | 6.24 | pKi | 569 | nM | Ki | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | Functional activity against adenosine A1 receptor from rat atria. | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Activity at Adenosine A1 receptor of rat atria | F | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
ChEMBL | [S]GTP gamma-S binding against adenosine A1 receptor in rat brain | B | 7 | pEC50 | >100 | nM | EC50 | Bioorg Med Chem Lett (1998) 8: 691-694 [PMID:9871584] |
Adenosine A1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2304404] [UniProtKB: P47745] | ||||||||
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 | 4.61 | pEC50 | 24547.09 | 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 | Saturation binding of wild type human Adenosine A2A receptor at pH 8.4 | B | 6.2 | pKd | 632 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding of human Adenosine A2A receptor H250N at pH 8.4 | B | 7 | pKd | 99 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding characteristics of wild type human Adenosine A2A receptor at pH 7.5 | B | 7.13 | pKd | 74 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding of wild type human Adenosine A2A receptor at pH 6.8 | B | 7.44 | pKd | 36.4 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Kd in saturation experiments using [3H]CGS-21680 at WT receptor in COS-7 cells | B | 7.44 | pKd | 36.4 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Kd in saturation experiments using [3H]CGS-21680 at V84L mutant receptor in COS-7 cells | B | 7.56 | pKd | 27.3 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding characteristics of wild type human Adenosine A2A receptor at pH 5.5 | B | 7.66 | pKd | 22 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding of human Adenosine A2A receptor H250N at pH 7.5 | B | 7.94 | pKd | 11.6 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Saturation binding of human Adenosine A2A receptor (H250N) at pH 6.8 | B | 8.12 | pKd | 7.6 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Kd in saturation experiments using [3H]CGS-21680 at H250N mutant receptor in COS-7 cells | B | 8.12 | pKd | 7.6 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Displacement of [3H]4-[2-[7-amino-2-(2-furyl)-1,2,4-triazolo[1,5-a][1,3,5]triazin-5-yl-amino]ethylphenol from wild type human adenosine A2a receptor expressed in HEK293 cells assessed as radioligand Kd compound preincubated for 30 mins | B | 8.36 | pKd | 4.36 | nM | Kd | ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664] |
ChEMBL | Saturation binding of mutant human Adenosine A2A receptor (H250N) at pH 5.5 | B | 8.37 | pKd | 4.3 | nM | Kd | J Med Chem (1997) 40: 2588-2595 [PMID:9258366] |
ChEMBL | Displacement of [3H]-ZM24135 from human adenosine A2A receptor expressed in HEK293 cells after 1 hr by scintillation counting | B | 6.3 | pKi | 503 | nM | Ki | Eur J Med Chem (2015) 106: 15-25 [PMID:26513641] |
ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from human adenosine A2a receptor expressed in HEK293 cells | B | 7.15 | pKi | 70 | nM | Ki | ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664] |
ChEMBL | Displacement of [3H]2-[p-(2-carboxyethyl)phenylethylamino]-5'-N-ethylcarboxamido-adenosine from human A2A adenosine receptor expressed in HEK293 cell membranes after 60 mins | B | 7.15 | pKi | 70 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
ChEMBL | Inhibition of [3H]ZM-241385 binding to human adenosine A2A receptor expressed in HeLa cells | B | 7.3 | pKi | 50 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells by scintillation counting | B | 7.34 | pKi | 46.2 | nM | Ki | Bioorg Med Chem (2009) 17: 4280-4284 [PMID:19481943] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells | B | 7.34 | pKi | 46.2 | nM | Ki | Bioorg Med Chem (2008) 16: 3825-3830 [PMID:18262425] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293T cells | B | 7.34 | pKi | 46.2 | nM | Ki | Bioorg Med Chem (2007) 15: 3235-3240 [PMID:17350268] |
ChEMBL | Binding affinity for human adenosine A2A receptor | B | 7.57 | pKi | 27.1 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
ChEMBL | Agonist activity at human adenosine receptor A2A | B | 7.57 | pKi | 27 | nM | Ki | Eur J Med Chem (2019) 179: 310-324 [PMID:31255928] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor | B | 7.57 | pKi | 27 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK cells | B | 7.57 | pKi | 27 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Binding affinity to human recombinant adenosine receptor A2a | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [3H]CGS21680 from human recombinant adenosine 2A receptor after 60 mins by gamma counting analysis | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2016) 59: 788-809 [PMID:26356532] |
ChEMBL | Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in Sf21 cells co-expressing GalphaS2, beta4, gamma2 | B | 7.68 | pKi | 21 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
ChEMBL | Displacement of [3H]CGS21680 from human adenosine A2A receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method | B | 7.9 | pKi | 12.48 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
GtoPdb | - | - | 8.1 | pKi | 7.94 | nM | Ki |
J Med Chem (2004) 47: 4041-53 [PMID:15267242]; Br J Pharmacol (1997) 121: 353-60 [PMID:9179373]; Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376]; J Biol Chem (1995) 270: 13987-97 [PMID:7775460]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Biochem Pharmacol (1999) 57: 65-75 [PMID:9920286]; J Pharmacol Exp Ther (2005) 315: 329-36 [PMID:16020631] |
ChEMBL | Agonist activity at adenosine A2A receptor in human neutrophils assessed as inhibition of fMLP-induced reactive oxygen species release by chemiluminescence assay | F | 7.72 | pIC50 | 19 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
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 | 4.7 | pEC50 | 19952.62 | nM | EC50 | J Med Chem (2016) 59: 947-964 [PMID:26756468] |
ChEMBL | Agonist activity at human adenosine A2A receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method | F | 7.73 | pEC50 | 18.47 | nM | EC50 | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
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 cAMP formation after 24 hrs | F | 8.67 | pEC50 | 2.12 | nM | EC50 | ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664] |
ChEMBL | Partial agonist activity at human A2A receptor expressed in HEK293 cell membranes assessed as intrinsic activity by measuring cell index change within 60 mins by Label-Free Impedance-Based Assay | F | 8.85 | pEC50 | 1.41 | nM | EC50 | J Med Chem (2021) 64: 3827-3842 [PMID:33764785] |
A2A receptor/Adenosine A2a receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL302] [GtoPdb: 19] [UniProtKB: P30543] | ||||||||
ChEMBL | Displacement of [3H]CGS21680 from A2A adenosine receptor expressed in rat striatal membranes after 30 mins by liquid scintillation counting | B | 7.57 | pKi | 27 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
GtoPdb | - | - | 7.72 | pKi | 19 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
ChEMBL | Binding affinity towards adenosine A2A receptor in rat brain striatum | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2001) 44: 531-539 [PMID:11170643] |
ChEMBL | Binding affinity to rat recombinant adenosine receptor A2a | B | 7.72 | pKi | 19 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatum | B | 7.74 | pKi | 18 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
ChEMBL | Displacement of [3H]CGS21680 from adenosine A2A receptor in rat brain striatal membrane after 60 mins by liquid scintillation counting analysis | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Tested for the binding affinity of A2a receptor by displacing the [3H]-CGS- 21680 in rat striatal membranes | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Ability to displace radioligand [3H]- CGS 21680 from adenosine A2A receptor on rat striatal membrane | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
ChEMBL | Displacement of [3H]NECA from Adenosine A2A receptor in rat striatal membrane | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
ChEMBL | Displacement of [3H]-CGS- 21680 from adenosine A2A receptor of rat striatal tissue | B | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1999) 42: 3463-3477 [PMID:10479279] |
ChEMBL | Displacement of [3H]-CGS- 21680 from Adenosine A2A receptor of rat striatum | B | 7.96 | pKi | 11 | 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 | 7.96 | pKi | 11 | nM | Ki | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Functional activity against adenosine A2a receptor from rat aorta. | F | 6.94 | pEC50 | 115 | nM | EC50 | J Med Chem (1995) 38: 1462-1472 [PMID:7739005] |
ChEMBL | Functional activity at Adenosine A2A receptor as vasorelaxation of rat aorta | F | 6.94 | pEC50 | 115 | nM | EC50 | J Med Chem (1995) 38: 3581-3585 [PMID:7658444] |
A2B receptor/Adenosine A2b receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL255] [GtoPdb: 20] [UniProtKB: P29275] | ||||||||
GtoPdb | - | - | 5 | pKi | - | - | - |
Mol Pharmacol (1999) 56: 705-13 [PMID:10496952]; Mol Pharmacol (2000) 58: 1349-56 [PMID:11093773]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
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 | pKi | >10000 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
ChEMBL | Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as effect on cAMP production by luciferase reporter gene assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
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 | 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 | 7.4 | pEC50 | 39.81 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
A2B receptor in Rat [GtoPdb: 20] [UniProtKB: P29276] | ||||||||
GtoPdb | - | - | 5 | pKi | >10000 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
A3 receptor/Adenosine A3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL256] [GtoPdb: 21] [UniProtKB: P0DMS8] | ||||||||
ChEMBL | Displacement of [125I]APNEA from human Adenosine A3 receptor expressed in HEK 293 cells | B | 6.23 | pKi | 584 | nM | Ki | J Med Chem (2002) 45: 420-429 [PMID:11784146] |
ChEMBL | Displacement of [125I]I-AB-MECA from human adenosine A3 receptor expressed in CHO cells | B | 6.24 | pKi | 570 | nM | Ki | ACS Med Chem Lett (2014) 5: 1043-1048 [PMID:25221664] |
ChEMBL | Displacement of [125I]N6-(4-amino-3-iodobenzyl)adenosine-5'-N-methyluronamide from human A3 adenosine receptor expressed in CHO cell membranes after 60 mins | B | 6.24 | pKi | 570 | nM | Ki | J Med Chem (2012) 55: 538-552 [PMID:22104008] |
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 | 6.42 | pKi | 384 | nM | Ki | J Med Chem (2015) 58: 3253-3267 [PMID:25780876] |
ChEMBL | Displacement of [125I]I-AB-MECA from human recombinant adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis | B | 6.94 | pKi | 114 | nM | Ki | Bioorg Med Chem (2013) 21: 436-447 [PMID:23245803] |
ChEMBL | Displacement of [125I]-AB-MECA from human recombinant adenosine A3 receptor | B | 6.94 | pKi | 114 | nM | Ki | ACS Med Chem Lett (2011) 2: 890-895 [PMID:24900277] |
ChEMBL | Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells | B | 7.17 | pKi | 68 | nM | Ki | J Med Chem (2004) 47: 4041-4053 [PMID:15267242] |
ChEMBL | Displacement of [125I]AB-MECA from membranes of HEK 293 cells expressing human Adenosine A3 receptor | B | 7.17 | pKi | 67.1 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
ChEMBL | Binding affinity to human recombinant adenosine A3 receptor | B | 7.17 | pKi | 67 | nM | Ki | J Med Chem (2014) 57: 3623-3650 [PMID:24164628] |
ChEMBL | Displacement of [125I]I-AB-MECA from recombinant human adenosine A3 receptor expressed in CHO cells after 60 mins by gamma counting analysis | B | 7.17 | pKi | 67 | nM | Ki | J Med Chem (2016) 59: 788-809 [PMID:26356532] |
GtoPdb | - | - | 7.2 | pKi | - | - | - |
Biochem Pharmacol (2004) 68: 1985-93 [PMID:15476669]; Naunyn Schmiedebergs Arch Pharmacol (1998) 357: 1-9 [PMID:9459566]; Mol Pharmacol (2000) 57: 968-75 [PMID:10779381]; J Med Chem (2004) 47: 4041-53 [PMID:15267242]; Nat Rev Drug Discov (2006) 5: 247-64 [PMID:16518376] |
ChEMBL | Agonist activity at human adenosine A3 receptor expressed in CHO cells by GTPPgammaS binding assay | B | 6.21 | pEC50 | 613 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 1219-1224 [PMID:20031406] |
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 | pEC50 | 10 | nM | EC50 | Medchemcomm (2014) 5: 192-196 |
A3 receptor/Adenosine A3 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3360] [GtoPdb: 21] [UniProtKB: P28647] | ||||||||
GtoPdb | - | - | 6.23 | pKi | 584 | nM | Ki | . A3 Adenosine Receptors from Cell Biology to Pharmacology and Therapeutics (2010) |
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 | 6.23 | pKi | 584 | nM | Ki | J Med Chem (1994) 37: 3614-3621 [PMID:7932588] |
ChEMBL | Binding affinity for rat adenosine A3 receptor | B | 6.23 | pKi | 584 | nM | Ki | J Med Chem (1999) 42: 1384-1392 [PMID:10212124] |
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]