isoprenaline [Ligand Id: 536] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL434 (A-21, Aleudrin, Aludrine, Asiprenol, Asmalar, Assiprenol, Bellasthman, Isonorin, Isoprenalina, Isoprenaline, Isopropydrin, Isoproterenol, Isoproterenol dl-form, Isorenin, Isupren, Neodrenal, Neo-epinine, Novodrin, NSC-33791, NSC-9975, Proternol, Respifral, Saventrine, Vapo-n-iso) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
| ChEMBL | DRUGMATRIX: Lipoxygenase 15-LO enzyme inhibition (substrate: Linoleic acid) | B | 5.75 | pIC50 | 1770 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Binding Affinity against human Beta-1 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand | B | 5.8 | pKi | 1584.89 | nM | Ki | J Med Chem (1999) 42: 2287-2294 [PMID:10377236] |
| ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.71 | pKi | 193 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 7 | pKi | - | - | - |
Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677]; Proc Natl Acad Sci USA (1988) 85: 9494-8 [PMID:2849109]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | DRUGMATRIX: Adrenergic beta1 radioligand binding (ligand: [125I] Cyanopindolol) | B | 6.48 | pIC50 | 333 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Agonist activity at beta1 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2022) 65: 5514-5527 [PMID:35360904] |
| ChEMBL | Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem (2009) 17: 3283-3294 [PMID:19362005] |
| ChEMBL | Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay | F | 7.92 | pEC50 | 12 | nM | EC50 | Eur J Med Chem (2009) 44: 2533-2543 [PMID:19232786] |
| ChEMBL | Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay | F | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation | F | 8.1 | pEC50 | 7.94 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| ChEMBL | Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation | F | 8.1 | pEC50 | 7.94 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| ChEMBL | Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Eur J Med Chem (2018) 152: 424-435 [PMID:29751236] |
| ChEMBL | Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay | F | 8.5 | pEC50 | 3.16 | nM | EC50 | Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952] |
| GtoPdb | - | - | 8.6 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation | F | 8.9 | pEC50 | 1.26 | nM | EC50 | Eur J Med Chem (2021) 224: 113697-113697 [PMID:34273662] |
| ChEMBL | Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2006) 49: 2758-2771 [PMID:16640337] |
| ChEMBL | Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells. | F | 9 | pEC50 | 1 | nM | EC50 | J Med Chem (2002) 45: 567-583 [PMID:11806709] |
| ChEMBL | Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay | F | 9.08 | pEC50 | 0.84 | nM | EC50 | J Med Chem (2009) 52: 3063-3072 [PMID:19366244] |
| ChEMBL | Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor | F | 10.08 | pEC50 | 0.08 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 251-254 [PMID:15603933] |
| ChEMBL | Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA | F | 10.08 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2008) 51: 1925-1944 [PMID:18307290] |
| ChEMBL | Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 10.08 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2008) 51: 4804-4822 [PMID:18651730] |
| ChEMBL | Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay | F | 10.08 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2008) 51: 4002-4020 [PMID:18553954] |
| ChEMBL | Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation | F | 10.08 | pEC50 | 0.08 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5037-5040 [PMID:18752946] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971] | ||||||||
| ChEMBL | Displacement of [3H]CGP12177 from mouse beta1 receptor expressed in HEK293 cells | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
| ChEMBL | Compound was evaluated for the inhibition of binding of [3H]dihydroalprenolol from beta-1 adrenergic receptor of rat cerebral cortical membranes | B | 6.17 | pKi | 670 | nM | Ki | J Med Chem (1991) 34: 1063-1068 [PMID:1672155] |
| ChEMBL | Tested for binding affinity against beta-1 adrenergic receptor in rat brain using [3H]-CGP- 26505 as radioligand | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (1993) 36: 3077-3086 [PMID:8230093] |
| ChEMBL | Compound was evaluated for beta adrenergic binding affinity towards Beta-1 adrenergic receptor of rat brain | B | 7.1 | pKi | 80 | nM | Ki | J Med Chem (1992) 35: 1009-1018 [PMID:1313109] |
| ChEMBL | Compound was evaluated for its binding affinity towards beta-1 adrenergic receptor in rat heart membrane by displacing [125I]- iodocyanopindolol | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (1992) 35: 3081-3084 [PMID:1354264] |
| ChEMBL | In vitro beta-adrenergic activity against beta-1 adrenergic receptor by the inhibition of insulin stimulated [14C]- glucose incorporation into glycogen in isolated rat soleus muscle | F | 8.28 | pIC50 | 5.3 | nM | IC50 | J Med Chem (1992) 35: 3081-3084 [PMID:1354264] |
| Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73] | ||||||||
| ChEMBL | Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria | F | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (1991) 34: 1063-1068 [PMID:1672155] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550] | ||||||||
| ChEMBL | Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes assessed as intrinsic Kd by liquid scintillation counting | B | 6.13 | pKd | 740 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| ChEMBL | Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM | B | 6.6 | pKd | 251.19 | nM | Kd | Bioorg Med Chem Lett (2013) 23: 5376-5381 [PMID:23954364] |
| ChEMBL | Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting | B | 6.89 | pKd | 130 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| ChEMBL | Binding affinity to human adrenergic beta2 receptor | B | 7.3 | pKd | 50 | nM | Kd | Eur J Med Chem (2009) 44: 2840-2846 [PMID:19168263] |
| ChEMBL | Binding Affinity against human beta-2 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand | B | 6.17 | pKi | 676.08 | nM | Ki | J Med Chem (1999) 42: 2287-2294 [PMID:10377236] |
| GtoPdb | - | - | 6.6 | pKi | - | - | - |
Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Br J Pharmacol (2002) 137: 400-8 [PMID:12237261] |
| ChEMBL | Displacement of [3H]-CGP-12177 from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis | B | 6.72 | pKi | 192 | nM | Ki | Bioorg Med Chem (2014) 22: 234-246 [PMID:24326276] |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.77 | pKi | 169 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | B | 7.34 | pKi | 46 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]-(R,R')-methoxyfenoterol from human beta2 adrenergic receptor expressed in HEK cells by liquid scintillation counting analysis | B | 8.61 | pKi | 2.44 | nM | Ki | Bioorg Med Chem (2014) 22: 234-246 [PMID:24326276] |
| ChEMBL | DRUGMATRIX: Adrenergic beta2 radioligand binding (ligand: [3H] CGP-12177) | B | 6.61 | pIC50 | 246 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ChEMBL | Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay | F | 6.83 | pEC50 | 147.91 | nM | EC50 | J Med Chem (2023) 66: 17118-17137 [PMID:38060818] |
| ChEMBL | Agonist activity at PK-tagged beta2 receptor (unknown origin) transfected in HEK293 cells after 90 mins by beta-arrestin assay | B | 6.92 | pEC50 | 120 | nM | EC50 | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol | F | 7.06 | pEC50 | 87 | nM | EC50 | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4027-4031 [PMID:21652207] |
| ChEMBL | Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| ChEMBL | Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| GtoPdb | - | - | 8.2 | pEC50 | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Br J Pharmacol (2002) 137: 400-8 [PMID:12237261] |
| ChEMBL | Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis | F | 8.23 | pEC50 | 5.95 | nM | EC50 | J Med Chem (2022) 65: 5514-5527 [PMID:35360904] |
| ChEMBL | Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 8.52 | pEC50 | 3 | nM | EC50 | Bioorg Med Chem (2009) 17: 3283-3294 [PMID:19362005] |
| ChEMBL | Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay | F | 8.52 | pEC50 | 3 | nM | EC50 | Eur J Med Chem (2009) 44: 2533-2543 [PMID:19232786] |
| ChEMBL | Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2008) 51: 4002-4020 [PMID:18553954] |
| ChEMBL | Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2009) 52: 3063-3072 [PMID:19366244] |
| ChEMBL | Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 251-254 [PMID:15603933] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 8.7 | pEC50 | 2 | nM | EC50 | J Med Chem (2008) 51: 4804-4822 [PMID:18651730] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay | F | 8.92 | pEC50 | 1.2 | nM | EC50 | J Nat Prod (2019) 82: 2986-2993 [PMID:31625751] |
| ChEMBL | Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay | F | 9.08 | pEC50 | 0.84 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 4679-4683 [PMID:19608416] |
| ChEMBL | Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay | F | 9.15 | pEC50 | 0.7 | nM | EC50 | J Nat Prod (2018) 81: 768-777 [PMID:29517238] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Eur J Med Chem (2018) 152: 424-435 [PMID:29751236] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952] |
| ChEMBL | Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation | F | 9.67 | pEC50 | 0.21 | nM | EC50 | Eur J Med Chem (2021) 224: 113697-113697 [PMID:34273662] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation | F | 9.7 | pEC50 | 0.2 | nM | EC50 | Bioorg Med Chem (2014) 22: 234-246 [PMID:24326276] |
| ChEMBL | Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production | F | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2006) 49: 2758-2771 [PMID:16640337] |
| ChEMBL | Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cells | F | 9.8 | pEC50 | 0.16 | nM | EC50 | J Med Chem (2002) 45: 567-583 [PMID:11806709] |
| Beta-2 adrenergic receptor in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2289] [UniProtKB: P54833] | ||||||||
| ChEMBL | Compound was evaluated for its binding affinity towards beta-2 adrenergic receptor in rat soleus membrane by displacing (-)-isoproterenol (50 uM) | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1992) 35: 3081-3084 [PMID:1354264] |
| ChEMBL | Agonistic activity for Beta-2 adrenergic receptor was assessed by it's inhibitory effect on spontaneous contractions in isolated rat uterus | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2003) 46: 105-112 [PMID:12502364] |
| ChEMBL | Agonistic activity towards beta-2 adrenoceptor. IC50, the mean concentration required to produce 50% inhibition of uterine contraction | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2001) 44: 1436-1445 [PMID:11311067] |
| Beta-2 adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3373] [UniProtKB: Q28044] | ||||||||
| ChEMBL | Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) | B | 6.48 | pKd | 330 | nM | Kd | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
| ChEMBL | Affinity for cow beta-2 adrenergic receptor by measuring displacement (-)-[3H]dihydroalprenolol (DHA) | B | 6.51 | pKd | 6.51 | - | -Log KD | J Med Chem (1985) 28: 1328-1334 [PMID:2993621] |
| ChEMBL | Tested for binding affinity against beta-2 adrenergic receptor in bovine lung using [3H]DHA as radioligand | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (1993) 36: 3077-3086 [PMID:8230093] |
| ChEMBL | Compound was evaluated for beta adrenergic binding affinity towards beta-2 receptor of bovine lung | B | 6.96 | pKi | 110 | nM | Ki | J Med Chem (1992) 35: 1009-1018 [PMID:1313109] |
| β2-adrenoceptor/Beta-2 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3754] [GtoPdb: 29] [UniProtKB: P10608] | ||||||||
| ChEMBL | Inhibition of spontaneous contractions in isolated rat uterus | F | 10 | pIC50 | 0.1 | nM | IC50 | J Med Chem (2003) 46: 105-112 [PMID:12502364] |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring at basal tone assessed as bronchorelaxation activity | B | 7.6 | pKd | 25.12 | nM | Kd | Bioorg Med Chem Lett (2015) 25: 820-825 [PMID:25592716] |
| ChEMBL | Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction | B | 7.75 | pKd | 17.78 | nM | Kd | Bioorg Med Chem Lett (2015) 25: 820-825 [PMID:25592716] |
| ChEMBL | Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea | F | 7.24 | pEC50 | 58 | nM | EC50 | J Med Chem (1991) 34: 1063-1068 [PMID:1672155] |
| ChEMBL | Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction | B | 7.5 | pEC50 | 31.64 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734] |
| ChEMBL | Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction | F | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1523-1526 [PMID:22297114] |
| ChEMBL | Agonist activity at guinea pig trachea beta2-adrenergic receptor assessed as relaxation of histamine-induced tracheal ring contraction | B | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 249-253 [PMID:24300734] |
| ChEMBL | Agonist activity at beta2-adrenoceptor in guinea pig trachea assessed as relaxation of histamine-induced precontracted tracheal rings | B | 7.54 | pEC50 | 28.84 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 1548-1552 [PMID:23375225] |
| ChEMBL | Agonist activity at beta2 adrenergic receptor in guinea pig tracheal smooth muscle assessed as inhibition of histamine-induced tracheal smooth muscle contraction by measuring spasmolysis preincubated for 15 mins in presence of beta adrenergic receptor antagonist propranolol followed by histamine addition | B | 8.1 | pEC50 | 7.9 | nM | EC50 | J Nat Prod (2019) 82: 2986-2993 [PMID:31625751] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| ChEMBL | Binding Affinity against human Beta-3 adrenergic receptor expressed in Chinese hamster ovary(CHO) cells was measured by using [125I]ICYP radioligand | B | 4.73 | pKi | 18620.87 | nM | Ki | J Med Chem (1999) 42: 2287-2294 [PMID:10377236] |
| GtoPdb | - | - | 6.2 | pKi | - | - | - |
Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677]; Annu Rev Pharmacol Toxicol (1997) 37: 421-50 [PMID:9131260]; Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421]; Br J Pharmacol (1997) 120: 165-76 [PMID:9117106]; Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619]; Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | Agonist efficacy for human Beta-3 adrenergic receptor expressed in chinese hamster ovary cells | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (1997) 7: 219-224 |
| ChEMBL | Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay | F | 7 | pEC50 | 100 | nM | EC50 | Eur J Med Chem (2009) 44: 2533-2543 [PMID:19232786] |
| ChEMBL | Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay | F | 7 | pEC50 | 100 | nM | EC50 | Bioorg Med Chem (2009) 17: 5510-5519 [PMID:19581100] |
| ChEMBL | Agonistic activity for Beta-3 adrenergic receptor as relaxing ability of isolated ferret detrusor basal tone | F | 7.06 | pEC50 | 87.1 | nM | EC50 | J Med Chem (2003) 46: 105-112 [PMID:12502364] |
| ChEMBL | Concentration required to effect a 50% relaxation of rat ferret detrusor basal tone | F | 7.06 | pEC50 | 87 | nM | EC50 | J Med Chem (2003) 46: 105-112 [PMID:12502364] |
| ChEMBL | Agonist activity at recombinant human beta3 adrenergic receptor expressed in CHO cells assessed as accumulation of cyclic AMP after 30 mins | B | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2017) 60: 3252-3265 [PMID:28355078] |
| ChEMBL | Agonist activity at human recombinant beta3-adrenergic receptor expressed in CHO cells assessed as increase of cAMP level after 30 mins | F | 7.07 | pEC50 | 86 | nM | EC50 | J Med Chem (2015) 58: 6048-6057 [PMID:26125514] |
| ChEMBL | Agonist activity at human beta3 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay | F | 7.27 | pEC50 | 53.7 | nM | EC50 | Eur J Med Chem (2018) 152: 424-435 [PMID:29751236] |
| GtoPdb | - | - | 7.4 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| ChEMBL | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| ChEMBL | Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.4 | pEC50 | 39.81 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| ChEMBL | Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins | F | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 7.92 | pEC50 | 12 | nM | EC50 | Bioorg Med Chem (2009) 17: 3283-3294 [PMID:19362005] |
| ChEMBL | Agonist activity at human adrenergic beta-3 receptor expressed in CHO cells assessed as cAMP levels by DELFIA method | F | 8.24 | pEC50 | 5.8 | nM | EC50 | Bioorg Med Chem (2008) 16: 2473-2488 [PMID:18083578] |
| ChEMBL | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as [3H]cAMP levels by radiolabeled ligand based assay | F | 8.41 | pEC50 | 3.9 | nM | EC50 | Bioorg Med Chem (2008) 16: 2473-2488 [PMID:18083578] |
| ChEMBL | Activity against human beta 3 adrenergic receptor (AR), expressed in CHO cells. | F | 8.5 | pEC50 | 3.16 | nM | EC50 | J Med Chem (2002) 45: 567-583 [PMID:11806709] |
| ChEMBL | Activity at human beta-3 adrenergic receptor expressed in CHO cells by stimulation of cAMP production | F | 8.5 | pEC50 | 3.16 | nM | EC50 | J Med Chem (2006) 49: 2758-2771 [PMID:16640337] |
| ChEMBL | Agonist activity at human recombinant adrenergic beta3 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay | F | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2009) 19: 4679-4683 [PMID:19608416] |
| ChEMBL | Agonist activity at human beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA | F | 9.01 | pEC50 | 0.97 | nM | EC50 | J Med Chem (2008) 51: 1925-1944 [PMID:18307290] |
| ChEMBL | Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay | F | 9.01 | pEC50 | 0.97 | nM | EC50 | J Med Chem (2008) 51: 4002-4020 [PMID:18553954] |
| ChEMBL | Agonist activity at human recombinant beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay | F | 9.01 | pEC50 | 0.97 | nM | EC50 | J Med Chem (2009) 52: 3063-3072 [PMID:19366244] |
| ChEMBL | Agonist activity at human cloned beta3 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation | F | 9.01 | pEC50 | 0.97 | nM | EC50 | J Med Chem (2008) 51: 4804-4822 [PMID:18651730] |
| ChEMBL | Agonist activity at human cloned adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation | F | 9.01 | pEC50 | 0.97 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 5037-5040 [PMID:18752946] |
| ChEMBL | Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-3 adrenergic receptor | F | 9.01 | pEC50 | 0.97 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 251-254 [PMID:15603933] |
| β3-adrenoceptor in Mouse [GtoPdb: 30] [UniProtKB: P25962] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - |
Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421]; Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4031] [GtoPdb: 30] [UniProtKB: P26255] | ||||||||
| GtoPdb | - | - | 5.3 | pKi | - | - | - | Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421] |
| ChEMBL | Agonistic activity towards beta-3 adrenoceptor. EC50, the mean concentration required to produce 50% relaxation of detrusor before the addition in the ferret detrusor | F | 7.06 | pEC50 | 87.1 | nM | EC50 | J Med Chem (2001) 44: 1436-1445 [PMID:11311067] |
| ChEMBL | In vitro beta adrenergic receptor activity against beta-3 adrenergic receptor in rat epididymal fat pads by stimulation of glycerol release from adipocytes. | F | 7.89 | pEC50 | 13 | nM | EC50 | J Med Chem (1992) 35: 3081-3084 [PMID:1354264] |
| D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] | ||||||||
| ChEMBL | Displacement of [3H]SCH23390 from human D1 receptor expressed in HEK293 cells | B | 4.3 | pKi | >50000 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D2L receptor expressed in CHO cells | B | 4.32 | pKi | 48000 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells | B | 4.92 | pKi | 12000 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D3 receptor expressed in CHO cells | B | 5.33 | pKi | 4700 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D4.4 receptor expressed in CHO cells | B | 5.54 | pKi | 2900 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| TAS2R1/Taste receptor type 2 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523475] [GtoPdb: 659] [UniProtKB: Q9NYW7] | ||||||||
| ChEMBL | Agonist activity at human TAS2R1 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R10/Taste receptor type 2 member 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559704] [GtoPdb: 666] [UniProtKB: Q9NYW0] | ||||||||
| ChEMBL | Agonist activity at human TAS2R10 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R13/Taste receptor type 2 member 13 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523471] [GtoPdb: 667] [UniProtKB: Q9NYV9] | ||||||||
| ChEMBL | Agonist activity at human TAS2R13 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R14/Taste receptor type 2 member 14 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309105] [GtoPdb: 668] [UniProtKB: Q9NYV8] | ||||||||
| ChEMBL | Agonist activity at human TAS2R14 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R16/Taste receptor type 2 member 16 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309106] [GtoPdb: 669] [UniProtKB: Q9NYV7] | ||||||||
| ChEMBL | Agonist activity at human TAS2R16 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R19/Taste receptor type 2 member 19 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523255] [GtoPdb: 670] [UniProtKB: P59542] | ||||||||
| ChEMBL | Agonist activity at human TAS2R48 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R20/Taste receptor type 2 member 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559705] [GtoPdb: 671] [UniProtKB: P59543] | ||||||||
| ChEMBL | Agonist activity at human TAS2R49 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R3/Taste receptor type 2 member 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523474] [GtoPdb: 660] [UniProtKB: Q9NYW6] | ||||||||
| ChEMBL | Agonist activity at human TAS2R3 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R30/Taste receptor type 2 member 30 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523254] [GtoPdb: 673] [UniProtKB: P59541] | ||||||||
| ChEMBL | Agonist activity at human TAS2R47 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R31/Taste receptor type 2 member 31 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034804] [GtoPdb: 674] [UniProtKB: P59538] | ||||||||
| ChEMBL | Agonist activity at human TAS2R44 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R38/Taste receptor type 2 member 38 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523248] [GtoPdb: 682] [UniProtKB: P59533] | ||||||||
| ChEMBL | Agonist activity at human TAS2R38 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R39/Taste receptor type 2 member 39 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523249] [GtoPdb: 675] [UniProtKB: P59534] | ||||||||
| ChEMBL | Agonist activity at human TAS2R39 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R4/Taste receptor type 2 member 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309107] [GtoPdb: 661] [UniProtKB: Q9NYW5] | ||||||||
| ChEMBL | Agonist activity at human TAS2R4 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R40/Taste receptor type 2 member 40 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523250] [GtoPdb: 676] [UniProtKB: P59535] | ||||||||
| ChEMBL | Agonist activity at human TAS2R40 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R41/Taste receptor type 2 member 41 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309108] [GtoPdb: 680] [UniProtKB: P59536] | ||||||||
| ChEMBL | Agonist activity at human TAS2R41 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R42/Taste receptor type 2 member 42 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523360] [GtoPdb: 672] [UniProtKB: Q7RTR8] | ||||||||
| ChEMBL | Agonist activity at human TAS2R55 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R43/Taste receptor type 2 member 43 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523251] [GtoPdb: 678] [UniProtKB: P59537] | ||||||||
| ChEMBL | Agonist activity at human TAS2R43 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R45/Taste receptor type 2 member 45 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523252] [GtoPdb: 2828] [UniProtKB: P59539] | ||||||||
| ChEMBL | Agonist activity at human TAS2R45 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R46/Taste receptor type 2 member 46 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523253] [GtoPdb: 679] [UniProtKB: P59540] | ||||||||
| ChEMBL | Agonist activity at human TAS2R46 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R5/Taste receptor type 2 member 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523473] [GtoPdb: 662] [UniProtKB: Q9NYW4] | ||||||||
| ChEMBL | Agonist activity at human TAS2R5 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R50/Taste receptor type 2 member 50 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3559706] [GtoPdb: 677] [UniProtKB: P59544] | ||||||||
| ChEMBL | Agonist activity at human TAS2R50 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R60/Taste receptor type 2 member 60 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309109] [GtoPdb: 681] [UniProtKB: P59551] | ||||||||
| ChEMBL | Agonist activity at human TAS2R60 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R7/Taste receptor type 2 member 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523472] [GtoPdb: 663] [UniProtKB: Q9NYW3] | ||||||||
| ChEMBL | Agonist activity at human TAS2R7 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R8/Taste receptor type 2 member 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988599] [GtoPdb: 664] [UniProtKB: Q9NYW2] | ||||||||
| ChEMBL | Agonist activity at human TAS2R8 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
| TAS2R9/Taste receptor type 2 member 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3309110] [GtoPdb: 665] [UniProtKB: Q9NYW1] | ||||||||
| ChEMBL | Agonist activity at human TAS2R9 expressed in HEK293T cells co-expressing Galpha15 assessed as increase in intracellular calcium level by Calcium-3 dye based fluorescence assay | F | 8.31 | pEC50 | 4.9 | nM | EC50 | EP-2769216-A1. Assays for identifying compounds that modulate bitter taste (2014) |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
