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, 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 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 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 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 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 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 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 | 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 | 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 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 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 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] |
| 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 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 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 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] |
| 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 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 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 | 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 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 | 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 | Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952] |
| 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 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 | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Naunyn Schmiedebergs Arch Pharmacol (2004) 369: 151-9 [PMID:14730417]; Br J Pharmacol (1997) 120: 165-76 [PMID:9117106]; Eur J Pharmacol (1995) 291: 359-66 [PMID:8719421]; Eur J Pharmacol (2004) 484: 323-31 [PMID:14744619]; Eur J Pharmacol (1996) 315: 363-7 [PMID:8982677]; Annu Rev Pharmacol Toxicol (1997) 37: 421-50 [PMID:9131260] |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
| 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 (null) |
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]
