salmeterol [Ligand Id: 559] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1263 (Beglan, Cryogenine, GR 33343 X, GR-33343-X, GR-33343X, Neovent, NSC-272693, Salmaterol, Salmeterol, Serevent, SN408D, Soltel, Vertine) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| ADGRF1/Adhesion G-protein coupled receptor F1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523872] [GtoPdb: 190] [UniProtKB: Q5T601] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADGRF1 | F | 5.47 | pIC50 | 3409.69 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA1A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.26 | pKi | 548.66 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.02 | pKi | 963.16 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5 | pKi | >10000 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| ChEMBL | PDSP Secondary Binding target: ADRA2B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.71 | pKi | 1942.9 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588] | ||||||||
| ChEMBL | Displacement of [3H]dihydroalprenolol from beta1 receptor (unknown origin) by liquid scintillation counting and cell based assay | B | 5.6 | pKi | 2511.89 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Displacement of [125I]-CYP from human beta1-adrenergic receptor expressed in COS-7 cells by gamma counting | B | 5.64 | pKi | 2300 | nM | Ki | Bioorg Med Chem (2010) 18: 728-736 [PMID:20036561] |
| ChEMBL | Displacement of [3H]CGP12177 from human beta-1 adrenoceptor | B | 6.1 | pKi | 801 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5302-5307 [PMID:20655218] |
| ChEMBL | Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta1 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay | B | 6.11 | pKi | 784 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| ChEMBL | PDSP Secondary Binding target: ADRB1 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.16 | pKi | 694.46 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | Binding affinity to adrenergic beta1 receptor | B | 6.3 | pIC50 | 501.19 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4612-4616 [PMID:21723724] |
| ChEMBL | Binding affinity to beta1 adrenoceptor | B | 6.3 | pIC50 | 501.19 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 689-695 [PMID:22079756] |
| ChEMBL | Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay | B | 5.3 | pEC50 | 5011.87 | nM | EC50 | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| 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 | 5.91 | pEC50 | 1230.27 | nM | EC50 | Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952] |
| ChEMBL | Agonist activity at adrenergic beta1 receptor | F | 6.1 | pEC50 | 794.33 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4612-4616 [PMID:21723724] |
| ChEMBL | Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation | F | 6.1 | pEC50 | 794.33 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation | F | 6.1 | pEC50 | 794.33 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| 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 | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| ChEMBL | Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay | B | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2014) 57: 159-170 [PMID:24359185] |
| 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 | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human beta1 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation | F | 6.43 | pEC50 | 371.54 | nM | EC50 | Eur J Med Chem (2021) 224: 113697-113697 [PMID:34273662] |
| ChEMBL | Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay | F | 6.6 | pEC50 | 251.19 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2871-2876 [PMID:24835980] |
| ChEMBL | Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay | F | 6.6 | pEC50 | 251.19 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay | F | 6.6 | pEC50 | 251.19 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1213-1218 [PMID:22178551] |
| ChEMBL | Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay | B | 6.7 | pEC50 | 199.53 | nM | EC50 | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| ChEMBL | Agonist activity at human beta1 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology | F | 7.17 | pEC50 | 67 | nM | EC50 | J Med Chem (2020) 63: 15218-15242 [PMID:33213146] |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3440] [GtoPdb: 28] [UniProtKB: P34971] | ||||||||
| ChEMBL | Displacement of [3H]-CGP-12177 from murine beta1-adrenergic receptor expressed in HEK293T cells after 60 mins by radioligand competition binding assay | B | 6.26 | pKi | 550 | nM | Ki | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| Beta-1 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73] | ||||||||
| ChEMBL | Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction | F | 8.3 | pEC50 | 5.01 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| 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 | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| ChEMBL | Displacement of [3H]DHA from inactive/G protein-uncoupled human beta2-AR expressed in CHO cell membranes by liquid scintillation counting | B | 9.52 | pKd | 0.3 | nM | Kd | J Med Chem (2016) 59: 5780-5789 [PMID:27239696] |
| ChEMBL | Displacement of [125I]-CYP from human beta2-adrenergic receptor Y308A mutant expressed in COS-7 cells by gamma counting | B | 6.74 | pKi | 184 | nM | Ki | Bioorg Med Chem (2010) 18: 728-736 [PMID:20036561] |
| ChEMBL | PDSP Secondary Binding target: ADRB2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 8.26 | pKi | 5.46 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 adrenoceptor | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2010) 20: 5302-5307 [PMID:20655218] |
| ChEMBL | Displacement of [125I]iodo-(+/-)-cyanopindolol from human adrenergic beta2 receptor expressed in CHO cells after 3 hrs by radio-ligand binding assay | B | 8.49 | pKi | 3.2 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| ChEMBL | Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay | B | 8.6 | pKi | 2.51 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 2871-2876 [PMID:24835980] |
| ChEMBL | Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs | B | 8.62 | pKi | 2.4 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1354-1358 [PMID:21310610] |
| ChEMBL | Displacement of [125I]-CYP from human beta2-adrenergic receptor expressed in COS-7 cells by gamma counting | B | 8.82 | pKi | 1.5 | nM | Ki | Bioorg Med Chem (2010) 18: 728-736 [PMID:20036561] |
| ChEMBL | Binding affinity for human beta-2 adrenergic receptor | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2004) 14: 4705-4710 [PMID:15324892] |
| GtoPdb | - | - | 9.3 | pKi | - | - | Kd |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Br J Pharmacol (2022) 179: 4692-4708 [PMID:35732075]; Mol Pharmacol (2015) 87: 103-20 [PMID:25324048] |
| ChEMBL | Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay | B | 9.41 | pKi | 0.39 | nM | Ki | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| ChEMBL | Displacement of [3H]-CGP-12177 from human beta2-adrenergic receptor expressed in CHO cells after 60 mins by radioligand competition binding assay | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| ChEMBL | Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells | B | 9.74 | pKi | 0.18 | nM | Ki | Bioorg Med Chem (2016) 24: 2641-2653 [PMID:27132867] |
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2 | F | 7.83 | pIC50 | 14.93 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| ChEMBL | Displacement of [3H]dihydroalprenolol from beta2-adrenoceptor after 90 mins by liquid scintillation counting | B | 8.3 | pIC50 | 5.01 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1213-1218 [PMID:22178551] |
| ChEMBL | Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry | F | 9.1 | pEC50 | 0.79 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 689-695 [PMID:22079756] |
| ChEMBL | Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay | B | 9.1 | pEC50 | 0.79 | nM | EC50 | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| ChEMBL | Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr | F | 9.1 | pEC50 | 0.79 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4027-4031 [PMID:21652207] |
| ChEMBL | Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins | F | 9.1 | pEC50 | 0.79 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 4612-4616 [PMID:21723724] |
| ChEMBL | Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology | F | 9.15 | pEC50 | 0.71 | nM | EC50 | J Med Chem (2020) 63: 15218-15242 [PMID:33213146] |
| ChEMBL | Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1213-1218 [PMID:22178551] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay | F | 9.3 | pEC50 | 0.5 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2871-2876 [PMID:24835980] |
| ChEMBL | Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay | F | 9.48 | pEC50 | 0.33 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 1354-1358 [PMID:21310610] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay | F | 9.49 | pEC50 | 0.32 | nM | EC50 | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| ChEMBL | Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2871-2876 [PMID:24835980] |
| ChEMBL | Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 1213-1218 [PMID:22178551] |
| ChEMBL | Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay | F | 9.5 | pEC50 | 0.32 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation | F | 9.6 | pEC50 | 0.25 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay | F | 9.6 | pEC50 | 0.25 | nM | EC50 | J Med Chem (2014) 57: 159-170 [PMID:24359185] |
| 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 | 9.6 | pEC50 | 0.25 | 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 | 9.6 | pEC50 | 0.25 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation | F | 9.6 | pEC50 | 0.25 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| ChEMBL | Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation | F | 9.87 | pEC50 | 0.13 | nM | EC50 | Eur J Med Chem (2021) 224: 113697-113697 [PMID:34273662] |
| ChEMBL | Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK2 and coelenterazine 400a by BRET assay | B | 9.9 | pEC50 | 0.13 | nM | EC50 | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| GtoPdb | - | - | 9.9 | pEC50 | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; J Pharmacol Exp Ther (2006) 317: 762-70 [PMID:16434564] |
| ChEMBL | Agonist activity at beta2-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GSK5 and coelenterazine 400a by BRET assay | B | 10.1 | pEC50 | 0.08 | nM | EC50 | J Med Chem (2019) 62: 5111-5131 [PMID:31042379] |
| 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 | 10.11 | pEC50 | 0.08 | nM | EC50 | Bioorg Med Chem (2019) 27: 2306-2314 [PMID:30392952] |
| ChEMBL | Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method | F | 10.15 | pEC50 | 0.07 | nM | EC50 | J Med Chem (2010) 53: 6640-6652 [PMID:20804199] |
| ChEMBL | Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP | F | 10.15 | pEC50 | 0.07 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 4012-4015 [PMID:17498952] |
| ChEMBL | Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels | F | 10.15 | pEC50 | 0.07 | nM | EC50 | Bioorg Med Chem Lett (2007) 17: 6188-6191 [PMID:17897826] |
| ChEMBL | Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay | F | 10.35 | pEC50 | 0.04 | nM | EC50 | Bioorg Med Chem (2020) 28: 115178-115178 [PMID:31753798] |
| Beta-2 adrenergic receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4] | ||||||||
| ChEMBL | Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response after 30 mins | F | 8.46 | pIC50 | 3.5 | nM | IC50 | J Med Chem (2010) 53: 3675-3684 [PMID:20402514] |
| ChEMBL | Agonist activity at adrenergic beta2 receptor in electrically-stimulated Dunkin-Hartley guinea pig tracheal strip assessed as inhibition of contraction | B | 8.46 | pIC50 | 3.5 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| ChEMBL | Agonist activity at beta2 receptor in guinea pig trachea assessed as slow onset of inhibition of electrically stimulated contraction | B | 7.5 | pEC50 | 31.62 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction | F | 8.3 | pEC50 | 5.01 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response | F | 8.3 | pEC50 | 5.01 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| ChEMBL | Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as inhibition of histamine-induced contraction | B | 8.57 | pEC50 | 2.7 | nM | EC50 | Bioorg Med Chem Lett (2015) 25: 5121-5126 [PMID:26471092] |
| β3-adrenoceptor/Beta-3 adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945] | ||||||||
| 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 | 5.9 | pEC50 | 1258.93 | nM | EC50 | J Med Chem (2009) 52: 2280-2288 [PMID:19317397] |
| 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 | 5.9 | pEC50 | 1258.93 | nM | EC50 | J Med Chem (2010) 53: 4522-4530 [PMID:20462258] |
| ChEMBL | Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation | F | 5.9 | pEC50 | 1258.93 | nM | EC50 | Bioorg Med Chem (2011) 19: 4192-4201 [PMID:21696967] |
| ChEMBL | Agonist activity at human beta3 receptor expressed in CHO cells assessed as cAMP accumulation | F | 5.9 | pEC50 | 1258.93 | nM | EC50 | Bioorg Med Chem (2011) 19: 6026-6032 [PMID:21925889] |
| ChEMBL | Agonist activity at human beta3 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay | B | 5.9 | pEC50 | 1258.93 | nM | EC50 | J Med Chem (2014) 57: 159-170 [PMID:24359185] |
| ChEMBL | Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2625-2630 [PMID:24813741] |
| ChEMBL | Agonist activity at human beta3 adrenergic receptor expressed in cells by cAMP accumulation assay | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 2871-2876 [PMID:24835980] |
| CX3CR1/C-X3-C chemokine receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4843] [GtoPdb: 74] [UniProtKB: P49238] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1 | F | 5.5 | pIC50 | 3138.6 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Displacement of [3H]spiperone from human D2S receptor expressed in CHO cells | B | 4.49 | pKi | 32000 | 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 | PDSP Secondary Binding target: DRD3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.9 | pKi | 1260.37 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | Displacement of [125I]7-HO-PIPAT from human D3R expressed in HEK cells | B | 5.98 | pKi | 1049 | nM | Ki | Bioorg Med Chem Lett (2014) 24: 4341-4347 [PMID:25065493] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | PDSP Secondary Binding target: DRD4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.97 | pKi | 1076.34 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A3 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.83 | pKi | 149.42 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| GPR183/G-protein coupled receptor 183 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259470] [GtoPdb: 81] [UniProtKB: P32249] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR183 | F | 5.37 | pIC50 | 4255.52 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: CHRM2 | F | 5 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | PDSP Secondary Binding target: CHRM5 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.01 | pKi | 971.3 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5.25 | pIC50 | 5657.9 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A2 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.42 | pKi | 381.86 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 | F | 5.61 | pIC50 | 2463.2 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR1B - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.7 | pKi | 1985.41 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR1D - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.98 | pKi | 1036.33 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2A - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.89 | pKi | 1274.77 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR2C - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 5.39 | pKi | 4092.61 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | PDSP Secondary Binding target: HTR7 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.59 | pKi | 256.92 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | PDSP Secondary Binding target: SLC6A4 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 6.53 | pKi | 294.2 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| σ2/Sigma intracellular receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105907] [GtoPdb: 2553] [UniProtKB: Q5BJF2] | ||||||||
| ChEMBL | PDSP Secondary Binding target: TMEM97 - Compounds are tested at 10 uM concentration, plate are incubated at room temperature in the dark for 90 minutes. Reaction are stopped by vacuum filtration onto 0.3% polyethyleneimine soaked filter mats using Filtermate harvester. Scintillation cocktail is then melted onto microwave-dried filters on a hot plate and the radio activity is counted in Microbia counter. Compounds showing a minimum of 50% inhibition at 10 uM concentration are carried forward in this secondary binding assay to determine equilibrium binding affinity. | B | 7.49 | pKi | 32.43 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
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]
