formoterol [Ligand Id: 3465] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1256786 (Foradil, Formoterol)
  • β1-adrenoceptor/Beta-1 adrenergic receptor in Human [ChEMBL: CHEMBL213] [GtoPdb: 28] [UniProtKB: P08588]
  • Beta-1 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5471] [UniProtKB: B0FL73]
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  • β2-adrenoceptor/Beta-2 adrenergic receptor in Human [ChEMBL: CHEMBL210] [GtoPdb: 29] [UniProtKB: P07550]
  • Beta-2 adrenergic receptor in Guinea pig [ChEMBL: CHEMBL5414] [UniProtKB: Q8K4Z4]
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  • β3-adrenoceptor/Beta-3 adrenergic receptor in Human [ChEMBL: CHEMBL246] [GtoPdb: 30] [UniProtKB: P13945]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 5.7 pKi 1995.26 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Displacement of [3H]CGP12177 from human beta-1 adrenoceptor B 6.5 pKi 319 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 6.5 pKi 315 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Binding affinity to adrenergic beta1 receptor B 6.2 pIC50 >630.96 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Binding affinity to beta1 adrenoceptor B 6.2 pIC50 >630.96 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 689-695 [PMID:22079756]
ChEMBL Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation F 7.07 pEC50 86 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 6640-6644 [PMID:19875286]
ChEMBL Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level F 7.07 pEC50 86 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5237-5240 [PMID:19643607]
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 7.4 pEC50 39.81 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human adrenergic beta1 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 recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay F 7.9 pEC50 12.59 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
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 9.5 pEC50 0.32 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 Binding affinity to beta-2 adrenergic receptor (unknown origin) at 1 to 10000 nM B 8.6 pKd 2.51 nM Kd Bioorg. Med. Chem. Lett. (2013) 23: 5376-5381 [PMID:23954364]
ChEMBL Displacement of [3H]-dihydroalprenolol from human beta2-adrenoceptor expressed in HEK cells after 4 hrs B 7.48 pKi 33 nM Ki Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
ChEMBL Displacement of [3H]dihydroalprenolol from human beta2 adrenergic receptor expressing cell membrane by competition binding assay B 7.5 pKi 31.62 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Displacement of [3H]dihydroalprenolol from beta2 receptor (unknown origin) by liquid scintillation counting and cell based assay B 7.5 pKi 31.62 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Displacement of [3H]CGP12177 from human beta2 receptor expressed in CHO cells B 7.59 pKi 26 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Displacement of [125I]cyanopindolol from human recombinant beta2 adrenergic receptor expressed in CHO cells by filtration assay B 7.64 pKi 23 nM Ki J. Med. Chem. (2010) 53: 3675-3684 [PMID:20402514]
ChEMBL Displacement of [3H]CGP12177 from human beta2 adrenoceptor B 8.59 pKi 2.6 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 8.59 pKi 2.6 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Binding affinity for human beta-2 adrenergic receptor B 8.59 pKi 2.6 nM Ki Bioorg. Med. Chem. Lett. (2004) 14: 4705-4710 [PMID:15324892]
ChEMBL Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation F 8.1 pEC50 7.94 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 5302-5307 [PMID:20655218]
ChEMBL Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay F 8.6 pEC50 2.51 nM EC50 ACS Med. Chem. Lett. (2014) 5: 416-421 [PMID:24900851]
ChEMBL Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay F 8.6 pEC50 2.51 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
ChEMBL Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay F 8.6 pEC50 2.51 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay F 8.89 pEC50 1.3 nM EC50 J. Med. Chem. (2010) 53: 3675-3684 [PMID:20402514]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins F 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry F 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 689-695 [PMID:22079756]
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 9.3 pEC50 0.5 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr F 9.3 pEC50 0.5 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4027-4031 [PMID:21652207]
ChEMBL Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level F 9.4 pEC50 0.4 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 5237-5240 [PMID:19643607]
ChEMBL Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation F 9.4 pEC50 0.4 nM EC50 Bioorg. Med. Chem. Lett. (2009) 19: 6640-6644 [PMID:19875286]
ChEMBL Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 9.7 pEC50 0.2 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2625-2630 [PMID:24813741]
ChEMBL Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay F 9.7 pEC50 0.2 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 9.72 pEC50 0.19 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 1354-1358 [PMID:21310610]
GtoPdb - - 10.08 pEC50 - - - Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]
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 9.4 pIC50 0.4 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 9.4 pIC50 0.4 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
ChEMBL Agonist activity at beta2 receptor in guinea pig trachea assessed as fast onset of inhibition of electrically stimulated contraction B 8.8 pEC50 1.58 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 9.5 pEC50 0.32 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
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 7.6 pEC50 25.12 nM EC50 J. Med. Chem. (2009) 52: 2280-2288 [PMID:19317397]
ChEMBL Agonist activity at human adrenergic beta3 receptor expressed in CHO cells assessed as cAMP accumulation F 7.6 pEC50 25.12 nM EC50 Bioorg. Med. Chem. (2011) 19: 4192-4201 [PMID:21696967]
ChEMBL Agonist activity at human recombinant beta3 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay F 7.6 pEC50 25.12 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 7.6 pEC50 25.12 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2871-2876 [PMID:24835980]
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 4.89 pKi 13000 nM Ki Bioorg. Med. Chem. (2016) 24: 2641-2653 [PMID:27132867]
ChEMBL Binding affinity to dopamine 2 receptor B 5 pIC50 >10000 nM IC50 Bioorg. Med. Chem. Lett. (2011) 21: 4612-4616 [PMID:21723724]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Displacement of [125I]7-HO-PIPAT from human D3R expressed in HEK cells B 5.79 pKi 1626 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 4341-4347 [PMID:25065493]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]