formoterol [Ligand Id: 3465] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1256786 (Foradil, Formoterol) |
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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] |
| GtoPdb | - | - | 6.5 | pKi | - | - | - |
Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599]; Bioorg Med Chem Lett (2010) 20: 5302-7 [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] |
| GtoPdb | - | - | 8.3 | pEC50 | - | - | - | Br J Pharmacol (2010) 160: 1048-61 [PMID:20590599] |
| 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]; Bioorg Med Chem Lett (2004) 14: 4705-10 [PMID:15324892]; Mol Pharmacol (2015) 87: 103-20 [PMID:25324048]; J Pharmacol Exp Ther (2006) 317: 762-70 [PMID:16434564]; J Pharmacol Exp Ther (2015) 355: 183-90 [PMID:26306764] |
| 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 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]
