formoterol [Ligand Id: 3465] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1256786 (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 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]
