phenylephrine [Ligand Id: 485] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1215 (AB-101 (PHENYLEPHRINE), Cyclomydril, Duo-Medihaler, Fenilefrina, J8.601K, Meta-synephrine, Metasynephrine, M-oxedrine, M-sympathol, M-sympatol, M-synephrine, (-)-phenylephrine, Phenylephrine, Phenylephrine minims, Phenylephrine, (r)-, R(-)-mezaton, (r)-phenylephrine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| GtoPdb | - | - | 5.4 | pKi | - | - | - |
Br J Pharmacol (1999) 127: 962-8 [PMID:10433504]; Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate | F | 5.53 | pEC50 | 2951.21 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | Intrinsic activity at alpha1A adrenergic receptor (unknown origin) after 5 hrs in presence of CCF4-AM by cell based beta lactamase reporter gene assay | B | 7.25 | pEC50 | 55.99 | nM | EC50 | Bioorg Med Chem (2016) 24: 5582-5591 [PMID:27658792] |
| ChEMBL | Agonist activity at alpha-1A adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay | B | 7.26 | pEC50 | 55 | nM | EC50 | Bioorg Med Chem (2015) 23: 2104-2111 [PMID:25813897] |
| GtoPdb | - | - | 8.3 | pEC50 | - | - | - |
Mol Pharmacol (2011) 79: 298-307 [PMID:20978120]; Br J Pharmacol (2017) 174: 2318-2333 [PMID:28444738]; Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| Alpha-1a adrenergic receptor in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4892] [UniProtKB: P18130] | ||||||||
| ChEMBL | Binding affinity towards bovine clonal Alpha-1A adrenergic receptor | B | 6.03 | pKi | 933.25 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 8.05 | pEC50 | 9 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
| ChEMBL | Binding affinity towards Alpha-1A adrenergic receptor in rat submaxillary glands | B | 6.01 | pKi | 977.24 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens | F | 5.78 | pEC50 | 1659.59 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] | ||||||||
| GtoPdb | - | - | 3.9 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| GtoPdb | - | - | 7.5 | pEC50 | - | - | - |
Br J Pharmacol (1997) 121: 1127-35 [PMID:9249248]; Mol Pharmacol (1994) 46: 929-36 [PMID:7969082] |
| ChEMBL | Agonist activity at alpha-1B adrenergic receptor (unknown origin) after 5 hrs by CCF4-AM staining-based cellular assay | B | 8.23 | pEC50 | 5.9 | nM | EC50 | Bioorg Med Chem (2015) 23: 2104-2111 [PMID:25813897] |
| GtoPdb | - | - | 9 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| ChEMBL | Intrinsic activity at human alpha1B adrenergic receptor expressed in CHOK1 cells co-expressing aequorin assessed as calcium mobilization measured for 20 secs in presence of coelenterazine H by luminescence assay | F | 9.07 | pEC50 | 0.86 | nM | EC50 | Bioorg Med Chem (2016) 24: 5582-5591 [PMID:27658792] |
| Alpha-1B adrenergic receptor in Cricetulus griseus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3988626] [UniProtKB: G3HDX1] | ||||||||
| ChEMBL | Agonist activity at hamster recombinant alpha-1B receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay | F | 8 | pEC50 | 10 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| Alpha-1b adrenergic receptor in Hamster (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3122] [UniProtKB: P18841] | ||||||||
| ChEMBL | Binding affinity towards hamster clonal Alpha-1B adrenergic receptor | B | 5.9 | pKi | 1258.93 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
| ChEMBL | In vitro agonist potency towards Alpha-1B adrenergic receptor in rat spleen | F | 4.96 | pEC50 | 10964.78 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| α1D-adrenoceptor in Human [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| GtoPdb | - | - | 4.7 | pKi | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| GtoPdb | - | - | 7.2 | pEC50 | - | - | - | Pharmacol Res Perspect (2021) 9: e00799 [PMID:34355529] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL326] [GtoPdb: 24] [UniProtKB: P23944] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - | Mol Pharmacol (1994) 46: 929-36 [PMID:7969082] |
| ChEMBL | Binding affinity towards rat clonal Alpha-1D adrenergic receptor | B | 6.79 | pKi | 162.18 | nM | Ki | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| ChEMBL | In vitro agonist potency towards Alpha-1D adrenergic receptor in rat aorta | F | 6.81 | pEC50 | 154.88 | nM | EC50 | J Med Chem (1996) 39: 4116-4119 [PMID:8831777] |
| 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 | 5.49 | pKi | 3216.62 | nM | Ki | EUbOPEN Chemogenomics Library - PDSP Secondary Binding |
| ChEMBL | GPCR PRESTO-Tango dose-response in agonist mode with target: ADRA2A | F | 6.32 | pEC50 | 476.65 | nM | EC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| ChEMBL | Agonist activity at human recombinant alpha-2A receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 6.51 | pEC50 | 306 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Agonist activity at human recombinant alpha-2C receptor expressed in PC12 cells assessed as inhibition of forskolin-stimulated intracellular cAMP accumulation measured after 10 mins by cAMP enzyme immunoassay | F | 6.47 | pEC50 | 340 | nM | EC50 | US-20050059664-A1. Novel methods for identifying improved, non-sedating alpha-2 agonists (2005) |
| β1-adrenoceptor/Beta-1 adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3252] [GtoPdb: 28] [UniProtKB: P18090] | ||||||||
| ChEMBL | Displacement of [3H]dihydroalprenolol from adrenergic beta 1 receptor of rat cerebral cortical membranes | B | 4.89 | pKi | 13000 | nM | Ki | J Med Chem (1993) 36: 3947-3955 [PMID:8254623] |
| 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 | pIC50 | >10000 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| 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 | 5.95 | pKi | 1110.07 | 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]
