tyramine [Ligand Id: 2150] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL11608 (2-p-hydroxyphenylethylamine, FEMA NO. 4215, NSC-249188, Ractopamine hydrochloride suspension impurity, tyramine-, Systogene, Tocosine, Tyramine, Tyrosamine, Uteramine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Potency was measured by the displacement of [3H]spiperone binding to human D2 dopaminergic receptor | B | 4.77 | pKi | >17000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | Potency was measured by the displacement of [3H]-spiperone binding to human D4 dopaminergic receptor | B | 4.46 | pKi | >35000 | nM | Ki | Bioorg Med Chem Lett (1997) 7: 1207-1212 |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| ChEMBL | Antagonistic activity of corresponding methoxy compound against serotonin 5-HT receptor | F | 5.1 | pKd | 7943.28 | nM | Kd | J Med Chem (1980) 23: 990-994 [PMID:7411554] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Activity at SER3 receptor expressed in HEK293 cells assessed as increase in calcium by calcium imaging assay | B | 4.59 | pEC50 | 26000 | nM | EC50 | Nature (2007) 450: 553-556 [PMID:18033297] |
| TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] | ||||||||
| ChEMBL | Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay | F | 6.14 | pEC50 | 731 | nM | EC50 | Bioorg Med Chem (2008) 16: 7415-7423 [PMID:18602830] |
| GtoPdb | - | - | 6.7 | pEC50 | - | - | - |
Proc Natl Acad Sci USA (2001) 98: 8966-71 [PMID:11459929]; Mol Pharmacol (2008) 74: 585-594 [PMID:18524885]; J Pharmacol Exp Ther (2007) 320: 475-85 [PMID:17038507]; Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733]; Biochem J (2009) 424: 39-45 [PMID:19725810]; PLoS ONE (2011) 6: e27073 [PMID:22073124] |
| ChEMBL | Agonist activity at recombinant human TAAR1 expressed in CHO-K1 cells assessed as increase in intracellular cAMP incubated for 30 mins by HTRF analysis | F | 7.12 | pEC50 | 76 | nM | EC50 | ACS Med Chem Lett (2022) 13: 92-98 [PMID:35047111] |
| TA1 receptor in Mouse [GtoPdb: 364] [UniProtKB: Q923Y8] | ||||||||
| GtoPdb | - | - | 6.4 | pKi | 404 | nM | Ki | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| GtoPdb | - | - | 7.1 | pEC50 | - | - | - |
J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486]; Genes Brain Behav (2007) 6: 628-39 [PMID:17212650]; Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733]; Biochem J (2009) 424: 39-45 [PMID:19725810] |
| TA1 receptor/Trace amine-associated receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9] | ||||||||
| GtoPdb | - | - | 7.2 | pKi | 70 | nM | Ki | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| ChEMBL | Agonist activity at rat N-terminal FLAG-tagged TAAR1 expressed in HEK293 cells assessed as [3H]cAMP accumulation measured after 1 hr | F | 7.16 | pEC50 | 69 | nM | EC50 | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| GtoPdb | - | - | 7.2 | pEC50 | - | - | - |
J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486]; Mol Pharmacol (2001) 60: 1181-8 [PMID:11723224]; Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
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]
