ChEMBL ligand: CHEMBL11608 (2-p-hydroxyphenylethylamine, FEMA NO. 4215, NSC-249188, Ractopamine hydrochloride suspension impurity, tyramine-, Systogene, Tocosine, Tyramine, Tyrosamine, Uteramine)
beta-secretase 1/Beta-secretase 1 in Human [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817] There should be some charts here, you may need to enable JavaScript!
D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] There should be some charts here, you may need to enable JavaScript!
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] TA1 receptor/Trace amine-associated receptor 1 in Mouse [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8] TA1 receptor/Trace amine-associated receptor 1 in Rat [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
beta-secretase 1/Beta-secretase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4822] [GtoPdb: 2330] [UniProtKB: P56817]
ChEMBL	Binding affinity to BACE1 by surface plasmon resonance method	B	2.7	pKd	2000000	nM	Kd	Bioorg Med Chem Lett (2008) 18: 1304-1307 [PMID:18226904]
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 TAAR1 stably expressed in HEK293 cells incubated for 30 mins by cAMP assay	F	6	pEC50	990	nM	EC50	J Nat Prod (2021) 84: 2398-2407 [PMID:34264089]
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/Trace amine-associated receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8]
GtoPdb	-	-	6.4	pKi	404	nM	Ki	Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733]
ChEMBL	Agonist activity at mouse TAAR1 stably expressed in HEK293 cells incubated for 30 mins by cAMP assay	F	6.55	pEC50	280	nM	EC50	J Nat Prod (2021) 84: 2398-2407 [PMID:34264089]
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	Agonist activity at rat TAAR1 stably expressed in HEK293 cells incubated for 30 mins by cAMP assay	F	7.52	pEC50	30	nM	EC50	J Nat Prod (2021) 84: 2398-2407 [PMID:34264089]

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]