β-phenylethylamine [Ligand Id: 2144] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL610 (Phenethylamine, Phenylethylamine)
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 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]
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  • TAAR4P in Mouse [GtoPdb: 169] [UniProtKB: Q5QD15]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
lysyl oxidase like 2/Lysyl oxidase homolog 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714029] [GtoPdb: 2853] [UniProtKB: Q9Y4K0]
ChEMBL Inhibition of full length recombinant human LOXL2 expressed in CHO cells assessed as reduction in H2O2 production using DAP as substrate preincubated for 2 hrs followed by substrate addition measured every 2 minutes for 50 minutes by Amplex red dye based fluorescence assay B 4.22 pIC50 60100 nM IC50 ACS Med Chem Lett (2017) 8: 423-427 [PMID:28435530]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity was performed using [3H]ketanserin as the radioligand and stably transfected NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor (GF-62 cells). B 4.77 pKi 16800 nM Ki J. Med. Chem. (2002) 45: 1656-1664 [PMID:11931619]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor expressed in NIH3T3 cells B 4.77 pKi 16800 nM Ki J. Med. Chem. (2008) 51: 6808-6828 [PMID:18847250]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity against 5-hydroxytryptamine 2A receptor expressed NIH3T3 cells using [3H]ketanserin B 4.77 pKi 16820 nM Ki Bioorg. Med. Chem. Lett. (2001) 11: 563-566 [PMID:11229772]
ChEMBL Displacement of [3H]ketanserin from rat 5HT2A expressed in mouse NIH/3T3 cell membranes after 30 mins by scintillation counting method B 5 pKi >10000 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
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 6.89 pEC50 129 nM EC50 Bioorg. Med. Chem. (2008) 16: 7415-7423 [PMID:18602830]
ChEMBL Agonist activity at human TAAR1 receptor expressed in HEK293T cells cotransfected with beta-2 receptor assessed as cAMP production by BRET assay B 6.96 pEC50 110 nM EC50 MedChemComm (2015) 6: 2216-2223
ChEMBL Activation of human TAAR1 expressed in Syrian hamster AV12-664 cells co-expressing GalphaS protein assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method in presence of RX821002 and alprenolol B 6.97 pEC50 106 nM EC50 Bioorg. Med. Chem. (2011) 19: 7044-7048 [PMID:22037049]
GtoPdb - - 7 pEC50 - - - Mol Pharmacol (2008) 74: 585-594 [PMID:18524885];
Proc Natl Acad Sci U S A (2001) 98: 8966-8971 [PMID:11459929];
Biochem. J. (2009) 424: 39-45 [PMID:19725810];
PLoS ONE (2011) 6: e27073 [PMID:22073124];
Bioorg. Med. Chem. (2008) 16: 7415-23 [PMID:18602830];
J Pharmacol Exp Ther (2007) 320: 475-485 [PMID:17038507]
TA1 receptor/Trace amine-associated receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8]
ChEMBL Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay B 6.72 pEC50 189 nM EC50 J. Med. Chem. (2014) 57: 378-390 [PMID:24354319]
ChEMBL Agonist activity at mouse TAAR1 expressed in HEK293 cells coexpressing cAMP BRET biosensor assessed as induction of CAMP production after 20 mins by bioluminescence resonance energy transfer assay B 6.86 pEC50 138 nM EC50 J. Med. Chem. (2015) 58: 5096-5107 [PMID:26010728]
GtoPdb - - 7.4 pEC50 - - - J Pharmacol Exp Ther (2007) 321: 178-186 [PMID:17218486];
Genes Brain Behav (2007) 6: 628-639 [PMID:17212650];
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 - - 6.6 pEC50 - - - J Pharmacol Exp Ther (2007) 321: 178-186 [PMID:17218486];
Mol Pharmacol (2001) 60: 1181-1188 [PMID:11723224]
ChEMBL Agonist activity at rat N-terminal FLAG-tagged TAAR1 expressed in HEK293 cells assessed as [3H]cAMP accumulation measured after 1 hr B 6.62 pEC50 240 nM EC50 J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL Activation of rat TAAR1 expressed in Syrian hamster AV12-664 cells assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method B 6.68 pEC50 209 nM EC50 Bioorg. Med. Chem. (2011) 19: 7044-7048 [PMID:22037049]
ChEMBL Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay B 7.39 pEC50 40.33 nM EC50 J. Med. Chem. (2014) 57: 378-390 [PMID:24354319]
serine protease 1/Trypsin I in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL209] [GtoPdb: 2397] [UniProtKB: P07477]
ChEMBL Binding affinity against trypsin B 1.96 pKd -1.96 - Log Kd J. Med. Chem. (2002) 45: 2770-2780 [PMID:12061879]
Trypsin I in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3769] [UniProtKB: P00760]
ChEMBL Binding affinity against bovine trypsin B 4.96 pKi 11000 nM Ki J. Med. Chem. (2002) 45: 2469-2483 [PMID:12036355]
TAAR4P in Mouse [GtoPdb: 169] [UniProtKB: Q5QD15]
GtoPdb - - 6 pEC50 1000 nM EC50 Nature (2006) 442: 645-650 [PMID:16878137]

ChEMBL data shown on this page come from version 25:

A.P. Bento, A. Gaulton, A. Hersey, et al. (2014). The ChEMBL bioactivity database: an update. Nucl. Acids Res. Database Issue. 42 D1083-D1090. [PMID:24214965]