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Assay Detail

CHEMBL4009953

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Agonist activity at rat N-terminal FLAG-tagged TAAR1 expressed in HEK293 cells assessed as [3H]cAMP accumulation measured after 1 hr
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trace amine-associated receptor 1 (CHEMBL3833)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Glennon RA.
J Med Chem (2017) 60 : 2605 -2628
PubMed 28244748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.69 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1546 HYDROXYAMPHETAMINE 4.0 1 7.29
CHEMBL11608 TYRAMINE 3.0 1 7.16
CHEMBL610 PHENETHYLAMINE 1 6.62
CHEMBL6640 TRYPTAMINE 1 6.51
CHEMBL53929 OCTOPAMINE 2.0 1 5.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1546 HYDROXYAMPHETAMINE EC50 = 51.0 nM 7.29
CHEMBL11608 TYRAMINE EC50 = 69.0 nM 7.16
CHEMBL610 PHENETHYLAMINE EC50 = 240.0 nM 6.62
CHEMBL6640 TRYPTAMINE EC50 = 310.0 nM 6.51
CHEMBL53929 OCTOPAMINE EC50 = 1300.0 nM 5.89