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Assay Detail

CHEMBL3583705

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

Functional
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
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trace amine-associated receptor 1 (CHEMBL4908)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, Synthesis, and Evaluation of Thyronamine Analogues as Novel Potent Mouse Trace Amine Associated Receptor 1 (mTAAR1) Agonists.
Chiellini G, Nesi G, Digiacomo M, Malvasi R, Espinoza S, Sabatini M, Frascarelli S, Laurino A, Cichero E, Macchia M, Gainetdinov RR, Fossa P, Raimondi L, Zucchi R, Rapposelli S.
J Med Chem (2015) 58 : 5096 -5107
PubMed 26010728 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 6.29 6.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL610 PHENETHYLAMINE 1 6.86
CHEMBL1182312 1 6.72
CHEMBL3580902 1 6.62
CHEMBL3580905 1 6.10
CHEMBL3580901 1 5.77
CHEMBL3580906 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL610 PHENETHYLAMINE EC50 = 138.0 nM 6.86
CHEMBL1182312 EC50 = 189.0 nM 6.72
CHEMBL3580902 EC50 = 240.0 nM 6.62
CHEMBL3580905 EC50 = 800.0 nM 6.10
CHEMBL3580901 EC50 = 1700.0 nM 5.77
CHEMBL3580906 EC50 = 2200.0 nM 5.66