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Assay Detail

CHEMBL3788461

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

Functional
Antagonist activity at mouse TAAR5 expressed in HEK293 cells assessed as inhibition of agonist induced cAMP release preincubated for 5 mins followed by addition of agonist by BRET assay
2
Total Activities
2
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 5 (CHEMBL3784908)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

A homology modelling-driven study leading to the discovery of the first mouse trace amine-associated receptor 5 (TAAR5) antagonists
Cichero E, Espinoza S, Tonelli M, Franchini S, Gerasimov AS, Sorbi C, Gainetdinov RR, Brasili L, Fossa P
Medchemcomm (2016) 7 : 353 -364
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 4.93 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1962870 1 5.32
CHEMBL1962769 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1962870 IC50 = 4800.0 nM 5.32
CHEMBL1962769 IC50 = 29000.0 nM 4.54