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Assay Detail

CHEMBL3110493

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

Functional
Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay
5
Total Activities
5
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

Exploring the determinants of trace amine-associated receptor 1's functional selectivity for the stereoisomers of amphetamine and methamphetamine.
Reese EA, Norimatsu Y, Grandy MS, Suchland KL, Bunzow JR, Grandy DK.
J Med Chem (2014) 57 : 378 -390
PubMed 24354319 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.50 7.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 7.07
CHEMBL610 PHENETHYLAMINE 1 6.72
CHEMBL1201201 METHAMPHETAMINE 4.0 1 6.55
CHEMBL19393 LEVAMFETAMINE 4.0 1 6.11
CHEMBL1927030 LEVMETAMFETAMINE 2.0 1 6.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL612 DEXTROAMPHETAMINE EC50 = 84.6 nM 7.07
CHEMBL610 PHENETHYLAMINE EC50 = 189.0 nM 6.72
CHEMBL1201201 METHAMPHETAMINE EC50 = 278.9 nM 6.55
CHEMBL19393 LEVAMFETAMINE EC50 = 785.5 nM 6.11
CHEMBL1927030 LEVMETAMFETAMINE EC50 = 843.3 nM 6.07