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Assay Detail

CHEMBL3110492

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

Functional
Activation of rat TAAR1 transmembrane domain 6 Met268(6.55)Thr mutant 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 Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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 6.21 6.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19393 LEVAMFETAMINE 4.0 1 6.67
CHEMBL610 PHENETHYLAMINE 1 6.58
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.17
CHEMBL1927030 LEVMETAMFETAMINE 2.0 1 5.96
CHEMBL1201201 METHAMPHETAMINE 4.0 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19393 LEVAMFETAMINE EC50 = 214.4 nM 6.67
CHEMBL610 PHENETHYLAMINE EC50 = 261.2 nM 6.58
CHEMBL612 DEXTROAMPHETAMINE EC50 = 677.4 nM 6.17
CHEMBL1927030 LEVMETAMFETAMINE EC50 = 1109.0 nM 5.96
CHEMBL1201201 METHAMPHETAMINE EC50 = 2044.0 nM 5.69