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Assay Detail

CHEMBL1930655

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

Functional
Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting
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

Trace amine-associated receptor 1 is a stereoselective binding site for compounds in the amphetamine class.
Lewin AH, Miller GM, Gilmour B.
Bioorg Med Chem (2011) 19 : 7044 -7048
PubMed 22037049 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 5.91 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.68
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE 1 6.55
CHEMBL1201201 METHAMPHETAMINE 4.0 1 6.04
CHEMBL1927030 LEVMETAMFETAMINE 2.0 1 5.61
CHEMBL19393 LEVAMFETAMINE 4.0 1 5.30
CHEMBL1230845 1 5.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL612 DEXTROAMPHETAMINE EC50 = 210.0 nM 6.68
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE EC50 = 280.0 nM 6.55
CHEMBL1201201 METHAMPHETAMINE EC50 = 920.0 nM 6.04
CHEMBL1927030 LEVMETAMFETAMINE EC50 = 2440.0 nM 5.61
CHEMBL19393 LEVAMFETAMINE EC50 = 4960.0 nM 5.30
CHEMBL1230845 EC50 = 5650.0 nM 5.25