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Assay Detail

CHEMBL1930653

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

Functional
Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by competitive binding assay
4
Total Activities
4
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

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 4 6.53 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1546 HYDROXYAMPHETAMINE 4.0 1 7.30
CHEMBL19393 LEVAMFETAMINE 4.0 1 6.68
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.36
CHEMBL43048 MIDOMAFETAMINE 3.0 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1546 HYDROXYAMPHETAMINE EC50 = 50.0 nM 7.30
CHEMBL19393 LEVAMFETAMINE EC50 = 210.0 nM 6.68
CHEMBL612 DEXTROAMPHETAMINE EC50 = 440.0 nM 6.36
CHEMBL43048 MIDOMAFETAMINE EC50 = 1700.0 nM 5.77