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Assay Detail

CHEMBL1930650

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

Functional
Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Macaca mulatta
Cell Type RD-HGA16
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Trace amine-associated receptor 1 (CHEMBL1926495)
Type SINGLE PROTEIN
Organism Macaca mulatta

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 20 5.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE 1 7.00
CHEMBL1230845 1 6.37
CHEMBL102594 1 6.05
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.00
CHEMBL1788307 1 5.87
CHEMBL19393 LEVAMFETAMINE 4.0 1 5.73
CHEMBL468880 1 5.67
CHEMBL1927025 1 5.61
CHEMBL1927030 LEVMETAMFETAMINE 2.0 1 5.60
CHEMBL1927026 (S)-M-METHOXYAMPHETAMINE 1 5.48
CHEMBL1201201 METHAMPHETAMINE 4.0 1 5.28
CHEMBL382757 1 5.13
CHEMBL69700 1 4.86
CHEMBL195390 1 4.79
CHEMBL1927027 1 -
CHEMBL253811 NORDEXFENFLURAMINE 1 -
CHEMBL250881 1 -
CHEMBL317634 1 -
CHEMBL1927028 1 -
CHEMBL1927029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE EC50 = 101.0 nM 7.00
CHEMBL1230845 EC50 = 424.0 nM 6.37
CHEMBL102594 EC50 = 900.0 nM 6.05
CHEMBL612 DEXTROAMPHETAMINE EC50 = 1010.0 nM 6.00
CHEMBL1788307 EC50 = 1350.0 nM 5.87
CHEMBL19393 LEVAMFETAMINE EC50 = 1860.0 nM 5.73
CHEMBL468880 EC50 = 2140.0 nM 5.67
CHEMBL1927025 EC50 = 2480.0 nM 5.61
CHEMBL1927030 LEVMETAMFETAMINE EC50 = 2500.0 nM 5.60
CHEMBL1927026 (S)-M-METHOXYAMPHETAMINE EC50 = 3300.0 nM 5.48
CHEMBL1201201 METHAMPHETAMINE EC50 = 5300.0 nM 5.28
CHEMBL382757 EC50 = 7400.0 nM 5.13
CHEMBL69700 EC50 = 13900.0 nM 4.86
CHEMBL195390 EC50 = 16100.0 nM 4.79
CHEMBL1927027 EC50 - -
CHEMBL253811 NORDEXFENFLURAMINE EC50 - -
CHEMBL250881 EC50 - -
CHEMBL317634 EC50 - -
CHEMBL1927028 EC50 - -
CHEMBL1927029 EC50 - -