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Assay Detail

CHEMBL1930561

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

Functional
Activation of C-terminal HA epitope tagged human TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein, Galpha16 by cAMP accumulation assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trace amine-associated receptor 1 (CHEMBL5857)
Type SINGLE PROTEIN
Organism Homo sapiens

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 19 5.30 6.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL612 DEXTROAMPHETAMINE 4.0 1 6.22
CHEMBL19393 LEVAMFETAMINE 4.0 1 5.89
CHEMBL1201201 METHAMPHETAMINE 4.0 1 5.82
CHEMBL1927026 (S)-M-METHOXYAMPHETAMINE 1 5.72
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE 1 5.53
CHEMBL1230845 1 5.50
CHEMBL1927030 LEVMETAMFETAMINE 2.0 1 5.48
CHEMBL1927028 1 5.30
CHEMBL1927027 1 5.19
CHEMBL1788307 1 5.18
CHEMBL1927025 1 4.93
CHEMBL468880 1 4.81
CHEMBL69700 1 4.50
CHEMBL195390 1 4.13
CHEMBL382757 1 -
CHEMBL250881 1 -
CHEMBL102594 1 -
CHEMBL317634 1 -
CHEMBL1927029 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL612 DEXTROAMPHETAMINE EC50 = 600.0 nM 6.22
CHEMBL19393 LEVAMFETAMINE EC50 = 1300.0 nM 5.89
CHEMBL1201201 METHAMPHETAMINE EC50 = 1500.0 nM 5.82
CHEMBL1927026 (S)-M-METHOXYAMPHETAMINE EC50 = 1900.0 nM 5.72
CHEMBL1927024 (S)-P-HYDROXYAMPHETAMINE EC50 = 2960.0 nM 5.53
CHEMBL1230845 EC50 = 3160.0 nM 5.50
CHEMBL1927030 LEVMETAMFETAMINE EC50 = 3300.0 nM 5.48
CHEMBL1927028 EC50 = 5020.0 nM 5.30
CHEMBL1927027 EC50 = 6500.0 nM 5.19
CHEMBL1788307 EC50 = 6570.0 nM 5.18
CHEMBL1927025 EC50 = 11730.0 nM 4.93
CHEMBL468880 EC50 = 15340.0 nM 4.81
CHEMBL69700 EC50 = 31940.0 nM 4.50
CHEMBL195390 EC50 = 73700.0 nM 4.13
CHEMBL382757 EC50 - -
CHEMBL250881 EC50 - -
CHEMBL102594 EC50 - -
CHEMBL317634 EC50 - -
CHEMBL1927029 EC50 - -