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Assay Detail

CHEMBL2213508

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

Functional
Agonist activity at human TAAR1 receptor expressed in HEK293 cells after 30 mins
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Optimisation of imidazole compounds as selective TAAR1 agonists: discovery of RO5073012.
Galley G, Stalder H, Goergler A, Hoener MC, Norcross RD.
Bioorg Med Chem Lett (2012) 22 : 5244 -5248
PubMed 22795332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.58 8.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2206890 1 8.34
CHEMBL2206404 1 8.17
CHEMBL2206375 1 7.64
CHEMBL2206381 1 7.43
CHEMBL2206388 1 7.40
CHEMBL2206371 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2206890 EC50 = 4.6 nM 8.34
CHEMBL2206404 EC50 = 6.8 nM 8.17
CHEMBL2206375 EC50 = 23.0 nM 7.64
CHEMBL2206381 EC50 = 37.0 nM 7.43
CHEMBL2206388 EC50 = 40.0 nM 7.40
CHEMBL2206371 EC50 = 320.0 nM 6.50