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Assay Detail

CHEMBL1775392

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Functional
Agonist activity at human FFA1 transfected in 1321N1 cells under serum-free condition after 1 hr by dose response curve/dynamic mass redistribution optical biosensor assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469.
Christiansen E, Due-Hansen ME, Urban C, Merten N, Pfleiderer M, Karlsen KK, Rasmussen SS, Steensgaard M, Hamacher A, Schmidt J, Drewke C, Petersen RK, Kristiansen K, Ullrich S, Kostenis E, Kassack MU, Ulven T.
ACS Med Chem Lett (2010) 1 : 345 -349
PubMed 24900217 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.80 7.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773261 1 7.46
CHEMBL207881 GW9508 1 7.06
CHEMBL1688465 1 6.58
CHEMBL1688452 BENZYLOXYPHENYLPROPANOIC ACID 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773261 EC50 = 34.67 nM 7.46
CHEMBL207881 GW9508 EC50 = 87.1 nM 7.06
CHEMBL1688465 EC50 = 263.03 nM 6.58
CHEMBL1688452 BENZYLOXYPHENYLPROPANOIC ACID EC50 = 831.76 nM 6.08