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Assay Detail

CHEMBL2166567

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Functional
Agonist activity at GPR120 assessed as stimulation of calcium mobilization
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Free fatty acid receptor 4 (CHEMBL5339)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Free fatty acid receptor 1 (FFA1/GPR40) agonists: mesylpropoxy appendage lowers lipophilicity and improves ADME properties.
Christiansen E, Due-Hansen ME, Urban C, Grundmann M, Schröder R, Hudson BD, Milligan G, Cawthorne MA, Kostenis E, Kassack MU, Ulven T.
J Med Chem (2012) 55 : 6624 -6628
PubMed 22724451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 4.87 5.37
pEC50 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164240 1 5.37
CHEMBL1773261 1 5.20
CHEMBL1688473 1 5.08
CHEMBL2164239 1 5.07
CHEMBL2163924 1 4.96
CHEMBL2164242 1 4.36
CHEMBL2164241 1 4.03
CHEMBL2163925 1 -
CHEMBL2163923 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164240 EC50 = 4265.8 nM 5.37
CHEMBL1773261 EC50 = 6309.57 nM 5.20
CHEMBL1688473 EC50 = 8317.64 nM 5.08
CHEMBL2164239 EC50 = 8511.38 nM 5.07
CHEMBL2163924 EC50 = 10964.78 nM 4.96
CHEMBL2164242 EC50 = 43651.58 nM 4.36
CHEMBL2164241 EC50 = 93325.43 nM 4.03
CHEMBL2163925 pEC50 - -
CHEMBL2163923 pEC50 - -