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Assay Detail

CHEMBL2389880

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Functional
Agonist activity at human FFA1 receptor transfected in human 1321N1 cells by calcium mobilization assay
23
Total Activities
22
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

Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes.
Christiansen E, Hansen SV, Urban C, Hudson BD, Wargent ET, Grundmann M, Jenkins L, Zaibi M, Stocker CJ, Ullrich S, Kostenis E, Kassack MU, Milligan G, Cawthorne MA, Ulven T.
ACS Med Chem Lett (2013) 4 : 441 -445
PubMed 23687558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 6.97 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2386353 2 8.22
CHEMBL2386363 1 7.77
CHEMBL2386355 1 7.74
CHEMBL2386364 1 7.74
CHEMBL2315528 1 7.70
CHEMBL2386362 1 7.65
CHEMBL2386361 1 7.48
CHEMBL2386359 1 7.45
CHEMBL2386365 1 7.42
CHEMBL449588 1 7.34
CHEMBL2386354 1 7.13
CHEMBL2386360 1 6.85
CHEMBL2386358 1 6.84
CHEMBL488384 1 6.70
CHEMBL2386369 1 6.44
CHEMBL2386371 1 6.43
CHEMBL2386368 1 6.21
CHEMBL2386370 1 6.14
CHEMBL2386366 1 5.84
CHEMBL2386367 1 5.71
CHEMBL2386356 1 5.67
CHEMBL2386357 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2386353 EC50 = 6.0 nM 8.22
CHEMBL2386353 EC50 = 6.166 nM 8.21
CHEMBL2386363 EC50 = 16.98 nM 7.77
CHEMBL2386355 EC50 = 18.2 nM 7.74
CHEMBL2386364 EC50 = 18.2 nM 7.74
CHEMBL2315528 EC50 = 19.95 nM 7.70
CHEMBL2386362 EC50 = 22.39 nM 7.65
CHEMBL2386361 EC50 = 33.11 nM 7.48
CHEMBL2386359 EC50 = 35.48 nM 7.45
CHEMBL2386365 EC50 = 38.02 nM 7.42
CHEMBL449588 EC50 = 45.71 nM 7.34
CHEMBL2386354 EC50 = 74.13 nM 7.13
CHEMBL2386360 EC50 = 141.25 nM 6.85
CHEMBL2386358 EC50 = 144.54 nM 6.84
CHEMBL488384 EC50 = 199.53 nM 6.70
CHEMBL2386369 EC50 = 363.08 nM 6.44
CHEMBL2386371 EC50 = 371.54 nM 6.43
CHEMBL2386368 EC50 = 616.6 nM 6.21
CHEMBL2386370 EC50 = 724.44 nM 6.14
CHEMBL2386366 EC50 = 1445.44 nM 5.84
CHEMBL2386367 EC50 = 1949.84 nM 5.71
CHEMBL2386356 EC50 = 2137.96 nM 5.67
CHEMBL2386357 EC50 = 2511.89 nM 5.60