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Assay Detail

CHEMBL4404862

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

Functional
Agonist activity at human FFA3 receptor stably expressed in Flp-In T-Rex HEK293 cells cotransfected with eYFP assessed as inhibition of forskolin-induced cAMP production measured after 1 hr by fluorescence plate reader assay
64
Total Activities
64
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Free fatty acid receptor 3 (CHEMBL5201)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators.
Ulven ER, Quon T, Sergeev E, Barki N, Brvar M, Hudson BD, Dutta P, Hansen AH, Bielefeldt LØ, Tobin AB, McKenzie CJ, Milligan G, Ulven T.
J Med Chem (2020) 63 : 3577 -3595
PubMed 32141297 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 53 5.72 6.89
pEC50 11 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4564389 1 6.89
CHEMBL4436229 1 6.84
CHEMBL4530642 1 6.79
CHEMBL4567723 1 6.72
CHEMBL4547569 1 6.61
CHEMBL4581781 1 6.60
CHEMBL4442868 1 6.60
CHEMBL4513816 1 6.54
CHEMBL4567192 1 6.43
CHEMBL4448591 1 6.28
CHEMBL4569482 1 6.27
CHEMBL4547759 1 6.22
CHEMBL4440835 1 6.19
CHEMBL4545039 1 6.16
CHEMBL4452922 1 6.15
CHEMBL4592426 1 6.06
CHEMBL4439667 1 6.00
CHEMBL4450056 1 5.97
CHEMBL4476587 1 5.96
CHEMBL4449702 1 5.96
CHEMBL4457531 1 5.92
CHEMBL4578663 1 5.91
CHEMBL4574477 1 5.87
CHEMBL4471380 1 5.86
CHEMBL4584743 1 5.86
CHEMBL4470372 1 5.80
CHEMBL4570341 1 5.79
CHEMBL4517214 1 5.79
CHEMBL4443263 1 5.78
CHEMBL4470404 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4564389 EC50 = 128.82 nM 6.89
CHEMBL4436229 EC50 = 144.54 nM 6.84
CHEMBL4530642 EC50 = 162.18 nM 6.79
CHEMBL4567723 EC50 = 190.55 nM 6.72
CHEMBL4547569 EC50 = 245.47 nM 6.61
CHEMBL4581781 EC50 = 251.19 nM 6.60
CHEMBL4442868 EC50 = 251.19 nM 6.60
CHEMBL4513816 EC50 = 288.4 nM 6.54
CHEMBL4567192 EC50 = 371.54 nM 6.43
CHEMBL4448591 EC50 = 524.81 nM 6.28
CHEMBL4569482 EC50 = 537.03 nM 6.27
CHEMBL4547759 EC50 = 602.56 nM 6.22
CHEMBL4440835 EC50 = 645.65 nM 6.19
CHEMBL4545039 EC50 = 691.83 nM 6.16
CHEMBL4452922 EC50 = 707.95 nM 6.15
CHEMBL4592426 EC50 = 870.96 nM 6.06
CHEMBL4439667 EC50 = 1000.0 nM 6.00
CHEMBL4450056 EC50 = 1071.52 nM 5.97
CHEMBL4476587 EC50 = 1096.48 nM 5.96
CHEMBL4449702 EC50 = 1096.48 nM 5.96
CHEMBL4457531 EC50 = 1202.26 nM 5.92
CHEMBL4578663 EC50 = 1230.27 nM 5.91
CHEMBL4574477 EC50 = 1348.96 nM 5.87
CHEMBL4471380 EC50 = 1380.38 nM 5.86
CHEMBL4584743 EC50 = 1380.38 nM 5.86
CHEMBL4470372 EC50 = 1584.89 nM 5.80
CHEMBL4517214 EC50 = 1621.81 nM 5.79
CHEMBL4570341 EC50 = 1621.81 nM 5.79
CHEMBL4443263 EC50 = 1659.59 nM 5.78
CHEMBL4470404 EC50 = 1778.28 nM 5.75
CHEMBL4579352 EC50 = 1949.84 nM 5.71
CHEMBL4516265 EC50 = 2511.89 nM 5.60
CHEMBL4446232 EC50 = 2818.38 nM 5.55
CHEMBL4462079 EC50 = 3388.44 nM 5.47
CHEMBL4440699 EC50 = 3548.13 nM 5.45
CHEMBL4451216 EC50 = 3630.78 nM 5.44
CHEMBL4473184 EC50 = 4168.69 nM 5.38
CHEMBL4473169 EC50 = 4897.79 nM 5.31
CHEMBL4569894 EC50 = 5495.41 nM 5.26
CHEMBL4560771 EC50 = 6760.83 nM 5.17
CHEMBL4551085 EC50 = 6760.83 nM 5.17
CHEMBL4476349 EC50 = 7762.47 nM 5.11
CHEMBL4447610 EC50 = 10000.0 nM 5.00
CHEMBL4470184 EC50 = 10000.0 nM 5.00
CHEMBL4466772 EC50 = 10471.29 nM 4.98
CHEMBL4446176 EC50 = 10471.29 nM 4.98
CHEMBL4472390 EC50 = 11220.18 nM 4.95
CHEMBL14021 PROPIONIC ACID EC50 = 11748.98 nM 4.93
CHEMBL4516837 EC50 = 22387.21 nM 4.65
CHEMBL4483052 EC50 = 35481.34 nM 4.45