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Assay Detail

CHEMBL3868258

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

Functional
Agonist activity at human GPR120 expressed in CHOK1 cells measured after 60 mins by IP1-HTRF assay
38
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of benzofuran propanoic acid GPR120 agonists: From uHTS hit to mechanism-based pharmacodynamic effects.
Lombardo M, Bender K, London C, Plotkin MA, Kirkland M, Mane J, Pachanski M, Geissler W, Cummings J, Habulihaz B, Akiyama TE, Di Salvo J, Madeira M, Pols J, Powles MA, Finley MF, Johnson E, Roussel T, Uebele VN, Crespo A, Leung D, Alleyne C, Trusca D, Lei Y, Howard AD, Ujjainwalla F, Tata JR, Sinz CJ.
Bioorg Med Chem Lett (2016) 26 : 5724 -5728
PubMed 27815121 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 6.71 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3973101 1 7.70
CHEMBL3968947 1 7.24
CHEMBL3953203 1 7.22
CHEMBL3896657 1 7.20
CHEMBL3944507 1 7.18
CHEMBL3920591 1 7.17
CHEMBL3939004 2 7.11
CHEMBL3921062 1 7.08
CHEMBL3938783 1 7.06
CHEMBL3909872 1 7.03
CHEMBL3927879 1 7.01
CHEMBL3985509 1 7.00
CHEMBL3899885 1 6.99
CHEMBL3924759 1 6.92
CHEMBL3985939 1 6.83
CHEMBL3968537 1 6.82
CHEMBL3897776 1 6.77
CHEMBL3916564 1 6.74
CHEMBL3892019 1 6.73
CHEMBL3942922 1 6.73
CHEMBL3947787 1 6.73
CHEMBL3961950 1 6.70
CHEMBL3972973 1 6.69
CHEMBL3961009 1 6.59
CHEMBL3896714 1 6.54
CHEMBL3900990 1 6.51
CHEMBL3984072 1 6.32
CHEMBL3934450 1 6.30
CHEMBL3952316 1 6.26
CHEMBL3940493 1 6.26

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3973101 EC50 = 20.0 nM 7.70
CHEMBL3968947 EC50 = 57.0 nM 7.24
CHEMBL3953203 EC50 = 60.0 nM 7.22
CHEMBL3896657 EC50 = 63.0 nM 7.20
CHEMBL3944507 EC50 = 66.0 nM 7.18
CHEMBL3920591 EC50 = 68.0 nM 7.17
CHEMBL3939004 EC50 = 77.0 nM 7.11
CHEMBL3921062 EC50 = 83.0 nM 7.08
CHEMBL3938783 EC50 = 88.0 nM 7.06
CHEMBL3909872 EC50 = 94.0 nM 7.03
CHEMBL3927879 EC50 = 97.0 nM 7.01
CHEMBL3985509 EC50 = 100.0 nM 7.00
CHEMBL3899885 EC50 = 102.0 nM 6.99
CHEMBL3924759 EC50 = 121.0 nM 6.92
CHEMBL3939004 EC50 = 137.0 nM 6.86
CHEMBL3985939 EC50 = 149.0 nM 6.83
CHEMBL3968537 EC50 = 153.0 nM 6.82
CHEMBL3897776 EC50 = 170.0 nM 6.77
CHEMBL3916564 EC50 = 182.0 nM 6.74
CHEMBL3892019 EC50 = 185.0 nM 6.73
CHEMBL3947787 EC50 = 188.0 nM 6.73
CHEMBL3942922 EC50 = 186.0 nM 6.73
CHEMBL3961950 EC50 = 198.0 nM 6.70
CHEMBL3972973 EC50 = 204.0 nM 6.69
CHEMBL3961009 EC50 = 254.0 nM 6.59
CHEMBL3896714 EC50 = 290.0 nM 6.54
CHEMBL3900990 EC50 = 308.0 nM 6.51
CHEMBL3984072 EC50 = 474.0 nM 6.32
CHEMBL3934450 EC50 = 498.0 nM 6.30
CHEMBL3952316 EC50 = 544.0 nM 6.26
CHEMBL3940493 EC50 = 546.0 nM 6.26
CHEMBL3914253 EC50 = 819.0 nM 6.09
CHEMBL3915765 EC50 = 946.0 nM 6.02
CHEMBL3974501 EC50 = 2999.0 nM 5.52
CHEMBL3943430 EC50 = 8174.0 nM 5.09
CHEMBL3929976 EC50 > 9950.0 nM -
CHEMBL3953859 EC50 > 9950.0 nM -
CHEMBL3980036 EC50 > 9950.0 nM -