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Assay Detail

CHEMBL3872141

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Functional
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as increase in IP1 accumulation after 60 mins by HTRF assay
28
Total Activities
28
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 Chromane Propionic Acid Analogues as Selective Agonists of GPR120 with in Vivo Activity in Rodents.
Adams GL, Velazquez F, Jayne C, Shah U, Miao S, Ashley ER, Madeira M, Akiyama TE, Di Salvo J, Suzuki T, Wang N, Truong Q, Gilbert E, Zhou D, Verras A, Kirkland M, Pachanski M, Powles M, Yin W, Ujjainwalla F, Venkatraman S, Edmondson SD.
ACS Med Chem Lett (2017) 8 : 96 -101
PubMed 28105282 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 7.26 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3952043 1 7.85
CHEMBL3972870 1 7.85
CHEMBL3960738 1 7.82
CHEMBL3940429 1 7.82
CHEMBL3898962 1 7.75
CHEMBL3947070 1 7.68
CHEMBL3890089 1 7.60
CHEMBL3970166 1 7.60
CHEMBL3970238 1 7.55
CHEMBL3946820 1 7.52
CHEMBL3980898 1 7.46
CHEMBL3943315 1 7.43
CHEMBL3909773 1 7.40
CHEMBL3959068 1 7.35
CHEMBL3932664 1 7.29
CHEMBL3907996 1 7.28
CHEMBL3890035 1 7.26
CHEMBL3971308 1 7.16
CHEMBL3959144 1 7.14
CHEMBL3900705 1 7.10
CHEMBL3978465 1 6.89
CHEMBL3960231 1 6.77
CHEMBL3941726 1 6.75
CHEMBL3986721 1 6.66
CHEMBL3916986 1 6.62
CHEMBL3971857 1 6.60
CHEMBL3950444 1 6.50
CHEMBL3979448 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3952043 EC50 = 14.0 nM 7.85
CHEMBL3972870 EC50 = 14.0 nM 7.85
CHEMBL3960738 EC50 = 15.0 nM 7.82
CHEMBL3940429 EC50 = 15.0 nM 7.82
CHEMBL3898962 EC50 = 18.0 nM 7.75
CHEMBL3947070 EC50 = 21.0 nM 7.68
CHEMBL3890089 EC50 = 25.0 nM 7.60
CHEMBL3970166 EC50 = 25.0 nM 7.60
CHEMBL3970238 EC50 = 28.0 nM 7.55
CHEMBL3946820 EC50 = 30.0 nM 7.52
CHEMBL3980898 EC50 = 35.0 nM 7.46
CHEMBL3943315 EC50 = 37.0 nM 7.43
CHEMBL3909773 EC50 = 40.0 nM 7.40
CHEMBL3959068 EC50 = 45.0 nM 7.35
CHEMBL3932664 EC50 = 51.0 nM 7.29
CHEMBL3907996 EC50 = 53.0 nM 7.28
CHEMBL3890035 EC50 = 55.0 nM 7.26
CHEMBL3971308 EC50 = 69.0 nM 7.16
CHEMBL3959144 EC50 = 72.0 nM 7.14
CHEMBL3900705 EC50 = 79.0 nM 7.10
CHEMBL3978465 EC50 = 130.0 nM 6.89
CHEMBL3960231 EC50 = 170.0 nM 6.77
CHEMBL3941726 EC50 = 180.0 nM 6.75
CHEMBL3986721 EC50 = 220.0 nM 6.66
CHEMBL3916986 EC50 = 240.0 nM 6.62
CHEMBL3971857 EC50 = 250.0 nM 6.60
CHEMBL3950444 EC50 = 320.0 nM 6.50
CHEMBL3979448 EC50 = 330.0 nM 6.48