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Assay Detail

CHEMBL3874977

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Binding
Agonist activity at mouse GPR120 assessed as induction of beta-arrestin recruitment
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Free fatty acid receptor 4 (CHEMBL2052036)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists.
Cox JM, Chu HD, Chelliah MV, Debenham JS, Eagen K, Lan P, Lombardo M, London C, Plotkin MA, Shah U, Sun Z, Vaccaro HM, Venkatraman S, Suzuki T, Wang N, Ashley ER, Crespo A, Madeira M, Leung DH, Alleyne C, Ogawa AM, Souza S, Thomas-Fowlkes B, Di Salvo J, Weinglass A, Kirkland M, Pachanski M, Powles MA, Tozzo E, Akiyama TE, Ujjainwalla F, Tata JR, Sinz CJ.
ACS Med Chem Lett (2017) 8 : 49 -54
PubMed 28105274 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 6.91 7.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3896657 1 7.68
CHEMBL3909872 1 7.46
CHEMBL3933619 1 6.50
CHEMBL3906716 1 6.00
CHEMBL3964985 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3896657 EC50 = 21.0 nM 7.68
CHEMBL3909872 EC50 = 35.0 nM 7.46
CHEMBL3933619 EC50 = 320.0 nM 6.50
CHEMBL3906716 EC50 = 990.0 nM 6.00
CHEMBL3964985 EC50 > 10000.0 nM -