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Assay Detail

CHEMBL3874983

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Functional
Agonist activity at human GPR120 short isoform expressed in CHOK1 cells assessed as induction of IP1 accumulation after 60 mins by HTRF assay
19
Total Activities
19
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

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 19 5.98 7.01

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3919973 1 7.01
CHEMBL3891920 1 6.89
CHEMBL3973034 1 6.70
CHEMBL3893026 1 6.66
CHEMBL3953289 1 6.44
CHEMBL3901994 1 6.38
CHEMBL3940359 1 6.36
CHEMBL3947837 1 5.92
CHEMBL3977361 1 5.68
CHEMBL3949142 1 5.66
CHEMBL3897637 1 5.57
CHEMBL3954140 1 5.51
CHEMBL3937916 1 5.48
CHEMBL3928591 1 5.46
CHEMBL3969920 1 5.39
CHEMBL3967504 1 5.37
CHEMBL3986483 1 5.24
CHEMBL3920891 1 -
CHEMBL3957767 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3919973 EC50 = 98.0 nM 7.01
CHEMBL3891920 EC50 = 130.0 nM 6.89
CHEMBL3973034 EC50 = 200.0 nM 6.70
CHEMBL3893026 EC50 = 220.0 nM 6.66
CHEMBL3953289 EC50 = 360.0 nM 6.44
CHEMBL3901994 EC50 = 420.0 nM 6.38
CHEMBL3940359 EC50 = 440.0 nM 6.36
CHEMBL3947837 EC50 = 1200.0 nM 5.92
CHEMBL3977361 EC50 = 2100.0 nM 5.68
CHEMBL3949142 EC50 = 2200.0 nM 5.66
CHEMBL3897637 EC50 = 2700.0 nM 5.57
CHEMBL3954140 EC50 = 3100.0 nM 5.51
CHEMBL3937916 EC50 = 3300.0 nM 5.48
CHEMBL3928591 EC50 = 3500.0 nM 5.46
CHEMBL3969920 EC50 = 4100.0 nM 5.39
CHEMBL3967504 EC50 = 4300.0 nM 5.37
CHEMBL3986483 EC50 = 5700.0 nM 5.24
CHEMBL3920891 EC50 > 10000.0 nM -
CHEMBL3957767 EC50 > 10000.0 nM -