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Assay Detail

CHEMBL2060786

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

Functional
Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Free fatty acid receptor 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent and selective GPR120 agonist.
Shimpukade B, Hudson BD, Hovgaard CK, Milligan G, Ulven T.
J Med Chem (2012) 55 : 4511 -4515
PubMed 22519963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 38 6.30 7.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1773261 1 7.89
CHEMBL1688465 1 7.78
CHEMBL207881 GW9508 1 7.55
CHEMBL1688458 1 7.20
CHEMBL1773254 1 7.12
CHEMBL1773258 1 7.08
CHEMBL1773257 1 7.04
CHEMBL234057 1 7.01
CHEMBL2058530 1 6.96
CHEMBL1688454 1 6.81
CHEMBL1773252 1 6.78
CHEMBL1773256 1 6.70
CHEMBL234269 1 6.66
CHEMBL394666 1 6.62
CHEMBL2058531 1 6.39
CHEMBL1773253 1 6.34
CHEMBL2058522 1 6.29
CHEMBL2058519 1 6.28
CHEMBL1688452 BENZYLOXYPHENYLPROPANOIC ACID 1 6.26
CHEMBL2058529 1 6.22
CHEMBL2058518 1 6.22
CHEMBL2058520 1 6.20
CHEMBL2058527 1 6.20
CHEMBL1688457 1 6.17
CHEMBL1773255 1 6.13
CHEMBL2058523 1 6.07
CHEMBL2058521 1 6.03
CHEMBL2058532 1 6.02
CHEMBL234834 1 5.94
CHEMBL2058524 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1773261 EC50 = 12.88 nM 7.89
CHEMBL1688465 EC50 = 16.6 nM 7.78
CHEMBL207881 GW9508 EC50 = 28.18 nM 7.55
CHEMBL1688458 EC50 = 63.1 nM 7.20
CHEMBL1773254 EC50 = 75.86 nM 7.12
CHEMBL1773258 EC50 = 83.18 nM 7.08
CHEMBL1773257 EC50 = 91.2 nM 7.04
CHEMBL234057 EC50 = 97.72 nM 7.01
CHEMBL2058530 EC50 = 109.65 nM 6.96
CHEMBL1688454 EC50 = 154.88 nM 6.81
CHEMBL1773252 EC50 = 165.96 nM 6.78
CHEMBL1773256 EC50 = 199.53 nM 6.70
CHEMBL234269 EC50 = 218.78 nM 6.66
CHEMBL394666 EC50 = 239.88 nM 6.62
CHEMBL2058531 EC50 = 407.38 nM 6.39
CHEMBL1773253 EC50 = 457.09 nM 6.34
CHEMBL2058522 EC50 = 512.86 nM 6.29
CHEMBL2058519 EC50 = 524.81 nM 6.28
CHEMBL1688452 BENZYLOXYPHENYLPROPANOIC ACID EC50 = 549.54 nM 6.26
CHEMBL2058529 EC50 = 602.56 nM 6.22
CHEMBL2058518 EC50 = 602.56 nM 6.22
CHEMBL2058520 EC50 = 630.96 nM 6.20
CHEMBL2058527 EC50 = 630.96 nM 6.20
CHEMBL1688457 EC50 = 676.08 nM 6.17
CHEMBL1773255 EC50 = 741.31 nM 6.13
CHEMBL2058523 EC50 = 851.14 nM 6.07
CHEMBL2058521 EC50 = 933.25 nM 6.03
CHEMBL2058532 EC50 = 954.99 nM 6.02
CHEMBL2058524 EC50 = 1148.15 nM 5.94
CHEMBL234834 EC50 = 1148.15 nM 5.94
CHEMBL2058525 EC50 = 2041.74 nM 5.69
CHEMBL8739 LINOLENIC ACID EC50 = 2884.03 nM 5.54
CHEMBL2058528 EC50 = 3548.13 nM 5.45
CHEMBL2058526 EC50 = 4466.84 nM 5.35
CHEMBL1773259 EC50 = 4786.3 nM 5.32
CHEMBL463785 EC50 = 9772.37 nM 5.01
CHEMBL1688455 EC50 = 10000.0 nM 5.00
CHEMBL2058533 EC50 = 64565.42 nM 4.19