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Assay Detail

CHEMBL4354542

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Functional
Agonist activity at FFA1 receptor (unknown origin) stably expressed in CHO cells assessed as increase in calcium flux by Fluo4-AM based FLIPR assay
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold.
Li Z, Liu C, Yang J, Zhou J, Ye Z, Feng D, Yue N, Tong J, Huang W, Qian H.
Eur J Med Chem (2019) 179 : 608 -622
PubMed 31279294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 29 7.16 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4460582 1 8.32
CHEMBL4575598 1 7.94
CHEMBL1688473 1 7.85
CHEMBL4593950 1 7.80
CHEMBL4438440 1 7.71
CHEMBL4537190 1 7.65
CHEMBL4570807 1 7.62
CHEMBL4534840 1 7.44
CHEMBL4471403 1 7.44
CHEMBL1829174 FASIGLIFAM 3.0 1 7.43
CHEMBL4450552 1 7.41
CHEMBL4442354 1 7.38
CHEMBL4468987 1 7.38
CHEMBL4550165 1 7.34
CHEMBL4461611 1 7.29
CHEMBL4574808 1 7.29
CHEMBL4577954 1 7.23
CHEMBL4537797 1 7.22
CHEMBL3628756 1 7.16
CHEMBL4561122 1 7.16
CHEMBL4458669 1 7.06
CHEMBL4516052 1 6.71
CHEMBL4469534 1 6.65
CHEMBL4464317 1 6.40
CHEMBL4519415 1 6.27
CHEMBL4469691 1 6.14
CHEMBL206880 1 5.69
CHEMBL486145 1 5.43
CHEMBL4442156 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4460582 EC50 = 4.8 nM 8.32
CHEMBL4575598 EC50 = 11.6 nM 7.94
CHEMBL1688473 EC50 = 14.2 nM 7.85
CHEMBL4593950 EC50 = 15.7 nM 7.80
CHEMBL4438440 EC50 = 19.3 nM 7.71
CHEMBL4537190 EC50 = 22.5 nM 7.65
CHEMBL4570807 EC50 = 24.2 nM 7.62
CHEMBL4534840 EC50 = 36.1 nM 7.44
CHEMBL4471403 EC50 = 36.5 nM 7.44
CHEMBL1829174 FASIGLIFAM EC50 = 37.1 nM 7.43
CHEMBL4450552 EC50 = 38.7 nM 7.41
CHEMBL4442354 EC50 = 41.9 nM 7.38
CHEMBL4468987 EC50 = 41.3 nM 7.38
CHEMBL4550165 EC50 = 45.6 nM 7.34
CHEMBL4461611 EC50 = 51.7 nM 7.29
CHEMBL4574808 EC50 = 51.6 nM 7.29
CHEMBL4577954 EC50 = 58.5 nM 7.23
CHEMBL4537797 EC50 = 59.8 nM 7.22
CHEMBL3628756 EC50 = 69.3 nM 7.16
CHEMBL4561122 EC50 = 69.6 nM 7.16
CHEMBL4458669 EC50 = 86.2 nM 7.06
CHEMBL4516052 EC50 = 196.7 nM 6.71
CHEMBL4469534 EC50 = 225.3 nM 6.65
CHEMBL4464317 EC50 = 397.5 nM 6.40
CHEMBL4519415 EC50 = 536.2 nM 6.27
CHEMBL4469691 EC50 = 728.6 nM 6.14
CHEMBL206880 EC50 = 2041.0 nM 5.69
CHEMBL486145 EC50 = 3715.0 nM 5.43
CHEMBL4442156 EC50 > 1000.0 nM -