Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL946732

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

Functional
Agonist activity at human GPR40 expressed in CHOK1 cells by fluorescence assay
10
Total Activities
5
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 1 (CHEMBL4422)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of diacylphloroglucinols as a new class of GPR40 (FFAR1) agonists.
Bharate SB, Rodge A, Joshi RK, Kaur J, Srinivasan S, Kumar SS, Kulkarni-Almeida A, Balachandran S, Balakrishnan A, Vishwakarma RA.
Bioorg Med Chem Lett (2008) 18 : 6357 -6361
PubMed 18993064 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.95 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470757 DIDODECANOYLPHLOROGLUCINOL 2 7.16
CHEMBL267476 LINOLEIC ACID 2.0 2 6.27
CHEMBL481542 2 6.01
CHEMBL277845 2 5.22
CHEMBL6931 2 5.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470757 DIDODECANOYLPHLOROGLUCINOL EC50 = 70.0 nM 7.16
CHEMBL470757 DIDODECANOYLPHLOROGLUCINOL EC50 = 75.86 nM 7.12
CHEMBL267476 LINOLEIC ACID EC50 = 540.0 nM 6.27
CHEMBL267476 LINOLEIC ACID EC50 = 549.54 nM 6.26
CHEMBL481542 EC50 = 970.0 nM 6.01
CHEMBL481542 EC50 = 977.24 nM 6.01
CHEMBL277845 EC50 = 6000.0 nM 5.22
CHEMBL277845 EC50 = 6025.6 nM 5.22
CHEMBL6931 EC50 = 8000.0 nM 5.10
CHEMBL6931 EC50 = 8128.31 nM 5.09