BDBM22496 3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propanoic acid::CHEMBL207881::carboxylic acid agonist, 2

SMILES c1ccc(cc1)Oc2cccc(c2)CNc3ccc(cc3)CCC(=O)O

InChI Key InChIKey=DGENZVKCTGIDRZ-UHFFFAOYSA-N

Data  1 KI  24 EC50

PDB links: 1 PDB ID matches this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 25 hits for monomerid = 22496   

TargetFree fatty acid receptor 4(Human)
University of Southern Denmark

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  1.41E+3nMAssay Description:Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetFree fatty acid receptor 4(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  3.50E+3nMAssay Description:Agonist activity at GPR120 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMedPDB3D3D Structure (crystal)
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  48nMAssay Description:Agonist activity at GPR40 (unknown origin)More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/19/2024
Entry Details
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  50nMAssay Description:Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hr...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/18/2022
Entry Details Article
PubMed
TargetFree fatty acid receptor 4(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  3.16E+3nMAssay Description:Agonist activity at human FFA4 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at every 1 secs for 6...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  50nMAssay Description:Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interv...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/25/2022
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  65nMAssay Description:Agonist potency at human GPR40 expressed in CHO cellsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
8/23/2020
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  48nMAssay Description:Agonist activity at human GPR40 expressed in HEK293 cells assessed as increase in calcium flux measured every 2 secs for 90 secs by Calcium-3 dye bas...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMed
TargetFree fatty acid receptor 4(Human)
University of Southern Denmark

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  3.50E+3nMAssay Description:Agonist activity at human GPR120 expressed in baculovirus infected sf9 cells assessed as increase in calcium flux measured every 1 sec for 60 secs by...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/17/2020
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  50nMAssay Description:Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
7/18/2020
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  47.9nMAssay Description:Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
1/11/2010
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  100nMAssay Description:Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSAMore data for this Ligand-Target Pair
In Depth
Date in BDB:
9/1/2010
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  47.9nMAssay Description:Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  79nMT: 2°CAssay Description:The reporter assay for the stable hGPR40-Gal4-Elk1/5xGal4-luc+-expressing CHO cells was first carried out in the serum-free medium in the presence of...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/30/2008
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  28.2nMAssay Description:Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/22/2013
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  28nMAssay Description:Agonist activity at human C-terminal eYFP-tagged FFA1 receptor expressed in HEK-293 cells assessed as beta-arrestin2 recruitment incubated for 5 mins...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/23/2017
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  1.78E+4nMAssay Description:Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  6.80E+3nMAssay Description:Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  2.20E+3nMAssay Description:Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50: >3.00E+4nMAssay Description:Agonist activity at human GPR40 H137A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  1.20E+3nMAssay Description:Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calciumMore data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  316nMAssay Description:Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylationMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/14/2016
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Rat)
Daiichi Sankyo

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  99nMAssay Description:Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataEC50:  13nMAssay Description:Agonist activity at human GPR40 expressed in CHO cells by calcium flux assayMore data for this Ligand-Target Pair
In Depth
Date in BDB:
2/11/2015
Entry Details Article
PubMed
TargetFree fatty acid receptor 1(Human)
University of Siena

Curated by ChEMBL
LigandPNGBDBM22496(CHEMBL207881 | 3-(4-{[(3-phenoxyphenyl)methyl]amin...)
Affinity DataKi:  219nMAssay Description:Displacement of 3-(2-Fluoro-4-((2'-methyl-4'-(2-(2-((7-nitrobenzo[c][1,2,5]-oxadiazol-4-yl)amino)ethoxy)ethoxy)-[1,1'-biphenyl]-3-yl)-methoxy)phenyl)...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/23/2017
Entry Details Article
PubMed