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| Target/Host (Institution) | Ligand | Target/Host Links | Ligand Links | Trg + Lig Links | Ki nM | ΔG° kJ/mole | IC50 nM | Kd nM | EC50/IC50 nM | koff s-1 | kon M-1s-1 | pH | Temp °C |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet  | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | 219 | n/a | n/a | n/a | n/a | n/a | n/a | n/a | n/a |
University of Southern Denmark Curated by ChEMBL | Assay 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)... | J Med Chem 59: 4849-58 (2016) Article DOI: 10.1021/acs.jmedchem.6b00202 BindingDB Entry DOI: 10.7270/Q24T6M9W | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | n/a | n/a | n/a | n/a | 48 | n/a | n/a | n/a | n/a | |
TBA | Assay Description Antagonist effect against 2-methyl-5-HT activity at 5-HT3 receptor in longitudinal muscle myenteric plexus from guinea pig ileum | Citation and Details | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Rattus norvegicus) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | KEGG UniProtKB/SwissProt GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 99 | n/a | n/a | n/a | n/a |
Daiichi Sankyo Co., Ltd. Curated by ChEMBL | Assay Description Agonist activity at rat GPR40 expressed in CHO cells by calcium flux assay | Bioorg Med Chem Lett 24: 2949-53 (2014) Article DOI: 10.1016/j.bmcl.2014.04.065 BindingDB Entry DOI: 10.7270/Q2WD424Z | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 316 | n/a | n/a | n/a | n/a |
Suez Canal University Curated by ChEMBL | Assay Description Agonist activity at FFAR1 (unknown origin) assessed as increase in ERK1/2 MAP kinase phosphorylation | Bioorg Med Chem Lett 24: 5330-6 (2014) Article DOI: 10.1016/j.bmcl.2014.07.043 BindingDB Entry DOI: 10.7270/Q2PR7XM9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 1.20E+3 | n/a | n/a | n/a | n/a |
National Institute of Diabetes and Digestive and Kidney Diseases Curated by ChEMBL | Assay Description Agonist activity at human GPR40 H86F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium | J Med Chem 50: 2981-9 (2007) Article DOI: 10.1021/jm0614782 BindingDB Entry DOI: 10.7270/Q2XG9QV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | >3.00E+4 | n/a | n/a | n/a | n/a |
National Institute of Diabetes and Digestive and Kidney Diseases Curated by ChEMBL | Assay Description Agonist activity at human GPR40 H137A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium | J Med Chem 50: 2981-9 (2007) Article DOI: 10.1021/jm0614782 BindingDB Entry DOI: 10.7270/Q2XG9QV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 2.20E+3 | n/a | n/a | n/a | n/a |
National Institute of Diabetes and Digestive and Kidney Diseases Curated by ChEMBL | Assay Description Agonist activity at human GPR40 H86A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium | J Med Chem 50: 2981-9 (2007) Article DOI: 10.1021/jm0614782 BindingDB Entry DOI: 10.7270/Q2XG9QV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 6.80E+3 | n/a | n/a | n/a | n/a |
National Institute of Diabetes and Digestive and Kidney Diseases Curated by ChEMBL | Assay Description Agonist activity at human GPR40 H137F mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium | J Med Chem 50: 2981-9 (2007) Article DOI: 10.1021/jm0614782 BindingDB Entry DOI: 10.7270/Q2XG9QV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 1.78E+4 | n/a | n/a | n/a | n/a |
National Institute of Diabetes and Digestive and Kidney Diseases Curated by ChEMBL | Assay Description Agonist activity at human GPR40 N244A mutant expressed in HEK-EM 293 cells assessed as increase in intracellular calcium | J Med Chem 50: 2981-9 (2007) Article DOI: 10.1021/jm0614782 BindingDB Entry DOI: 10.7270/Q2XG9QV4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 28 | n/a | n/a | n/a | n/a |
University of Southern Denmark Curated by ChEMBL | Assay 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... | J Med Chem 59: 4849-58 (2016) Article DOI: 10.1021/acs.jmedchem.6b00202 BindingDB Entry DOI: 10.7270/Q24T6M9W | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 28.2 | n/a | n/a | n/a | n/a |
University of Southern Denmark Curated by ChEMBL | Assay Description Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay | J Med Chem 55: 4511-5 (2012) Article DOI: 10.1021/jm300215x BindingDB Entry DOI: 10.7270/Q21Z45P4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 47.9 | n/a | n/a | n/a | n/a |
University of Southern Denmark Curated by ChEMBL | Assay Description Agonist activity at human FFA1 receptor expressed in human 1321N1 cells assessed as calcium mobilization by fluorescence spectrophotometry | J Med Chem 54: 6691-703 (2011) Article DOI: 10.1021/jm2005699 BindingDB Entry DOI: 10.7270/Q25T3MRW | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 100 | n/a | n/a | n/a | n/a |
Merck Research Laboratories Curated by ChEMBL | Assay Description Agonist activity at human GPR40 by FLIPR assay in presence of 1% BSA | Bioorg Med Chem Lett 20: 1298-301 (2010) Article DOI: 10.1016/j.bmcl.2009.10.052 BindingDB Entry DOI: 10.7270/Q2QC03KS | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 47.9 | n/a | n/a | n/a | n/a |
University of Southern Denmark Curated by ChEMBL | Assay Description Agonist activity at human FFA1 expressed in CHO cells by Gal4 luciferase reporter gene assay | J Med Chem 51: 7061-4 (2009) Article DOI: 10.1021/jm8010178 BindingDB Entry DOI: 10.7270/Q2D79B8W | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 50 | n/a | n/a | n/a | n/a |
Sungkyunkwan University Curated by ChEMBL | Assay Description Agonist activity at human GPR40 expressed in CHO cells after 24 hrs by NFAT-luciferase reporter gene assay | ACS Med Chem Lett 8: 1336-1340 (2017) Article DOI: 10.1021/acsmedchemlett.7b00460 BindingDB Entry DOI: 10.7270/Q2WW7M7W | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 48 | n/a | n/a | n/a | n/a |
China Pharmaceutical University Curated by ChEMBL | Assay 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... | Bioorg Med Chem Lett 28: 2599-2604 (2018) Article DOI: 10.1016/j.bmcl.2018.06.047 BindingDB Entry DOI: 10.7270/Q2WS8WW2 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 65 | n/a | n/a | n/a | n/a |
GlaxoSmithKline Research and Development Curated by ChEMBL | Assay Description Agonist potency at human GPR40 expressed in CHO cells | Bioorg Med Chem Lett 16: 1840-5 (2006) Article DOI: 10.1016/j.bmcl.2006.01.007 BindingDB Entry DOI: 10.7270/Q2RF5XS9 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 50 | n/a | n/a | n/a | n/a |
TBA | Assay Description Agonist activity at human FFA1 expressed in HEK293 cells assessed as stimulation of intracellular calcium mobilization measured at 2 secs time interv... | Citation and Details Article DOI: 10.1016/j.bmcl.2020.127650 BindingDB Entry DOI: 10.7270/Q21V5JM4 | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 50 | n/a | n/a | n/a | n/a |
TBA | Assay Description Agonist activity at GPR40 (unknown origin) expressed in CHO cells co-expressing luc2P/SRE assessed as firefly luciferase activity incubated for 24 hr... | Citation and Details Article DOI: 10.1021/acs.jmedchem.1c00031 BindingDB Entry DOI: 10.7270/Q2GQ72HD | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 79 | n/a | n/a | n/a | 22 |
GSK | Assay 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... | Bioorg Med Chem Lett 17: 1584-9 (2007) Article DOI: 10.1016/j.bmcl.2006.12.084 BindingDB Entry DOI: 10.7270/Q2862DRR | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
| Free fatty acid receptor 1 (Homo sapiens (Human)) | BDBM22496 (3-(4-{[(3-phenoxyphenyl)methyl]amino}phenyl)propan...) | PDB UniProtKB/SwissProt antibodypedia GoogleScholar AffyNet | Purchase CHEMBL MCE PC cid PC sid PDB UniChem Patents Similars | Article PubMed | n/a | n/a | n/a | n/a | 13 | n/a | n/a | n/a | n/a |
Daiichi Sankyo Co., Ltd. Curated by ChEMBL | Assay Description Agonist activity at human GPR40 expressed in CHO cells by calcium flux assay | Bioorg Med Chem Lett 24: 2949-53 (2014) Article DOI: 10.1016/j.bmcl.2014.04.065 BindingDB Entry DOI: 10.7270/Q2WD424Z | |||||||||||
| More data for this Ligand-Target Pair | |||||||||||||
