Details of the Drug-Related molecule(s) Interaction Atlas

General Information of Drug (ID: DMVKZ5I)

• Drug Name: GW9508 Drug Info
• Synonyms: GW-9508; GW 9508

Indication

Disease Entry	ICD 11	Status	REF
Discovery agent	N.A.	Investigative	[1]

• Cross-matching ID:
  PubChem CID: 11595431
  ChEBI ID: CHEBI:93259
  CAS Number: CAS 885101-89-3
  TTD Drug ID: DMVKZ5I

Molecule-Related Drug Atlas

Drug(s) Targeting Free fatty acid receptor 1 (GPR40)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
TAK-875	DMIM5AP	Type-2 diabetes	5A11	Phase 3	[4]
Fasiglifam hemihydrate	DMTGYSO	Type-2 diabetes	5A11	Phase 3	[5]
PBI-4050	DMPXK27	Idiopathic pulmonary fibrosis	CB03.4	Phase 2	[6]
P-1736	DMEYQPN	Diabetic complication	5A2Y	Phase 2	[7]
JTT-851	DMED5J6	Type-2 diabetes	5A11	Phase 2	[8]
SHR0534	DMGFTAI	Type 2 diabetes	5A11	Phase 1	[9]
LY-2881835	DM5EXJV	Type-2 diabetes	5A11	Phase 1	[8]
P11187	DMXZOI0	Type-2 diabetes	5A11	Phase 1	[8]
CPL207-280CA	DMFMGZR	Type 2 diabetes	5A11	Phase 1	[9]
LY2922470	DMGLTE2	Type 2 diabetes	5A11	Phase 1	[10]

Drug(s) Targeting G-protein coupled receptor 120 (GPR120)

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
alpha-linolenic acid	DMY64HE	Discovery agent	N.A.	Investigative	[11]
PMID24997608CA	DML0PFU	Discovery agent	N.A.	Investigative	[12]
grifolic acid	DMGTRZE	Discovery agent	N.A.	Investigative	[13]
TUG-891	DMJRGZT	Discovery agent	N.A.	Investigative	[14]
NCG21	DMMRWJG	Discovery agent	N.A.	Investigative	[15]

Molecular Interaction Atlas of This Drug

Drug Therapeutic Target (DTT)

DTT Name	DTT ID	UniProt ID	MOA	REF
Free fatty acid receptor 1 (GPR40)	TTB8FUC	FFAR1_HUMAN	Agonist	[2]
G-protein coupled receptor 120 (GPR120)	TT08JVB	FFAR4_HUMAN	Agonist	[3]

References

• [1] URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 1050).
• [2] Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small... Br J Pharmacol. 2006 Jul;148(5):619-28.
• [3] Free fatty acid receptors and drug discovery. Biol Pharm Bull. 2008 Oct;31(10):1847-51.
• [4] Efficacy and safety of fasiglifam (TAK-875), a G protein-coupled receptor 40 agonist, in Japanese patients with type 2 diabetes inadequately controlled by diet and exercise: a randomized, double-blind, placebo-controlled, phase III trial. Diabetes Obes Metab. 2015 Jul;17(7):675-81.
• [5] A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1. PLoS One. 2013 Oct 10;8(10):e76280.
• [6] Phase 2 clinical trial of PBI-4050 in patients with idiopathic pulmonary fibrosis. Eur Respir J. 2019 Mar 18;53(3):1800663.
• [7] Discovery of p1736, a novel antidiabetic compound that improves peripheral insulin sensitivity in mice models. PLoS One. 2013 Oct 23;8(10):e77946.
• [8] Treatment of Type 2 Diabetes by Free Fatty Acid Receptor Agonists. Front Endocrinol (Lausanne) 2014; 5: 137.
• [9] Targeting metabolic dysregulation for fibrosis therapy. Nat Rev Drug Discov. 2020 Jan;19(1):57-75.
• [10] The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470). J Med Chem. 2016 Dec 22;59(24):10891-10916.
• [11] Cloning and characterization of the rat free fatty acid receptor GPR120: in vivo effect of the natural ligand on GLP-1 secretion and proliferation of pancreatic beta cells. Naunyn Schmiedebergs Arch Pharmacol. 2008 Jun;377(4-6):515-22.
• [12] A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med. 2014 Aug;20(8):942-7.
• [13] Novel selective ligands for free fatty acid receptors GPR120 and GPR40. Naunyn Schmiedebergs Arch Pharmacol. 2009 Sep;380(3):247-55.
• [14] Discovery of a potent and selective GPR120 agonist. J Med Chem. 2012 May 10;55(9):4511-5.
• [15] Identification of G protein-coupled receptor 120-selective agonists derived from PPARgamma agonists. J Med Chem. 2008 Dec 11;51(23):7640-4.