GW-803430

Details

Stereochemistry	ACHIRAL
Molecular Formula	C25H24ClN3O3S
Molecular Weight	481.994
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=CC(=CC=C1OCCN2CCCC2)N3C=NC4=C(SC(=C4)C5=CC=C(Cl)C=C5)C3=O

InChI

InChIKey=MWULMTACIBZPGN-UHFFFAOYSA-N

InChI=1S/C25H24ClN3O3S/c1-31-22-14-19(8-9-21(22)32-13-12-28-10-2-3-11-28)29-16-27-20-15-23(33-24(20)25(29)30)17-4-6-18(26)7-5-17/h4-9,14-16H,2-3,10-13H2,1H3

HIDE SMILES / InChI

Molecular Formula	C25H24ClN3O3S
Molecular Weight	481.994
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: http://adisinsight.springer.com/drugs/800021434
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/16870432 | https://www.ncbi.nlm.nih.gov/pubmed/19182070

GW-803430 is centrally active and selective antagonist of melanin-concentrating hormone receptor (MCHR) 1. GlaxoSmithKline was developing orally active, potent and selective GW-803430 for the treatment of obesity. GW803430 produces robust antiobesity and antidepressant-like effects in rodents.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Melanin-concentrating hormone receptor 1 5 Target ID: CHEMBL344 Sources: https://www.ncbi.nlm.nih.gov/pubmed/16870432	Antagonist 2849		9.3 null [pIC50]

Conditions

Condition	Modality	Highest Phase	Product
Obesity 206 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19182070 https://www.ncbi.nlm.nih.gov/pubmed/23512845 https://www.ncbi.nlm.nih.gov/pubmed/22705492	Primary	Basic research	Unknown Approved Use Unknown
Alcohol drinking 1 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20628734	Primary	Basic research	Unknown Approved Use Unknown
Depression 240 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19182070	Primary	Basic research	Unknown Approved Use Unknown
Anxiety 275 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19182070	Primary	Basic research	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats.	2010-09	20628734
Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression.	2009-05	19182070
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.	2006-09-15	16870432

Patents

Sample Use Guides

In Vivo Use Guide

GW803430 attenuated food intake in rats on intermittent access to sucrose at all doses examined (3, 10, 30 mg/kg ip). Effective doses of GW803430 (1 and 3 mg/kg p.o.) were correlated with antiobesity activity in a 14-day study of diet-induced obese rats.

Route of Administration: Other

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Mon Mar 31 23:33:11 GMT 2025` Edited by `admin` on `Mon Mar 31 23:33:11 GMT 2025`
Record UNII	4R0136W1PR
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GW-803430

Common Name

English

GW-3430

Preferred Name

English

THIENO(3,2-D)PYRIMIDIN-4(3H)-ONE, 6-(4-CHLOROPHENYL)-3-(3-METHOXY-4-(2-(1-PYRROLIDINYL)ETHOXY)PHENYL)-

Systematic Name

English

6-(4-CHLOROPHENYL)-3-(3-METHOXY-4-(2-(PYRROLIDIN-1-YL)ETHOXY)PHENYL)THIENO(3,2-D)PYRIMIDIN-4(3H)-ONE

Systematic Name

English

Code System Code Type Description

FDA UNII

4R0136W1PR