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 2778		9.3 null [pIC50]

Conditions

Condition	Modality	Highest Phase	Product
Obesity 203 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 235 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19182070	Primary	Basic research	Unknown Approved Use Unknown
Anxiety 267 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19182070	Primary	Basic research	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
		252160261
The discovery and optimization of pyrimidinone-containing MCH R1 antagonists.	2006 Sep 15	16870432
Preclinical evaluation of melanin-concentrating hormone receptor 1 antagonism for the treatment of obesity and depression.	2009 May	19182070
Suppression of alcohol self-administration and reinstatement of alcohol seeking by melanin-concentrating hormone receptor 1 (MCH1-R) antagonism in Wistar rats.	2010 Sep	20628734

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 `Sat Dec 16 10:58:52 GMT 2023` Edited by `admin` on `Sat Dec 16 10:58:52 GMT 2023`
Record UNII	4R0136W1PR
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

GW-803430

Common Name

English

GW-3430

Code

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