Inxight Drugs

U.S. Department of Health & Human Services Divider Arrow

National Institutes of Health Divider Arrow

NCATS

This repository is under review for potential modification in compliance with Administration directives.

Return Home Inxight Drugs

Home
Browse Drugs
Search
- Structure Search
- Sequence Search
Downloads
About

Show Filters

Hide Filters

Primary Target

Isoprenylcysteine carboxyl methyltransferase

2

Histamine H1 receptor

316

Dopamine D2 receptor

311

DNA

282

Serotonin 2a (5-HT2a) receptor

237

All Match

Any Match

Exclude Selected

Exclude Selected

Development Status

Investigational

1

Other

1

All Match

Any Match

Exclude Selected

Exclude Selected

Highest Phase

Phase II

1

All Match

Any Match

Exclude Selected

Exclude Selected

Approval Year

Unknown

2

All Match

Any Match

Exclude Selected

Exclude Selected

Condition

Non-small cell lung cancer

1

Pancreatic cancer

1

All Match

Any Match

Exclude Selected

Exclude Selected

Treatment Modality

Primary

1

All Match

Any Match

Exclude Selected

Exclude Selected

Originator

Marciano, D. et al.

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Class

Chemical

2

All Match

Any Match

Exclude Selected

Exclude Selected

Code System

CAS

2

EPA CompTox

2

FDA UNII

2

PUBCHEM

2

ChEMBL

1

All Match

Any Match

Exclude Selected

Exclude Selected

Substance Form

Principal Form

2

All Match

Any Match

Exclude Selected

Exclude Selected

Showing 1 - 2 of 2 results

First page disabled
Previous page disabled
1
Next page disabled
Next page disabled

SALIRASIB

MZH0OM550M

Export Data
Search for Structure

Status:

Investigational

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Ras protein signal transduction

Isoprenylcysteine carboxyl methyltransferase

Conditions:

Non-small cell lung cancer

Pancreatic cancer

Salirasib or S-trans,trans-Farnesylthiosalicylic acid (FTS) is a salicylic acid derivative with potential antineoplastic activity. It acts as a potent competitive inhibitor of the enzyme prenylated protein methyltransferase (PPMTase), which methylate...

s the carboxyl-terminal S-prenylcysteine in a large number of prenylated proteins including Ras. In such systems, Salirasib inhibits Ras methylation but not Ras farnesylation. Salirasib selectively disrupts the association of chronically active Ras proteins with the plasma membrane. Salirasib competes with Ras for binding to Ras-escort proteins, which possess putative farnesyl-binding domains and interact only with the activated form of Ras proteins, thereby promoting Ras nanoclusterization in the plasma membrane and robust signals. Salirasib was studied in the clinical trials in patients with solid tumors, however its development was discontinued.

CYSMETHYNIL

R5MT8HFQ9E

Export Data
Search for Structure

Status:

Other

Class (Stereo):

CHEMICAL (ACHIRAL)

Targets:

Isoprenylcysteine carboxyl methyltransferase

HHS VULNERABILITY DISCLOSURE

For language access assistance, contact the NCATS Public Information Officer

National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966


			version 1.1