EO-1428

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H16BrClN2O
Molecular Weight	415.711
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=CC=CC=C1C(=O)C2=CC=C(NC3=CC=C(Br)C=C3N)C=C2Cl

InChI

InChIKey=HDCLCHNAEZNGNV-UHFFFAOYSA-N

InChI=1S/C20H16BrClN2O/c1-12-4-2-3-5-15(12)20(25)16-8-7-14(11-17(16)22)24-19-9-6-13(21)10-18(19)23/h2-11,24H,23H2,1H3

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/21865167

EO 1428 is a selective inhibitor of p38 MAP kinases alpha and beta, that displays no activity at p38 gamma, p38 delta, ERK1/2 and JNK1. It was developed by Leo Pharmaceutical as a topical anti-inflammatory agent. It also inhibits inflammatory cytokines including IL-8, TNF-α, IL-6, IL-1β and IL-10

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
MAP kinase p38 beta 11 Target ID: CHEMBL3961 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14667219	Inhibitor 8504
MAP kinase p38 alpha 34 Target ID: CHEMBL260 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14667219	Inhibitor 8504

Conditions

Condition	Modality	Targets	Highest Phase	Product
Inflammation 105 Sources: https://www.ncbi.nlm.nih.gov/pubmed/14667219	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Reactive oxygen species and p38 mitogen-activated protein kinase mediate tumor necrosis factor α-converting enzyme (TACE/ADAM-17) activation in primary human monocytes.	2011-10-14	21865167
Synthesis and structure-activity relationship of aminobenzophenones. A novel class of p38 MAP kinase inhibitors with high antiinflammatory activity.	2003-12-18	14667219

Patents

Sample Use Guides

In Vivo Use Guide

Unknown

Route of Administration: Unknown

In Vitro Use Guide

CD14+ monocytes were purified from Peripheral blood mononuclear cells (PBMCs) by negative immunomagnetic bead separation. Both 10 μM SB202190 and 1 μM EO 1428 markedly attenuated LPS-induced TACE (Tumor necrosis factor α-converting enzyme )activity up-regulation. Treatment of monocytes with EO 1428 alone resulted in a modest reduction of TACE activity compared with unstimulated cells though this was not significant.

Name

Type

Language

(4-((2-AMINO-4-BROMOPHENYL)AMINO)-2-CHLOROPHENYL)(2-METHYLPHENYL)METHANONE

Preferred Name

English

EO-1428

Common Name

English

METHANONE, (4-((2-AMINO-4-BROMOPHENYL)AMINO)-2-CHLOROPHENYL)(2-METHYLPHENYL)-

Systematic Name

English

Code System Code Type Description

CAS

479543-48-1