CMPD101

Names

[ Name ]:
CMPD101

[Synonym ]:
3-({[4-Methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl}amino)-N-[2-(trifluoromethyl)benzyl]benzamide
Benzamide, 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-
CMPD101

Biological Activity

[Description]:

CMPD101, is a novel membrane-permeable, small-molecule inhibitor of both GRK2 and GRK3 with IC50s of 18 nM and 5.4 nM. CMPD101 also inhibits ROCK-2 and PKCα (IC50s=1.4 μM and 8.1 μM, respectively)[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Cell Cycle/DNA Damage >> ROCK

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> Stem Cell/Wnt >> ROCK

Signaling Pathways >> TGF-beta/Smad >> ROCK

[Target]

GRK2:18 nM (IC50)

GRK3:5.4 nM (IC50)

PKCα:8.1 μM (IC50)

ROCK2:1.4 μM (IC50)

[References]

[1]. Okawa T, et al. Design, Synthesis, and Evaluation of the Highly Selective and Potent G-Protein-Coupled Receptor Kinase 2 (GRK2) Inhibitor for the Potential Treatment of Heart Failure. J Med Chem. 2017 Aug 24;60(16):6942-6990.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₄H₂₁F₃N₆O

[ Molecular Weight ]:
466.458

[ Exact Mass ]:
466.172882

[ LogP ]:
3.30

[ Index of Refraction ]:
1.622

Related Compounds

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