1. GPCR/G Protein PI3K/Akt/mTOR
  2. Prostaglandin Receptor PDK-1
  3. CRTh2 antagonist 3

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation.

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CRTh2 antagonist 3 Chemical Structure

CRTh2 antagonist 3 Chemical Structure

CAS No. : 312928-72-6

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Description

CRTh2 antagonist 3 is a potent chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTh2) antagonist[1]. CRTh2 antagonist 3 enhances the activity of PDK1 toward a short peptide substrate, with an EC50 of 2 μM and a Kd of 8.4 μM. CRTh2 antagonist 3 has the potential for cardiovascular inflammation[2].

IC50 & Target

CRTh2[1]
EC50: 2 μM (PDK1)[2]
Ki: 8.4 μM (PDK1)[2]

In Vitro

CRTh2 antagonist 3 (compound 4) is a small-molecule allosteric modulator of the protein kinase PDK1 from structure-based docking. CRTh2 antagonist 3 is 5-fold more potent than its parent compound[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

356.44

Formula

C19H20N2O3S

CAS No.
SMILES

O=C(O)CN1C2=CC=CC=C2N=C1SCCOC3=C(C)C=CC=C3C

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CRTh2 antagonist 3
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HY-135773
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