Drug intelligence / Profile preview

GSK-626616

Development stage
Phase 1
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

GSK-626616 is a potent, orally bioavailable small molecule inhibitor of dual-specificity tyrosine-regulated kinase 3 (DYRK3), with an IC50 of 0.7 nM. It also inhibits other DYRK family members such as DYRK1A and DYRK2 with similar potency, showing approximately 20-fold selectivity over casein kinase 2 and negligible activity against a broad panel of other kinases. Preclinical studies indicate that GSK‑626616 enhances erythroid colony formation in response to erythropoietin and increases hemoglobin levels in anemic mice, suggesting its potential as a therapy for anemia. The compound was initially developed by GSK for research purposes[1][2][3][4][7].

Other names
(5Z)-2-[(2,6-Dichlorophenyl)amino]-5-(6-quinoxalinylmethylene)-4(5H)-thiazoloneCHEMBL5081787CHEMBL-5081787CHEMBL 5081787OKY0RM282VOKY-0RM282VOKY 0RM282V1025821-33-3
02

Targets

DYRK3 (Dual-specificity tyrosine-phosphorylation-regulated kinase 3)DYRK2 (Dual-specificity tyrosine-phosphorylation-regulated kinase 2)DYRK1A (Dual-specificity tyrosine-phosphorylation-regulated kinase 1A)CK2 (Casein kinase II subunit alpha)

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