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CCR7 Ligand 1

Names

[ CAS No. ]:
681514-83-0

[ Name ]:
CCR7 Ligand 1

Biological Activity

[Description]:

CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM[1].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> CCR
Research Areas >> Cancer
Signaling Pathways >> Immunology/Inflammation >> CCR
Signaling Pathways >> PROTAC >> Ligand for E3 Ligase

[Target]

Human CCR7:3 nM (Kd)

Cereblon


[In Vitro]

CCR7 Ligand 1 (CCR7-Cmp2105) binds to a pocket at the intracellular part of CCR7 between the ends of TM1, TM2, TM3, and TM6 and the loop between TM7 and H8[1]. CCR7 Ligand 1 allosterically inhibits binding of the native chemokine CCL19 ligand in scintillation proximity assays (bottom) with an IC50 of 35 nM[1]. CCR7 Ligand 1 (20, 40, 60, 80, 100 μM) has dose-dependent thermo-stabilizing effect on CCR7[1].

[References]

[1]. Jaeger K, et al. Structural Basis for Allosteric Ligand Recognition in the Human CC Chemokine Receptor 7. Cell. 2019 Aug 22;178(5):1222-1230.e10.

Chemical & Physical Properties

[ Molecular Formula ]:
C22H29N5O5S

[ Molecular Weight ]:
475.56

Related Compounds