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.

CCR7 (human):3 nM (kd)

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].