CCR2 ligand-2

CCR2 ligand-2 (compound 14) (0-3000 nM; 30-90 min) selectively binds to the intracellular allosteric binding site of CCR2 on the membrane of HEK293T cells expressing CCR2_GSSG_Nluc, with a K_d value of 266 nM^[1].
CCR2 ligand-2 rapidly binds to and dissociates from the allosteric intracellular binding site of CCR2 on the membrane of HEK293T cells expressing CCR2_GSSG_Nluc, with an association rate constant k_on of 6.00 × 10⁶ M^-1 min^-1 and a dissociation rate constant k_off of 0.101 min^-1[1].
CCR2 ligand-2 (650 nM; 30 min) acts as an effective tracer in membrane-based NanoBRET competition assays to detect the binding affinity of non-fluorescent ligands to the intracellular allosteric binding site of CCR2 on the membrane of HEK293T cells expressing CCR2_GSSG_Nluc, thereby enabling the detection of high-affinity antagonists^[1].
CCR2 ligand-2 (0-2000 nM) penetrates live HEK293T cells expressing CCR2_Nluc and binds to the intracellular allosteric binding site of CCR2 with a K_d of 114 nM; moreover, the binding rate to the allosteric binding site is slower than that in the cell-free membrane system, with a k_on of 4.59 × 10⁴ M^-1 min^-1 and a k_off of 0.247 min^-1[1].
CCR2 ligand-2 (1000 nM; 90 min) acts as an effective tracer in live-cell NanoBRET competition assays for measuring the intracellular binding affinity between non-fluorescent ligands and CCR2 in live HEK293T cells expressing CCR2_Nluc^[1].