Table 1.
Compound | MC4R cells |
Dual Express |
Fold increase‡ | CCK2R cells |
Dual Express |
Fold increase‡ | ||||
Ki or Kd nM | n¶ | Ki or Kd nM | n | Ki or Kd nM | n | Ki or Kd nM | n | |||
htMVL 1* | 353.6 ± 97.1 | 4 | 14.6 ± 1.4 | 4 | 24.2§ | 237.5 ± 26.5 | 4 | 88.9 ± 9.2 | 4 | 2.7§ |
htMVL 2† | 381.4 ± 15.0 | 3 | 16.7 ± 2.0 | 4 | 22.9§ | 31.3 ± 1.2 | 3 | 16.7 ± 2.0 | 4 | 1.9§ |
*htMVL1 is expressed as Ki value. For MC4R receptors, Ki values were calculated with the equation Ki = IC50/(1+([ligand]/Kd), where IC50 values from competition binding assays; [ligand] = 10 nM Eu-NDP-α-MSH; Kd = 8.3 nM. For CCK2R receptor, where [ligand] = 1 nM Eu-CCK; Kd = 35 nM.
†htMVL 2 is expressed as Kd value from saturation binding assay.
‡Ratio of monovalent (MC4R or CCK2R cells) to bivalent binding (dual receptor expressing cells).
§P < 0.05 (MC4R or CCK2R cells vs. dual receptor expressing cells).
¶n refers to the number of independent binding experiments.