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Custom Receptor Binding Assay Services

Radioligand binding assay methods are preferred to study the binding properties of test compounds in drug discovery, such GPCRs and ion channels. However, the regulatory requirements, high construction and maintenance costs prohibit most of labs from utilizing an exclusive radioisotope-based assay platform.

To address the problem, GenScript has constructed a powerful radioisotope-based assay platform as a low cost solution for your project. Based on the platform, scintillation proximity assay (SPA) and filtration binding assay are available tailored to your specifications. In addition, GenScript has validated many GPCR binding assays and hERG binding assay for your immediate screening.

Filtration Assays

   
Filtration: Saturation Binding Assay   Filtration: Competition Binding Assay
Fig 1. 10 μg of membranes prepared from CHO cells stably expressing ADRA1A receptors were incubated with indicated concentrations of [3H]Prazosin in the absence (total binding) or presence of 1000-fold excess unlabeled Prazosin (nonspecific binding, NSB). Binding was terminated by rapid filtration. Specific binding was defined by subtracting NSB from total binding. Data were fit to one-site binding equation using a non-linear regression method.
Fig 2. 10 μg of membranes prepared from CHO cells stably expressing ADRA1A receptors were incubated with indicated concentrations of Phentolamine in the presence of 1nM [3H]Prazosin. Binding was terminated by rapid filtration. Data were fit to one-site competition equation using a non-linear regression method.

SPA Assays

   
SPA: Saturation Binding Assay
SPA: Competition Binding Assay
Fig 3. 10 μg of membranes prepared from HEK293 cells stably expressing 5-HT2C receptors were incubated with 0.5 mg of WGA SPA beads and increasing concentrations of [3H]5-HT in the absence (total binding) or presence of 1000-fold excess unlabeled 5-HT (nonspecific binding, NSB) overnight at room temperature. Radioactivity was counted on TopCount. Specific binding was defined by subtracting NSB from total binding. Data were fit to one-site binding equation using a non-linear regression method.
Fig 4. 10 μg of membranes prepared from HEK293 cells stably expressing 5-HT2C receptors were incubated with 0.5 mg of WGA SPA beads and increasing concentrations of 5-HT at room temperature overnight in the presence of 25 nM [3H]5-HT. Radioactivity was counted on TopCount. Data were fit to one-site competition equation using a non-linear regression method.
Family
Receptor
Assay Character
Membrane Preparation
Potassium, voltage-gated hERG (Kv11.1) Radioligand Binding Assay
Acetylcholine (muscarinic) M1 / CHRM1 Radioligand Binding Assay
Acetylcholine (muscarinic) M2 / CHRM2 Radioligand Binding Assay
Acetylcholine (muscarinic) M3 / CHRM3 Radioligand Binding Assay
Acetylcholine (muscarinic) M4 / CHRM4 Radioligand Binding Assay
Acetylcholine (muscarinic) M5 / CHRM5 Radioligand Binding Assay
Adrenoceptors ADRA1A Radioligand Binding Assay
Adrenoceptors ADRA1B Radioligand Binding Assay
Adrenoceptors ADRA1D Radioligand Binding Assay
Adrenoceptors ADRB2 Radioligand Binding Assay
Dopamine D1 Radioligand Binding Assay
Dopamine D2S Radioligand Binding Assay
Dopamine D5 Radioligand Binding Assay
Opioid OPRD1 Radioligand Binding Assay
Serotonin 5-HT1A / HTR1A Radioligand Binding Assay
Serotonin 5-HT2C / HTR2C Radioligand Binding Assay
Serotonin 5-HT7 / HTR7 Radioligand Binding Assay
Vasopressin V1B / AVPR1B Radioligand Binding Assay
Vasopressin V2 / AVPR2 Radioligand Binding Assay
Sigma Sigma2 Radioligand Binding Assay
Cat. No. Service
Price (USD)
SC1485
Custom Receptor Binding Assay Services
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