OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Targets: 20
Target Family: Class B (secretin) GPCR
Target Subfamilies: Glucagon (6), Calcitonin (7), Corticotropin-Releasing Factor (2), Parathyroid Hormone (2), VIP and PACAP (3)
Rationale: Class B GPCRs regulate key physiological processes, including glucose and calcium homeostasis, pain signaling, and gastrointestinal function, making them important drug targets for diseases such as diabetes, obesity, osteoporosis, cancer, neurodegeneration, cardiovascular, and psychiatric disorders. However, their conserved extracellular domains and similar peptide-binding mechanisms increase the risk of cross-reactivity among closely related receptors.
Testing: Evaluate selective activity at intended receptor(s) while minimizing cross-reactivity with closely related Class B GPCRs.
Mechanism: Activation of stimulatory G protein alpha subunit (Gsα) subunit leads to stimulation of adenylyl cyclase triggering conversion of ATP to cAMP.
Results: 10-point (3-fold) dose-response curves for cAMP production; EC50 values where feasible
No. of Assays on Panel:
20
Assays on Panel:
Family
GPCR
Name
CT Human Calcitonin GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2245AG
Protein
CT
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CGRP (CLR/RAMP1) Human Calcitonin GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2248AG
Protein
CLR
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AM2 (CLR/RAMP3) Human Calcitonin GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2249AG
Protein
CLR
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CRF1 Human Corticotropin-Releasing Factor GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2293AG
Protein
CRF1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
CRF2 Human Corticotropin-Releasing Factor GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2294AG
Protein
CRF2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
Glucagon Human Glucagon GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2306AG
Protein
Glucagon
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GHRH Human Glucagon GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2307AG
Protein
GHRH
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GIP Human Glucagon GPCR in CHO Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2308AG
Protein
GIP
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GLP-1 Human Glucagon GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2309AG
Protein
GLP-1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
GLP-2 Human Glucagon GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2310AG
Protein
GLP-2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
Secretin Human Glucagon GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2311AG
Protein
Secretin
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
PTH1 Human Parathyroid Hormone GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2343AG
Protein
PTH1
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
PTH2 Human Parathyroid Hormone GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2344AG
Protein
PTH2
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
PAC1 (PACAP) Human VIP and PACAP GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2360AG
Protein
PAC1 (PACAP)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
VIP1 (VPAC1) Human VIP and PACAP GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2361AG
Protein
VIP1 (VPAC1)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
VIP2 (VPAC2) Human VIP and PACAP GPCR Cell Based Agonist cAMP LeadHunter Assay - US
Item
86-0007P-2362AG
Protein
VIP2 (VPAC2)
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AMY2 (CT/RAMP2) Human Calcitonin GPCR Cell Based Agonist cAMP (TR-FRET in Arrestin Cell Line) LeadHunter Assay - US
Item
86-3002P-2115AG
Protein
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AM1 (CLR/RAMP2) Human Calcitonin GPCR Cell Based Agonist cAMP (TR-FRET in Arrestin Cell Line) LeadHunter Assay - US
Item
86-3002P-2118AG
Protein
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AMY1 (CT/RAMP1) Human Calcitonin GPCR Cell Based Agonist cAMP (TR-FRET in Arrestin Cell Line) LeadHunter Assay - US
Item
86-3002P-2245AG
Protein
Organism
Human
Assay Sub Type
Cell Based
Family
GPCR
Name
AMY3 (CT/RAMP3) Human Calcitonin GPCR Cell Based Agonist cAMP (TR-FRET in Arrestin Cell Line) LeadHunter Assay - US
Item
86-3002P-2276AG
Protein
CT
Organism
Human
Assay Sub Type
Cell Based
Family:
GPCR
Organism:
Human
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Testing Information
Test Sample Requirements:
75uL of a 1000X DMSO stock or 1.5mL of 10X aqueous stock based on the final concentration being tested
Turnaround Time
Standard:
20 Business Days
Service Scheduling Note:
Turnaround time is twenty (20) business days from the project initiation.
Additional Information
Brand:
DiscoverX
Testing Location:
USA - Fremont, CA
Questions? Contact Us
You can easily get in touch with a Eurofins Discovery Expert or get help from our Customer Service team. Reach out with questions, or to discuss your specific discovery challenges.
