Peer-Reviewed Papers

MULTISCREEN™ stable cell lines, division-arrested cells, membrane preparations and assay kits have been referenced in over 100 peer reviewed journals and patents.

Filters
APPLICATION
TARGET FAMILY
All families
PRODUCT USED
  • Glucagon
  • Peptide
2018

Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2

Han, J., et al.
MedChemComm
9(1): 67–80
Product used
HEK293 cell lines
View paper
  • Neuropeptide Y
  • Peptide
2021

The effect of fatty diacid acylation of human PYY3-36 on Y2 receptor potency and half-life in minipigs

Østergaard, S., et al.
Scientific Reports
11: 21179
Product used
CHO cells stably expressing human Y2R, Cat # CG1274
View paper
  • Antibody, Review
2010

Therapeutic antibodies directed at G protein-coupled receptors

Hutchings, C. J., et al.
mAbs
2(6): 594–606
Product used
Cell and cell membrane proteins
View paper
  • Metabotropic glutamate
  • Small molecule
2023

Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

Dickson, L., et al.
ACS Medicinal Chemistry Letters
14(4): 442-449
Product used
mGluR2, 6, 8 cAMP assays and mGluR1, 3, 5 Gaqi5 calcium flux assays
View paper
  • Adenosine
  • Antibody
2024

Discovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptor

Wang, L., et al.
PLOS ONE
19(6): e0301223
Product used
MULTISCREEN Division-Arrested HEK293T
View paper
  • Opioid
  • Assay method
2022

Retro Drug Design: From Target Properties to Molecular Structures

Wang, Y., et al.
Journal of Chemical Information and Modeling
62(11): 2659-2669
Product used
hMOR-CHO-K1 stable cell line
View paper
  • Opioid
  • Target biology
2024

Field and laboratory perspectives on fentanyl and carfentanil decontamination

Linden, P., et al.
Scientific Reports
14: 25381
Product used
hMOR-CHO-K1-Gaqi5 stable cell line
View paper
  • Frizzled
  • Small molecule
2024

Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

Tomassi, S., et al.
RSC Medicinal Chemistry
16(1): 77-97
Product used
HEK293T-WT SMO membranes
View paper
  • Free fatty acid
  • Small molecule
2018

Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose Homeostasis

Syed, I., et al.
Cell Metabolism
27(2): 419-427.e4
Product used
GPR40 stable cell line; cyclic AMP assay
View paper
  • Orphan
  • Small molecule
2025

Discovery of Novel and Selective GPR17 Antagonists as Pharmacological Tools for Developing New Therapeutic Strategies in Diabetes and Obesity

Zhu, H., et al.
European Journal of Medicinal Chemistry
295: 117794
Product used
1321N1 GPR17 stable cell line (Cat # Cr1525-3)
View paper
  • Calcium-sensing
  • Small molecule
2023

Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo

Moritaka Goto, et al.
European Journal of Pharmacology
3888:16:00
Product used
Human CaSR-expressing HEK-293T stable cell line
View paper
  • Free fatty acid
  • Small molecule
2024

Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes

Jongmin Yoon, et al.
Biomedicine & Pharmacotherapy
2127:44:00
Product used
MULTISCREEN™ TR-FRET cAMP 1.0 No Wash Assay Kit
View paper
  • Parathyroid hormone
  • Peptide
2024

Preclinical development of EXT608, an investigational parathyroid hormone derivative with extended half-life for the treatment of hypoparathyroidism

Daniel B. Hall, et al.
JBMR Plus
8(6): ziae045
Product used
PTHR1 stable cell line
View paper
  • Adrenergic
  • Small molecule
2024

Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine

Chayka A, et al.
Journal of Medicinal Chemistry
67(12): 10135-10151
Product used
Calcium assay
View paper
  • Peptide
2022

D-VITylation: Harnessing the biology of vitamin D to improve the pharmacokinetic properties of peptides and small proteins Author links open overlay panel

Daniel B. Hall, et al.
International Journal of Pharmaceutics
2657:51:00
Product used
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2022

Competitive Binding of Ozanimod and Other Sphingosine 1-Phosphate Receptor Modulators at Receptor Subtypes 1 and 5

Selkirk JV, et al.
Frontiers in Pharmacology
14881:17:00
Product used
MULTISCREEN™ stable cell lines for S1P2, S1P3 and S1P4 (Cat # C1051-1, CG1049-1, CG1052-1)
View paper
  • Lysophospholipid
  • Small molecule
2022

Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effects

Zhang D, et al.
European Journal of Medicinal Chemistry
2155:21:00
Product used
LPA5 stable cell line
View paper
  • Free fatty acid
  • Small molecule
2021

In vitro pharmacodynamic studies of IDG-16177, a Potent GPR40 agonist, for the Treatment of Type 2 Diabetes

Jongmin Yoon, et al.
Diabetes
70(Suppl 1): 122-LB
Product used
GPR40 stable cell line
View paper
  • Opioid
  • Small molecule
2024

Identification and In Vivo Evaluation of Myelination Agent PIPE-3297, a Selective Kappa Opioid Receptor Agonist Devoid of β-Arrestin-2 Recruitment Efficacy

Schrader, T. O., et al.
ACS Chemical Neuroscience
15(3): 685-698
Product used
Membranes from CHO-K1 cells stably expressing human KOR
View paper
  • Free fatty acid
  • Small molecule
2022

A FFAR1 full agonist restores islet function in models of impaired glucose-stimulated insulin secretion and diabetic non-human primates

Rady, B., et al.
Frontiers in Endocrinology
13
Product used
FFAR1 assay
View paper
2010

Cannabinoids for the control of experimental multiple sclerosis

Product used
View paper
  • Glucagon
  • Assay method
2022

Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 System

Dewi Safitri, Matthew Harris, Abigail Pearce, Xianglin Huang, Matthew Rosa, Kerry Barkan, Edward Wills, Maria Marti-Solano, Matthew D. Falk, Graham Ladds
bioRxiv
2022.09.01.506210
Product used
HEK293T cells overexpressing GIPR or GLP-1R
View paper
  • Neuropeptide S
  • Small molecule
2021

New quinolone derivatives as neuropeptide S receptor antagonists: Design, synthesis, homology modeling, dynamic simulations and modulation of Gq/Gs signaling pathways.

Batran RZ, Gugnani KS, Maher TJ, Khedr MA.
Bioorganic Chemistry
1857:57:00
Product used
Calcium and cAMP assays
View paper
  • Free fatty acid
  • Small molecule
2021

Distinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs). 

Aryal P, Syed I, Lee J, Patel R, Nelson AT, Siegel D, Saghatelian A, Kahn BB
Journal of Lipid Research
1730:28:00
Product used
Calcium assay
View paper
  • Galanin
  • Target biology
2022

Preferential Gs protein coupling of the galanin Gal1 receptor in the µ-opioid-Gal1 receptor heterotetramer

Paulo A. De Oliveira, Estefanía Moreno, Nil Casajuana-Martin, Verònica Casadó-Anguera, Ning-Sheng Cai, Gisela Andrea Camacho-Hernandez, Hu Zhu, Alessandro Bonifazi, Matthew D. Hall, David Weinshenker, Amy Hauck Newman, Diomedes E. Logothetis, Vicent Casadó, Leigh D. Plant, Leonardo Pardo, Sergi Ferré
Pharmacological Research
1954:02:00
Product used
CHO-K1-Gaqi5 Gal1R stable cell line
View paper
2021

A Novel Maintenance Therapeutic for Opioid Use Disorder

Product used
View paper
2022

In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B2 receptor antagonist in clinical development

Product used
View paper
2020

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

Product used
View paper
2021

Predictive models to identify small molecule activators and inhibitors of opioid receptors

Product used
View paper
  • Opioid
  • Small molecule
2022

A novel luminescence-based β-arrestin recruitment assay for unmodified receptors.

Beth Youngblood, Kevin Li, Donald R. Gehlert, Julio C. Medina and Neil Schwartz
Journal of Pharmacology and Experimental Therapeutics
378(2): 133-145
Product used
MOR GTPyS assays performed at Multispan in membrane preparations
View paper
  • Chemokine
  • Antibody
2016

I-bodies: human single domain antibodies that antagonize chemokine receptor CXCR4

Katherine Griffithsa, et al.
Journal of Biological Chemistry
291(20): 12641-12657
Product used
CXCR4 stable cell line
View paper
  • Orphan
  • Target biology
2009

GPR37 Surface Expression Enhancement via N-Terminal Truncation or Protein-Protein Interactions

Jill H. Dunham, et al.
Biochemistry
48(43): 10286-10297
Product used
GPR37L1 cell line
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2020

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

Jing Jin, Nina Xue, Yuan Liu, Rong Fu, Mingjin Wang, Ming Ji, Fangfang Lai, Jinping Hu, Xiaojian Wang, Qiong Xiao, Xiaoying Zhang, Dali Yin, Liping Bai, Xiaoguang Chen, Shuan Rao,
Acta Pharmaceutica Sinica B
10(2): 276-288
Product used
CHO-K1 Gaqi5 cells stably expressing S1P1
View paper
  • Orphan
  • Target biology
2020

The N-terminus of GPR37L1 is proteolytically processed by matrix metalloproteases

James L. J. Coleman, et al.
Scientific Reports
343:15:00
Product used
GPR37L1 cell line
View paper
  • Bradykinin
  • Small molecule
2020

In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor Antagonist

Anne Lesage, et al.
Frontiers in Pharmacology
Product used
Calcium assay
View paper
  • Opioid
  • Assay method
2021

A novel luminescence-based β-arrestin membrane recruitment assay for unmodified GPCRs

Hauge Pedersen M, Pham J, Mancebo H, Inoue A, Asher WB, Javitch JA.
Journal of Biological Chemistry
Product used
CHO-K1 stable cell lines expressing human MOR, KOR, DOR and NOP
View paper
  • Orphan
  • Target biology
2018

GPR37L1 modulates seizure susceptibility: Evidence from mouse studies and analyses of a human GPR37L1 variant

Michelle M.Giddensa, et al.
Neurobiology of Disease
Pages: 181-190. Volume: Volume 106
Product used
GPR37L1 cell line
View paper
  • Antibody, Review
2012

Chapter Two – Potential Use of G Protein-Coupled Receptor-Blocking Monoclonal Antibodies as Therapeutic Agents for Cancers

Deron R.Herr
International Review of Cell and Molecular Biology
297: 45-81
Product used
View paper
  • Frizzled
  • Small molecule
2018

Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein

Susanne Höing, et al.
Cell Chemical Biology
25(4): 357-369.e6
Product used
SMO stable cell line
View paper
  • Opioid
  • Peptide
2009

Anticonvulsant Met-Enkephalin Analogues Containing Backbone Spacers Reveal Alternative Non-Opioid Signaling in the Brain

Hee-Kyoung Lee, et al.
ACS Chemical Biology
4(8): 659-671
Product used
Opioid receptor assays
View paper
  • Lysophospholipid
  • Target biology
2013

Comparing the differential effects of LPA on the barrier function of human pulmonary endothelial cells

Yonglin Ren, et al.
Microvascular Research
85: 59-67
Product used
LPA2 and LPA5 cell lines
View paper
  • Cannabinoid
  • Small molecule
2017

Big conductance calcium‐activated potassium channel openers control spasticity without sedation

David Baker, et al.
British Journal of Pharmacology
Product used
GPR55 cell line
View paper
  • Frizzled
  • Small molecule
2017

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer

Floriana Morgillo, et al.
Journal of Medicinal Chemistry
60(17): 7447-7458
Product used
SMO stable cell line
View paper
  • Glucagon
  • Peptide
2017

Synthesis and pharmaceutical characterization of site specific mycophenolic acid-modified Xenopus glucagon-like peptide-1 analogs

Han, J., et al.
MedChemComm
9(1): 67-80
Product used
HEK293 stable cell line
View paper
  • Calcium-sensing
  • Peptide
2019

Pharmacology of Parsabiv® (etelcalcetide, ONO-5163/AMG 416), a novel allosteric modulator of the calcium-sensing receptor, for secondary hyperparathyroidism in hemodialysis patients

Kazutsune Harada, et al.
European Journal of Pharmacology
842: 139-145
Product used
HEK-293T cells stably expressing human Ca-sensing receptor, plus matched parental cells
View paper
  • Free fatty acid
  • Target biology
2016

Loss of Free Fatty Acid Receptor 2 leads to impaired islet mass and beta cell survival

Stephanie R. Villa, et al.
Scientific Reports
475:19:00
Product used
FFA2 cell line
View paper
  • Free fatty acid
  • Small molecule
2017

Homology modeling of FFA2 identifies novel agonists that potentiate insulin secretion.

Villa SR, et al.
Journal of Investigative Medicine
65(8): 1116-1124
Product used
Free fatty acid receptor assays
View paper
  • Leukotriene
  • Small molecule
2010

Effects of LTB4 receptor antagonism on pulmonary inflammation in rodents and non-human primates.

Hicks A, et al.
Prostaglandins & Other Lipid Mediators
92(1-4): 33-43
Product used
BLT1 and BLT2 cell lines
View paper
  • Mas-related
  • Assay method
2010

Development of a FLIPR assay for the simultaneous identification of MrgD agonists and antagonists from a single screen.

Ajit SK, et al.
Journal of Biomedicine and Biotechnology
7443:40:00
Product used
MrgX1 cell line
View paper
  • Calcium-sensing
  • Peptide
2015

Critical Cysteine Residues in Both the Calcium-Sensing Receptor and the Allosteric Activator AMG 416 Underlie the Mechanism of Action.

Alexander ST, et al.
Molecular Pharmacology
88(5): 853-865
Product used
CaSR cell line
View paper
  • Gonadotrophin-releasing hormone
  • Small molecule
2009

Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor

Richard Fjellaksel, et al.
Bioorganic & Medicinal Chemistry Letters
19(7)
Product used
GnRH cell line
View paper
  • Cannabinoid
  • Target biology
2013

Genetic Background Can Result in a Marked or Minimal Effect of Gene Knockout (GPR55 and CB2 Receptor) in Experimental Autoimmune Encephalomyelitis Models of Multiple Sclerosis

Sofia Sisay, et al.
PLOS ONE
8(10): e76907
Product used
GPR55 and CB2 cell lines
View paper
  • Multiple
  • Radioligand
2011

20-Iodo-14,15-epoxyeicosa-8(Z)-enoyl-3-azidophenylsulfonamide: Photoaffinity Labeling of a 14,15-Epoxyeicosatrienoic Acid Receptor

Yuenmu Chen, et al.
Biochemistry
50(18): 3840-3848
Product used
79-GPCR panel screening
View paper
  • Multiple
  • Target biology
2013

In Silico Molecular Comparisons of C. elegans and Mammalian Pharmacology Identify Distinct Targets That Regulate Feeding

George A. Lemieux, et al.
PLOS Biology
Product used
Cholecystokinin and nicotinic acid receptor assays
View paper
  • Gonadotrophin-releasing hormone
  • Radioligand
2018

First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor

Richard Fjellaksel, et al.
BMC Research Notes
24:31:00
Product used
GnRH cell line
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2019

Sphingosine-1-Phosphate Receptor Subtype 1 (S1P1) Modulator IMMH001 Regulates Adjuvant- and Collagen-Induced Arthritis

Jing Jin, et al.
Frontiers in Pharmacology
28:05:00
Product used
S1P1 cell line
View paper
  • Purinergic
  • Small molecule
2016

Nucleoside 5′-O-monophosphorothioates as modulators of the P2Y14 receptor and mast cell degranulation

Edyta Gendaszewska-Darmach, et al.
Oncotarget
7(43): 69358-69370
Product used
P2Y14 cell line
View paper
  • Calcium-sensing
  • Peptide
2013

Pharmacology of AMG 416 (Velcalcetide), a Novel Peptide Agonist of the Calcium-Sensing Receptor, for the Treatment of Secondary Hyperparathyroidism in Hemodialysis Patients

Sarah Walter, et al.
Journal of Pharmacology and Experimental Therapeutics
346(2): 229-240
Product used
Human CaSR cell line
View paper
  • Metabotropic glutamate
  • Small molecule
2018

Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators

Roy J.Vaza, et al.
Bioorganic & Medicinal Chemistry Letters
28(19): 3194-3198
Product used
mGluR2 cell line
View paper
  • Leukotriene
  • Small molecule
2010

Discovery of Novel and Potent Leukotriene B4 Receptor Antagonists. Part 1

Robert A. Goodnow Jr., et al.
Journal of Medicinal Chemistry
53(9): 3502-3516
Product used
BLT1 and BLT2 cell lines
View paper
  • Free fatty acid
  • Target biology
2015

An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion

Medha Priyadarshini, et al.
Molecular Endocrinology
29(7): 1055-1066
Product used
hFFAR2 cell line
View paper
  • Purinergic
  • Small molecule
2016

Thymidine 5′-O-monophosphorothioate induces HeLa cell migration by activation of the P2Y6 receptor

Edyta Gendaszewska-Darmach, et al.
Purinergic Signalling
12: 199-209
Product used
P2Y6 cell line
View paper
  • Metabotropic glutamate
  • Small molecule
2016

The mGluR2 positive allosteric modulator, SAR218645, improves memory and attention deficits in translational models of cognitive symptoms associated with schizophrenia

Guy Griebel, et al.
Scientific Reports
594:40:00
Product used
mGluR2 cell line
View paper
  • Prostanoid
  • Assay method
2013

Analyzing Surface Protein Expression and Internalization

William Truong, et al.
Santa Clara University Scholar Commons
Product used
Prostanoid receptor assays
View paper
Filters
APPLICATION
TARGET FAMILY
All families
PRODUCT USED
  • Glucagon
  • Peptide
2018

Synthesis and characterization of [125I]TZ6544, a promising radioligand for investigating sphingosine-1-phosphate receptor 2

Han, J., et al.
MedChemComm
9(1): 67–80
Product used
HEK293 cell lines
View paper
  • Neuropeptide Y
  • Peptide
2021

The effect of fatty diacid acylation of human PYY3-36 on Y2 receptor potency and half-life in minipigs

Østergaard, S., et al.
Scientific Reports
11: 21179
Product used
CHO cells stably expressing human Y2R, Cat # CG1274
View paper
  • Antibody, Review
2010

Therapeutic antibodies directed at G protein-coupled receptors

Hutchings, C. J., et al.
mAbs
2(6): 594–606
Product used
Cell and cell membrane proteins
View paper
  • Metabotropic glutamate
  • Small molecule
2023

Discovery of CVN636: A Highly Potent, Selective, and CNS Penetrant mGluR7 Allosteric Agonist

Dickson, L., et al.
ACS Medicinal Chemistry Letters
14(4): 442-449
Product used
mGluR2, 6, 8 cAMP assays and mGluR1, 3, 5 Gaqi5 calcium flux assays
View paper
  • Adenosine
  • Antibody
2024

Discovery of a potent, selective, and tumor-suppressing antibody antagonist of adenosine A2A receptor

Wang, L., et al.
PLOS ONE
19(6): e0301223
Product used
MULTISCREEN Division-Arrested HEK293T
View paper
  • Opioid
  • Assay method
2022

Retro Drug Design: From Target Properties to Molecular Structures

Wang, Y., et al.
Journal of Chemical Information and Modeling
62(11): 2659-2669
Product used
hMOR-CHO-K1 stable cell line
View paper
  • Opioid
  • Target biology
2024

Field and laboratory perspectives on fentanyl and carfentanil decontamination

Linden, P., et al.
Scientific Reports
14: 25381
Product used
hMOR-CHO-K1-Gaqi5 stable cell line
View paper
  • Frizzled
  • Small molecule
2024

Discovery of N-substituted-2-oxoindolin benzoylhydrazines as c-MET/SMO modulators in EGFRi-resistant non-small cell lung cancer

Tomassi, S., et al.
RSC Medicinal Chemistry
16(1): 77-97
Product used
HEK293T-WT SMO membranes
View paper
  • Free fatty acid
  • Small molecule
2018

Palmitic Acid Hydroxystearic Acids Activate GPR40, Which Is Involved in Their Beneficial Effects on Glucose Homeostasis

Syed, I., et al.
Cell Metabolism
27(2): 419-427.e4
Product used
GPR40 stable cell line; cyclic AMP assay
View paper
  • Orphan
  • Small molecule
2025

Discovery of Novel and Selective GPR17 Antagonists as Pharmacological Tools for Developing New Therapeutic Strategies in Diabetes and Obesity

Zhu, H., et al.
European Journal of Medicinal Chemistry
295: 117794
Product used
1321N1 GPR17 stable cell line (Cat # Cr1525-3)
View paper
  • Calcium-sensing
  • Small molecule
2023

Pharmacological profile of upacicalcet, a novel positive allosteric modulator of calcium-sensing receptor, in vitro and in vivo

Moritaka Goto, et al.
European Journal of Pharmacology
3888:16:00
Product used
Human CaSR-expressing HEK-293T stable cell line
View paper
  • Free fatty acid
  • Small molecule
2024

Xelaglifam, a novel GPR40/FFAR1 agonist, exhibits enhanced β-arrestin recruitment and sustained glycemic control for type 2 diabetes

Jongmin Yoon, et al.
Biomedicine & Pharmacotherapy
2127:44:00
Product used
MULTISCREEN™ TR-FRET cAMP 1.0 No Wash Assay Kit
View paper
  • Parathyroid hormone
  • Peptide
2024

Preclinical development of EXT608, an investigational parathyroid hormone derivative with extended half-life for the treatment of hypoparathyroidism

Daniel B. Hall, et al.
JBMR Plus
8(6): ziae045
Product used
PTHR1 stable cell line
View paper
  • Adrenergic
  • Small molecule
2024

Structure-Based Drug Design of ADRA2A Antagonists Derived from Yohimbine

Chayka A, et al.
Journal of Medicinal Chemistry
67(12): 10135-10151
Product used
Calcium assay
View paper
  • Peptide
2022

D-VITylation: Harnessing the biology of vitamin D to improve the pharmacokinetic properties of peptides and small proteins Author links open overlay panel

Daniel B. Hall, et al.
International Journal of Pharmaceutics
2657:51:00
Product used
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2022

Competitive Binding of Ozanimod and Other Sphingosine 1-Phosphate Receptor Modulators at Receptor Subtypes 1 and 5

Selkirk JV, et al.
Frontiers in Pharmacology
14881:17:00
Product used
MULTISCREEN™ stable cell lines for S1P2, S1P3 and S1P4 (Cat # C1051-1, CG1049-1, CG1052-1)
View paper
  • Lysophospholipid
  • Small molecule
2022

Isoquinolone derivatives as lysophosphatidic acid receptor 5 (LPA5) antagonists: Investigation of structure-activity relationships, ADME properties and analgesic effects

Zhang D, et al.
European Journal of Medicinal Chemistry
2155:21:00
Product used
LPA5 stable cell line
View paper
  • Free fatty acid
  • Small molecule
2021

In vitro pharmacodynamic studies of IDG-16177, a Potent GPR40 agonist, for the Treatment of Type 2 Diabetes

Jongmin Yoon, et al.
Diabetes
70(Suppl 1): 122-LB
Product used
GPR40 stable cell line
View paper
  • Opioid
  • Small molecule
2024

Identification and In Vivo Evaluation of Myelination Agent PIPE-3297, a Selective Kappa Opioid Receptor Agonist Devoid of β-Arrestin-2 Recruitment Efficacy

Schrader, T. O., et al.
ACS Chemical Neuroscience
15(3): 685-698
Product used
Membranes from CHO-K1 cells stably expressing human KOR
View paper
  • Free fatty acid
  • Small molecule
2022

A FFAR1 full agonist restores islet function in models of impaired glucose-stimulated insulin secretion and diabetic non-human primates

Rady, B., et al.
Frontiers in Endocrinology
13
Product used
FFAR1 assay
View paper
2010

Cannabinoids for the control of experimental multiple sclerosis

Product used
View paper
  • Glucagon
  • Assay method
2022

Cancer-Associated Mutations Enhance The Sensitivity Of The Trupath GαQ/11 System

Dewi Safitri, Matthew Harris, Abigail Pearce, Xianglin Huang, Matthew Rosa, Kerry Barkan, Edward Wills, Maria Marti-Solano, Matthew D. Falk, Graham Ladds
bioRxiv
2022.09.01.506210
Product used
HEK293T cells overexpressing GIPR or GLP-1R
View paper
  • Neuropeptide S
  • Small molecule
2021

New quinolone derivatives as neuropeptide S receptor antagonists: Design, synthesis, homology modeling, dynamic simulations and modulation of Gq/Gs signaling pathways.

Batran RZ, Gugnani KS, Maher TJ, Khedr MA.
Bioorganic Chemistry
1857:57:00
Product used
Calcium and cAMP assays
View paper
  • Free fatty acid
  • Small molecule
2021

Distinct biological activities of isomers from several families of branched fatty acid esters of hydroxy fatty acids (FAHFAs). 

Aryal P, Syed I, Lee J, Patel R, Nelson AT, Siegel D, Saghatelian A, Kahn BB
Journal of Lipid Research
1730:28:00
Product used
Calcium assay
View paper
  • Galanin
  • Target biology
2022

Preferential Gs protein coupling of the galanin Gal1 receptor in the µ-opioid-Gal1 receptor heterotetramer

Paulo A. De Oliveira, Estefanía Moreno, Nil Casajuana-Martin, Verònica Casadó-Anguera, Ning-Sheng Cai, Gisela Andrea Camacho-Hernandez, Hu Zhu, Alessandro Bonifazi, Matthew D. Hall, David Weinshenker, Amy Hauck Newman, Diomedes E. Logothetis, Vicent Casadó, Leigh D. Plant, Leonardo Pardo, Sergi Ferré
Pharmacological Research
1954:02:00
Product used
CHO-K1-Gaqi5 Gal1R stable cell line
View paper
2021

A Novel Maintenance Therapeutic for Opioid Use Disorder

Product used
View paper
2022

In vitro pharmacological profile of PHA-022121, a small molecule bradykinin B2 receptor antagonist in clinical development

Product used
View paper
2020

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

Product used
View paper
2021

Predictive models to identify small molecule activators and inhibitors of opioid receptors

Product used
View paper
  • Opioid
  • Small molecule
2022

A novel luminescence-based β-arrestin recruitment assay for unmodified receptors.

Beth Youngblood, Kevin Li, Donald R. Gehlert, Julio C. Medina and Neil Schwartz
Journal of Pharmacology and Experimental Therapeutics
378(2): 133-145
Product used
MOR GTPyS assays performed at Multispan in membrane preparations
View paper
  • Chemokine
  • Antibody
2016

I-bodies: human single domain antibodies that antagonize chemokine receptor CXCR4

Katherine Griffithsa, et al.
Journal of Biological Chemistry
291(20): 12641-12657
Product used
CXCR4 stable cell line
View paper
  • Orphan
  • Target biology
2009

GPR37 Surface Expression Enhancement via N-Terminal Truncation or Protein-Protein Interactions

Jill H. Dunham, et al.
Biochemistry
48(43): 10286-10297
Product used
GPR37L1 cell line
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2020

A novel S1P1 modulator IMMH002 ameliorates psoriasis in multiple animal models

Jing Jin, Nina Xue, Yuan Liu, Rong Fu, Mingjin Wang, Ming Ji, Fangfang Lai, Jinping Hu, Xiaojian Wang, Qiong Xiao, Xiaoying Zhang, Dali Yin, Liping Bai, Xiaoguang Chen, Shuan Rao,
Acta Pharmaceutica Sinica B
10(2): 276-288
Product used
CHO-K1 Gaqi5 cells stably expressing S1P1
View paper
  • Orphan
  • Target biology
2020

The N-terminus of GPR37L1 is proteolytically processed by matrix metalloproteases

James L. J. Coleman, et al.
Scientific Reports
343:15:00
Product used
GPR37L1 cell line
View paper
  • Bradykinin
  • Small molecule
2020

In Vitro Pharmacological Profile of a New Small Molecule Bradykinin B2 Receptor Antagonist

Anne Lesage, et al.
Frontiers in Pharmacology
Product used
Calcium assay
View paper
  • Opioid
  • Assay method
2021

A novel luminescence-based β-arrestin membrane recruitment assay for unmodified GPCRs

Hauge Pedersen M, Pham J, Mancebo H, Inoue A, Asher WB, Javitch JA.
Journal of Biological Chemistry
Product used
CHO-K1 stable cell lines expressing human MOR, KOR, DOR and NOP
View paper
  • Orphan
  • Target biology
2018

GPR37L1 modulates seizure susceptibility: Evidence from mouse studies and analyses of a human GPR37L1 variant

Michelle M.Giddensa, et al.
Neurobiology of Disease
Pages: 181-190. Volume: Volume 106
Product used
GPR37L1 cell line
View paper
  • Antibody, Review
2012

Chapter Two – Potential Use of G Protein-Coupled Receptor-Blocking Monoclonal Antibodies as Therapeutic Agents for Cancers

Deron R.Herr
International Review of Cell and Molecular Biology
297: 45-81
Product used
View paper
  • Frizzled
  • Small molecule
2018

Dynarrestin, a Novel Inhibitor of Cytoplasmic Dynein

Susanne Höing, et al.
Cell Chemical Biology
25(4): 357-369.e6
Product used
SMO stable cell line
View paper
  • Opioid
  • Peptide
2009

Anticonvulsant Met-Enkephalin Analogues Containing Backbone Spacers Reveal Alternative Non-Opioid Signaling in the Brain

Hee-Kyoung Lee, et al.
ACS Chemical Biology
4(8): 659-671
Product used
Opioid receptor assays
View paper
  • Lysophospholipid
  • Target biology
2013

Comparing the differential effects of LPA on the barrier function of human pulmonary endothelial cells

Yonglin Ren, et al.
Microvascular Research
85: 59-67
Product used
LPA2 and LPA5 cell lines
View paper
  • Cannabinoid
  • Small molecule
2017

Big conductance calcium‐activated potassium channel openers control spasticity without sedation

David Baker, et al.
British Journal of Pharmacology
Product used
GPR55 cell line
View paper
  • Frizzled
  • Small molecule
2017

Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer

Floriana Morgillo, et al.
Journal of Medicinal Chemistry
60(17): 7447-7458
Product used
SMO stable cell line
View paper
  • Glucagon
  • Peptide
2017

Synthesis and pharmaceutical characterization of site specific mycophenolic acid-modified Xenopus glucagon-like peptide-1 analogs

Han, J., et al.
MedChemComm
9(1): 67-80
Product used
HEK293 stable cell line
View paper
  • Calcium-sensing
  • Peptide
2019

Pharmacology of Parsabiv® (etelcalcetide, ONO-5163/AMG 416), a novel allosteric modulator of the calcium-sensing receptor, for secondary hyperparathyroidism in hemodialysis patients

Kazutsune Harada, et al.
European Journal of Pharmacology
842: 139-145
Product used
HEK-293T cells stably expressing human Ca-sensing receptor, plus matched parental cells
View paper
  • Free fatty acid
  • Target biology
2016

Loss of Free Fatty Acid Receptor 2 leads to impaired islet mass and beta cell survival

Stephanie R. Villa, et al.
Scientific Reports
475:19:00
Product used
FFA2 cell line
View paper
  • Free fatty acid
  • Small molecule
2017

Homology modeling of FFA2 identifies novel agonists that potentiate insulin secretion.

Villa SR, et al.
Journal of Investigative Medicine
65(8): 1116-1124
Product used
Free fatty acid receptor assays
View paper
  • Leukotriene
  • Small molecule
2010

Effects of LTB4 receptor antagonism on pulmonary inflammation in rodents and non-human primates.

Hicks A, et al.
Prostaglandins & Other Lipid Mediators
92(1-4): 33-43
Product used
BLT1 and BLT2 cell lines
View paper
  • Mas-related
  • Assay method
2010

Development of a FLIPR assay for the simultaneous identification of MrgD agonists and antagonists from a single screen.

Ajit SK, et al.
Journal of Biomedicine and Biotechnology
7443:40:00
Product used
MrgX1 cell line
View paper
  • Calcium-sensing
  • Peptide
2015

Critical Cysteine Residues in Both the Calcium-Sensing Receptor and the Allosteric Activator AMG 416 Underlie the Mechanism of Action.

Alexander ST, et al.
Molecular Pharmacology
88(5): 853-865
Product used
CaSR cell line
View paper
  • Gonadotrophin-releasing hormone
  • Small molecule
2009

Small molecule piperazinyl-benzimidazole antagonists of the gonadotropin-releasing hormone (GnRH) receptor

Richard Fjellaksel, et al.
Bioorganic & Medicinal Chemistry Letters
19(7)
Product used
GnRH cell line
View paper
  • Cannabinoid
  • Target biology
2013

Genetic Background Can Result in a Marked or Minimal Effect of Gene Knockout (GPR55 and CB2 Receptor) in Experimental Autoimmune Encephalomyelitis Models of Multiple Sclerosis

Sofia Sisay, et al.
PLOS ONE
8(10): e76907
Product used
GPR55 and CB2 cell lines
View paper
  • Multiple
  • Radioligand
2011

20-Iodo-14,15-epoxyeicosa-8(Z)-enoyl-3-azidophenylsulfonamide: Photoaffinity Labeling of a 14,15-Epoxyeicosatrienoic Acid Receptor

Yuenmu Chen, et al.
Biochemistry
50(18): 3840-3848
Product used
79-GPCR panel screening
View paper
  • Multiple
  • Target biology
2013

In Silico Molecular Comparisons of C. elegans and Mammalian Pharmacology Identify Distinct Targets That Regulate Feeding

George A. Lemieux, et al.
PLOS Biology
Product used
Cholecystokinin and nicotinic acid receptor assays
View paper
  • Gonadotrophin-releasing hormone
  • Radioligand
2018

First in vivo evaluation of a potential SPECT brain radiotracer for the gonadotropin releasing hormone receptor

Richard Fjellaksel, et al.
BMC Research Notes
24:31:00
Product used
GnRH cell line
View paper
  • Sphingosine 1-phosphate
  • Small molecule
2019

Sphingosine-1-Phosphate Receptor Subtype 1 (S1P1) Modulator IMMH001 Regulates Adjuvant- and Collagen-Induced Arthritis

Jing Jin, et al.
Frontiers in Pharmacology
28:05:00
Product used
S1P1 cell line
View paper
  • Purinergic
  • Small molecule
2016

Nucleoside 5′-O-monophosphorothioates as modulators of the P2Y14 receptor and mast cell degranulation

Edyta Gendaszewska-Darmach, et al.
Oncotarget
7(43): 69358-69370
Product used
P2Y14 cell line
View paper
  • Calcium-sensing
  • Peptide
2013

Pharmacology of AMG 416 (Velcalcetide), a Novel Peptide Agonist of the Calcium-Sensing Receptor, for the Treatment of Secondary Hyperparathyroidism in Hemodialysis Patients

Sarah Walter, et al.
Journal of Pharmacology and Experimental Therapeutics
346(2): 229-240
Product used
Human CaSR cell line
View paper
  • Metabotropic glutamate
  • Small molecule
2018

Amelioration of PXR-mediated CYP3A4 induction by mGluR2 modulators

Roy J.Vaza, et al.
Bioorganic & Medicinal Chemistry Letters
28(19): 3194-3198
Product used
mGluR2 cell line
View paper
  • Leukotriene
  • Small molecule
2010

Discovery of Novel and Potent Leukotriene B4 Receptor Antagonists. Part 1

Robert A. Goodnow Jr., et al.
Journal of Medicinal Chemistry
53(9): 3502-3516
Product used
BLT1 and BLT2 cell lines
View paper
  • Free fatty acid
  • Target biology
2015

An Acetate-Specific GPCR, FFAR2, Regulates Insulin Secretion

Medha Priyadarshini, et al.
Molecular Endocrinology
29(7): 1055-1066
Product used
hFFAR2 cell line
View paper
  • Purinergic
  • Small molecule
2016

Thymidine 5′-O-monophosphorothioate induces HeLa cell migration by activation of the P2Y6 receptor

Edyta Gendaszewska-Darmach, et al.
Purinergic Signalling
12: 199-209
Product used
P2Y6 cell line
View paper
  • Metabotropic glutamate
  • Small molecule
2016

The mGluR2 positive allosteric modulator, SAR218645, improves memory and attention deficits in translational models of cognitive symptoms associated with schizophrenia

Guy Griebel, et al.
Scientific Reports
594:40:00
Product used
mGluR2 cell line
View paper
  • Prostanoid
  • Assay method
2013

Analyzing Surface Protein Expression and Internalization

William Truong, et al.
Santa Clara University Scholar Commons
Product used
Prostanoid receptor assays
View paper