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Compound Libraries GPCR Compound Library

GPCR Compound Library

Catalog No. L1500
  Library Compound List   Excel SDF

G-protein-coupled receptors (GPCRs) are the largest and most diverse group of membrane receptors in eukaryotes that detect molecules outside the cell and activate internal signal transduction pathways and, ultimately, cellular responses. GPCRs are involved in nearly every aspect of animal life, from early development and heart function to neuronal activity. Mutations in GPCRs are linked to a number of human diseases. GPCRs are an important drug target and approximately 34% of the marketed drugs target 108 members of this family, with an additional 66 receptors targeted by agents that are/were in clinical trials. GPCR-based drug discovery remains active campaigns in major pharmaceutical companies. To date more than 140 orphan GPCRs, whose endogenous ligands are unknown, are the focus of an intense drug discovery effort in many programs.

Specifically, the optimal ligands to GPCRs need to possess high affinity and specificity for the target protein, and reasonable membrane permeability for biological activity in whole cell assays and in vivo models. GPCR Compound Library from TargetMol, a focused small molecule libraries developed against particular GPCRs containing 1406 GPCR-active agents for GPCR drug discovery.

Pack Size Price/USD
100 μL * 10 mM (in DMSO) 15948.00
250 μL * 10 mM (in DMSO) 22708.00
1 mg 22708.00
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Product Description

  • A unique collection of 1406 GPCR-active agents for high throughput screening and high content screening for GPCR drug discovery, and new GPCR target identification and research;
  • Potential to find new GPCR drug candidates by screening against orphan GPCRs;
  • Bioactivity and safety confirmed by pre-clinical research and clinical trials, and some of them are approved by FDA;
  • Targets include 5-HT receptor, dopamine receptor, opioid receptor, adrenergic receptor, mGluR, Cannabinoid receptor, ETA-receptor, etc;
  • Detailed compound information with structure, target, activity, IC50 value, and biological activity description;
  • Structurally diverse, medicinally active, and cell permeable;
  • NMR and HPLC validated to ensure high purity and quality;

Library Customization

Targetmol Compound Libraries can be highly customized! Learn More

Packaging And Storage

  • Powder or pre-dissolved DMSO solutions in 96/384 well plate with optional 2D barcode
  • Shipped with blue ice
Request Library Compound List (L1500)

Library Composition

5-HT Receptor (128)
Adrenergic Receptor (106)
Dopamine Receptor (81)
AChR (73)
Histamine Receptor (72)
Estrogen/progestogen Receptor (33)
Glucocorticoid Receptor (33)
GR (31)
RAAS (19)
Norepinephrine (19)
GluR (18)
GPR (16)
GABA Receptor (15)
Hedgehog/Smoothened (14)
PKA (14)
Opioid Receptor (14)
Prostaglandin Receptor (13)
Potassium Channel (11)
PDE (11)
Adenosine Receptor (11)
CXCR (10)
S1P Receptor (10)
Cannabinoid Receptor (9)
Calcium Channel (9)
Sigma receptor (8)
SGLT (7)
P2 Receptor (7)
PKC (7)
NMDAR (7)
MRP (7)
OX Receptor (6)
Androgen Receptor (6)
Annexin A (6)
CDK (6)
COX (5)
Endothelin Receptor (5)
GPCR19 (4)
HDAC (4)
IL Receptor (4)
CCR (4)
CaMK (4)
P450 (4)
Phospholipase (4)
TNF (4)
Vasopressin Receptor (4)
VEGFR (4)
Serine/threonin kinase (4)
Protease-activated Receptor (4)
Rho (4)
ROCK (4)
Sodium Channel (3)
Somatostatin (3)
PPAR (3)
NOS (3)
LTR (3)
MAO (3)
cholecystokinin (3)
GTPase (3)
GRK (3)
GNRH Receptor (3)
Glucagon Receptor (3)
EGFR (3)
Endogenous Metabolite (2)
GSK-3 (2)
Integrin (2)
LDL (2)
Histone Methyltransferase (2)
Dehydrogenase (2)
Bombesin Receptor (2)
Carbonic Anhydrase (2)
Casein Kinase (2)
cAMP (2)
ATPase (2)
Aurora Kinase (2)
ABC (2)
Melatonin Receptor (2)
MMP (2)
LPA Receptor (2)
MT Receptor (2)
NADPH (2)
Neurokinin receptor (2)
NF-κB (2)
Raf (2)
PAFR (2)
SGK (2)
Syk (2)
Proteasome (2)
S6 Kinase (2)
ROS (2)
UGT (2)
Vitamin (1)
Wnt/beta-catenin (1)
Topoisomerase (1)
Transferase (1)
Trk receptor (1)
TRP/TRPV Channel (1)
Tyrosinase (1)
ROR (1)
TGF-beta/Smad (1)
Src (1)
STAT (1)
PI3K (1)
PDK (1)
Phosphatase (1)
RAR/RXR (1)
Ras (1)
Reductase (1)
mTOR (1)
Monoamine Transporter (1)
Monocarboxylate transporter (1)
MPO (1)
lysosomal autophagy (1)
HER (1)
HIF (1)
ACAT (1)
Acyltransferase (1)
Adiponectin receptor (1)
Akt (1)
Amino Acids and Derivatives (1)
Autophagy (1)
Antibacterial (1)
Antifungal (1)
Antioxidant (1)
Apoptosis inducer (1)
ATP Citrate Lyase (1)
Caspase (1)
CaSR (1)
Chk (1)
Chloride channel (1)
Discoidin Domain Receptor (DDR) (1)
DNA Alkylation (1)
DNA/RNA Synthesis (1)
c-Met/HGFR (1)
c-Myc (1)
Cysteine Protease (1)
Hydroxylase (1)
IAP (1)
Lipoxygenase (1)
Liver X Receptor (1)
GST (1)
Guanylate cyclase (1)
ERK (1)
FAK (1)
FOXO1 (1)
Free radical scavengers (1)
Gamma-secretase (1)
Gap Junction Protein (1)
GlyT (1)