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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 1633 GPCR-active agents for GPCR drug discovery.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Please contact us for prices and availability for the specification of product you are interested at.
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If the above compound libraries do not match your needs,
please contact our compound library specialist for a customized compound library at inquiry@targetmol.com
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Product Description

  • A unique collection of 1633 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 (245)
Adrenergic Receptor (194)
Dopamine Receptor (159)
Histamine Receptor (110)
AChR (104)
Opioid Receptor (72)
GPR (55)
Glucocorticoid Receptor (44)
Prostaglandin Receptor (43)
GluR (35)
Adenosine Receptor (32)
CXCR (30)
Cannabinoid Receptor (29)
RAAS (25)
Norepinephrine (24)
Ras (24)
S1P Receptor (24)
Neurokinin receptor (22)
Hedgehog/Smoothened (21)
Protease-activated Receptor (20)
Sigma receptor (20)
CCR (19)
Glucagon Receptor (18)
GNRH Receptor (18)
Potassium Channel (14)
OX Receptor (14)
Calcium Channel (13)
Neuropeptide Y Receptor (13)
Endothelin Receptor (13)
SGLT (13)
Vasopressin Receptor (13)
Bradykinin Receptor (13)
P2 Receptor (12)
PDE (12)
GPCR19 (11)
Endogenous Metabolite (11)
Melanocortin Receptor (11)
Rho (10)
CDK (10)
GHSR (10)
LPA Receptor (10)
P450 (9)
cAMP (9)
cholecystokinin (8)
COX (8)
Raf (7)
Estrogen/progestogen Receptor (7)
Guanylate cyclase (7)
GTPase (7)
NF-κB (6)
Neurotensin Receptor (6)
CaSR (6)
NOS (6)
TNF (6)
PPAR (5)
PKA (5)
VEGFR (5)
Sodium Channel (5)
Annexin A (5)
GRK (5)
LTR (5)
Oxytocin Receptor (5)
HIV Protease (5)
CaMK (4)
Somatostatin (4)
IL Receptor (4)
Lipoxygenase (4)
MAO (4)
MT Receptor (4)
PAFR (4)
Autophagy (4)
PI3K (4)
PKC (3)
Thrombin (3)
Syk (3)
Transferase (3)
Apoptosis (3)
AMPK (3)
GABA Receptor (3)
TSH Receptor (3)
ROS (3)
ATPase (3)
EGFR (3)
EBI2/GPR183 (3)
Phospholipase (3)
CRFR (3)
Antifection (3)
MAPK (3)
Casein Kinase (3)
MRP (3)
Bombesin Receptor (3)
ABC (2)
FXR (2)
Tyrosinase (2)
Glucokinase (2)
TRP/TRPV Channel (2)
Adiponectin receptor (2)
Serotonin Transporter (2)
TGF-beta/Smad (2)
HSP (2)
Integrin (2)
NO Synthase (2)
Melanin-concentrating Hormone Receptor (MCHR) (2)
NMDAR (2)
NADPH (2)
Pim (2)
Leukotriene Receptor (2)
LRRK2 (2)
HIF (2)
Microtubule Associated (2)
STAT (2)
GSK-3 (2)
Melatonin Receptor (2)
LDL (2)
HDAC (2)
ROCK (2)
HER (2)
Cysteine Protease (1)
Dehydrogenase (1)
c-RET (1)
DNA/RNA Synthesis (1)
Liver X Receptor (1)
lysosomal autophagy (1)
Lipid (1)
DNA Alkylation (1)
ERK (1)
DYRK (1)
IκB/IKK (1)
Epigenetic Reader Domain (1)
Immunology & Inflammation related (1)
FAK (1)
FGFR (1)
FLT (1)
Free radical scavengers (1)
IAP (1)
Hydroxylase (1)
Gap Junction Protein (1)
Histone Methyltransferase (1)
HCV Protease (1)
HBV (1)
GST (1)
c-Myc (1)
MMP (1)
CGRP Receptor (1)
Antibacterial (1)
Src (1)
Serine Protease (1)
ROR (1)
Wnt/beta-catenin (1)
Retinoid Receptor (1)
Reductase (1)
RAR/RXR (1)
Acyltransferase (1)
Proteasome (1)
Adenylyl cyclase (1)
P-gp (1)
PDGFR (1)
Androgen Receptor (1)
PARP (1)
Parasite (1)
cell cycle arrest (1)
NADPH-oxidase (1)
Topoisomerase (1)
Caspase (1)
Monoamine Transporter (1)
Carbonic Anhydrase (1)
Motilin Receptor (1)
MPO (1)
BCL (1)
Antifolate (1)
NOD (1)
Aurora Kinase (1)
NPC1L1 (1)
Nucleoside Antimetabolite/Analog (1)
Apelin receptor (1)
Antifungal (1)
GPX (1)

Library Information Sample

Empty 1000025-07-9 1000413-72-8 229005-80-5 1000787-75-6 946387-07-1 1000998-59-3 1175526-27-8 1001288-58-9 1001350-96-4 1001404-83-6 Empty
Vadadustat TAK875 TAK-779 Tegobuvir RN-1734 BMS-687453 AM211 FT011 BMS754807 AAI101
Empty 1001625-82-6 1001645-58-4 1001753-24-7 1001908-89-9 1002304-34-8 1002-84-2 100291-86-9 100299-08-9 10030-52-1 10040-45-6 Empty
RPW-24 SRT1720 hydrochloride INH6 SRT 2183 AMG208 Pentadecanoic acid Apiopaeonoside Pemirolast potassium L-Anserine nitrate salt Sodium Picosulfate
Empty 100427-26-7 1004316-88-4 10045-45-1 100462-37-1 1004990-28-6 100-51-6 1005-24-9 1005264-47-0 1005334-57-5 1005342-46-0 Empty
Lercanidipine Cobicistat 1-Ethyl-2-benzimidazolinone ROSIRIDIN PF-AKT400 Benzyl alcohol 1-Methylnicotinamide chloride MX69 CVT-10216 LCL161
Empty 1005491-05-3 100-55-0 1005504-62-0 1005883-72-6 100643-71-8 1007207-67-1 10075-50-0 1007647-73-5 100784-20-1 10083-24-6 Empty
Tirasemtiv Roniacol Rg3039 Z433927330 Desloratadine CH5132799 5-Bromoindole Smurf1-IN-A01 Halosulfuron-methyl Piceatannol
Empty 100872-83-1 100874-08-6 1009119-64-5 1009119-65-6 100929-71-3 1009298-09-2 1009298-59-2 100929-99-5 1009734-33-1 10097-84-4 Empty
ML346 SB 4 Daclatasvir Daclatasvir dihydrochloride NADPH (tetracyclohexanamine) AZD8055 Vistusertib PAβN dihydrochloride HZ1157 Rotundine
Empty 1009816-48-1 1009817-63-3 1009820-21-6 100986-85-4 101001-34-7 1010411-21-8 1010-60-2 1011244-68-0 1011301-27-1 1011529-10-4 Empty
Thiamet G B-AP15 Silmitasertib Levofloxacin Pamicogrel GSK369796 Dihydrochloride 2-Chloronaphthoquinone TFAP Tenovin3 Azvudine
Empty 101152-94-7 101155-02-6 1011557-82-6 1011-74-1 101-20-2 1012054-59-9 101-21-3 101-26-8 101303-98-4 1013101-36-4 Empty
Milnacipran hydrochloride BW-A78U Tenovin-6 DL-Normetanephrine hydrochloride Triclocarban CUDC101 Chlorpropham Mestinon Zacopride hydrochloride PF04691502
Empty 101-31-5 1013-69-0 1013750-77-0 1013753-99-5 10138-52-0 1013920-15-4 1013937-63-7 1014691-61-2 101477-54-7 101494-95-5 Empty
L-Hyoscyamine Noreugenin ML-030 BC-1382 Gadolinium chloride Vorolanib VTP-27999 TFA GSK0660 Lomerizine hydrochloride 8-CHLOROQUINAZOLIN-4(1H)-ONE