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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.
Compound Libraries | TargetMol
Pack Size
1 mg
30 μL * 10 mM (in DMSO)
50 μL * 10 mM (in DMSO)
100 μL * 10 mM (in DMSO)
250 μL * 10 mM (in DMSO)
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)

Publications Cited TargetMol Libraries

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Library Composition

5-HT Receptor (281)
Adrenergic Receptor (201)
Dopamine Receptor (187)
Histamine Receptor (139)
AChR (112)
Prostaglandin Receptor (78)
Apoptosis (74)
Autophagy (73)
GPR (73)
Endogenous Metabolite (67)
Opioid Receptor (65)
Adenosine Receptor (63)
Ras (59)
Cannabinoid Receptor (37)
Glucocorticoid Receptor (37)
GluR (35)
CXCR (33)
S1P Receptor (31)
LPL Receptor (29)
Hedgehog/Smoothened (27)
Serotonin Transporter (25)
RAAS (24)
Norepinephrine (24)
Antibacterial (23)
Neurokinin receptor (23)
Potassium Channel (22)
CCR (21)
Sigma receptor (21)
Protease-activated Receptor (21)
Calcium Channel (21)
Endothelin Receptor (17)
OX Receptor (16)
PDE (16)
Neuropeptide Y Receptor (16)
P450 (15)
SGLT (15)
NO Synthase (15)
Guanylate cyclase (15)
P2Y Receptor (15)
Glucagon Receptor (14)
NF-κB (13)
Melanocortin Receptor (13)
GNRH Receptor (13)
Parasite (12)
Leukotriene Receptor (12)
Smo (12)
Rho (12)
GTPase (12)
Influenza Virus (11)
cAMP (11)
HIV Protease (11)
LPA Receptor (10)
COX (10)
GPCR19 (10)
Vasopressin Receptor (10)
Antibiotic (10)
Sodium Channel (10)
Bradykinin Receptor (9)
Neurotensin Receptor (9)
CDK (9)
Raf (8)
GHSR (8)
CaSR (8)
Antifungal (8)
Melatonin Receptor (8)
Mitophagy (8)
cholecystokinin (7)
PPAR (7)
Drug Metabolite (7)
GRK (7)
AChE (7)
CaMK (7)
Reactive Oxygen Species (7)
PI3K (6)
Estrogen/progestogen Receptor (6)
PKA (6)
TRP/TRPV Channel (6)
Virus Protease (6)
LTR (5)
TNF (5)
MT Receptor (5)
NOS (5)
IL Receptor (5)
Transferase (5)
VEGFR (5)
Imidazoline Receptor (5)
PAFR (5)
Bombesin Receptor (5)
P-gp (5)
Annexin A (5)
GABA Receptor (5)
Lipoxygenase (5)
HER (5)
Ferroptosis (4)
HDAC (4)
MAPK (4)
DNA/RNA Synthesis (4)
Monoamine Oxidase (4)
HSP (4)
HCV Protease (4)
CGRP Receptor (4)
Oxytocin Receptor (4)
Adenylyl cyclase (4)
AMPK (4)
Histone Methyltransferase (4)
Phospholipase (3)
MAO (3)
PKC (3)
Progesterone Receptor (3)
iGluR (3)
Somatostatin (3)
Adiponectin receptor (3)
Thrombin (3)
STAT (3)
FXR (3)
Caspase (3)
SARS-CoV (3)
ROCK (3)
NMDAR (3)
CRFR (3)
Wnt/beta-catenin (3)
TSH Receptor (3)
ROS (3)
Anti-infection (3)
FGFR (2)
TGF-beta/Smad (2)
HIF (2)
Akt (2)
Syk (2)
Interleukin (2)
ATPase (2)
Microtubule Associated (2)
Casein Kinase (2)
EBI2/GPR183 (2)
Apelin receptor (2)
transporter (2)
Tyrosinase (2)
FLT (2)
Melanin-concentrating Hormone Receptor (MCHR) (2)
Topoisomerase (2)
HSV (2)
DYRK (2)
Monoamine Transporter (2)
BCL (2)
P2X Receptor (2)
ERK (2)
LDL (2)
PAK (2)
PARP (2)
Estrogen Receptor/ERR (2)
HBV (2)
MRP (2)
Androgen Receptor (2)
Glutathione Peroxidase (2)
p38 MAPK (2)
ABC (2)
GSK-3 (2)
Neuropeptide W (1)
NPC1L1 (1)
c-RET (1)
Adenosine deaminase (1)
RAR/RXR  (1)
Glucokinase (1)
MEK (1)
Liver X Receptor (1)
Carbonic Anhydrase (1)
Complement System (1)
Nucleoside Antimetabolite/Analog (1)
NOD (1)
Gap Junction Protein (1)
Platelet aggregation (1)
Cysteine Protease (1)
cell cycle arrest (1)
Hydroxylase (1)
NADPH-oxidase (1)
Antifolate (1)
Serine Protease (1)
Pim (1)
c-Myc (1)
lysosomal autophagy (1)
FAK (1)
HIF/HIF Prolyl-Hydroxylase (1)
OCT (1)
Phosphatase (1)
Amylase (1)
Integrin (1)
Immunology/Inflammation related (1)
MMP (1)
PDGFR (1)
Free radical scavengers (1)
Trk receptor (1)
LRRK2 (1)
Stearoyl-CoA Desaturase (SCD) (1)
Dehydrogenase (1)
PAD (1)
PROTAC Linker (1)
Aurora Kinase (1)
NADPH (1)
PGE Synthase (1)
Epigenetic Reader Domain (1)
IGF-1R (1)
Lipid (1)
DNA (1)
Proteasome (1)
RSV (1)
IAP (1)
Glucosidase (1)
ROR (1)
Na+/Ca2+ Exchanger (1)
FLAP (1)
Motilin Receptor (1)
Reductase (1)
CRISPR/Cas9 (1)
GlyT (1)
Src (1)
IκB/IKK (1)
Retinoid Receptor (1)
Mitochondrial Metabolism (1)
Reverse Transcriptase (1)
GPX (1)
Beta Amyloid (1)
GST (1)
Neprilysin (1)
Histone Demethylase (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
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