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 1940 GPCR-active agents for GPCR drug discovery.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

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)

Request for Quote

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

Request Library

Product Description

A unique collection of 1940 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

Supporting Files

Library Handling Instructions (635 KB) Targetmol Library Catalog (13.2 MB) Request for Library Compostion in Excel and SDF files

Publications Cited TargetMol Libraries

1. Nature Genetics. 2018, 50(12): 1666-1673. 2. Viruses. 2021 Jun 3;13(6):1061. 3. Microbiology and Immunology. 2020, 64(5): 345-355. 4. bioRxiv. 2023: 2023.05. 24.542186.. 5. Cell Stem Cell. 2022 Apr 29(4) 545–558. 6. Science Bulletin. 2022. 7. Science Translational Medicine. 2022, 14(656): eabn3231. 8. Science Advances. 2023, 9(9): eade3760. 9. Nature. 2020, 582: 289-293.

10. Nature Biotechnology. 2021, 39(11): 1444-1452. 11. Nature Communications. 2022, 13(1): 1-15.. 12. Nature Communications. 2023, 14(1): 1020.. 13. Nature Communications. 2023, 14(1): 2756.. 14. Blood. 2021, 137(11): 1478-1490. 15. Nucleic Acids Research. 2021. 16. Nature Communications. 2023, 14(1): 7574. 17. Advanced Science. 2020, 7(16): 2000925. 18. Angewandte Chemie. 2021. 19. Acta Pharmaceutica Sinica B. 2022. 20. Protein & Cell. 2021, 12(11): 877-888. 21. Bone Research. 2023, 11(1): 54. 22. Pharmacology & Therapeutics. (2021): 107930. 23. Nature Communications. 2021, 12(1): 1-12. 24. Journal of Cell Biology. 2022, 221(5): e202112024.

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Library Composition

5-HT Receptor (378)

Adrenergic Receptor (270)

Dopamine Receptor (233)

Histamine Receptor (180)

GPR (102)

Prostaglandin Receptor (100)

Adenosine Receptor (97)

Opioid Receptor (84)

Ras (75)

Apoptosis (68)

Autophagy (67)

Cannabinoid Receptor (66)

Endogenous Metabolite (58)

AChR (50)

S1P Receptor (39)

CXCR (39)

Hedgehog/Smoothened (35)

LPL Receptor (33)

Sigma receptor (30)

Neurokinin receptor (28)

Norepinephrine (26)

Serotonin Transporter (26)

Protease-activated Receptor (25)

Endothelin Receptor (24)

Antibacterial (24)

Glucagon Receptor (23)

SGLT (22)

Calcium Channel (22)

cAMP (21)

P2Y Receptor (21)

PDE (20)

Leukotriene Receptor (20)

Potassium Channel (20)

Neuropeptide Y Receptor (19)

Guanylate cyclase (19)

LPA Receptor (18)

OX Receptor (17)

P450 (15)

cholecystokinin (14)

GTPase (14)

Rho (13)

GPCR19 (12)

Smo (12)

Parasite (11)

Vasopressin Receptor (11)

CaSR (11)

GHSR (11)

NO Synthase (11)

Melatonin Receptor (10)

COX (10)

Influenza Virus (10)

GRK (10)

Bradykinin Receptor (9)

Raf (9)

Neurotensin Receptor (9)

Sodium Channel (9)

Antibiotic (9)

NF-κB (9)

Antifungal (8)

PAFR (8)

TRP/TRPV Channel (8)

PPAR (8)

Somatostatin (8)

Arrestin (7)

Reactive Oxygen Species (7)

LTR (7)

Annexin A (7)

CaMK (7)

HIV Protease (7)

Lipoxygenase (6)

IL Receptor (6)

Monoamine Oxidase (6)

Glucocorticoid Receptor (6)

Melanocortin Receptor (6)

CDK (6)

MT Receptor (6)

Mitophagy (6)

AChE (6)

P-gp (6)

PKA (6)

TSH Receptor (6)

PI3K (6)

Drug Metabolite (5)

Bombesin Receptor (5)

GABA Receptor (5)

HCV Protease (5)

TNF (5)

CGRP Receptor (5)

Transferase (5)

EGFR (5)

NOS (5)

CRFR (5)

GNRH Receptor (5)

Thrombin (4)

Phospholipase (4)

DNA/RNA Synthesis (4)

MAPK (4)

HSP (4)

Melanin-concentrating Hormone Receptor (MCHR) (4)

ROS (4)

P2X Receptor (4)

Histone Methyltransferase (4)

Virus Protease (4)

PKC (4)

ERK (4)

MAO (4)

HER (4)

NMDAR (4)

Immunology/Inflammation related (3)

RAAS (3)

HDAC (3)

STAT (3)

ABC (3)

Ferroptosis (3)

Anti-infection (3)

Glutathione Peroxidase (3)

Akt (3)

VEGFR (3)

p38 MAPK (3)

ROCK (3)

GluR (3)

iGluR (3)

FXR (3)

Oxytocin Receptor (3)

Adiponectin receptor (3)

Apelin receptor (3)

CCR (3)

FAAH (3)

ATPase (3)

Imidazoline Receptor (3)

MRP (2)

Reductase (2)

HBV (2)

transporter (2)

PAK (2)

HSV (2)

Monoamine Transporter (2)

Wnt/beta-catenin (2)

Beta Amyloid (2)

DYRK (2)

HIF (2)

Hydroxylase (2)

Phosphatase (2)

SARS-CoV (2)

MMP (2)

Microtubule Associated (2)

DNA (2)

EBI2/GPR183 (2)

Topoisomerase (2)

Estrogen/progestogen Receptor (2)

Caspase (2)

LDL (2)

Syk (2)

NADPH (1)

RAR/RXR (1)

HIF/HIF Prolyl-Hydroxylase (1)

FAK (1)

Carbonic Anhydrase (1)

ROR (1)

PERK (1)

RXFP receptor (1)

Mitochondrial Metabolism (1)

Adenosine deaminase (1)

FLT (1)

FGFR (1)

Tyrosinase (1)

AhR (1)

MEK (1)

Platelet aggregation (1)

Neuropeptide W (1)

Integrin (1)

Na+/Ca2+ Exchanger (1)

NADPH-oxidase (1)

Adenylyl cyclase (1)

lysosomal autophagy (1)

Gap Junction Protein (1)

Dehydrogenase (1)

YAP (1)

GST (1)

AMPK (1)

GlyT (1)

TGF-beta/Smad (1)

Interleukin (1)

PROTAC Linker (1)

Androgen Receptor (1)

BCL (1)

Amylase (1)

Epigenetic Reader Domain (1)

Aurora Kinase (1)

PGE Synthase (1)

PAD (1)

IAP (1)

PTEN (1)

Angiotensin-converting Enzyme (ACE) (1)

FLAP (1)

Motilin Receptor (1)

Stearoyl-CoA Desaturase (SCD) (1)

Proteasome (1)

ATP Citrate Lyase (1)

Cysteine Protease (1)

CRISPR/Cas9 (1)

IκB/IKK (1)

GSK-3 (1)

Progesterone Receptor (1)

Glucosidase (1)

OCT (1)

Retinoid Receptor (1)

Reverse Transcriptase (1)

GPX (1)

c-Myc (1)

Antifolate (1)

RSV (1)

Free radical scavengers (1)

Trk receptor (1)

LRRK2 (1)

Estrogen Receptor/ERR (1)

PARP (1)

Acyltransferase (1)

Serine Protease (1)

Casein Kinase (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
Empty	Vadadustat	TAK875	TAK-779	Tegobuvir	RN-1734	BMS-687453	AM211	FT011	BMS754807	AAI101	Empty
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
Empty	RPW-24	SRT1720 hydrochloride	INH6	SRT 2183	AMG208	Pentadecanoic acid	Apiopaeonoside	Pemirolast potassium	L-Anserine nitrate salt	Sodium Picosulfate	Empty
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
Empty	Lercanidipine	Cobicistat	1-Ethyl-2-benzimidazolinone	ROSIRIDIN	PF-AKT400	Benzyl alcohol	1-Methylnicotinamide chloride	MX69	CVT-10216	LCL161	Empty
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
Empty	Tirasemtiv	Roniacol	Rg3039	Z433927330	Desloratadine	CH5132799	5-Bromoindole	Smurf1-IN-A01	Halosulfuron-methyl	Piceatannol	Empty
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
Empty	ML346	SB 4	Daclatasvir	Daclatasvir dihydrochloride	NADPH (tetracyclohexanamine)	AZD8055	Vistusertib	PAβN dihydrochloride	HZ1157	Rotundine	Empty
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
Empty	Thiamet G	B-AP15	Silmitasertib	Levofloxacin	Pamicogrel	GSK369796 Dihydrochloride	2-Chloronaphthoquinone	TFAP	Tenovin3	Azvudine	Empty
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
Empty	Milnacipran hydrochloride	BW-A78U	Tenovin-6	DL-Normetanephrine hydrochloride	Triclocarban	CUDC101	Chlorpropham	Mestinon	Zacopride hydrochloride	PF04691502	Empty
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
Empty	L-Hyoscyamine	Noreugenin	ML-030	BC-1382	Gadolinium chloride	Vorolanib	VTP-27999 TFA	GSK0660	Lomerizine hydrochloride	8-CHLOROQUINAZOLIN-4(1H)-ONE	Empty