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GPCR Compound Library Plus

Catalog No. L1580
  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.

GPCR Compound Library Plus from TargetMol, a focused small molecule library, was developed against particular GPCRs containing 338 GPCR-active agents with IC50 less than 3.5 μM for GPCR drug discovery, target identification, and research in signaling pathway.

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
Request Library
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Product Description

  • Quantity: well-chosen 338 GPCR targeting compounds with unique structures;
  • High bioactivity: All compounds with IC50 below 3.5 μM;
  • Targets include 21 various GPCR subtypes;
  • Detailed compound information with structure, target, activity, IC50 value, and biological activity description;
  • HNMR/LCMS validated to ensure high purity and quality;
  • A powerful tool for GPCR drug development and target identification.

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
Request Library Compound List (L1580)

Publications Cited TargetMol Libraries

1. Cell Stem Cell. 2022 Apr 29(4) 545–558. 2. Science Bulletin. 2022. 3. Science Translational Medicine. 2022, 14(656): eabn3231. 4. Science Advances. 2023, 9(9): eade3760. 5. Nature. 2020, 582: 289-293. 6. Nature Biotechnology. 2021, 39(11): 1444-1452. 7. Nature Communications. 2022, 13(1): 1-15.. 8. Nature Communications. 2023, 14(1): 1020.. 9. Nature Communications. 2023, 14(1): 2756..
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Library Composition

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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