David Lapinsky

Associate Professor
School of Pharmacy
Graduate School of Pharmaceutical Sciences

Mellon 422B
Phone: 412.396.6069


Wiess Instructor of Chemistry, Rice University, 2004–07
Post-Doctoral Researcher, Johns Hopkins University, 2003–04
Ph.D., Medicinal Chemistry, The Ohio State University, 2003
B.S., Pharmacy, Duquesne University, 1997

In the areas of chemical biology and medicinal chemistry, the Lapinsky research group primarily focuses on the rational design and synthesis of clickable photoaffinity ligands. These are valuable compounds that can be used for:

  • Target identification of hit compounds originating from phenotypic screening campaigns
  • Mechanism of action studies, confirmation of target engagement, or selectivity profiling (also known as Affinity-Based Protein Profiling (AfBPP))
  • Characterizing the interactions of small-molecules with drug targets
  • Determining binding sites within target proteins

In The Lab With Dr. David Lapinsky:

#MeetTheProfessors YouTube Series: Dr. David Lapinsky


Commonwealth Universal Research Enhancement (C.U.R.E.) Award
"Fully Functionalized Small-Molecule Probes for Oncology Drug Discovery"
1/1/16 - 12/31/17

R21MH098127 National Institute of Mental Health (NIMH) NIH Grant
Co-Principal Investigators: M. Cascio, Ph.D. and D. J. Lapinsky, Ph.D.
"Photoprobes for Identifying Potential Anti-Depressant and Anti-Anxiety Medications"
4/17/13 - 3/31/15

R03DA027081 NIDA NIH Grant (Early Career Award in the Chemistry of Drug Abuse)
Non-Tropane Irreversible Dopamine Transporter Ligands
7/1/09 to 6/30/11

Duquesne University Faculty Development Fund
The Search for Medications to Treat Psychostimulant Dependence: Rational Drug Design by Molecular Hybridization of Modafinil and Piperazine-Based Dopamine Transporter Inhibitors
5/1/09 to 6/30/11

Hunkele Dreaded Disease Award
"Molecular modeling-guided discovery and design of novel irreversible ligands for the dopamine transporter, the brain's cocaine receptor"
7/1/08 - 6/30/09

Select Publications

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators. Gregory, Karen J.; Velagaleti, Ranganadh; Thal, David M.; Brady, Ryan M.; Christopoulos, Arthur; Conn, P. Jeffrey; Lapinsky, David J. ACS Chemical Biology (2016), 11(7), 1870-1879.

Recent developments and applications of clickable photoprobes in medicinal chemistry and chemical biology. Lapinsky, David J.; Johnson, Douglas S. Future Medicinal Chemistry (2015), 7(16), 2143-2171.

Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram. Kumar, Vivek; Yarravarapu, Nageswari; Lapinsky, David J.; Perley, Danielle; Felts, Bruce; Tomlinson, Michael J.; Vaughan, Roxanne A.; Henry, L. Keith; Lever, John R.; Newman, Amy Hauck. Journal of Medicinal Chemistry (2015), 58(14), 5609-5619.

Tandem photoaffinity labeling-bioorthogonal conjugation in medicinal chemistry. Lapinsky, David J. Bioorganic & Medicinal Chemistry (2012), 20(21), 6237-6247.

Evolution of a Compact Photoprobe for the Dopamine Transporter Based on (±)-threo-Methylphenidate. Lapinsky, David J.; Yarravarapu, Nageswari; Nolan, Tammy L.; Surratt, Christopher K.; Lever, John R.; Tomlinson, Michael; Vaughan, Roxanne A.; Deutsch, Howard M. ACS Medicinal Chemistry Letters (2012), 3(5), 378-382.

Bupropion Binds to Two Sites in the Torpedo Nicotinic Acetylcholine Receptor Transmembrane Domain: A Photoaffinity Labeling Study with the Bupropion Analogue [125I]-SADU-3-72. Pandhare, Akash; Hamouda, Ayman K.; Staggs, Brandon; Aggarwal, Shaili; Duddempudi, Phaneendra K.; Lever, John R.; Lapinsky, David J.; Jansen, Michaela; Cohen, Jonathan B.; Blanton, Michael P. Biochemistry (2012), 51(12), 2425-2435.

Identification of a Novel Selective Serotonin Reuptake Inhibitor by Coupling Monoamine Transporter-Based Virtual Screening and Rational Molecular Hybridization. Nolan, Tammy L.; Lapinsky, David J.; Talbot, Jeffery N.; Indarte, Martin; Liu, Yi; Manepalli, Sankar; Geffert, Laura M.; Amos, Mary Ellen; Taylor, Phillip N.; Madura, Jeffry D.; et al. ACS Chemical Neuroscience (2011), 2(9), 544-552.

A novel photoaffinity ligand for the dopamine transporter based on pyrovalerone. Lapinsky, David J.; Aggarwal, Shaili; Huang, Yurong; Surratt, Christopher K.; Lever, John R.; Foster, James D.; Vaughan, Roxanne A. Bioorganic & Medicinal Chemistry (2009), 17(11), 3770-3774.


PHBM 435 - Pain, Musculoskeletal, and Connective Tissue Disorders Module

PHBM 436 - Respiratory, Dermatology, and Ophthalmic Disorders Module

PHBM 437 - Endocrine Module

PHBM 441 - Hematology, Oncology, and Transplantation Module

GPSC 516 - Synthetic Organic Medicinal Chemistry I

GPSC 517 - Synthetic Organic Medicinal Chemistry II