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 covalent compounds. 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


Duquesne University Faculty Development/Robert Wintermeyer Fund
"Tackling African Cryptosporidiosis with Chemical Probes"
4/17/20 - 8/1/22

Neurocrine Biosciences, Inc. (Sponsored Research Agreement)
"Drug Target Identification for CNS Disorders"
1/16/19 - 1/15/20

Duquesne University Undergraduate Summer Research Fellowship (Matthew Wolowski)
"Confronting Cancer with Cysteine-Reactive Probes"
4/16/18 - 8/25/18

Charles Henry Leach II Fund
"Tackling Cancer with Fully-Functionalized Small-Molecule Probes"
8/15/17 - 5/15/18

Hunkele Dreaded Disease Award
"Fully Functionalized Small-Molecule Probes for Oncology Drug Discovery"
1/1/17 - 12/31/18

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

Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes.
Hellyer SD, Aggarwal S, Chen ANY, Leach K, Lapinsky DJ, Gregory KJ.
ACS Chem Neurosci. 2020 Jun 3;11(11):1597-1609. doi: 10.1021/acschemneuro.0c00009. Epub 2020 May 22.
PMID: 32396330

Clickable photoaffinity ligands for the human serotonin transporter based on the selective serotonin reuptake inhibitor (S)-citalopram.
Yarravarapu N, Geffert L, Surratt CK, Cascio M, Lapinsky DJ.
Bioorg Med Chem Lett. 2018 Nov 15;28(21):3431-3435. doi: 10.1016/j.bmcl.2018.09.029. Epub 2018 Sep 22.
PMID: 30266542

Appendage and Scaffold Diverse Fully Functionalized Small-Molecule Probes via a Minimalist Terminal Alkyne-Aliphatic Diazirine Isocyanide.
Jackson P, Lapinsky DJ.
J Org Chem. 2018 Sep 21;83(18):11245-11253. doi: 10.1021/acs.joc.8b01831. Epub 2018 Aug 31.
PMID: 30132667

Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 5 Based on Select Acetylenic Negative Allosteric Modulators.
Gregory KJ, Velagaleti R, Thal DM, Brady RM, Christopoulos A, Conn PJ, Lapinsky DJ.
ACS Chem Biol. 2016 Jul 15;11(7):1870-9. doi: 10.1021/acschembio.6b00026. Epub 2016 May 4.
PMID: 27115427

Novel Azido-Iodo Photoaffinity Ligands for the Human Serotonin Transporter Based on the Selective Serotonin Reuptake Inhibitor (S)-Citalopram.
Kumar V, Yarravarapu N, Lapinsky DJ, Perley D, Felts B, Tomlinson MJ, Vaughan RA, Henry LK, Lever JR, Newman AH.
J Med Chem. 2015 Jul 23;58(14):5609-19. doi: 10.1021/acs.jmedchem.5b00682. Epub 2015 Jul 8.
PMID: 26153715

Recent developments and applications of clickable photoprobes in medicinal chemistry and chemical biology.
Lapinsky DJ, Johnson DS.
Future Med Chem. 2015;7(16):2143-71. doi: 10.4155/fmc.15.136. Epub 2015 Oct 29.
PMID: 26511756


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