Please note that all times listed currently reflect US Eastern Time (ET). The schedule is subject to change.
Presentations are pre-recorded followed by live Q&A

Tuesday, August 10th, 2021
Time Event
8:30 am – 8:45 am Introduction and Welcome:
Bryan Roth (University of North Carolina, Chapel Hill) & Lily Jan (University of California, San Francisco)
8:45 am – 9:30 am Keynote Address: Ardem Patapoutian (Scripps/HHMI) 
The role of mechanosensitive PIEZO proteins in physiology and disease
9:30 am – 9:45 am Break
9:45 am – 12:00 pm Session 1: Integrative approaches to illuminate the Dark Genome
Chair: Tudor Oprea
9:45 am – 10:15 am Dac-Trung Nguyen/Ewy Mathé  (NIH)  
The PHAROS Resource to Illuminate the Dark Genome
10:15 am – 10:45 am Ellen McDonagh (Open Targets)
The OPEN-TARGETS Initiative
10:45 am – 11:15 am Avi Ma'ayan (Icahn School of Medicine at Mount Sinai)
Data Integration
11:15 am – 11:45 am Michael Sundstrom (Karolinska Institute)
Chemical Probes for the druggable genome (IMI initiative)
11:45 am – 12:00 pm Questions and Answers
12:00 pm – 1:15 pm Break 
12:15 pm – 1:00 pm Meet the Experts Session - John Allen, PhD, University of Texas Medical Branch; and Fiona McMurray, PhD, Novo Nordisk
1:15 pm – 3:30 pm Session 2: Machine Learning & Artificial Intelligence
Chair: Avi Ma'ayan
1:15 pm – 1:42 pm Kim Branson (GSK)
AI in Pharma
1:42 pm – 2:10 pm Ivan Ozerov (Insilico Medicine)
PandaOmics as a tool for omics research and target identification
2:10 pm – 2:37 pm Monica Munoz-Torres (University of Colorado Anschutz Medical Campus) and Justin Reese (Lawrence Berkeley National Laboratory)
The Monarch Initiative
2:37 pm – 3:05 pm Nadine Spielmann (Helmholz Zentrum Munich)
Mouse phenotypes and ML to identify novel genes in pediatric cardiology
3:05 pm – 3:17 pm Short Talk: Evangelia Petsalaki (EMBL-EBI)
Data-driven approaches to shed light on the understudied human cell signalling network
3:17 pm  – 3:30 pm Questions and Answers
3:30 pm – 3:45 pm Break
3:45 pm – 5:00 pm Session 3: Ion Channels as Understudied Targets
Chair: Lily Jan
(University of California, San Francisco)
3:45 pm – 3:57 pm Ryan Hibbs  (University of Texas Southwestern Medical Center)
Nicotinic acetylcholine receptor structure, gating and pharmacology
3:57 pm – 4:10 pm Amy Lee (University of Texas-Austin)
CACNA2D4: not just a retina-specific Ca++ channel
4:10 pm – 4:22 pm Annette Dolphin (University College London)
Physiological and medical implications of understudied calcium channels
4:22 pm – 4:34 pm Henry M. Colecraft (Columbia University)
Calcium channel beta subunits as understudied targets
4:34 pm – 4:46 pm Edward C. Cooper (Baylor College of Medicine)
4:46 pm – 5:00 pm Questions and Answers
5:00 pm – 6:00 pm General Discussion and Short Talks
Short Talk: Jessica Maiers
(Indiana School of Medicine)
The ER-resident ion channel TMEM38B drives fibrogenesis through promoting procollagen I secretion
Short Talk: Thomas Brett (Washington University)
Structural and functional investigations of CLCA proteins as potentiators of TMEM16 family members
Wednesday, August 11th, 2021
Time Event
9:30 am – 9:45 am Day Two: Greetings and Intro to Day 2
Bryan Roth and Lily Jan
9:45 am – 11:50 am Session 4: Understudied Ion Channels
Chair: Lily Jan
9:45 am – 10:07 am Zhaozhu Qiu (Johns Hopkins Medicine)
From SWELL to PAC: Discovery of Novel Chloride Channels
10:07 am – 10:30 am Emily Liman (University of Southern California)
OTOP Proton Channels: From Function to Structure 
10:30 am – 10:52 am Juan Du (Van Andel Institute)
Activation and inhibition mechanisms of the "taste channel" TRPM5
10:52 am – 11:15 am Manuel L. Covarrubias (Thomas Jefferson University)
The unique extracellular turret region of Kv3 channels determines the selective mode of action of a new class of positive allosteric modulators
11:15 am – 11:37 am Mark T. Nelson (University of Vermont)
Novel ion channels in the vasculature
11:37 am – 11:50 am Questions and Answers
11:50 am – 1:15 pm Break
12:15 pm – 1:00 pm Career Development Session: NIH and Academic Roundtable - Bryan Roth, PhD,  UNC Chapel Hill, Karlie Sharma, PhD, NIH, and Larry Sklar, PhD, Intellicyt
1:15 pm – 2:30 pm Poster Session 1 - Session time will be devoted to Q&A between poster presenters and attendees
2:30 pm – 2:45 pm Break
2:45 pm – 4:50 pm Session 5: Understudied Kinases as Druggable Targets 
Chair: Gary Johnson
(UNC Chapel Hill)
2:45 pm – 3:07 pm Ben Turk (Yale School of Medicine)
Substrate specificity profiling of dark kinases
3:07 pm – 3:30 pm Anne Claude Gingras (Lunenfeld-Tanenbaum Research Institute)
Protein kinase and phosphatase networks in control of cell phenotypes
3:30 pm – 3:52 pm Natalie Ahn (University of Colorado Boulder/HHMI)
Intermittent Treatment of BRAFV600E Melanoma Cells Delays Resistance by Adaptive Resensitization to Drug Rechallenge
3:52 pm – 4:15 pm Nienke Moret (Harvard Medical School)
Redefining the human kinome
4:15 pm – 4:37 pm Patrick Eyers (University of Liverpool)
Function and targeting of pseudokinases
4:37 pm  – 4:50 pm Questions and Answers
Thursday, August 12th, 2021
Time Event
8:30 am – 8:45 am Introduction
Bryan Roth and Lily Jan
8:45 am – 9:30 am Poster Session 2 - Session time will be devoted to Q&A between poster presenters and attendees
9:30 am – 9:45 am Break
9:45 am – 11:50 am Session 6: Kinases as Understudied Targets and Computational Approaches
Chair: Shawn Gomez (UNC - Chapel Hill)
9:45 am – 10:07 am Fleur Ferguson (University of California San Diego)
Chemoproteomic approaches to interrogate the understudied degradable kinome
10:07 am – 10:30 am Robert Sprung (Washington University in St. Louis)
Multiplexed PRM for Comprehensive Quantitation of Human Protein Kinase Networks
10:30 am – 10:52 am Nicola Smith (UNSW Sydney)
Not all mice are created equal - challenges understanding the cardiovascular role of orphan GPR37L1
10:52 am – 11:15 am John Allen (University of Texas Medical Branch)
Illuminating signaling and agonists for the self-activating brain orphan GPR52
11:15 am – 11:37 am David E. Gloriam (University of Copenhagen)
Novel pairings in the human peptide-receptor signaling system
11:37 am  – 11:50 am Questions and Answers
11:50 am – 12:15 pm Break
12:15 pm – 12:45 pm Discussion led by Bryan Roth
The understudied proteome in the era of AlphaFold
12:45 pm – 1:00 pm Break
1:00 pm – 2:40 pm Session 7: Computational and Novel Approaches to Discover Drug-Like Molecules at Understudied Targets
Chair: Bryan Roth
1:00 pm – 1:17 pm Brian Shoichet (University of California San Francisco)
Ultra-Large Library Docking for Novel Ligands with New Pharmacology
1:17 pm – 1:35 pm Andrew Hopkins (Exscientia)
Network pharmacology as an integrative approach to illuminate the druggable genome
1:35 pm – 1:52 pm Jonathan Fay (UNC Chapel Hill)
Active state ensemble of an itch receptor revealed by cryo-EM
1:52 pm – 2:10 pm Daniel Isom (University of Miami)
Proton-gated coincidence detection in GPCR signaling
2:10 pm – 2:27 pm Laura M. Wingler (Duke University)
Illuminating the role of conformational heterogeneity in GPCR pharmacology
2:27 pm – 2:40 pm Questions and Answers
2:40 pm – 3:00 pm Break
3:00 pm – 4:45 pm Session 8: GPCRs as Understudied Targets
Chair: Brian Shoichet
3:00 pm – 3:22 pm Olivier Civelli (University of California Irvine)
Reverse pharmaceutical research
3:22 pm – 3:45 pm Heidi Hamm (Vanderbilt University)
Role of beta/gamma subunits in illuminating GPCR function
3:45 pm – 4:07 pm Lakshmi A. Devi (Icahn School of Medicine at Mount Sinai)
Targeted Deorphanization of G protein-coupled Receptors
4:07 pm – 4:19 pm Short Talk: Anthony Abeyta-Lopez (University of New Mexico)
Development of CX3CR1 agonists using drug repurposing methods
4:19 pm – 4:31 pm Short Talk: Cesare Orlandi (University of Rochester)
In vitro profiling of orphan G protein coupled receptor (GPCR) constitutive activity
4:31 pm – 4:45 pm Questions and Answers
4:45 pm – 5:00 pm Wrap-up 
Michael McManus, Brian Shoichet