Huang Huang

• Led small molecule drug discovery projects through hit identification, hit-to-lead, lead optimization, PK/PD, efficacy, toxicity study, formulation development, development candidate (DC) nomination, and process development (GMP scale-up) • Led the internal chemistry team (4 PhD chemists) for structure-based drug design (SBDD) and multi-parameter optimization across the portfolio • Supported platform establishment, worked with multi-disciplinary team to validate molecular glue/degrader series • Managed external chemistry team (multiple CROs, up to 30 FTEs) for communication, troubleshooting, and synthesis prioritization • Routinely prepared and presented project progress to Joint Steering Committee (JSC) • Review and nominate new targets together with leadership team • Worked actively with IP team and patent attorneys to support patent filings

• Leading chemistry and design for oncology drug discovery projects • Managing Chemistry and Design Group Meeting and organizing educational seminar series • Integrating MOE and SeeSAR into molecular design for prioritizing synthesis

• Functioned as chemistry lead/co-lead for 3 drug discovery projects • Designed and synthesized 2 chemical series (>100 compounds), explored structure-activity relationship, and performed multiparameter optimization for developing small molecule agonist of STING. Phase I clinical trial of SNX281 was initiated in Nov 2020 • Creatively used SeeSAR in preliminary molecular modeling to support computational team on Free Energy Perturbation (FEP) • Performed troubleshooting for external chemistry team (10-15 FTEs), and synthesized gram-scale of deuterated development candidate to support CMC/process chemistry

Principal Investigators: Dr. Tomasz Cierpicki & Dr. Jolanta Grembecka • Designed and synthesized the first-in-class NSD1/3 covalent inhibitors with in vivo activity • Designed and synthesized novel Menin-MLL protein-protein interaction inhibitors • Applied fragment-based and structure-based drug design on structural optimization • Executed multi-step organic synthesis (up to 23 steps) and scale-up for biological assays • Analyzed structure-activity relationship based on in vitro and in vivo assays • Contributed in a team of multiple disciplines including medicinal chemistry, computational chemistry, chemical biology, structural biology and crystallography

• Provided organic synthesis service to support drug discovery for Takeda, San Diego • Designed and executed multi-step organic synthesis (up to 20 steps) for biological screening • Solved challenging organic chemistry problems and mentored 2 junior (B.S.) scientists

Principal Investigators: Dr. Tomasz Cierpicki & Dr. Jolanta Grembecka • Designed and synthesized the first-in-class NSD1/3 covalent inhibitors with in vivo activity • Designed and synthesized novel Menin-MLL protein-protein interaction inhibitors • Applied fragment-based and structure-based drug design on structural optimization • Executed multi-step organic synthesis (up to 23 steps) and scale-up for biological assays • Analyzed structure-activity relationship based on in vitro and in vivo assays • Contributed in a team of multiple disciplines including medicinal chemistry, computational chemistry, chemical biology, structural biology and crystallography

Principal Investigators: Dr. Hualiang Jiang & Dr. Jian Li Discovery of FXR ligands against metabolic syndrome • Designed and synthesized 1, 3, 4-trisubstituted-pyrazolone derivatives as novel, potent and non-steroidal FXR selective antagonists, elucidated molecular mechanism of FXR modulation • Applied pharmacophore combination to structural modification for mechanism study on agonism /antagonism of FXR Discovery of FP-2 & DHFR dual inhibitors as anti-Malaria agents • Designed and synthesized the first-in-class FP-2 & DHFR dual inhibitors for treatment of Malaria • Applied pharmacophore combination for optimization of DHFR inhibitor Organic synthesis methodology development for drug discovery • Developed novel approach to synthesize unnatural amino-acids with 3-hydroxyoxindole skeleton via a one-pot, three-component procedure • Developed the first oxidative amination towards primary amine/amides under I-/TBHP catalytic system in water