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. Author manuscript; available in PMC: 2026 Jul 11.
Published in final edited form as: Nat Rev Methods Primers. 2025 Aug 7;5:52. doi: 10.1038/s43586-025-00421-y

Table 2.

Examples of FEx/DOC-derived bioactive molecules.

Reference Library Size Biological Endpoint Example Hit Structure Potency
Bioactive Molecules Identified from Agnostic Compound Libraries
Wolan and Sharpless 201963 132 hNE (biochemical) graphic file with name nihms-2181599-t0006.jpg IC50 = 0.24 μM
Moses and Sharpless 2022183 88 hNE (biochemical) graphic file with name nihms-2181599-t0007.jpg IC50 = 2.1 μM
Rakesh and Qin 2019186 82 Staphylococcus aureus (bacterial) graphic file with name nihms-2181599-t0008.jpg MIC 0.81 μg/mL
Dong, Zhang and Sharpless 2021187 41 Staphylococcus aureus 43300 (bacterial) graphic file with name nihms-2181599-t0009.jpg MIC 1.1 μg/mL
Moses 202018 151 Staphylococcus aureus USA300 (bacterial) graphic file with name nihms-2181599-t0010.jpg MIC 0.625 μg/mL
Murthy 2019188 24 kanamycin-resistant Escherichia coli, MRSA (bacterial) graphic file with name nihms-2181599-t0011.jpg MIC99 0.66 μg/mL (E. coli) 5.28 μg/mL (MRSA)
Xu and Zhao 2024189 32 Rhizoctonia solani (fungi) graphic file with name nihms-2181599-t0012.jpg EC50 = 1.5 μg/mL
Wu 201985 40a HT-29 cell (cellular) graphic file with name nihms-2181599-t0013.jpg EC50 = 70 nM
Bioactive Molecules from FEx-enabled High-throughput Medicinal Chemistry (HTMC)
Sharpless and Wolan 202062 460a SpeB (biochemical) graphic file with name nihms-2181599-t0014.jpg Kd = 18 nM
Erb 2021190 576 (biochemical)a then 43 (cellular)a ENL-YEATS graphic file with name nihms-2181599-t0015.jpg EC50 = 63 nM (cellular)
Wilson and Wolan 202471 1,200a,b Influenza H1 (cellular) graphic file with name nihms-2181599-t0016.jpg EC50 = 0.7-19 nM (H1strains)
Erb 202488 3,180a CRBN/GSPT1 (cellular) graphic file with name nihms-2181599-t0017.jpg EC50 = 55 nM
Moses 202472 288c PDAC organoid proliferation (hM1A line) graphic file with name nihms-2181599-t0018.jpg IC50 = 6.8 nM
Liu, Qin and Tang 202346 102a AChE (biochemical) graphic file with name nihms-2181599-t0019.jpg IC50 = 94 nM
a

Unpurified reaction mixtures used for screening.

b

Total number including amide coupling products.

c

Used after removal of solvent and byproduct.

SpeB = streptococcal pyrogenic exotoxin B. ENL = eleven-nineteen leukemia. YEATS = Yaf9, ENL, AF9, Taf14, and Sas5. CRBN = cereblon. GSPT1 = G1 to S phase transition 1. PDAC = pancreatic ductal adenocarcinoma. AChE = acetylcholinesterase. IC50 = half maximal inhibitory concentration. MIC = minimum inhibitory concentration. EC50 = half maximal effective concentration. Kd = dissociation constant.