Rapid covalent-probe discovery by electrophile-fragment screening

Covalent probes can display unmatched potency, selectivity, and duration of action; however, their discovery is challenging. In principle, fragments that can irreversibly bind their target can overcome the low affinity that limits reversible fragment screening, but such electrophilic fragments were...

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Bibliographic Details
Main Authors:	Resnick, E, Bradley, A, Gan, J, Douangamath, A, Krojer, T, Sethi, R, Geurink, PP, Aimon, A, Amitai, G, Bellini, D, Bennett, J, Fairhead, M, Fedorov, O, Gabizon, R, Guo, J, Plotnikov, A, Reznik, N, Ruda, GF, Díaz-Sáez, L, Straub, VM, Szommer, T, Velupillai, S, Zaidman, D, Zhang, Y, Coker, AR, Dowson, CG, Barr, HM, Wang, C, Huber, KVM, Brennan, PE, Ovaa, H, Von Delft, F, London, N
Format:	Journal article
Language:	English
Published:	American Chemical Society 2019

Rapid covalent-probe discovery by electrophile-fragment screening

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