Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106

Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106 Descriptor: 2-methyl-4-[4-(trifluoromethyl)phenyl]pyrazolo[3,4-b]indole-7-carboxylic acid, SULFATE ION, Transcriptional enhancer factor TEF-1 Authors: Freire, F, Heinrich, T, Petersson, C, Schneider, R, Garg, S, Schwarz, D, Gunera, J, Seshire, A, Koetzner, L, Schlesiger, S, Musil, D, Schilke, H, Doerfel, B, Diehl, P, Boepple, P, Lemos, A.R, Sousa, P.M.F, Freire, F, Bandeiras, T.M, Carswell, E, Pearson, N, Sirohi, S, Hooker, M, Trivier, E, Broome, R, Balsiger, A, Crowden, A, Dillon, C, Wienke, D. Deposit date: 2022-04-11 Release date: 2022-07-13 Last modified: 2024-01-31 Method: X-RAY DIFFRACTION (2.19 Å) Cite: Optimization of TEAD P-Site Binding Fragment Hit into In Vivo Active Lead MSC-4106 . J.Med.Chem., 65, 2022

将结合TEAD转录因子（Transcriptional Enhancer Domain）P位点的片段命中物优化为体内活性先导化合物MSC-4106
化合物描述符：2-甲基-4-[4-(三氟甲基)苯基]吡唑并[3,4-b]吲哚-7-羧酸、硫酸根离子、转录增强因子TEF-1
作者：Freire F、Heinrich T、Petersson C、Schneider R、Garg S、Schwarz D、Gunera J、Seshire A、Koetzner L、Schlesiger S、Musil D、Schilke H、Doerfel B、Diehl P、Boepple P、Lemos A.R、Sousa P.M.F、Freire F、Bandeiras T.M、Carswell E、Pearson N、Sirohi S、Hooker M、Trivier E、Broome R、Balsiger A、Crowden A、Dillon C、Wienke D
入库日期：2022-04-11
发布日期：2022-07-13
最后修改日期：2024-01-31
实验方法：X射线衍射（分辨率2.19埃）
引用：《将结合TEAD P位点的片段命中物优化为体内活性先导化合物MSC-4106》，《药物化学杂志》，第65卷，2022年