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Query String: TGF-beta1

Callahan, JF; Burgess, JL; Fornwald, JA; Gaster, LM; Harling, JD; Harrington, FP; Heer, J; Kwon, C; Lehr, R; Mathur, A; Olson, BA; Weinstock, J; Laping, NJ Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5). J Med Chem 45: 999-1001 (2002)
Kinsella, T; Gelman, M; Hong, H; Darwish, IS; Singh, R; Yu, J; Borzilleri, RM; Velaparthi, U; Liu, P; Darne, CP; Rahaman, H; Warrier, JS TGF-β inhibitors US Patent US10287295 (2019)
Kinsella, T; Gelman, M; Hong, H; Darwish, IS; Singh, R; Yu, J; Borzilleri, RM; Velaparthi, U; Liu, P; Darne, C; Rahaman, H; Warrier, JS TGF-beta inhibitors US Patent US9884868 (2018)
Borzilleri, RM; Fink, BE; Harikrishnan, LS; Sankara Warrier, J TGF beta receptor antagonists US Patent US10292985 (2019)
Harikrishnan, LS; Fink, BE; Borzilleri, RM; Tonukunuru, G; Rahaman, H; Warrier, JS; Seshadri, B TGFβ receptor antagonist US Patent US10336761 (2019)
Kakeya, H; Hattori, A; Takasu, Y; Fujii, N; Oishi, S; Kojima, S; Hara, M TGF-β signal transduction inhibitor US Patent US8772297 (2014)
LU, L; LIU, X; ZHAO, S; ZHANG, L; HUANG, H; ZHANG, J; ZHU, J; WANG, X; CHEN, J; LING, S; LIAO, X TGF-ß INHIBITOR COMPOUND AND USE THEROF US Patent US20250215017 (2025)
LU, L; ZHAO, S; ZHANG, L; HUANG, H; ZHANG, J; ZHU, J; WANG, X; CHEN, J; LING, S; LIAO, X TGF-B INHIBITOR COMPOUND AND USE THEREOF US Patent US20250179094 (2025)
Bonafoux, D; Chuaqui, C; Boriack-Sjodin, PA; Fitch, C; Hankins, G; Josiah, S; Black, C; Hetu, G; Ling, L; Lee, WC 2-Aminoimidazoles inhibitors of TGF-beta receptor 1. Bioorg Med Chem Lett 19: 912-6 (2009)
Suto, MJ; Gupta, V; Mathew, B; Zhang, W; Pallero, MA; Murphy-Ullrich, JE Identification of Inhibitors of Thrombospondin 1 Activation of TGF-β. ACS Med Chem Lett 11: 1130-1136 (2020)
Sawyer, JS Substituted imidazoles for the inhibition of TGF-β and methods of treatment US Patent US12077548 (2024)
Sawyer, JS Tri-substituted imidazoles for the inhibition of TGF beta and methods of treatment US Patent US11124509 (2021)
Geldenhuys, WJ; Nakamura, H 3D-QSAR and docking studies on transforming growth factor (TGF)-beta receptor 1 antagonists. Bioorg Med Chem Lett 20: 1918-23 (2010)
BULLOUGH, DA; FOULKES, JG; Beeley, NR; Crystal, R METHODS FOR TREATING A PULMONARY DISEASE WITH AN ALK-5 (TGF BETA R1) INHIBITOR US Patent US20240307363 (2024)
Ye, L; Li, YL; Mellström, K; Mellin, C; Bladh, LG; Koehler, K; Garg, N; Garcia Collazo, AM; Litten, C; Husman, B; Persson, K; Ljunggren, J; Grover, G; Sleph, PG; George, R; Malm, J Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1. J Med Chem 46: 1580-8 (2003)
Baker, JG The selectivity of beta-adrenoceptor antagonists at the human beta1, beta2 and beta3 adrenoceptors. Br J Pharmacol 144: 317-22 (2005)
Wang, H; Chen, M; Sang, X; You, X; Wang, Y; Paterson, IC; Hong, W; Yang, X Development of small molecule inhibitors targeting TGF-β ligand and receptor: Structures, mechanism, preclinical studies and clinical usage. Eur J Med Chem 191: (2020)
Goldberg, FW; Ward, RA; Powell, SJ; Debreczeni, JE; Norman, RA; Roberts, NJ; Dishington, AP; Gingell, HJ; Wickson, KF; Roberts, AL Rapid generation of a high quality lead for transforming growth factor-beta (TGF-beta) type I receptor (ALK5). J Med Chem 52: 7901-5 (2009)
Schade, D; Lanier, M; Willems, E; Okolotowicz, K; Bushway, P; Wahlquist, C; Gilley, C; Mercola, M; Cashman, JR Synthesis and SAR of b-annulated 1,4-dihydropyridines define cardiomyogenic compounds as novel inhibitors of TGFß signaling. J Med Chem 55: 9946-57 (2012)
Roth, GJ; Heckel, A; Brandl, T; Grauert, M; Hoerer, S; Kley, JT; Schnapp, G; Baum, P; Mennerich, D; Schnapp, A; Park, JE Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factorß receptor I (TGFßRI). J Med Chem 53: 7287-95 (2010)
Gellibert, F; Woolven, J; Fouchet, MH; Mathews, N; Goodland, H; Lovegrove, V; Laroze, A; Nguyen, VL; Sautet, S; Wang, R; Janson, C; Smith, W; Krysa, G; Boullay, V; De Gouville, AC; Huet, S; Hartley, D Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem 47: 4494-506 (2004)
Zhou, B; Wang, Y; Zhang, C; Yang, G; Zhang, F; Yu, B; Chai, C; Cao, Z Ribemansides A and B, TRPC6 Inhibitors from Ribes manshuricum That Suppress TGF-β1-Induced Fibrogenesis in HK-2 Cells. J Nat Prod 81: 913-917 (2018)
Robinson, N; Gibson, TM; Chicarelli-Robinson, MI; Cameron, L; Hylands, PJ; Wilkinson, D; Simpson, TJ Cochliobolic acid, a novel metabolite produced by Cochliobolus lunatus, inhibits binding of TGF-alpha to the EGF receptor in a SPA assay. J Nat Prod 60: 6-8 (1997)
Rezmann-Vitti, LA; Nero, TL; Jackman, GP; Machida, CA; Duke, BJ; Louis, WJ; Louis, SN Role of Tyr(356(7.43)) and Ser(190(4.57)) in antagonist binding in the rat beta1-adrenergic receptor. J Med Chem 49: 3467-77 (2006)
Ciayadi, R; Potdar, M; Walton, KL; Harrison, CA; Kelso, GF; Harris, SJ; Hearn, MT 2-Phenyl and 2-heterocyclic-4-(3-(pyridin-2-yl)-1H-pyrazol-4-yl)pyridines as inhibitors of TGF-ß1 and activin A signalling. Bioorg Med Chem Lett 21: 5642-5 (2011)
Yu, WC; Yeh, TY; Ye, CH; Chong, PCT; Ho, YH; So, DK; Yap, KY; Peng, GR; Shao, CH; Jagtap, AD; Chern, JW; Lin, CS; Lin, SP; Lin, SL; Yu, SH; Yu, CW Discovery of HDAC6, HDAC8, and 6/8 Inhibitors and Development of Cell-Based Drug Screening Models for the Treatment of TGF-β-Induced Idiopathic Pulmonary Fibrosis. J Med Chem 66: 10528-10557 (2023)
van Beeren, HC; Bakker, O; Wiersinga, WM Structure-function relationship of the inhibition of the 3,5,3'-triiodothyronine binding to the alpha1- and beta1-thyroid hormone receptor by amiodarone analogs. Endocrinology 137: 2807-14 (1996)
Sidduri, A; Tilley, JW; Lou, J; Tare, N; Cavallo, G; Frank, K; Pamidimukkala, A; Choi, DS; Gerber, L; Railkar, A; Renzetti, L Identification of N-acyl 4-(5-pyrimidine-2,4-dionyl)phenylalanine derivatives and their orally active prodrug esters as dual-acting alpha4-beta1 and alpha4-beta7 receptor antagonists. Bioorg Med Chem Lett 23: 1026-31 (2013)
Tan, B; Zhang, X; Quan, X; Zheng, G; Li, X; Zhao, L; Li, W; Li, B Design, synthesis and biological activity evaluation of novel 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazol-4-yl) oxy) pyridine-2-yl) amino derivatives as potent transforming growth factor-β (TGF-β) type I receptor inhibitors. Bioorg Med Chem Lett 30: (2020)
Jin, CH; Krishnaiah, M; Sreenu, D; Subrahmanyam, VB; Rao, KS; Lee, HJ; Park, SJ; Park, HJ; Lee, K; Sheen, YY; Kim, DK Discovery of N-((4-([1,2,4]triazolo[1,5-a]pyridin-6-yl)-5-(6-methylpyridin-2-yl)-1H-imidazol-2-yl)methyl)-2-fluoroaniline (EW-7197): a highly potent, selective, and orally bioavailable inhibitor of TGF-ß type I receptor kinase as cancer immunotherapeutic/antifibrotic agent. J Med Chem 57: 4213-38 (2014)