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Items: 21


Targeting IRAK4 for Degradation with PROTACs.

Nunes J, McGonagle GA, Eden J, Kiritharan G, Touzet M, Lewell X, Emery J, Eidam H, Harling JD, Anderson NA.

ACS Med Chem Lett. 2019 Jun 14;10(7):1081-1085. doi: 10.1021/acsmedchemlett.9b00219. eCollection 2019 Jul 11.


PROTAC-Mediated Degradation of Bruton's Tyrosine Kinase Is Inhibited by Covalent Binding.

Tinworth CP, Lithgow H, Dittus L, Bassi ZI, Hughes SE, Muelbaier M, Dai H, Smith IED, Kerr WJ, Burley GA, Bantscheff M, Harling JD.

ACS Chem Biol. 2019 Mar 15;14(3):342-347. doi: 10.1021/acschembio.8b01094. Epub 2019 Feb 27.


Catalytic in vivo protein knockdown by small-molecule PROTACs.

Bondeson DP, Mares A, Smith IE, Ko E, Campos S, Miah AH, Mulholland KE, Routly N, Buckley DL, Gustafson JL, Zinn N, Grandi P, Shimamura S, Bergamini G, Faelth-Savitski M, Bantscheff M, Cox C, Gordon DA, Willard RR, Flanagan JJ, Casillas LN, Votta BJ, den Besten W, Famm K, Kruidenier L, Carter PS, Harling JD, Churcher I, Crews CM.

Nat Chem Biol. 2015 Aug;11(8):611-7. doi: 10.1038/nchembio.1858. Epub 2015 Jun 10.


HaloPROTACS: Use of Small Molecule PROTACs to Induce Degradation of HaloTag Fusion Proteins.

Buckley DL, Raina K, Darricarrere N, Hines J, Gustafson JL, Smith IE, Miah AH, Harling JD, Crews CM.

ACS Chem Biol. 2015 Aug 21;10(8):1831-7. doi: 10.1021/acschembio.5b00442. Epub 2015 Jun 23.


Identification of a Novel and Selective Series of Itk Inhibitors via a Template-Hopping Strategy.

Alder CM, Ambler M, Campbell AJ, Champigny AC, Deakin AM, Harling JD, Harris CA, Longstaff T, Lynn S, Maxwell AC, Mooney CJ, Scullion C, Singh OM, Smith IE, Somers DO, Tame CJ, Wayne G, Wilson C, Woolven JM.

ACS Med Chem Lett. 2013 Aug 12;4(10):948-52. doi: 10.1021/ml400206q. eCollection 2013 Oct 10.


Discovery of novel irreversible inhibitors of interleukin (IL)-2-inducible tyrosine kinase (Itk) by targeting cysteine 442 in the ATP pocket.

Harling JD, Deakin AM, Campos S, Grimley R, Chaudry L, Nye C, Polyakova O, Bessant CM, Barton N, Somers D, Barrett J, Graves RH, Hanns L, Kerr WJ, Solari R.

J Biol Chem. 2013 Sep 27;288(39):28195-206. doi: 10.1074/jbc.M113.474114. Epub 2013 Aug 9.


The discovery of potent and long-acting oral factor Xa inhibitors with tetrahydroisoquinoline and benzazepine P4 motifs.

Watson NS, Adams C, Belton D, Brown D, Burns-Kurtis CL, Chaudry L, Chan C, Convery MA, Davies DE, Exall AM, Harling JD, Irvine S, Irving WR, Kleanthous S, McLay IM, Pateman AJ, Patikis AN, Roethke TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Young RJ.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1588-92. doi: 10.1016/j.bmcl.2011.01.129. Epub 2011 Feb 2.


Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with aminoindane and phenylpyrrolidine P4 motifs.

Young RJ, Adams C, Blows M, Brown D, Burns-Kurtis CL, Chan C, Chaudry L, Convery MA, Davies DE, Exall AM, Foster G, Harling JD, Hortense E, Irvine S, Irving WR, Jackson S, Kleanthous S, Pateman AJ, Patikis AN, Roethka TJ, Senger S, Stelman GJ, Toomey JR, West RI, Whittaker C, Zhou P, Watson NS.

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1582-7. doi: 10.1016/j.bmcl.2011.01.131. Epub 2011 Feb 1.


A new, highly selective murine peroxisome proliferator-activated receptor δ agonist increases responsiveness to thermogenic stimuli and glucose uptake in skeletal muscle in obese mice.

Ngala RA, Stocker CJ, Roy AG, Hislop D, Wargent E, Bell R, Hassall DG, Harling JD, Billin AN, Willson TM, Arch JR, Cawthorne MA.

Diabetes Obes Metab. 2011 May;13(5):455-64. doi: 10.1111/j.1463-1326.2011.01371.x. Epub 2011 Jan 27.


Structure and property based design of factor Xa inhibitors: pyrrolidin-2-ones with monoaryl P4 motifs.

Kleanthous S, Borthwick AD, Brown D, Burns-Kurtis CL, Campbell M, Chaudry L, Chan C, Clarte MO, Convery MA, Harling JD, Hortense E, Irving WR, Irvine S, Pateman AJ, Patikis AN, Pinto IL, Pollard DR, Roethka TJ, Senger S, Shah GP, Stelman GJ, Toomey JR, Watson NS, West RI, Whittaker C, Zhou P, Young RJ.

Bioorg Med Chem Lett. 2010 Jan 15;20(2):618-22. doi: 10.1016/j.bmcl.2009.11.077. Epub 2009 Nov 20.


Phosphinates as new electrophilic partners for cross-coupling reactions.

Guo J, Harling JD, Steel PG, Woods TM.

Org Biomol Chem. 2008 Nov 7;6(21):4053-8. doi: 10.1039/b809577a. Epub 2008 Sep 15.


One-pot synthesis of benzothiazolines and napthathiazolines via cascade ortho-lithiation, cyclisation and elimination of N-arylsulfonyl lactams.

Harling JD, Steel PG, Woods TM, Yufit DS.

Org Biomol Chem. 2007 Nov 7;5(21):3472-6. Epub 2007 Sep 17.


(1H-imidazo[4,5-c]pyridin-2-yl)-1,2,5-oxadiazol-3-ylamine derivatives: a novel class of potent MSK-1-inhibitors.

Bamford MJ, Alberti MJ, Bailey N, Davies S, Dean DK, Gaiba A, Garland S, Harling JD, Jung DK, Panchal TA, Parr CA, Steadman JG, Takle AK, Townsend JT, Wilson DM, Witherington J.

Bioorg Med Chem Lett. 2005 Jul 15;15(14):3402-6. Erratum in: Bioorg Med Chem Lett. 2015 Mar 1;25(5):1151.


Utility of the ammonia-free Birch reduction of electron-deficient pyrroles: total synthesis of the 20s proteasome inhibitor, clasto-lactacystin beta-lactone.

Donohoe TJ, Sintim HO, Sisangia L, Ace KW, Guyo PM, Cowley A, Harling JD.

Chemistry. 2005 Jul 4;11(14):4227-38.


An efficient synthesis of lactacystin beta-lactone.

Donohoe TJ, Sintim HO, Sisangia L, Harling JD.

Angew Chem Int Ed Engl. 2004 Apr 19;43(17):2293-6. No abstract available.


The design of 8,8-dimethyl[1,6]naphthyridines as potential anticonvulsant agents.

Austin NE, Hadley MS, Harling JD, Harrington FP, Macdonald GJ, Mitchell DJ, Riley GJ, Stean TO, Stemp G, Stratton SC, Thompson M, Upton N.

Bioorg Med Chem Lett. 2003 May 19;13(10):1627-9.


SB-431542 is a potent and specific inhibitor of transforming growth factor-beta superfamily type I activin receptor-like kinase (ALK) receptors ALK4, ALK5, and ALK7.

Inman GJ, Nicolás FJ, Callahan JF, Harling JD, Gaster LM, Reith AD, Laping NJ, Hill CS.

Mol Pharmacol. 2002 Jul;62(1):65-74.


Identification of novel inhibitors of the transforming growth factor beta1 (TGF-beta1) type 1 receptor (ALK5).

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.

J Med Chem. 2002 Feb 28;45(5):999-1001.


Evaluation of a series of anticonvulsant 1,2,3,4-tetrahydroisoquinolinyl-benzamides.

Chan WN, Hadley MS, Harling JD, Herdon HJ, Orlek BS, Riley GJ, Stead RE, Stean TO, Thompson M, Upton N, Ward RW.

Bioorg Med Chem. 2000 Aug;8(8):2085-94.


Characterisation of SB-221420-A - a neuronal Ca(2+) and Na(+) channel antagonist in experimental models of stroke.

Campbell CA, Barone FC, Benham CD, Hadingham SJ, Harries MH, Harling JD, Hills JM, Lewis VA, Mackay KB, Orlek BS, White RF, Parsons AA, Hunter AJ.

Eur J Pharmacol. 2000 Aug 11;401(3):419-28.


Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl-benzamides with potential anticonvulsant activity.

Chan WN, Hadley MS, Harling JD, Herdon HJ, Jerman JC, Orlek BS, Stean TO, Thompson M, Upton N, Ward RW.

Bioorg Med Chem Lett. 1998 Oct 20;8(20):2903-6.


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