| Year |
Citation |
Score |
| 2016 |
Lee W, Crawford JJ, Aliagas I, Murray LJ, Tay S, Wang W, Heise CE, Hoeflich KP, La H, Mathieu S, Mintzer R, Ramaswamy S, Rouge L, Rudolph J. Synthesis and evaluation of a series of 4-azaindole-containing p21-activated kinase-1 inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 27346791 DOI: 10.1016/J.Bmcl.2016.06.031 |
0.37 |
|
| 2016 |
Rudolph J, Murray LJ, Ndubaku CO, O'Brien T, Blackwood EM, Wang W, Aliagas I, Gazzard L, Crawford JJ, Drobnick J, Lee W, Zhao X, Hoeflich KP, Favor DA, Dong P, ... ... Heise CE, et al. Chemically diverse Group I p21-activated kinase (PAK) inhibitors impart acute cardiovascular toxicity with a narrow therapeutic window. Journal of Medicinal Chemistry. PMID 27167326 DOI: 10.1021/Acs.Jmedchem.6B00638 |
0.365 |
|
| 2015 |
Ndubaku CO, Crawford JJ, Drobnick J, Aliagas I, Campbell D, Dong P, Dornan LM, Duron S, Epler J, Gazzard L, Heise CE, Hoeflich KP, Jakubiak D, La H, Lee W, et al. Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety. Acs Medicinal Chemistry Letters. 6: 1241-6. PMID 26713112 DOI: 10.1021/Acsmedchemlett.5B00398 |
0.36 |
|
| 2015 |
Burdick DJ, Wang S, Heise C, Pan B, Drummond J, Yin J, Goeser L, Magnuson S, Blaney J, Moffat J, Wang W, Chen H. Fragment-based discovery of potent ERK2 pyrrolopyrazine inhibitors. Bioorganic & Medicinal Chemistry Letters. PMID 26338362 DOI: 10.1016/J.Bmcl.2015.08.048 |
0.313 |
|
| 2015 |
Rudolph J, Aliagas I, Crawford JJ, Mathieu S, Lee W, Chao Q, Dong P, Rouge L, Wang W, Heise C, Murray LJ, La H, Liu Y, Manning G, Diederich F, et al. Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series. Acs Medicinal Chemistry Letters. 6: 711-5. PMID 26101579 DOI: 10.1021/Acsmedchemlett.5B00151 |
0.315 |
|
| 2015 |
Crawford JJ, Lee W, Aliagas I, Mathieu S, Hoeflich KP, Zhou W, Wang W, Rouge L, Murray L, La H, Liu N, Fan PW, Cheong J, Heise CE, Ramaswamy S, et al. Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors. Journal of Medicinal Chemistry. 58: 5121-36. PMID 26030457 DOI: 10.1021/Acs.Jmedchem.5B00572 |
0.343 |
|
| 2014 |
Staben ST, Feng JA, Lyle K, Belvin M, Boggs J, Burch JD, Chua CC, Cui H, DiPasquale AG, Friedman LS, Heise C, Koeppen H, Kotey A, Mintzer R, Oh A, et al. Back pocket flexibility provides group II p21-activated kinase (PAK) selectivity for type I 1/2 kinase inhibitors. Journal of Medicinal Chemistry. 57: 1033-45. PMID 24432870 DOI: 10.1021/Jm401768T |
0.349 |
|
| 2013 |
Lauffer BE, Mintzer R, Fong R, Mukund S, Tam C, Zilberleyb I, Flicke B, Ritscher A, Fedorowicz G, Vallero R, Ortwine DF, Gunzner J, Modrusan Z, Neumann L, Koth CM, ... ... Heise CE, et al. Histone deacetylase (HDAC) inhibitor kinetic rate constants correlate with cellular histone acetylation but not transcription and cell viability. The Journal of Biological Chemistry. 288: 26926-43. PMID 23897821 DOI: 10.1074/Jbc.M113.490706 |
0.312 |
|
| 2012 |
Heise CE, Murray J, Augustyn KE, Bravo B, Chugha P, Cohen F, Giannetti AM, Gibbons P, Hannoush RN, Hearn BR, Jaishankar P, Ly CQ, Shah K, Stanger K, Steffek M, et al. Mechanistic and structural understanding of uncompetitive inhibitors of caspase-6. Plos One. 7: e50864. PMID 23227217 DOI: 10.1371/Journal.Pone.0050864 |
0.329 |
|
| 2010 |
Ramaswamy S, Yen I, Sideris S, Malek S, Heise CE. A plate-based assay to measure cellular ERK substrate phosphorylation: utility for drug discovery of the MAPK-signaling cascade. Assay and Drug Development Technologies. 8: 497-503. PMID 20482377 DOI: 10.1089/Adt.2009.0259 |
0.319 |
|
| 2009 |
Yen I, Song K, Stokoe D, Brandhuber B, Gloor S, Aliagas I, Anderson D, Morales T, Vigers G, Ludlam M, Alvarado R, Liu B, Sideris S, Ramaswamy S, Heise C, et al. Abstract B90: Understanding the effects of RAF inhibitors on RAF signaling in B‐RAF V600E mutant versus wild type tumors Molecular Cancer Therapeutics. 8. DOI: 10.1158/1535-7163.Targ-09-B90 |
0.336 |
|
| 2007 |
Mesleh MF, Shirley WA, Heise CE, Ling N, Maki RA, Laura RP. NMR structural characterization of a minimal peptide antagonist bound to the extracellular domain of the corticotropin-releasing factor1 receptor. The Journal of Biological Chemistry. 282: 6338-46. PMID 17192263 DOI: 10.1074/Jbc.M609816200 |
0.381 |
|
| 2006 |
Schwarz DA, Allen MM, Petroski RE, Pomeroy JE, Heise CE, Mistry MS, Selkirk JV, Nottebaum LM, Grey J, Zhang M, Goodfellow VS, Maki RA. Manipulation of small-molecule inhibitory kinetics modulates MCH-R1 function. Molecular and Cellular Endocrinology. 259: 1-9. PMID 16987592 DOI: 10.1016/J.Mce.2006.07.003 |
0.397 |
|
| 2006 |
Dyck B, Zhao L, Tamiya J, Pontillo J, Hudson S, Ching B, Heise CE, Wen J, Norton C, Madan A, Schwarz D, Wade W, Goodfellow VS. Substituted chromones and quinolones as potent melanin-concentrating hormone receptor 1 antagonists. Bioorganic & Medicinal Chemistry Letters. 16: 4237-42. PMID 16762549 DOI: 10.1016/J.Bmcl.2006.05.075 |
0.305 |
|
| 2005 |
Rowbottom MW, Vickers TD, Dyck B, Tamiya J, Zhang M, Zhao L, Grey J, Provencal D, Schwarz D, Heise CE, Mistry M, Fisher A, Dong T, Hu T, Saunders J, et al. Synthesis and structure-activity relationships of biarylcarboxamide bis-aminopyrrolidine urea derived small-molecule antagonists of the melanin-concentrating hormone receptor-1 (MCH-R1). Bioorganic & Medicinal Chemistry Letters. 15: 3439-45. PMID 15950467 DOI: 10.1016/J.Bmcl.2005.05.015 |
0.349 |
|
| 2005 |
Heise CE, Pahuja A, Hudson SC, Mistry MS, Putnam AL, Gross MM, Gottlieb PA, Wade WS, Kiankarimi M, Schwarz D, Crowe P, Zlotnik A, Alleva DG. Pharmacological characterization of CXC chemokine receptor 3 ligands and a small molecule antagonist. The Journal of Pharmacology and Experimental Therapeutics. 313: 1263-71. PMID 15761110 DOI: 10.1124/Jpet.105.083683 |
0.358 |
|
| 2005 |
Grey J, Dyck B, Rowbottom MW, Tamiya J, Vickers TD, Zhang M, Zhao L, Heise CE, Schwarz D, Saunders J, Goodfellow VS. Bis(aminopyrrolidine)-derived ureas (APUs) as potent MCH1 receptor antagonists. Bioorganic & Medicinal Chemistry Letters. 15: 999-1004. PMID 15686900 DOI: 10.1016/J.Bmcl.2004.12.036 |
0.302 |
|
| 2002 |
Brinkmann V, Davis MD, Heise CE, Albert R, Cottens S, Hof R, Bruns C, Prieschl E, Baumruker T, Hiestand P, Foster CA, Zollinger M, Lynch KR. The immune modulator FTY720 targets sphingosine 1-phosphate receptors. The Journal of Biological Chemistry. 277: 21453-7. PMID 11967257 DOI: 10.1074/Jbc.C200176200 |
0.519 |
|
| 2001 |
Heise CE, Santos WL, Schreihofer AM, Heasley BH, Mukhin YV, Macdonald TL, Lynch KR. Activity of 2-substituted lysophosphatidic acid (LPA) analogs at LPA receptors: discovery of a LPA1/LPA3 receptor antagonist. Molecular Pharmacology. 60: 1173-80. PMID 11723223 DOI: 10.1124/Mol.60.6.1173 |
0.599 |
|
| 2001 |
Im DS, Heise CE, Nguyen T, O'Dowd BF, Lynch KR. Identification of a molecular target of psychosine and its role in globoid cell formation. The Journal of Cell Biology. 153: 429-34. PMID 11309421 DOI: 10.1083/Jcb.153.2.429 |
0.544 |
|
| 2001 |
Hooks SB, Santos WL, Im DS, Heise CE, Macdonald TL, Lynch KR. Lysophosphatidic acid-induced mitogenesis is regulated by lipid phosphate phosphatases and is Edg-receptor independent. The Journal of Biological Chemistry. 276: 4611-21. PMID 11042183 DOI: 10.1074/Jbc.M007782200 |
0.634 |
|
| 2000 |
Heise CE, O'Dowd BF, Figueroa DJ, Sawyer N, Nguyen T, Im DS, Stocco R, Bellefeuille JN, Abramovitz M, Cheng R, Williams DL, Zeng Z, Liu Q, Ma L, Clements MK, et al. Characterization of the human cysteinyl leukotriene 2 receptor. The Journal of Biological Chemistry. 275: 30531-6. PMID 10851239 DOI: 10.1074/Jbc.M003490200 |
0.608 |
|
| 2000 |
Im DS, Heise CE, Ancellin N, O'Dowd BF, Shei GJ, Heavens RP, Rigby MR, Hla T, Mandala S, McAllister G, George SR, Lynch KR. Characterization of a novel sphingosine 1-phosphate receptor, Edg-8. The Journal of Biological Chemistry. 275: 14281-6. PMID 10799507 DOI: 10.1074/Jbc.275.19.14281 |
0.561 |
|
| 2000 |
Im DS, Heise CE, Harding MA, George SR, O'Dowd BF, Theodorescu D, Lynch KR. Molecular cloning and characterization of a lysophosphatidic acid receptor, Edg-7, expressed in prostate. Molecular Pharmacology. 57: 753-9. PMID 10727522 DOI: 10.1124/Mol.57.4.753 |
0.597 |
|
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