| Year |
Citation |
Score |
| 2022 |
Caldwell TM, Kaufman MD, Wise SC, Mi Ahn Y, Hood MM, Lu WP, Patt WC, Samarakoon T, Vogeti L, Vogeti S, Yates KM, Bulfer SL, Le Bourdonnec B, Smith BD, Flynn DL. Discovery of Acyl Ureas as Highly Selective Small Molecule CSF1R Kinase Inhibitors. Bioorganic & Medicinal Chemistry Letters. 128929. PMID 35961461 DOI: 10.1016/j.bmcl.2022.128929 |
0.328 |
|
| 2019 |
Smith BD, Kaufman MD, Lu WP, Gupta A, Leary CB, Wise SC, Rutkoski TJ, Ahn YM, Al-Ani G, Bulfer SL, Caldwell TM, Chun L, Ensinger CL, Hood MM, McKinley A, et al. Ripretinib (DCC-2618) Is a Switch Control Kinase Inhibitor of a Broad Spectrum of Oncogenic and Drug-Resistant KIT and PDGFRA Variants. Cancer Cell. 35: 738-751.e9. PMID 31085175 DOI: 10.1016/J.Ccell.2019.04.006 |
0.322 |
|
| 2019 |
Smith BD, Vogeti L, Gupta A, Singh J, Al-Ani G, Bulfer SL, Caldwell TM, Timson MJ, Vogeti S, Ahn YM, Al-Hashimi H, Crawley CK, Heiniger CL, Leary CB, Proto JT, et al. Abstract B129: Preclinical studies with DCC-3116, an ULK kinase inhibitor designed to inhibit autophagy as a potential strategy to address mutant RAS cancers Molecular Cancer Therapeutics. 18. DOI: 10.1158/1535-7163.Targ-19-B129 |
0.334 |
|
| 2015 |
Henry JR, Kaufman MD, Peng SB, Ahn YM, Caldwell TM, Vogeti L, Telikepalli H, Lu WP, Hood MM, Rutkoski TJ, Smith BD, Vogeti S, Miller D, Wise SC, Chun L, et al. Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. Journal of Medicinal Chemistry. 58: 4165-79. PMID 25965804 DOI: 10.1021/Acs.Jmedchem.5B00067 |
0.324 |
|
| 2010 |
Hodgetts KJ, Blum CA, Caldwell T, Bakthavatchalam R, Zheng X, Capitosti S, Krause JE, Cortright D, Crandall M, Murphy BA, Boyce S, Brian Jones A, Chenard BL. Pyrido[2,3-b]pyrazines, discovery of TRPV1 antagonists with reduced potential for the formation of reactive metabolites. Bioorganic & Medicinal Chemistry Letters. 20: 4359-63. PMID 20615696 DOI: 10.1016/J.Bmcl.2010.06.069 |
0.353 |
|
| 2010 |
Blum CA, Caldwell T, Zheng X, Bakthavatchalam R, Capitosti S, Brielmann H, De Lombaert S, Kershaw MT, Matson D, Krause JE, Cortright D, Crandall M, Martin WJ, Murphy BA, Boyce S, et al. Discovery of novel 6,6-heterocycles as transient receptor potential vanilloid (TRPV1) antagonists. Journal of Medicinal Chemistry. 53: 3330-48. PMID 20307063 DOI: 10.1021/Jm100051G |
0.329 |
|
| 2002 |
Hsin LW, Tian X, Webster EL, Coop A, Caldwell TM, Jacobson AE, Chrousos GP, Gold PW, Habib KE, Ayala A, Eckelman WC, Contoreggi C, Rice KC. CRHR1 Receptor binding and lipophilicity of pyrrolopyrimidines, potential nonpeptide corticotropin-releasing hormone type 1 receptor antagonists. Bioorganic & Medicinal Chemistry. 10: 175-83. PMID 11738619 DOI: 10.1016/S0968-0896(01)00261-9 |
0.334 |
|
| 2001 |
Grunewald GL, Caldwell TM, Li Q, Criscione KR. Synthesis and evaluation of 4-fluoro-8-substituted-2,3,4,5-tetrahydro-1H-2-benzazapines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. Journal of Medicinal Chemistry. 44: 2849-56. PMID 11495596 DOI: 10.1021/Jm010147G |
0.784 |
|
| 1999 |
Grunewald GL, Caldwell TM, Li Q, Dahanukar VH, McNeil B, Criscione KR. Enantiospecific synthesis of 3-fluoromethyl-, 3-hydroxymethyl-, and 3-chloromethyl-1,2,3,4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. Journal of Medicinal Chemistry. 42: 4351-61. PMID 10543879 DOI: 10.1021/Jm990086A |
0.745 |
|
| 1999 |
Grunewald GL, Caldwell TM, Li Q, Slavica M, Criscione KR, Borchardt RT, Wang W. Synthesis and biochemical evaluation of 3-fluoromethyl-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. Journal of Medicinal Chemistry. 42: 3588-601. PMID 10479290 DOI: 10.1021/Jm990045E |
0.789 |
|
| 1999 |
Grunewald GL, Caldwell TM, Li Q, Criscione KR. Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. Journal of Medicinal Chemistry. 42: 3315-23. PMID 10464018 DOI: 10.1021/Jm980734A |
0.789 |
|
| 1999 |
Grunewald GL, Caldwell TM, Li Q, Criscione KR. 1,3-Dimethyl-7-substituted-1,2,3,4-tetrahydroisoquinolines as probes for the binding orientation of tetrahydroisoquinoline at the active site of phenylethanolamine N-methyltransferase. Bioorganic & Medicinal Chemistry. 7: 869-80. PMID 10400340 DOI: 10.1016/S0968-0896(99)00031-0 |
0.741 |
|
| 1999 |
Grunewald GL, Caldwell TM, Dahanukar VH, Jalluri RK, Criscione KR. Comparative molecular field analysis (CoMFA) models of phenylethanolamine N-methyltransferase (PNMT) and the alpha2-adrenoceptor: the development of new, highly selective inhibitors of PNMT. Bioorganic & Medicinal Chemistry Letters. 9: 481-6. PMID 10091706 DOI: 10.1016/S0960-894X(99)00022-0 |
0.611 |
|
| 1997 |
Grunewald GL, Dahanukar VH, Caldwell TM, Criscione KR. Examination of the role of the acidic hydrogen in imparting selectivity of 7-(aminosulfonyl)-1,2,3,4-tetrahydroisoquinoline (SK&F 29661) toward inhibition of phenylethanolamine N-methyltransferase vs the alpha 2-adrenoceptor. Journal of Medicinal Chemistry. 40: 3997-4005. PMID 9406590 DOI: 10.1021/Jm960235E |
0.744 |
|
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