Discovery and Characterization of 6-{4-[3-(R)-2-Methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, Irdabisant): A Potent, Selective Histamine H3 Receptor Inverse Agonist
Hudkins, Robert L, Raddatz, Rita, Tao, Ming, Mathiasen, Joanne R, Aimone, Lisa D, Becknell, Nadine C, Prouty, Catherine P, Knutsen, Lars J. S, Yazdanian, Mehran, Moachon, Gilbert, Ator, Mark A, Mallamo, John P, Marino, Michael J, Bacon, Edward R, Williams, Michael
Published in Journal of medicinal chemistry (14.07.2011)
Published in Journal of medicinal chemistry (14.07.2011)
Get full text
Journal Article
Anaplastic lymphoma kinase activity is essential for the proliferation and survival of anaplastic large-cell lymphoma cells
Wan, Weihua, Albom, Mark S., Lu, Lihui, Quail, Matthew R., Becknell, Nadine C., Weinberg, Linda R., Reddy, Dandu R., Holskin, Beverly P., Angeles, Thelma S., Underiner, Ted L., Meyer, Sheryl L., Hudkins, Robert L., Dorsey, Bruce D., Ator, Mark A., Ruggeri, Bruce A., Cheng, Mangeng
Published in Blood (15.02.2006)
Published in Blood (15.02.2006)
Get full text
Journal Article
Covalent Docking Identifies a Potent and Selective MKK7 Inhibitor
Shraga, Amit, Olshvang, Evgenia, Davidzohn, Natalia, Khoshkenar, Payam, Germain, Nicolas, Shurrush, Khriesto, Carvalho, Silvia, Avram, Liat, Albeck, Shira, Unger, Tamar, Lefker, Bruce, Subramanyam, Chakrapani, Hudkins, Robert L, Mitchell, Amir, Shulman, Ziv, Kinoshita, Takayoshi, London, Nir
Published in Cell chemical biology (17.01.2019)
Published in Cell chemical biology (17.01.2019)
Get full text
Journal Article
Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia
Hudkins, Robert L., Allen, Eric, Balcer, Alexandra, Hoffman, Isaac D., Iyer, Samhita, Neal, Melissa, Nelson, Kirk J., Rideout, Marc, Ye, Qing, Starrett, Jacqueline H., Patel, Piyush, Harris, Todd, Swanson, Ronald V., Bensen, Daniel C.
Published in Journal of medicinal chemistry (11.09.2024)
Published in Journal of medicinal chemistry (11.09.2024)
Get full text
Journal Article
Technically Extended MultiParameter Optimization (TEMPO): An Advanced Robust Scoring Scheme To Calculate Central Nervous System Druggability and Monitor Lead Optimization
Ghose, Arup K, Ott, Gregory R, Hudkins, Robert L
Published in ACS chemical neuroscience (18.01.2017)
Published in ACS chemical neuroscience (18.01.2017)
Get full text
Journal Article
Neurotrophic 3,9-Bis[(alkylthio)methyl]- and -Bis(alkoxymethyl)-K-252a Derivatives
Kaneko, Masami, Saito, Yutaka, Saito, Hiromitsu, Matsumoto, Tadashi, Matsuda, Yuzuru, Vaught, Jeffry L, Dionne, Craig A, Angeles, Thelma S, Glicksman, Marcie A, Neff, Nicola T, Rotella, David P, Kauer, James C, Mallamo, John P, Hudkins, Robert L, Murakata, Chikara
Published in Journal of medicinal chemistry (06.06.1997)
Published in Journal of medicinal chemistry (06.06.1997)
Get full text
Journal Article
Synthesis and Biological Profile of the pan-Vascular Endothelial Growth Factor Receptor/Tyrosine Kinase with Immunoglobulin and Epidermal Growth Factor-Like Homology Domains 2 (VEGF-R/TIE-2) Inhibitor 11-(2-Methylpropyl)-12,13-dihydro-2-methyl-8-(pyrimidin-2-ylamino)-4H-indazolo[5,4-a]pyrrolo[3,4-c]carbazol-4-one (CEP-11981): A Novel Oncology Therapeutic Agent
Hudkins, Robert L, Becknell, Nadine C, Zulli, Allison L, Underiner, Ted L, Angeles, Thelma S, Aimone, Lisa D, Albom, Mark S, Chang, Hong, Miknyoczki, Sheila J, Hunter, Kathryn, Jones-Bolin, Susan, Zhao, Hugh, Bacon, Edward R, Mallamo, John P, Ator, Mark A, Ruggeri, Bruce A
Published in Journal of medicinal chemistry (26.01.2012)
Published in Journal of medicinal chemistry (26.01.2012)
Get full text
Journal Article
3-(1′-Cyclobutylspiro[4H-1,3-benzodioxine-2,4′-piperidine]-6-yl)-5,5-dimethyl-1,4-dihydropyridazin-6-one (CEP-32215), a new wake-promoting histamine H3 antagonist/inverse agonist
Hudkins, Robert L., Gruner, John A., Raddatz, Rita, Mathiasen, Joanne R., Aimone, Lisa D., Marino, Michael J., Bacon, Edward R., Williams, Michael, Ator, Mark A.
Published in Neuropharmacology (01.07.2016)
Published in Neuropharmacology (01.07.2016)
Get full text
Journal Article
3,4-Diaza-bicyclo[4.1.0]hept-4-en-2-one phenoxypropylamine analogs of irdabisant (CEP-26401) as potent histamine-3 receptor inverse agonists with robust wake-promoting activity
Hudkins, Robert L., Becknell, Nadine C., Lyons, Jacquelyn A., Aimone, Lisa D., Olsen, Mark, Haltiwanger, R. Curtis, Mathiasen, Joanne R., Raddatz, Rita, Gruner, John A.
Published in European journal of medicinal chemistry (05.05.2015)
Published in European journal of medicinal chemistry (05.05.2015)
Get full text
Journal Article
Discovery of (1R, 6S)-5-[4-(1-cyclobutyl-piperidin-4-yloxy)-phenyl]3,4-diaza-bicyclo[4.1.0] hept-4-en-2-one (R, S-4a): Histamine H3 receptor inverse agonist demonstrating potent cognitive enhancing and wake promoting activity
Hudkins, Robert L., Josef, Kurt A., Becknell, Nadine C., Aimone, Lisa D., Lyons, Jacquelyn A., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita
Published in Bioorganic & medicinal chemistry letters (01.03.2014)
Published in Bioorganic & medicinal chemistry letters (01.03.2014)
Get full text
Journal Article
Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists
Josef, Kurt A., Aimone, Lisa D., Lyons, Jacquelyn, Raddatz, Rita, Hudkins, Robert L.
Published in Bioorganic & medicinal chemistry letters (15.06.2012)
Published in Bioorganic & medicinal chemistry letters (15.06.2012)
Get full text
Journal Article
Substituted phenoxypropyl-(R)-2-methylpyrrolidine aminomethyl ketones as histamine-3 receptor inverse agonists
Zulli, Allison L., Aimone, Lisa D., Mathiasen, Joanne R., Gruner, John A., Raddatz, Rita, Bacon, Edward R., Hudkins, Robert L.
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Published in Bioorganic & medicinal chemistry letters (15.04.2012)
Get full text
Journal Article