Concepedia

Structure-activity relationships for a series of (Bis(4-fluorophenyl)methyl)sulfinylethyl-aminopiperidines and -piperidine amines at the dopamine transporter: Bioisosteric replacement of the piperazine improves metabolic stability

JoLynn B. Giancola, Alessandro Bonifazi, Jianjing Cao, Therese Ku, Alexandra J. Haraczy, Jenny Lam, Rana Rais, Mark A. Coggiano, Gianluigi Tanda

European Journal of Medicinal Chemistry · 2020 · 15 citations · 37 references

Open access

References

37

Relationship between the inhibition constant (KI) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction

Yung-Chi Cheng, William H. Prusoff · Biochemical Pharmacology · 1973 · 12.9K citations

Life Sciences, Biochemistry, Chemical Kinetics +14

Moving beyond Rules: The Development of a Central Nervous System Multiparameter Optimization (CNS MPO) Approach To Enable Alignment of Druglike Properties

Travis T. Wager, Xinjun Hou, Patrick R. Verhoest et al. · ACS Chemical Neuroscience · 2010 · 1K citations

Pharmacy, Medicinal Chemistry, Pharmacology +17

Application of the Bicyclo[1.1.1]pentane Motif as a Nonclassical Phenyl Ring Bioisostere in the Design of a Potent and Orally Active γ-Secretase Inhibitor

Antonia F. Stepan, Chakrapani Subramanyam, Ivan Efremov et al. · Journal of Medicinal Chemistry · 2012 · 446 citations · Full text

Pharmacy, Medicinal Chemistry, Pharmacology +17

Drug Overdose Deaths Involving Cocaine and Psychostimulants with Abuse Potential — United States, 2003–2017

Mbabazi Kariisa, Lawrence Scholl, Nana O. Wilson et al. · MMWR Morbidity and Mortality Weekly Report · 2019 · 403 citations · Full text

Pharmacy, Toxicology, Forensic Toxicology +14

The binding sites for cocaine and dopamine in the dopamine transporter overlap

Thijs Beuming, Julie Kniazeff, M Bergmann et al. · Nature Neuroscience · 2008 · 351 citations · Full text

Life Sciences, Neuroscience, Pharmacology +14