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CNS Targets

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Description
• Library of compounds acting on central nervous system (CNS) targets
• In CNS drug discovery the drug targets are used for targeting CNS and neurological related diseases
like Parkinson’s disease, Alzheimer’s disease, schizophrenia, drug dependence, etc.
• Activity of drug target as a nucleic acid or a protein (e.g. an enzyme, a receptor) can be modulated by
a small-molecular-weight chemical compound.
• As the discovery, identification, characterization and validation of novel human drug targets for CNS
disease biology, and the emergence of new mechanisms and targets for misfolded proteins, tau,
GCPRs, kinase inhibitors, neuroinflammation, etc. continues to grow; this library is a valuable tool for
the neurological and CNS drug discovery.

A unique collection of small molecule compounds selected for CNS protein targets
❑ Therapeutically relevant CNS targets (98 protein sub-families/units targets in total)
❑ Recent literature data from 846 research papers and patents published since 2014
❑ The recent X-Ray and Cryo-EM structures from PDB
❑ Comprehensive CNS Targets Platform Library : 44,000 compounds

Publications
1. Section 1: Central Nervous System Diseases. Eds. Lindsley CW, Medicinal Chemistry Reviews 2018; 53:41-82.
2. Section 1: Central Nervous System Diseases. Eds. Lindsley CW, Medicinal Chemistry Reviews 2017; 52:3-105.
3. Section 1: Central Nervous System Diseases. Eds. Lindsley CW, Medicinal Chemistry Reviews 2016; 51:17-52.
4. Section 1: Central Nervous System Diseases. Eds. Robichaud A, Medicinal Chemistry Reviews 2015; 50:31-80.
5. Science 2014;344(6179):58-64. Structure of a class C GPCR metabotropic glutamate receptor 1 bound to an allosteric modulator. Wu H, Wang C, Gregory KJ, Han GW, Cho HP, Xia Y,
Niswender CM, Katritch V, Meiler J, Cherezov V, Conn PJ, Stevens RC.
6. Nature 2015;519(7542):247-50. Crystal structure of the human OX2 orexin receptor bound to the insomnia drug suvorexant. Yin J, Mobarec JC, Kolb P, Rosenbaum DM.
7. J Med Chem. 2015;58(18):7526-48. Synthesis and Pharmacological Characterization of C4-(Thiotriazolyl)-substituted-2-aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of
(1R,2S,4R,5R,6R)-2-Amino-4-(1H-1,2,4-triazol-3-ylsulfanyl)bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2812223), a Highly Potent, Functionally Selective mGlu2 Receptor Agonist. Monn JA,
Prieto L, Taboada L, Hao J, Reinhard MR, Henry SS, Beadle CD, [...], McKinzie DL.
8. J Med Chem. 2018;61(6):2303-2328. Synthesis and Pharmacological Characterization of C4β-Amide-Substituted 2-Aminobicyclo[3.1.0]hexane-2,6-dicarboxylates. Identification of (1 S,2 S,4
S,5 R,6 S)-2-Amino-4-[(3-methoxybenzoyl)amino]bicyclo[3.1.0]hexane-2,6-dicarboxylic Acid (LY2794193), a Highly Potent and Selective mGlu3 Receptor Agonist. Monn JA, Henry SS, Massey
SM, Clawson DK, Chen Q, Diseroad BA, Bhardwaj RM, Atwell S, Lu F, Wang J, Russell M, Heinz BA, Wang XS, Carter JH, Getman BG, Adragni K, Broad LM, Sanger HE, Ursu D, Catlow JT,
Swanson S, Johnson BG, Shaw DB, McKinzie DL, Hao J.
9. Acta Crystallogr D Biol Crystallogr. 2012;68(8):1041-1050. X-ray structure of p38α bound to TAK-715: comparison with three classic inhibitors. Azevedo R, van Zeeland M, Raaijmakers H,
Kazemier B, de Vlieg J, Oubrie A.
10. Bioorg. Med. Chem. Lett. 2019;29:406-412. Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors. Geneste H, Drescher K, Jakob C, Laplanche L, OchseM, Torrent M.
11. J.Med.Chem. 2014;57:9627-9643. Discovery of 1-[2-fluoro-4-(1H-pyrazol-1-yl)phenyl]-5-methoxy-3-(1-phenyl-1H-pyrazol-5-yl)pyridazin-4(1H)-one (TAK-063), a highly potent, selective, and
orally active phosphodiesterase 10A (PDE10A) inhibitor. Kunitomo J, Yoshikawa M, Fushimi M, Kawada A, Quinn JF, Oki H, Kokubo H, Kondo M, Nakashima K, Kamiguchi N, Suzuki K, Kimura H,
Taniguchi T.
12. Proc.Natl.Acad.Sci.USA 2015;112:493. Pf-06463922 is a Potent and Selective Next-Generation Ros1/Alk Inhibitor Capable of Blocking Crizotinib-Resistant Ros1 Mutations. Zou, H.Y., Li, Q.,
Engstrom, L.D., West, M., Appleman, V., Wong, K.A., Mctigue, M., Deng, Y., Liu, W., Brooun, A., Timofeevski, S., Mcdonnell, S.R.P., Jiang, P., Falk, M.D., Lappin, P.B., Affolter, T., Nichols, T., Hu,
W., Lam, J., Johnson, T.W., Smeal, T., Charest, A., Fantin, V.R.
13. J.Med.Chem. 2020;63:2263-2281. Discovery of AM-6494: A Potent and Orally Efficacious beta-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over
BACE2. Pettus LH, Bourbeau MP, Bradley J, Bartberger MD, Chen K, Hickman D, Johnson M, Liu Q, Manning JR, Nanez A, Siegmund AC, Wen PH, Whittington DA, Allen JR, Wood S.
14. EMBO Mol Med. 2018;10(11). pii: e9316. The BACE-1 inhibitor CNP520 for prevention trials in Alzheimer's disease. Neumann U, Ufer M, Jacobson LH, [...], Lopez Lopez C.
15. J. Biol. Chem. 2018;293:10985-10992. Structural basis for selective inhibition of human PKG I alpha by the balanol-like compound N46. Qin L, Sankaran B, Aminzai S, Casteel DE, Kim C.
16. AbbVie Inc US-9493431-B2 2016 Apoptosis-inducing agent for the treatment of cancer and immune and autoimmune diseases. Kunzer AR, Elmore SW, Sullivan GM,
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