Target Validation Information
Target ID T09960
Target Name C-C chemokinereceptor type 5
Target Type
Successful
Drug Potency against Target SCH-C Drug Info IC50 = 0.69 nM [552440]
GW873140 Drug Info IC50 = 0.6 nM [552718]
SCH-210971 Drug Info IC50 = 1200 nM [528341]
VARIECOLIN Drug Info IC50 = 9000 nM [527257]
INCB9471 Drug Info IC50 < 13 nM
Tak-220 Drug Info IC50 = 3.5 nM [536272]
(2-(4-chlorobenzyloxy)-5-bromophenyl)methanamine Drug Info IC50 = 1700 nM [528689]
TAK-779 Drug Info Ki = 1.1 nM [552440]
Vicriviroc Drug Info Ki = 4 nM [552718]
ANIBAMINE Drug Info IC50 = 1000 nM [527121]
N-(2-(4-chlorobenzyloxy)-5-bromobenzyl)ethanamine Drug Info IC50 = 1100 nM [528689]
Cenicriviroc Drug Info IC90 = 0.81 nM [528083]
Maraviroc Drug Info IC90 < 10 nM [527454]
4-(2-(4-chlorobenzyloxy)-5-bromobenzyl)morpholine Drug Info IC50 = 1000 nM [528511]
Maraviroc Drug Info IC50 = 0.7 nM [552718]
GT-1282 Drug Info IC50 = 64 nM [529307]
NIFEVIROC Drug Info IC50 = 2.9 nM [531070]
References
Ref 552440Chemokine receptor-directed agents as novel anti-HIV-1 therapies. Curr Top Med Chem. 2004;4(10):1017-33.
Ref 552718An update in the development of HIV entry inhibitors. Curr Top Med Chem. 2007;7(13):1273-89.
Ref 528341J Nat Prod. 2006 Jul;69(7):1025-8.Chemokine receptor CCR-5 inhibitors produced by Chaetomium globosum.
Ref 527257J Nat Prod. 2004 Oct;67(10):1681-4.Inhibition of the human chemokine receptor CCR5 by variecolin and variecolol and isolation of four new variecolin analogues, emericolins A-D, from Emericella aurantiobrunnea.
Ref 536272Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
Ref 528689Bioorg Med Chem Lett. 2007 Apr 1;17(7):1883-7. Epub 2007 Jan 25.CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives.
Ref 552440Chemokine receptor-directed agents as novel anti-HIV-1 therapies. Curr Top Med Chem. 2004;4(10):1017-33.
Ref 552718An update in the development of HIV entry inhibitors. Curr Top Med Chem. 2007;7(13):1273-89.
Ref 527121J Nat Prod. 2004 Jun;67(6):1036-8.Isolation and structure of antagonists of chemokine receptor (CCR5).
Ref 528689Bioorg Med Chem Lett. 2007 Apr 1;17(7):1883-7. Epub 2007 Jan 25.CCR5 receptor antagonists: discovery and SAR of novel 4-hydroxypiperidine derivatives.
Ref 528083J Med Chem. 2006 Mar 23;49(6):2037-48.Highly potent and orally active CCR5 antagonists as anti-HIV-1 agents: synthesis and biological activities of 1-benzazocine derivatives containing a sulfoxide moiety.
Ref 527454J Med Chem. 2005 Mar 10;48(5):1297-313.New approaches toward anti-HIV chemotherapy.
Ref 528511Bioorg Med Chem Lett. 2007 Jan 1;17(1):231-4. Epub 2006 Nov 1.CCR5 receptor antagonists: discovery and SAR study of guanylhydrazone derivatives.
Ref 552718An update in the development of HIV entry inhibitors. Curr Top Med Chem. 2007;7(13):1273-89.
Ref 529307Bioorg Med Chem Lett. 2008 Mar 15;18(6):2000-5. Epub 2008 Feb 2.Reduced cardiac side-effect potential by introduction of polar groups: discovery of NIBR-1282, an orally bioavailable CCR5 antagonist which is active in vivo.
Ref 531070Bioorg Med Chem Lett. 2010 Sep 1;20(17):5334-6. Epub 2010 May 19.Studies on the structure-activity relationship of 1,3,3,4-tetra-substituted pyrrolidine embodied CCR5 receptor antagonists. Part 2: Discovery of highly potent anti-HIV agents.

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