Koc-Kan Ho
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Explore the profile of Koc-Kan Ho including associated specialties, affiliations and a list of published articles.
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24
Citations
246
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Recent Articles
11.
Napier S, Letourneau J, Ansari N, Auld D, Baker J, Best S, et al.
Bioorg Med Chem Lett
. 2011 Mar;
21(6):1871-5.
PMID: 21353540
Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good...
12.
Palin R, Abernethy L, Ansari N, Cameron K, Clarkson T, Dempster M, et al.
Bioorg Med Chem Lett
. 2011 Jan;
21(3):892-8.
PMID: 21236666
Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and...
13.
Brown A, Bosies M, Cameron H, Clark J, Cowley A, Craighead M, et al.
Bioorg Med Chem Lett
. 2010 Dec;
21(1):137-40.
PMID: 21129964
High-throughput screening of 3.87 million compounds delivered a novel series of non-steroidal GR antagonists. Subsequent rounds of optimisation allowed progression from a non-selective ligand with a poor ADMET profile to...
14.
McGuinness B, Ho K, Stauffer T, Rokosz L, Mannava N, Kultgen S, et al.
Bioorg Med Chem Lett
. 2010 Nov;
20(24):7414-20.
PMID: 21055932
A novel series of quinolinone-based adenosine A(2B) receptor antagonists was identified via high throughput screening of an encoded combinatorial compound collection. Synthesis and assay of a series of analogs highlighted...
15.
Letourneau J, Jokiel P, Olson J, Riviello C, Ho K, McAleer L, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(18):5449-53.
PMID: 20719511
The discovery, synthesis and preliminary structure-activity relationships (SARs) of a novel class of CB1 antagonists is described. Initial optimization of benzimidazole-based screening hit 4 led to the identification of 'inverted'...
16.
Letourneau J, Riviello C, Li H, Cole A, Ho K, Zanetakos H, et al.
Bioorg Med Chem Lett
. 2010 Aug;
20(18):5394-7.
PMID: 20719508
The discovery, synthesis, and preliminary structure-activity relationship (SAR) of a novel class of vasopressin V3 (V1b) receptor antagonists is described. Compound 1, identified by high throughput screening of a diverse,...
17.
Cole A, Bohnstedt A, Paradkar V, Kingsbury C, Quintero J, Park H, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(23):6788-92.
PMID: 19836234
A novel class of Janus tyrosine kinase 3 (JAK3) inhibitors based on a 2-benzimidazoylpurinone core structure is described. Through substitution of the benzimidazoyl moiety and optimization of the N-9 substituent...
18.
Ho K, Beasley J, Belanger L, Black D, Chan J, Dunn D, et al.
Bioorg Med Chem Lett
. 2009 Oct;
19(21):6027-31.
PMID: 19800787
The profile of a series of triazine and pyrimidine based ROCK inhibitors is described. An initial binding mode was established based on a homology model and the proposed interactions are...
19.
de Kruijf P, van Heteren J, Lim H, Conti P, van der Lee M, Bosch L, et al.
J Pharmacol Exp Ther
. 2009 Feb;
329(2):783-90.
PMID: 19190236
The chemokine receptor CXCR2 is involved in different inflammatory diseases, like chronic obstructive pulmonary disease, psoriasis, rheumatoid arthritis, and ulcerative colitis; therefore, it is considered an attractive drug target. Different...
20.
Ho K, Auld D, Bohnstedt A, Conti P, Dokter W, Erickson S, et al.
Bioorg Med Chem Lett
. 2006 Mar;
16(10):2724-8.
PMID: 16540318
An imidazolylpyrimidine was identified in a CXCR2 chemokine receptor antagonist screen and was optimized for potency, in vitro metabolic stability, and oral bioavailability. It was found that subtle structural modification...