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Items: 44

1.

Receptor Binding Assays for HTS and Drug Discovery.

Auld DS, Farmen MW, Kahl SD, Kriauciunas A, McKnight KL, Montrose C, Weidner JR.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2018 Jul 1].

2.

Assay Guidance Manual: Quantitative Biology and Pharmacology in Preclinical Drug Discovery.

Coussens NP, Sittampalam GS, Guha R, Brimacombe K, Grossman A, Chung TDY, Weidner JR, Riss T, Trask OJ, Auld D, Dahlin JL, Devanaryan V, Foley TL, McGee J, Kahl SD, Kales SC, Arkin M, Baell J, Bejcek B, Gal-Edd N, Glicksman M, Haas JV, Iversen PW, Hoeppner M, Lathrop S, Sayers E, Liu H, Trawick B, McVey J, Lemmon VP, Li Z, McManus O, Minor L, Napper A, Wildey MJ, Pacifici R, Chin WW, Xia M, Xu X, Lal-Nag M, Hall MD, Michael S, Inglese J, Simeonov A, Austin CP.

Clin Transl Sci. 2018 Sep;11(5):461-470. doi: 10.1111/cts.12570. Epub 2018 Jul 24. Review.

3.

Structural basis for GPR40 allosteric agonism and incretin stimulation.

Ho JD, Chau B, Rodgers L, Lu F, Wilbur KL, Otto KA, Chen Y, Song M, Riley JP, Yang HC, Reynolds NA, Kahl SD, Lewis AP, Groshong C, Madsen RE, Conners K, Lineswala JP, Gheyi T, Saflor MD, Lee MR, Benach J, Baker KA, Montrose-Rafizadeh C, Genin MJ, Miller AR, Hamdouchi C.

Nat Commun. 2018 Apr 25;9(1):1645. doi: 10.1038/s41467-017-01240-w.

4.

Insulin exits skeletal muscle capillaries by fluid-phase transport.

Williams IM, Valenzuela FA, Kahl SD, Ramkrishna D, Mezo AR, Young JD, Wells KS, Wasserman DH.

J Clin Invest. 2018 Feb 1;128(2):699-714. doi: 10.1172/JCI94053. Epub 2018 Jan 8.

5.

Discovery of LY3104607: A Potent and Selective G Protein-Coupled Receptor 40 (GPR40) Agonist with Optimized Pharmacokinetic Properties to Support Once Daily Oral Treatment in Patients with Type 2 Diabetes Mellitus.

Hamdouchi C, Maiti P, Warshawsky AM, DeBaillie AC, Otto KA, Wilbur KL, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Cr S, Lineswala JP, Neathery GL, Bouaichi C, Diseroad BA, Campbell AN, Sweetana SA, Adams LA, Cabrera O, Ma X, Yumibe NP, Montrose-Rafizadeh C, Chen Y, Miller AR.

J Med Chem. 2018 Feb 8;61(3):934-945. doi: 10.1021/acs.jmedchem.7b01411. Epub 2018 Jan 5.

PMID:
29236497
6.

Assay Operations for SAR Support.

Beck B, Chen YF, Dere W, Devanarayan V, Eastwood BJ, Farmen MW, Iturria SJ, Iversen PW, Kahl SD, Moore RA, Sawyer BD, Weidner J.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2017 Nov 20].

7.

A selective GPR40 (FFAR1) agonist LY2881835 provides immediate and durable glucose control in rodent models of type 2 diabetes.

Chen Y, Song M, Riley JP, Hu CC, Peng X, Scheuner D, Bokvist K, Maiti P, Kahl SD, Montrose-Rafizadeh C, Hamdouchi C, Miller AR.

Pharmacol Res Perspect. 2016 Nov 21;4(6):e00278. doi: 10.1002/prp2.278. eCollection 2016 Dec.

8.

The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470).

Hamdouchi C, Kahl SD, Patel Lewis A, Cardona GR, Zink RW, Chen K, Eessalu TE, Ficorilli JV, Marcelo MC, Otto KA, Wilbur KL, Lineswala JP, Piper JL, Coffey DS, Sweetana SA, Haas JV, Brooks DA, Pratt EJ, Belin RM, Deeg MA, Ma X, Cannady EA, Johnson JT, Yumibe NP, Chen Q, Maiti P, Montrose-Rafizadeh C, Chen Y, Reifel Miller A.

J Med Chem. 2016 Dec 22;59(24):10891-10916. doi: 10.1021/acs.jmedchem.6b00892. Epub 2016 Nov 11.

PMID:
27749056
9.

In Vivo and In Vitro Characterization of Basal Insulin Peglispro: A Novel Insulin Analog.

Owens RA, Hansen RJ, Kahl SD, Zhang C, Ruan X, Koester A, Li S, Qian HR, Farmen MW, Michael MD, Moyers JS, Cutler GB Jr, Vick A, Beals JM.

J Pharmacol Exp Ther. 2016 Jun;357(3):459-65. doi: 10.1124/jpet.115.231035. Epub 2016 Mar 29.

PMID:
27026683
10.

Discovery of a novel series of orally active nociceptin/orphanin FQ (NOP) receptor antagonists based on a dihydrospiro(piperidine-4,7'-thieno[2,3-c]pyran) scaffold.

Toledo MA, Pedregal C, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Torrado A, Mateos C, Joshi EM, Kahl SD, Rash KS, Mudra DR, Barth VN, Shaw DB, McKinzie D, Witkin JM, Statnick MA.

J Med Chem. 2014 Apr 24;57(8):3418-29. doi: 10.1021/jm500117r. Epub 2014 Apr 11.

PMID:
24678969
11.

LY2456302 is a novel, potent, orally-bioavailable small molecule kappa-selective antagonist with activity in animal models predictive of efficacy in mood and addictive disorders.

Rorick-Kehn LM, Witkin JM, Statnick MA, Eberle EL, McKinzie JH, Kahl SD, Forster BM, Wong CJ, Li X, Crile RS, Shaw DB, Sahr AE, Adams BL, Quimby SJ, Diaz N, Jimenez A, Pedregal C, Mitch CH, Knopp KL, Anderson WH, Cramer JW, McKinzie DL.

Neuropharmacology. 2014 Feb;77:131-44. doi: 10.1016/j.neuropharm.2013.09.021. Epub 2013 Sep 23.

PMID:
24071566
12.

GTPγS Binding Assays.

DeLapp NW, Gough WH, Kahl SD, Porter AC, Wiernicki TR.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2012 Oct 1].

13.

Basics of Enzymatic Assays for HTS.

Brooks HB, Geeganage S, Kahl SD, Montrose C, Sittampalam S, Smith MC, Weidner JR.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-.
2012 May 1 [updated 2012 Oct 1].

14.

Calculations and Instrumentation used for Radioligand Binding Assays.

Kahl SD, Sittampalam GS, Weidner J.

In: Sittampalam GS, Grossman A, Brimacombe K, Arkin M, Auld D, Austin C, Baell J, Bejcek B, Caaveiro JMM, Chung TDY, Coussens NP, Dahlin JL, Devanaryan V, Foley TL, Glicksman M, Hall MD, Haas JV, Hoare SRJ, Inglese J, Iversen PW, Kahl SD, Kales SC, Kirshner S, Lal-Nag M, Li Z, McGee J, McManus O, Riss T, Trask OJ Jr., Weidner JR, Wildey MJ, Xia M, Xu X, editors. Assay Guidance Manual [Internet]. Bethesda (MD): Eli Lilly & Company and the National Center for Advancing Translational Sciences; 2004-. No abstract available.
2012 May 1 [updated 2012 Oct 1].

15.

Development of LC-MS/MS-based receptor occupancy tracers and positron emission tomography radioligands for the nociceptin/orphanin FQ (NOP) receptor.

Pedregal C, Joshi EM, Toledo MA, Lafuente C, Diaz N, Martinez-Grau MA, Jiménez A, Benito A, Navarro A, Chen Z, Mudra DR, Kahl SD, Rash KS, Statnick MA, Barth VN.

J Med Chem. 2012 Jun 14;55(11):4955-67. doi: 10.1021/jm201629q. Epub 2012 May 16.

PMID:
22541041
16.

Discovery of aminobenzyloxyarylamides as κ opioid receptor selective antagonists: application to preclinical development of a κ opioid receptor antagonist receptor occupancy tracer.

Mitch CH, Quimby SJ, Diaz N, Pedregal C, de la Torre MG, Jimenez A, Shi Q, Canada EJ, Kahl SD, Statnick MA, McKinzie DL, Benesh DR, Rash KS, Barth VN.

J Med Chem. 2011 Dec 8;54(23):8000-12. doi: 10.1021/jm200789r. Epub 2011 Oct 26.

PMID:
21958337
17.

Combination of a Beta adrenoceptor modulator and a norepinephrine-serotonin uptake inhibitor for the treatment of obesity.

Jesudason CD, Baker JE, Bryant RD, Fisher JW, O'Farrell LS, Gaich GA, He MM, Kahl SD, Kriauciunas AV, Heiman ML, Peters MA, Rito CJ, Satterwhite JH, Tinsley FC, Trankle WG, Shuker AJ.

ACS Med Chem Lett. 2011 May 23;2(8):583-6. doi: 10.1021/ml200071k. eCollection 2011 Aug 11.

18.

Scintillation proximity assay.

Kahl SD, Felder CC.

Curr Protoc Neurosci. 2005 Feb;Chapter 7:Unit 7.15. doi: 10.1002/0471142301.ns0715s30.

PMID:
18428624
19.

Structure-activity relationships of beta-MSH derived melanocortin-4 receptor peptide agonists.

Yan LZ, Hsiung HM, Heiman ML, Gadski RA, Emmerson PJ, Hertel J, Flora D, Edwards P, Smiley D, Zhang L, Husain S, Kahl SD, DiMarchi RD, Mayer JP.

Curr Top Med Chem. 2007;7(11):1052-67. Review.

PMID:
17584126
20.

pI-shifted insulin analogs with extended in vivo time action and favorable receptor selectivity.

Kohn WD, Micanovic R, Myers SL, Vick AM, Kahl SD, Zhang L, Strifler BA, Li S, Shang J, Beals JM, Mayer JP, DiMarchi RD.

Peptides. 2007 Apr;28(4):935-48. Epub 2007 Jan 25.

PMID:
17328992
21.

Potent and selective MC-4 receptor agonists based on a novel disulfide scaffold.

Yan LZ, Flora D, Edwards P, Smiley DL, Emmerson PJ, Hsiung HM, Gadski R, Hertel J, Heiman ML, Husain S, O'Brien TP, Kahl SD, Zhang L, Dimarchi RD, Mayer JP.

Bioorg Med Chem Lett. 2005 Oct 15;15(20):4611-4.

PMID:
16105738
22.

Discovery of a beta-MSH-derived MC-4R selective agonist.

Mayer JP, Hsiung HM, Flora DB, Edwards P, Smith DP, Zhang XY, Gadski RA, Heiman ML, Hertel JL, Emmerson PJ, Husain S, O'brien TP, Kahl SD, Smiley DL, Zhang L, Dimarchi RD, Yan LZ.

J Med Chem. 2005 May 5;48(9):3095-8.

PMID:
15857110
23.

Synthesis and structure-activity relationships of novel arylpiperazines as potent and selective agonists of the melanocortin subtype-4 receptor.

Richardson TI, Ornstein PL, Briner K, Fisher MJ, Backer RT, Biggers CK, Clay MP, Emmerson PJ, Hertel LW, Hsiung HM, Husain S, Kahl SD, Lee JA, Lindstrom TD, Martinelli MJ, Mayer JP, Mullaney JT, O'Brien TP, Pawlak JM, Revell KD, Shah J, Zgombick JM, Herr RJ, Melekhov A, Sampson PB, King CH.

J Med Chem. 2004 Jan 29;47(3):744-55.

PMID:
14736255
24.

Differential distribution of urocortin- and corticotropin-releasing factor-like immunoreactivities in the rat brain.

Morin SM, Ling N, Liu XJ, Kahl SD, Gehlert DR.

Neuroscience. 1999;92(1):281-91.

PMID:
10392850
25.

BOCILLIN FL, a sensitive and commercially available reagent for detection of penicillin-binding proteins.

Zhao G, Meier TI, Kahl SD, Gee KR, Blaszczak LC.

Antimicrob Agents Chemother. 1999 May;43(5):1124-8.

26.

Characterization of [125I-Tyr0]-corticotropin releasing factor (CRF) binding to the CRF binding protein using a scintillation proximity assay.

Kahl SD, Liu XJ, Ling N, De Souza EB, Gehlert DR.

J Neurosci Methods. 1998 Sep 1;83(2):103-11.

PMID:
9765123
27.

High-throughput screening: advances in assay technologies.

Sittampalam GS, Kahl SD, Janzen WP.

Curr Opin Chem Biol. 1997 Oct;1(3):384-91. Review.

PMID:
9667878
28.

A multiple-approach scintillation proximity assay to measure the association between Ras and Raf.

Kahl SD, Gygi T, Eichelberger LE, Manetta JV.

Anal Biochem. 1996 Dec 15;243(2):282-3. No abstract available.

PMID:
8954563
29.

Absence of the skeletal muscle sarcolemma chloride channel ClC-1 in myotonic mice.

Gurnett CA, Kahl SD, Anderson RD, Campbell KP.

J Biol Chem. 1995 Apr 21;270(16):9035-8.

30.

Photoaffinity labeling of the ryanodine receptor/Ca2+ release channel with an azido derivative of ryanodine.

Witcher DR, McPherson PS, Kahl SD, Lewis T, Bentley P, Mullinnix MJ, Windass JD, Campbell KP.

J Biol Chem. 1994 May 6;269(18):13076-9.

31.

Radioimmunoassay for the calcium release channel agonist ryanodine.

Kahl SD, McPherson PS, Lewis T, Bentley P, Mullinnix MJ, Windass JD, Campbell KP.

Anal Biochem. 1994 Apr;218(1):55-62.

PMID:
8053568
32.

Purification and reconstitution of N-type calcium channel complex from rabbit brain.

Witcher DR, De Waard M, Kahl SD, Campbell KP.

Methods Enzymol. 1994;238:335-48. No abstract available.

PMID:
7799800
33.

Subunit identification and reconstitution of the N-type Ca2+ channel complex purified from brain.

Witcher DR, De Waard M, Sakamoto J, Franzini-Armstrong C, Pragnell M, Kahl SD, Campbell KP.

Science. 1993 Jul 23;261(5120):486-9.

PMID:
8392754
34.

Disruption of the dystrophin-glycoprotein complex in the cardiomyopathic hamster.

Roberds SL, Ervasti JM, Anderson RD, Ohlendieck K, Kahl SD, Zoloto D, Campbell KP.

J Biol Chem. 1993 Jun 5;268(16):11496-9.

35.

Association of dystrophin-related protein with dystrophin-associated proteins in mdx mouse muscle.

Matsumura K, Ervasti JM, Ohlendieck K, Kahl SD, Campbell KP.

Nature. 1992 Dec 10;360(6404):588-91.

PMID:
1461282
36.

Dystrophin-related protein is localized to neuromuscular junctions of adult skeletal muscle.

Ohlendieck K, Ervasti JM, Matsumura K, Kahl SD, Leveille CJ, Campbell KP.

Neuron. 1991 Sep;7(3):499-508.

PMID:
1654951
37.

Purification of dystrophin from skeletal muscle.

Ervasti JM, Kahl SD, Campbell KP.

J Biol Chem. 1991 May 15;266(14):9161-5.

38.

Structural characterization of the dihydropyridine-sensitive calcium channel alpha 2-subunit and the associated delta peptides.

Jay SD, Sharp AH, Kahl SD, Vedvick TS, Harpold MM, Campbell KP.

J Biol Chem. 1991 Feb 15;266(5):3287-93.

39.

Deficiency of a glycoprotein component of the dystrophin complex in dystrophic muscle.

Ervasti JM, Ohlendieck K, Kahl SD, Gaver MG, Campbell KP.

Nature. 1990 May 24;345(6273):315-9.

PMID:
2188135
40.

Association of dystrophin and an integral membrane glycoprotein.

Campbell KP, Kahl SD.

Nature. 1989 Mar 16;338(6212):259-62.

PMID:
2493582
41.

Evidence for the association of dystrophin with the transverse tubular system in skeletal muscle.

Knudson CM, Hoffman EP, Kahl SD, Kunkel LM, Campbell KP.

J Biol Chem. 1988 Jun 15;263(17):8480-4.

43.

Identification and characterization of the high affinity [3H]ryanodine receptor of the junctional sarcoplasmic reticulum Ca2+ release channel.

Campbell KP, Knudson CM, Imagawa T, Leung AT, Sutko JL, Kahl SD, Raab CR, Madson L.

J Biol Chem. 1987 May 15;262(14):6460-3.

44.

High-affinity antibodies to the 1,4-dihydropyridine Ca2+-channel blockers.

Campbell KP, Sharp A, Strom M, Kahl SD.

Proc Natl Acad Sci U S A. 1986 May;83(9):2792-6.

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