Integrity profiling of high throughput screening hits using LC-MS and related techniques.
Integrity profiling of HTS hits is valuable for verification of the hit identity and purity. This provides early discovery researchers with more confident SAR theories. Methodology for integrity profiling of HTS hits must be high throughput, consume little material, and selectively provide structure-based data. Analytical techniques that can be utilized for integrity profiling methods are reviewed for their appropriateness in sample preparation, component separation, detection, purity quantitation, identity confirmation, and follow-up.
Kerns
Edward H
EH
Chemical and Screening Sciences, Wyeth Research Princeton, NJ 08543-8000, USA. kernse@wyeth.com
Di
Li
L
Bourassa
Jim
J
Gross
Jonathan
J
Huang
Nelson
N
Liu
Hanlan
H
Kleintop
Teresa
T
Nogle
Lisa
L
Mallis
Larry
L
Petucci
Chris
C
Petusky
Susan
S
Tischler
Mark
M
Sabus
Chantel
C
Sarkahian
Ani
A
Young
Mairead
M
Zhang
Mei-Yi
MY
Huryn
Donna
D
McConnell
Oliver
O
Carter
Guy
G
D002853:Chromatography, Liquid / Q000379:methods*; D020650:Combinatorial Chemistry Techniques; D013058:Mass Spectrometry / Q000379:methods*; D012542:Scattering, Radiation; D013056:Spectrophotometry, Ultraviolet; D013329:Structure-Activity Relationship