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BioAssay: AID 743137

Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis

Name: Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis. ..more
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AID: 743137
Data Source: The Scripps Research Institute Molecular Screening Center (LYPLA1&2_INH_LCMS_ABPP_SILAC)
BioAssay Type: Panel
Depositor Category: NIH Molecular Libraries Probe Production Network, Assay Provider
Deposit Date: 2013-11-26
Hold-until Date: 2014-11-25
Modify Date: 2014-11-25

Data Table ( Complete ):           View Active Data    View All Data
BioActive Compound: 1
Related Experiments
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AIDNameTypeProbeComment
2174Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Primary screen (LYPLA1 inhibitors in singlicate)
2177Counterscreen for PME1 inhibitors: fluorescence polarization-based primary biochemical high throughput screening assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening depositor-specified cross reference: Primary screen (LYPLA2 inhibitors in singlicate)
2202Summary of probe development efforts to identify inhibitors of lysophospholipase 1 (LYPLA1).Summary2 depositor-specified cross reference: Summary (LYPLA1 inhibitors)
2203Summary of probe development efforts to identify inhibitors of lysophospholipase 2 (LYPLA2).Summary1 depositor-specified cross reference: Summary (LYPLA2 inhibitors)
2232Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay to identify inhibitors of lysophospholipase 2 (LYPLA2).Screening depositor-specified cross reference: Confirmation screen (LYPLA2 inhibitors in triplicate)
2233Counterscreen for PME1 inhibitors: fluorescence polarization-based biochemical high throughput confirmation assay for inhibitors of lysophospholipase 1 (LYPLA1).Screening depositor-specified cross reference: Confirmation screen (LYPLA1 inhibitors in triplicate)
493105Assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition of recombinant and endogenous enzymeOther depositor-specified cross reference: Confirmation screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
493108Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: fluorescence-based cell-based inhibitionOther depositor-specified cross reference: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
493109Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: LC-MS/MS assay to assess binding of compounds to active siteOther depositor-specified cross reference: Late stage LCMS assay (LYPLA1)
493110Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for LYPLA1 and LYPLA2Confirmatory depositor-specified cross reference: Late stage dose response (LYPLA1 and LYPLA2 inhibitors in triplicate)
493111Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther depositor-specified cross reference: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
493154Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Gel-based Activity-Based Protein Profiling (ABPP) IC50 for off-target ABHD11Confirmatory depositor-specified cross reference: Late stage dose response counterscreen (ABHD11 inhibitors in triplicate)
493161Late stage assay provider results from the probe development effort to identify dual inhibitors of LYPLA1 and LYPLA2: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory depositor-specified cross reference: Late stage dose response counterscreen (T-cell cytotoxicity in quadruplicate)
504482Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based cell-based gel-based Activity-Based Protein Profiling (ABPP) IC50 for anti-target ABHD11Confirmatory depositor-specified cross reference: Late stage dose repsonse (ABHD11 inhibitors in triplicate)
504498Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: LC-MS/MS assay to assess binding of compounds to active site of anti-target ABHD11Other depositor-specified cross reference: Late stage MOA assay (ABDH11 LCMS)
504505Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based cell-based gel-based Activity-Based Protein Profiling (ABPP) percent inhibition for anti-target ABHD11Other depositor-specified cross reference: Late stage screen (ABHD11 inhibitors in singlicate, in situ)
504507Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) IC50 for anti-target ABHD11 Set 2Confirmatory depositor-specified cross reference: Late stage dose response (ABHD11 inhibitors in triplicate)
504510Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compounds set 2Confirmatory depositor-specified cross reference: Late stage dose repsonse counterscreen (T-cell cytotoxicity in quadruplicate)
504520Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) inhibition and selectivityOther depositor-specified cross reference: Late stage screen (LYPLA1 and LYPLA2 inhibitors in singlicate)
504522Late stage assay provider results from the probe development effort to identify inhibitors of LYPLA1: LC-MS-based cell-based SILAC Activity-Based Protein Profiling (ABPP) for anti-target ABHD11Other depositor-specified cross reference: Late stage (LC-MS-based cell-based SILAC ABPP for anti-target ABHD11)
504892Late stage assay provider results from the probe development effort to identify inhibitors of ABHD11: Fluorescence-based biochemical gel-based Activity-Based Protein Profiling (ABPP) inhibition of the human isoform of ABHD11Other depositor-specified cross reference: Late stage assay (human isoform of ABHD11 inhibitors)
651978Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitroOther depositor-specified cross reference: Late stage ABPP in vitro SILAC assay (LYPLA 1)
651979Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situOther depositor-specified cross reference: Late stage ABPP in situ SILAC assay (LYPLA 1)
651980Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in situOther depositor-specified cross reference: Late stage assay (SILAC selectivity analysis in situ)
651981Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitroOther depositor-specified cross reference: Late stage assay (SILAC selectivity analysis in vitro)
651985Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP evaluation of activity in vivoOther depositor-specified cross reference: Late stage assay (LYPLA1 and LYPLA2 inhibitors activity in vivo)
651986Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP evaluation of activity in situOther depositor-specified cross reference: Late stage assay (LYPLA1 and LYPLA2 inhibitors activity in situ)
651987Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP gel filtration assay to assess binding modeOther depositor-specified cross reference: Late stage assay (binding mode)
651988Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther depositor-specified cross reference: Late stage assay (inhibition and selectivity)
651990Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPPConfirmatory depositor-specified cross reference: Late stage dose-response (LYPLA1 and LYPLA2 inhibitors in triplicate)
651991Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1 and LYPLA2: Absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory depositor-specified cross reference: Late stage dose-response (cytotoxicity 6 replicates)
651998Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: Substrate-based fluorescence-based biochemical determination of kinetic parametersConfirmatory depositor-specified cross reference: Late stage ABPP biochemical kinetics assay (LYPLA 1)
652001Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Substrate-based fluorescence-based biochemical determination of kinetic parametersConfirmatory depositor-specified cross reference: Late stage assay (LYPLA2 kinetic parameters in quadruplicate)
652003Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: fluorescence-based biochemical dose-response assayConfirmatory depositor-specified cross reference: Late stage ABPP biochemical dose response assay (LYPLA 1) (4XIC50)
652004Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: fluorescence-based biochemical dose-response assayConfirmatory depositor-specified cross reference: Late stage dose response (LYPLA2 inhibitors in quadruplicate)
652018Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA1: LCMS-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis in vitro, Set 2Other depositor-specified cross reference: Late stage assay (LYPLA1 and LYPLA2 inhibition and selectivity in singlicate)
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 same project related to Summary assay
652029Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibitionOther same project related to Summary assay
652030Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther same project related to Summary assay
743117Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition potency and selectivityOther same project related to Summary assay
743118Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitroConfirmatory same project related to Summary assay
743119Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in situConfirmatory same project related to Summary assay
743127Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory same project related to Summary assay
743132Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitro in mouse brainConfirmatory same project related to Summary assay
743133Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP gel filtration assay to assess inhibitor binding modeOther same project related to Summary assay
743134Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP assay to assess in vivo activityOther same project related to Summary assay
2143Summary of probe development efforts to identify inhibitors of Protein Phosphatase Methylesterase 1 (PME-1).Summary3 same project related to Summary assay
652029Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibitionOther same project related to Summary assay
652030Late stage assay provider results from the probe development effort to identify selective inhibitors of LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition and selectivityOther same project related to Summary assay
743117Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP inhibition potency and selectivityOther same project related to Summary assay
743118Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitroConfirmatory same project related to Summary assay
743119Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in situConfirmatory same project related to Summary assay
743127Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Absorbance-based cell-based dose response assay to determine cytotoxicity of inhibitor compoundsConfirmatory same project related to Summary assay
743132Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical dose-response gel-based ABPP in vitro in mouse brainConfirmatory same project related to Summary assay
743133Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP gel filtration assay to assess inhibitor binding modeOther same project related to Summary assay
743134Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: Fluorescence-based biochemical gel-based ABPP assay to assess in vivo activityOther same project related to Summary assay
Description:
Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC)
Center Affiliation: The Scripps Research Institute (TSRI)
Assay Provider: Benjamin Cravatt, TSRI
Network: Molecular Libraries Probe Production Centers Network (MLPCN)
Grant Proposal Number: 1 R01 CA132630
Grant Proposal PI: Benjamin Cravatt, TSRI
External Assay ID: LYPLA1&2_INH_LCMS_ABPP_SILAC

Name: Late stage assay provider results from the extended probe development effort to identify inhibitors of LYPLA1 and LYPLA2: LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis.

Description:

Protein palmitoylation is an essential post-translational modification necessary for trafficking and localization of regulatory proteins that play key roles in cell growth and signaling. Numerous proteins have been identified as targets of palmitoylation, including cytoskeletal proteins, kinases, receptors, and other proteins involved in various aspects of cellular signaling and homeostasis [1]. Using a global chemo-proteomic method for the metabolic incorporation and identification of palmitoylated proteins, we were able to identify hundreds of palmitoylated proteins, revealing palmitoylation as a widespread post-translational modification (PTM) [2]. Palmitoylation involves an acyl-thioester linkage to specific cysteines [3,4]. Given the labile properties of thioesters, palmitoylation is potentially reversible and may be regulated in a manner analogous to other PTMs (e.g., phosphorylation). As such, identification of proteins responsible for the dynamic modulation of palmitoylation is paramount to understanding its patho/physiological roles. For example, multiple oncogenes, including HRAS and SRC, require palmitoylation for malignant transformation [5], suggesting protein palmitoyl thioesterases may have tumor suppressor activity required to repress aberrant growth signaling. More than a decade ago, the cytosolic serine hydrolase acyl-protein thioesterase 1 (APT1) was identified as an in vitro HRAS palmitoyl thioesterase [6]. Initially classified as lysophospholipase 1 (LYPLA1) [7], the enzyme has since been demonstrated to have several hundred-fold higher activity as a protein thioesterase. While the in vitro data [6,8] provided an intriguing clue to its possible role in vivo, prior to our studies, little was known about the in vivo thioesterase activity of LYPLA1. Upon retroviral shRNA knockdown of LYPLA1, we found that HRAS was robustly hyper-palmitoylated, providing the first evidence that the endogenous enzyme is a functional protein palmitoyl thioesterase capable of regulating HRAS palmitoylation in mammalian cells. However, shRNA resulted in only an 80% reduction in LYPLA1 expression (unpublished). LYPLA2 (a.k.a. APT2) is 65% identical to LYPLA1, and also exhibits lysophospholipase activity in vitro, but its potential role as a thioesterase is unknown [9]. shRNA knockdown studies of LYPLA2 revealed only partial knockdown of the enzyme, making substrate identification inconclusive (unpublished). A principle goal of post-genomic research is the determination of the molecular and cellular role of uncharacterized enzymes like LYPLA1 and LYPLA2. As such, selective inhibitors of LYPLA1 and/or LYPLA2 would greatly aid investigations into the biological function of these enzymes. Several inhibitors of LYPLA1 have been described [10,11], but none of these agents have proven capable of inhibiting LYPLA1 activity in cells. We recently reported optimization of a covalent dual LYPLA1/LYPLA2 inhibitor ML211 (SID 99445338), and identification of reversible compounds ML348 (SID 160654487) and ML349 (SID 160654496) that act as selective LYPLA1 and LYPLA2 inhibitors, respectively (see Probe Reports on the NIH Bookshelf at http://www.ncbi.nlm.nih.gov/books/NBK47352/). These compounds represent an important advance in chemical tools for investigating the biological function(s) of LYPLA1 and LYPLA2. However, ML211 (SID 99445338), owing to its modest solubility, does not have demonstrated in vivo activity. Irreversible chemical probes have distinct advantages vs. reversible compounds for use in living systems, as confirming target engagement is a comparatively straightforward process, and near-complete and sustained target inhibition can be achieved without extensive optimization of physicochemical and pharmacokinetic properties. The goal of this current investigation is to develop an irreversible, in vivo-active dual LYPLA1/LYPLA2 inhibitor to add to the arsenal of available chemical tools for identification of LYPLA1 and LYPLA2 substrates and evaluating the role of these enzymes in dynamic de-palmitoylation and tumorigenesis.

References:

1. Dekker, F.J., et al., Small-molecule inhibition of APT1 affects Ras localization and signaling. Nat. Chem. Biol., 2010. 6(6): p. 449-56.
2. Duncan, J.A. and A.G. Gilman, A cytoplasmic acyl-protein thioesterase that removes palmitate from G protein alpha subunits and p21(RAS). J. Biol. Chem., 1998. 273(25): p. 15830-7.
3. Sugimoto, H., H. Hayashi, and S. Yamashita, Purification, cDNA cloning, and regulation of lysophospholipase from rat liver. J. Biol. Chem., 1996. 271(13): p. 7705-11.
4. Toyoda, T., H. Sugimoto, and S. Yamashita, Sequence, expression in Escherichia coli, and characterization of lysophospholipase II. Biochim. Biophys. Acta, 1999. 1437(2): p. 182-93.
5. Biel, M., et al., Synthesis and evaluation of acyl protein thioesterase 1 (APT1) inhibitors. Chemistry, 2006. 12(15): p. 4121-43.
6. Deck, P., et al., Development and biological evaluation of acyl protein thioesterase 1 (APT1) inhibitors. Angew. Chem. Int. Ed. Engl., 2005. 44(31): p. 4975-80.
7. Jessani, N., et al., Enzyme activity profiles of the secreted and membrane proteome that depict cancer cell invasiveness. Proc. Natl. Acad. Sci. U. S. A., 2002. 99(16): p. 10335-40.
8. Leung, D., et al., Discovering potent and selective reversible inhibitors of enzymes in complex proteomes. Nat. Biotechnol., 2003. 21(6): p. 687-91.
9. Bachovchin, D.A., et al., Identification of selective inhibitors of uncharacterized enzymes by high-throughput screening with fluorescent activity-based probes. Nat. Biotechnol., 2009. 27(4): p. 387-94.
10. Forner, F., et al., Quantitative proteomic comparison of rat mitochondria from muscle, heart, and liver. Mol. Cell. Proteomics, 2006. 5(4): p. 608-19.
11. Schubert, C., The genomic basis of the Williams-Beuren syndrome. Cell. Mol. Life Sci., 2009. 66(7): p. 1178-97.

Keywords:

late stage, late stage AID, assay provider, powders, LYPLA1, lysophospholipase 1, LYPLA2, lysophospholipase 2, APT1, acyl-protein thioesterase 1, APT2, acyl-protein thioesterase 2, serine hydrolase, palmitoylation, counterscreen, inhibitor, inhibition, selectivity, anti-targets, liquid chromatography, LC, tandem mass spectrometry, MS/MS, activity-based protein profiling, ABPP, stable isotope labeling with amino acids in cell culture, SILAC, ABPP-SILAC, in situ, cell-based, fluorophosphonate biotin, FP-biotin, inhibitor, inhibition, HeLa, Scripps, Scripps Research Institute Molecular Screening Center, SRIMSC, Molecular Libraries Probe Production Centers Network, MLPCN.
Panel Information
LCMS-based cell-based Activity-Based Protein Profiling (ABPP) SILAC selectivity analysis.
    Data Table(Active)    Data Table(All)Show more
PID§NameSubstancePanel TargetsDescriptionAdditional Information
ActiveInactive
1LYPLA1 ratio1acyl-protein thioesterase 1 isoform 1 [Homo sapiens] [gi:5453722]
Taxonomy id: 9606
Gene id: 10434
2LYPLA2 ratio1acyl-protein thioesterase 2 [Homo sapiens] [gi:9966764]
Taxonomy id: 9606
Gene id: 11313
3ABHD6 ratio1monoacylglycerol lipase ABHD6 [Homo sapiens] [gi:189027141]
Taxonomy id: 9606
Gene id: 57406
4MAGL (MGLL) ratio1monoglyceride lipase isoform 1 [Homo sapiens] [gi:6005786]
Taxonomy id: 9606
Gene id: 11343
5ABHD12 ratio1monoacylglycerol lipase ABHD12 isoform a [Homo sapiens] [gi:109689718]
Taxonomy id: 9606
Gene id: 26090
6SCPEP1 ratio1retinoid-inducible serine carboxypeptidase precursor [Homo sapiens] [gi:11055992]
Taxonomy id: 9606
Gene id: 59342
7PRCP ratio1RecName: Full=Lysosomal Pro-X carboxypeptidase; AltName: Full=Angiotensinase C; AltName: Full=Lysosomal carboxypeptidase C; AltName: Full=Proline carboxypeptidase; AltName: Full=Prolylcarboxypeptidase; Short=PRCP; Flags: Precursor [gi:1172047]
Taxonomy id: 9606
Gene id: 5547
8NCEH1 ratio1neutral cholesterol ester hydrolase 1 isoform b [Homo sapiens] [gi:68051721]
Taxonomy id: 9606
Gene id: 57552
9FAM108B1 ratio1alpha/beta hydrolase domain-containing protein 17B isoform 1 precursor [Homo sapiens] [gi:71051600]
Taxonomy id: 9606
Gene id: 51104
10FAP ratio1RecName: Full=Seprase; AltName: Full=170 kDa melanoma membrane-bound gelatinase; AltName: Full=Fibroblast activation protein alpha; AltName: Full=Integral membrane serine protease [gi:292495099]
Taxonomy id: 9606
Gene id: 2191
11CTSA ratio1RecName: Full=Lysosomal protective protein; AltName: Full=Carboxypeptidase C; AltName: Full=Carboxypeptidase L; AltName: Full=Cathepsin A; AltName: Full=Protective protein cathepsin A; Short=PPCA; AltName: Full=Protective protein for beta-galactosidase; Contains: RecName: Full=Lysosomal protective protein 32 kDa chain; Contains: RecName: Full=Lysosomal protective protein 20 kDa chain; Flags: Precursor [gi:20178316]
Taxonomy id: 9606
Gene id: 5476
12ESD ratio1S-formylglutathione hydrolase [Homo sapiens] [gi:33413400]
Taxonomy id: 9606
Gene id: 2098
13PNPLA6 ratio1neuropathy target esterase isoform a [Homo sapiens] [gi:260656037]
Taxonomy id: 9606
Gene id: 10908
14PAFAH1B2 ratio1RecName: Full=Platelet-activating factor acetylhydrolase IB subunit beta; AltName: Full=PAF acetylhydrolase 30 kDa subunit; Short=PAF-AH 30 kDa subunit; AltName: Full=PAF-AH subunit beta; Short=PAFAH subunit beta [gi:55977294]
Taxonomy id: 9606
Gene id: 5049
15PNPLA4 ratio1RecName: Full=Patatin-like phospholipase domain-containing protein 4; AltName: Full=Protein GS2 [gi:116242718]
Taxonomy id: 9606
Gene id: 8228
16APEH ratio1acylamino-acid-releasing enzyme [Homo sapiens] [gi:23510451]
Taxonomy id: 9606
Gene id: 327
17ABHD10 ratio1mycophenolic acid acyl-glucuronide esterase, mitochondrial isoform 1 precursor [Homo sapiens] [gi:8923001]
Taxonomy id: 9606
Gene id: 55347
18ABHD11 ratio1RecName: Full=Alpha/beta hydrolase domain-containing protein 11; Short=Abhydrolase domain-containing protein 11; AltName: Full=Williams-Beuren syndrome chromosomal region 21 protein [gi:74751292]
Taxonomy id: 9606
Gene id: 83451
19PAFAH1B3 ratio1RecName: Full=Platelet-activating factor acetylhydrolase IB subunit gamma; AltName: Full=PAF acetylhydrolase 29 kDa subunit; Short=PAF-AH 29 kDa subunit; AltName: Full=PAF-AH subunit gamma; Short=PAFAH subunit gamma [gi:3024344]
Taxonomy id: 9606
Gene id: 5050
20PLA2G15 ratio1RecName: Full=Group XV phospholipase A2; AltName: Full=1-O-acylceramide synthase; Short=ACS; AltName: Full=LCAT-like lysophospholipase; Short=LLPL; AltName: Full=Lysophospholipase 3; AltName: Full=Lysosomal phospholipase A2; Short=LPLA2; Flags: Precursor [gi:44888104]
Taxonomy id: 9606
Gene id: 23659
21PAFAH2 ratio1RecName: Full=Platelet-activating factor acetylhydrolase 2, cytoplasmic; AltName: Full=Serine-dependent phospholipase A2; Short=SD-PLA2; Short=hSD-PLA2 [gi:6647691]
Taxonomy id: 9606
Gene id: 5051
22ACOT2 ratio1RecName: Full=Acyl-coenzyme A thioesterase 2, mitochondrial; Short=Acyl-CoA thioesterase 2; AltName: Full=Acyl-coenzyme A thioester hydrolase 2a; AltName: Full=CTE-Ia; AltName: Full=Long-chain acyl-CoA thioesterase 2; AltName: Full=ZAP128; Flags: Precursor [gi:269849771]
Taxonomy id: 9606
Gene id: 10965
23DPP8 ratio1RecName: Full=Dipeptidyl peptidase 8; Short=DP8; AltName: Full=Dipeptidyl peptidase IV-related protein 1; Short=DPRP-1; AltName: Full=Dipeptidyl peptidase VIII; Short=DPP VIII; AltName: Full=Prolyl dipeptidase DPP8 [gi:67460301]
Taxonomy id: 9606
Gene id: 54878
24FAM111B ratio1RecName: Full=Protein FAM111B; AltName: Full=Cancer-associated nucleoprotein [gi:74758524]
Taxonomy id: 9606
Gene id: 374393
25PREPL ratio1RecName: Full=Prolyl endopeptidase-like; AltName: Full=Prolylendopeptidase-like [gi:121944206]
Taxonomy id: 9606
Gene id: 9581
26LYPLAL1 ratio1lysophospholipase-like protein 1 [Homo sapiens] [gi:20270341]
Taxonomy id: 9606
Gene id: 127018

§ Panel component ID.
Protocol
Assay Overview:
The purpose of this assay is to determine the selectivity profile of powder samples of test compounds using stable isotope labeling with amino acids in cell culture (SILAC) ABPP. In this assay, cultured cells are metabolically labeled with light or heavy amino acids. Light and heavy cells are treated in situ with inhibitor and DMSO. Cells are harvested and proteome fractions isolated and reacted with the serine-hydrolase-specific activity-based affinity probe fluorophosphonate-biotin (FP-biotin). Light and heavy samples are combined in a 1:1 (w/w) ratio. Biotinylated proteins are enriched, trypsinized, and analyzed by LC/LC-MS/MS (MudPIT). Inhibition of target and anti-target activity is quantified by comparing intensities of light and heavy peptide peaks. As designed, compounds that act as inhibitors will block FP-biotin probe labeling, reducing enrichment in the inhibitor-treated (light) sample relative to the DMSO-treated (heavy) sample, giving a smaller light/heavy ratio for each protein. Proteins not targeted by inhibitors would be expected to have a ratio close to 1.
Protocol Summary:
Sample Preparation:
HeLa cells were initially grown for at least eight passages in either light or heavy SILAC DMEM medium supplemented with 10% dialyzed FCS and 1x PenStrep Glutamine in a humidified incubator (37 degrees Celsius, 5% CO2). Light medium was supplemented with 100 ug/mL L-arginine (Sigma) and 100 ug/mL L-lysine (Sigma). Heavy medium was supplemented with 100 ug/mL (13C[6]15N[4])-L-Arginine (Isotek) and 100 ug/mL (13C[6]15N[2])-L-Lysine (Isotek). Light cells were treated with test compound (1 uM, from 1000x stock in DMSO) and heavy cells were treated with DMSO for 2 hours at 37 degrees Celsius in a humidified incubator. Each treatment was performed in quadruplicate. Cells were washed (4x cold DPBS), harvested by scraping, and the quadruplicate samples for each condition pooled and lysed in DPBS by sonication. The pooled whole-cell extracts were adjusted to 2 mg/ml, and treated with 10 uM FP-biotin for 1 hour at room temperature in 500 uL DPBS (1 mg protein per condition). Light and heavy samples were then combined 1:1 (w/w protein), and the total protein was precipitated from the samples by addition of 1 mL MeOH and 250 uL CHCl3, followed by vortexing. The protein was pelleted by centrifugation (1400 x g, 20 minutes, 4 degrees C), the supernatant discarded, and the pellet then washed twice more with 2:1 MeOH/CHCl3 (500 uL, then 250 uL, with the protein pellet resuspended by sonication and pelleted by centrifugation, 16k x g for 10 minutes, following each wash). 1Protein pellets were solubilized first by sonication in 6M urea in aqueous 25 mM ammonium bicarbonate, and then by addition of 140 uL 10% aqueous SDS. Samples were reduced with 10 mM DTT at 65 degrees C for 15 minutes, and then alkylated with 10 mM iodoacetamide for 30 minutes at room temperature in the dark. Samples were added directly to 6 mL DPBS containing 50 uL avidin-agarose, and biotinylated proteins were then enriched from each sample by incubation over the avidin beads for 1.5 hours with agitation at room temperature. The beads were washed once with 1% SDS, then three times with DPBS, and then transferred to screw-cap tubes in 200 uL 2 M urea/25 mM ammonium bicarbonate. Calcium chloride was added to 2 mM final, and on-bead digestion was performed for 12 hours at 37 degrees C with sequencing grade modified trypsin (2 ug; Promega). Beads were then filtered from each sample and the resultant peptide samples were acidified with 16 uL formic acid (5% v/v) and stored at -80 degrees C until analysis.
LC-MS/MS analysis:
Samples were analyzed by multidimensional liquid chromatography tandem mass spectrometry (MudPIT) using an Agilent 1200-series quaternary pump and Thermo Scientific LTQ Orbitrap Velos ion trap mass spectrometer. Peptides were eluted in a 5-step MudPIT experiment using 0%, 25%, 50%, 80%, and 100% salt bumps of 500 mM aqueous ammonium acetate and data were collected in data-dependent acquisition mode with dynamic exclusion turned on (20 s, repeat count of 1). Specifically, one full MS (MS1) scan (400-1800 m/z) was followed by 30 MS2 scans of the most abundant ions. The MS2 spectra data were extracted from the raw file using RAW Xtractor (version 1.9.9.2; publicly available at http://fields.scripps.edu/researchtools.php). MS2 spectra data were searched using the Sequest algorithm against the latest version of the human UNIPROT database concatenated with the reversed database for assessment of false-discovery rates. Sequest searches allowed for static modification of cysteine residues (+57.02146 due to alkylation), methionine oxidation (+15.9949), mass shifts of labeled amino acids (+10.0083 R, +8.0142 K) and no enzyme specificity. The resulting MS2 spectra matches were assembled into protein identifications and filtered using DTASelect (version 2.0.41; publicly available at http://fields.scripps.edu/researchtools.php) using the --trypstat option (applies different statistical models for the analysis of high resolution masses, peptide digestion state, and methionine oxidation state respectively). Ratios of light/heavy (cpd/DMSO) peaks were calculated using in-house software and normalized at the peptide level to the average ratio of all non-serine hydrolase peptides. Reported ratios represent the mean of all unique, quantified peptides per protein and do not include peptides that were >3 standard deviations from the median peptide value. Proteins with less than three peptides per protein ID were not included in the analysis.
The ratio was calculated for all unique peptides:
Ratio = Mean_AUC_light / Mean_AUC_heavy
Where:
AUC_light is the area-under-the-curve for the light peptide pair from cells treated with test compound.
AUC_heavy is the area-under-the-curve for the heavy peptide pair from cells treated with DMSO.
Assay Outcome:
A compound was considered active for a particular target / anti-target with a light / heavy ratio of <= 0.5. A compound was considered inactive for a specified target / anti-target with a light / heavy ratio of > 0.5.
PubChem Activity Outcome:
A compound was considered active if it was active for LYPLA1, LYPLA2, and fewer than two anti-target serine hydrolases.
List of Reagents:
HeLa cells (provided by Assay Provider)
SILAC DMEM Medium (Thermo 89985)
dialyzed FCS (Gemini 100-108)
1x PenStrep Glutamine (CellGro 30-002-CI)
L-Arginine (Sigma A6969)
L-Lysine (Sigma L9037)
(13C[6]15N[4])-L-Arginine (Sigma 608033)
(13C[6]15N[2])-L-Lysine (Sigma 608041)
DPBS (Cellgro 20-031-CV)
FP-biotin (provided by Assay Provider)
PD-10 desalting columns (GE Healthcare 17-0851-01)
SDS (Sigma L6026)
Urea (Fisher U15-3)
DTT (Sigma 43815)
Iodoacetamide (Sigma I1149)
Trypsin (Promega V5111)
streptavidin beads (Pierce 20349)
Fused-silica (Agilent 160-2635-10)
Aqua C18 (Phenomenex 04A-4299)
Acetonitrile (Fisher A955-4)
Millipore-filtered Water
Formic acid (Fluka 06440)
Triton-X100 (Fisher AC21568-0010)
Comment
This assay was performed by the assay provider with powder samples of synthetic test compounds.
Result Definitions
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TIDNameDescriptionPID§Panel TargetsHistogramTypeUnit
OutcomeThe BioAssay activity outcomeOutcome
1LYPLA1: OutcomeOne of Active, Inactive, or Not Tested1acyl-protein thioesterase 1 isoform 1 [Homo sapiens]Outcome
2LYPLA1: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for LYPLA1 as mean for all unique peptides quantified1Floatratio
3LYPLA1: SEM for Inhibition/DMSO ratioCalculated standard error for mean1Float
4LYPLA2: OutcomeOne of Active, Inactive, or Not Tested2acyl-protein thioesterase 2 [Homo sapiens]Outcome
5LYPLA2: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for LYPLA2 as mean for all unique peptides quantified2Floatratio
6LYPLA2: SEM for Inhibition/DMSO ratioCalculated standard error for mean2Float
7ABHD6: OutcomeOne of Active, Inactive, or Not Tested3monoacylglycerol lipase ABHD6 [Homo sapiens]Outcome
8ABHD6: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ABHD6 as mean for all unique peptides quantified3Floatratio
9ABHD6: SEM for Inhibition/DMSO ratioCalculated standard error for mean3Float
10MAGL: OutcomeOne of Active, Inactive, or Not Tested4monoglyceride lipase isoform 1 [Homo sapiens]Outcome
11MAGL: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for MAGL as mean for all unique peptides quantified4Floatratio
12MAGL: SEM for Inhibition/DMSO ratioCalculated standard error for mean4Float
13ABHD12: OutcomeOne of Active, Inactive, or Not Tested5monoacylglycerol lipase ABHD12 isoform a [Homo sapiens]Outcome
14ABHD12: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ABHD12 as mean for all unique peptides quantified5Floatratio
15ABHD12: SEM for Inhibition/DMSO ratioCalculated standard error for mean5Float
16SCPEP1: OutcomeOne of Active, Inactive, or Not Tested6retinoid-inducible serine carboxypeptidase precursor [Homo sapiens]Outcome
17SCPEP1: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for SCPEP1 as mean for all unique peptides quantified6Floatratio
18SCPEP1: SEM for Inhibition/DMSO ratioCalculated standard error for mean6Float
19PRCP: OutcomeOne of Active, Inactive, or Not Tested7RecName: Full=Lysosomal Pro-X carboxypeptidase; AltName: Full=Angiotensinase C; AltName: Full=Lysosomal carboxypeptidase C; AltName: Full=Proline carboxypeptidase; AltName: Full=Prolylcarboxypeptidase; Short=PRCP; Flags: PrecursorOutcome
20PRCP: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PRCP as mean for all unique peptides quantified7Floatratio
21PRCP: SEM for Inhibition/DMSO ratioCalculated standard error for mean7Float
22NCEH1: OutcomeOne of Active, Inactive, or Not Tested8neutral cholesterol ester hydrolase 1 isoform b [Homo sapiens]Outcome
23NCEH1: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for NCEH1 as mean for all unique peptides quantified8Floatratio
24NCEH1: SEM for Inhibition/DMSO ratioCalculated standard error for mean8Float
25FAM108B1: OutcomeOne of Active, Inactive, or Not Tested9alpha/beta hydrolase domain-containing protein 17B isoform 1 precursor [Homo sapiens]Outcome
26FAM108B1: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for FAM108B1 as mean for all unique peptides quantified9Floatratio
27FAM108B1: SEM for Inhibition/DMSO ratioCalculated standard error for mean9Float
28FAP: OutcomeOne of Active, Inactive, or Not Tested10RecName: Full=Seprase; AltName: Full=170 kDa melanoma membrane-bound gelatinase; AltName: Full=Fibroblast activation protein alpha; AltName: Full=Integral membrane serine proteaseOutcome
29FAP: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for FAP as mean for all unique peptides quantified10Floatratio
30FAP: SEM for Inhibition/DMSO ratioCalculated standard error for mean10Float
31CTSA: OutcomeOne of Active, Inactive, or Not Tested11RecName: Full=Lysosomal protective protein; AltName: Full=Carboxypeptidase C; AltName: Full=Carboxypeptidase L; AltName: Full=Cathepsin A; AltName: Full=Protective protein cathepsin A; Short=PPCA; AltName: Full=Protective protein for beta-galactosidase; Contains: RecName: Full=Lysosomal protective protein 32 kDa chain; Contains: RecName: Full=Lysosomal protective protein 20 kDa chain; Flags: PrecursorOutcome
32CTSA: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for CTSA as mean for all unique peptides quantified11Floatratio
33CTSA: SEM for Inhibition/DMSO ratioCalculated standard error for mean11Float
34ESD: OutcomeOne of Active, Inactive, or Not Tested12S-formylglutathione hydrolase [Homo sapiens]Outcome
35ESD: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ESD as mean for all unique peptides quantified12Floatratio
36ESD: SEM for Inhibition/DMSO ratioCalculated standard error for mean12Float
37PNPLA6: OutcomeOne of Active, Inactive, or Not Tested13neuropathy target esterase isoform a [Homo sapiens]Outcome
38PNPLA6: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PNPLA6 as mean for all unique peptides quantified13Floatratio
39PNPLA6: SEM for Inhibition/DMSO ratioCalculated standard error for mean13Float
40PAFAH1B2: OutcomeOne of Active, Inactive, or Not Tested14RecName: Full=Platelet-activating factor acetylhydrolase IB subunit beta; AltName: Full=PAF acetylhydrolase 30 kDa subunit; Short=PAF-AH 30 kDa subunit; AltName: Full=PAF-AH subunit beta; Short=PAFAH subunit betaOutcome
41PAFAH1B2: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PAFAH1B2 as mean for all unique peptides quantified14Floatratio
42PAFAH1B2: SEM for Inhibition/DMSO ratioCalculated standard error for mean14Float
43PNPLA4: OutcomeOne of Active, Inactive, or Not Tested15RecName: Full=Patatin-like phospholipase domain-containing protein 4; AltName: Full=Protein GS2Outcome
44PNPLA4: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PNPLA4 as mean for all unique peptides quantified15Floatratio
45PNPLA4: SEM for Inhibition/DMSO ratioCalculated standard error for mean15Float
46APEH: OutcomeOne of Active, Inactive, or Not Tested16acylamino-acid-releasing enzyme [Homo sapiens]Outcome
47APEH: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for APEH as mean for all unique peptides quantified16Floatratio
48APEH: SEM for Inhibition/DMSO ratioCalculated standard error for mean16Float
49ABHD10: OutcomeOne of Active, Inactive, or Not Tested17mycophenolic acid acyl-glucuronide esterase, mitochondrial isoform 1 precursor [Homo sapiens]Outcome
50ABHD10: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ABHD10 as mean for all unique peptides quantified17Floatratio
51ABHD10: SEM for Inhibition/DMSO ratioCalculated standard error for mean17Float
52ABHD11: OutcomeOne of Active, Inactive, or Not Tested18RecName: Full=Alpha/beta hydrolase domain-containing protein 11; Short=Abhydrolase domain-containing protein 11; AltName: Full=Williams-Beuren syndrome chromosomal region 21 proteinOutcome
53ABHD11: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ABHD11 as mean for all unique peptides quantified18Floatratio
54ABHD11: SEM for Inhibition/DMSO ratioCalculated standard error for mean18Float
55PAFAH1B3: OutcomeOne of Active, Inactive, or Not Tested19RecName: Full=Platelet-activating factor acetylhydrolase IB subunit gamma; AltName: Full=PAF acetylhydrolase 29 kDa subunit; Short=PAF-AH 29 kDa subunit; AltName: Full=PAF-AH subunit gamma; Short=PAFAH subunit gammaOutcome
56PAFAH1B3: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PAFAH1B3 as mean for all unique peptides quantified19Floatratio
57PAFAH1B3: SEM for Inhibition/DMSO ratioCalculated standard error for mean19Float
58PLA2G15: OutcomeOne of Active, Inactive, or Not Tested20RecName: Full=Group XV phospholipase A2; AltName: Full=1-O-acylceramide synthase; Short=ACS; AltName: Full=LCAT-like lysophospholipase; Short=LLPL; AltName: Full=Lysophospholipase 3; AltName: Full=Lysosomal phospholipase A2; Short=LPLA2; Flags: PrecursorOutcome
59PLA2G15: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PLA2G15 as mean for all unique peptides quantified20Floatratio
60PLA2G15: SEM for Inhibition/DMSO ratioCalculated standard error for mean20Float
61PAFAH2: OutcomeOne of Active, Inactive, or Not Tested21RecName: Full=Platelet-activating factor acetylhydrolase 2, cytoplasmic; AltName: Full=Serine-dependent phospholipase A2; Short=SD-PLA2; Short=hSD-PLA2Outcome
62PAFAH2: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PAFAH2 as mean for all unique peptides quantified21Floatratio
63PAFAH2: SEM for Inhibition/DMSO ratioCalculated standard error for mean21Float
64ACOT2: OutcomeOne of Active, Inactive, or Not Tested22RecName: Full=Acyl-coenzyme A thioesterase 2, mitochondrial; Short=Acyl-CoA thioesterase 2; AltName: Full=Acyl-coenzyme A thioester hydrolase 2a; AltName: Full=CTE-Ia; AltName: Full=Long-chain acyl-CoA thioesterase 2; AltName: Full=ZAP128; Flags: PrecursorOutcome
65ACOT2: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for ACOT2 as mean for all unique peptides quantified22Floatratio
66ACOT2: SEM for Inhibition/DMSO ratioCalculated standard error for mean22Float
67DPP8: OutcomeOne of Active, Inactive, or Not Tested23RecName: Full=Dipeptidyl peptidase 8; Short=DP8; AltName: Full=Dipeptidyl peptidase IV-related protein 1; Short=DPRP-1; AltName: Full=Dipeptidyl peptidase VIII; Short=DPP VIII; AltName: Full=Prolyl dipeptidase DPP8Outcome
68DPP8: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for DPP8 as mean for all unique peptides quantified23Floatratio
69DPP8: SEM for Inhibition/DMSO ratioCalculated standard error for mean23Float
70FAM111B: OutcomeOne of Active, Inactive, or Not Tested24RecName: Full=Protein FAM111B; AltName: Full=Cancer-associated nucleoproteinOutcome
71FAM111B: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for FAM111B as mean for all unique peptides quantified24Floatratio
72FAM111B: SEM for Inhibition/DMSO ratioCalculated standard error for mean24Float
73PREPL: OutcomeOne of Active, Inactive, or Not Tested25RecName: Full=Prolyl endopeptidase-like; AltName: Full=Prolylendopeptidase-likeOutcome
74PREPL: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for PREPL as mean for all unique peptides quantified25Floatratio
75PREPL: SEM for Inhibition/DMSO ratioCalculated standard error for mean25Float
76LYPLAL1: OutcomeOne of Active, Inactive, or Not Tested26lysophospholipase-like protein 1 [Homo sapiens]Outcome
77LYPLAL1: Average Inhibition/DMSO ratio (1μM**)Calculated inhibitor-treated/DMSO ratio for LYPLAL1 as mean for all unique peptides quantified26Floatratio
78LYPLAL1: SEM for Inhibition/DMSO ratioCalculated standard error for mean26Float

** Test Concentration. § Panel component ID.
Additional Information
Grant Number: 1 R01 CA132630

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