#243
Identification of ROP/GAP interaction inhibitors

Yong-Jik Lee (P.I.: Natasha Raikhel and Zhenbiao Yang )

Augusta Jamin

SCREEN DETAILS: 90 ul of early logarithmic yeast culture in selective SD media (SD-Leu-Trp-His+30 mM 3AT) was dispensed to 96-well test plates and 0.9 ul of chemical compounds were added to each wells to 50 - 100 uM final concentration. After 24 h of incubation, growth in each well was determined by absorbance with a plate reader. Chemical compounds that produced a clear growth reduction were scored as "hits". Using this assay, we screened library of 22,000 chemical compounds (Microsource Spectrum (SP) (2 000), Chembridge Nova Core Library (NC) (10,000), Sigma TimTec Myria Screen (MS) (10,000)). SUMMARY STATISTICS: The screen of 22,000 chemical compounds yielded a total of 125 (0.6 %) reproducible inhibitors of ROP/GAP interaction with low toxicity. 18 of 125 chemical compounds induced obvious morphological changes in pollen tubes, including decrease in the tube length and tip swelling.

NSF: 2010-0520325

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  • Forward Screen yes
  • Target Pathway or Process: ROP2 and Ph-GAP3 interaction
  • Organism Saccharomyces cerevisae
  • Genotype: DBD-Ph-GAP3 and AD-CA-rop2-CS
  • Tissue and/or Cell Type(s) yeast (MaV203)
  • Sample Age: 24 h
  • Growth Conditions yeast cells exposed to drugs for 24 h at 30C in selective media (-WLH+30 mM 3AT)

In total, 18 compounds from 2 libraries are annotated. Out of these, 18 have a score of 1 or higher, and 0 are annotated as inactive.


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Screen-level Files

Forward yeast two-hybrid screen

Screening of ROP/GAP interaction inhibitor

#15420
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Compound Files

LibraryMicrosource Spectrum
ID01500505
NamePROCHLORPERAZINE-EDISYLATE
FormulaC22H30ClN3O6S3
Molecular Weight 564.138
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117025
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 40 uM

Pollen tube phenotype

#15421
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LibraryMicrosource Spectrum
ID01500575
NameTHIORIDAZINE-HYDROCHLORIDE
FormulaC21H27ClN2S2
Molecular Weight 407.036
Use in structure search

Tip growth Phenotype
Assay 1: 3

#117034
Assay 1: Pollen tube phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 30 uM

Pollen tube phenotype

#15422
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Root hair phenotype (Wild type)

#15423
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Root hair phenotype (ROP2 OX)

#15424
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LibraryMicrosource Spectrum
ID01503637
NameMETHIOTHEPIN-MALEATE
FormulaC24H28N2O4S2
Molecular Weight 472.620
Use in structure search

Tip growth phenotype
Assay 1: 3

#117030
Assay 1: Pollen tube phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 30 uM

Pollen tube phenotype

#15425
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Root hair phenotype (Wild type)

#15426
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Root hair phenotype (ROP2 OX)

#15427
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LibraryMicrosource Spectrum
ID01503118
NameTRIFLUPROMAZINE-HYDROCHLORIDE
FormulaC19H23F3N2S
Molecular Weight 368.460
Use in structure search

Tip growth phenotype
Assay 1: 3

#117026
Assay 1: Pollen tube phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 70 uM

Pollen tube phenotype

#15428
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Root hair phenotype (Wild type)

#15429
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Root hair phenotype (ROP2 OX)

#15430
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LibraryMicrosource Spectrum
ID01500184
NameCHLORPROMAZINE
FormulaC17H19ClN2S
Molecular Weight 318.864
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117033
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 70 uM

Pollen tube phenotype

#15431
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LibraryMicrosource Spectrum
ID01503203
NameCHLORPROTHIXENE-HYDROCHLORIDE
FormulaC18H19Cl2NS
Molecular Weight 352.321
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117024
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 80 uM

Pollen tube phenotype

#15433
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LibraryChemBridge NovaCore
ID95899180
Name
FormulaC21H22N2O2
Molecular Weight 334.412
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117031
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 30 uM

Pollen tube phenotype

#15435
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LibraryChemBridge NovaCore
ID70126345
Name
FormulaC23H27FN4O
Molecular Weight 394.485
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117036
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 25 uM

Pollen tube phenotype

#15437
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LibraryChemBridge NovaCore
ID46057927
Name
FormulaC24H26FN5
Molecular Weight 403.495
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117020
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 25 uM

Pollen tube phenotype

#15438
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LibraryChemBridge NovaCore
ID10966731
Name
FormulaC24H26FN5
Molecular Weight 403.495
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117032
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 25 uM

Pollen tube phenotype

#15439
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LibraryChemBridge NovaCore
ID13677592
Name
FormulaC24H25F3N4O
Molecular Weight 442.477
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117028
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 23 uM

Pollen tube phenotype

#15440
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LibraryChemBridge NovaCore
ID63857884
Name
FormulaC23H24F3NO2
Molecular Weight 403.437
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117022
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 25 uM

Pollen tube phenotype

#15441
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LibraryChemBridge NovaCore
ID21092972
Name
FormulaC22H23ClN4O
Molecular Weight 394.897
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117027
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 25 uM

Pollen tube phenotype

#15442
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LibraryChemBridge NovaCore
ID87448421
Name
FormulaC27H33N3O
Molecular Weight 415.570
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117029
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 24 uM

Pollen tube phenotype

#15443
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LibraryChemBridge NovaCore
ID23341433
Name
FormulaC22H23F6NO
Molecular Weight 431.415
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117023
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 23 uM

Pollen tube phenotype

#15444
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LibraryChemBridge NovaCore
ID94790606
Name
FormulaC27H27N3O2
Molecular Weight 425.522
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117021
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 24 uM

Pollen tube phenotype

#15445
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LibraryChemBridge NovaCore
ID50770662
Name
FormulaC26H27N3O2
Molecular Weight 413.512
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117035
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 24 uM

Pollen tube phenotype

#15446
Download
LibraryChemBridge NovaCore
ID55510880
Name
FormulaC24H23FN4
Molecular Weight 386.465
Use in structure search

Pollen tube phenotype
Assay 1: 3

#117037
Assay 1: visual phenotype
  • Score 3: active in all previous and follow-up screens
  • Concentration 26 uM

Pollen tube phenotype

#15518
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