hit-to-lead discovery

UbiQ can assist your lead discovery in the UPS with our wide range of activity assay reagents. Perfect tools for high throughput compound screening;


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UbiQ-Assay, DUB activity assay reagents, proved effective in multiple industrial scale HTS campaigns. They are available in various flavors for a wide range of assay read outs, e.g. fluorogenic substrates for fluorescence intensity read-out, substrates for FP assays, or as highly specialized context specific FP reagents (our class II FP reagents). All of them targeting DUBs & Ub-like proteases. 

 

applications 

  • compound library screening
  • activity assays

 

targets

  • DUBs and Ubl proteases 

 

experience

  • substrate supply for an undisclosed number of large library screens by our industrial partners
  • development of >10 highly specialized context specific custom assay reagents
  • demonstrated performance at independent European screening centers – Pivot Park Screening Center and European ScreeningPort (table 1)
  • five DUB screening campaigns (>1.7 million small molecules) 
table 1: UbiQ’s screening reagents used in HTS campaigns*

screen#

primary screen +

dose-response

orthogonal
assay for hit validation

small-molecule

library size

Z'-value

validated hits

hit selected for

dose-response

DUB-001

UbiQ-012 (Ub FP)

UbiQ-002 (Ub-Rh110)

225K

0.7 - 0.8

293 (0.14%)

99 (0.05%)

310K

0.7 - 0.8

664 (0.21%)

182 (0.06%)

DUB-002

UbiQ-012 (Ub FP)

UbiQ-002 (Ub-Rh110)

310K

0.7 - 0.8

516 (0.17%)

152 (0.05%)

DUB-003

Ub-like FP reagent

Ub-like (AMC)

310K

0.7 - 0.8

1009 (0.33%)

170 (0.05%)

DUB-004

Ub-like FP

Ub-like (AMC)

310K

0.7 - 0.8

ongoing

ongoing

DUB-005

Ub FP class II reagent

UbiQ-002 (Ub-Rh110)

310K

0.75 - 0.8

ongoing

ongoing

 

*Completed and ongoing HTS programs in which UbiQ’s FP assay reagents were used for the primary screen (single point at 10 μM), and dose-response experiments of validated hits. All assays showed excellent Z' values (>0.7). After confirmation of the hits with the FP substrate, an orthogonal Ub-Rh110Gly (UbiQ-002) or Ub-like AMC assay was used for validation; the number of hits identified at this stage varied from 0.33−0.14% of the total library. A subset of compounds (in general 0.05% of the total library) is then selected for IC50 determination using the FP assay reagent (10 concentration steps from 0.15 nM−5 μM).

 

> See UbiQ-Assay fact sheets for more information, available options and references. Also available in Japanese