AB680

AB680 : Reversible Competitive Inhibitor of NT5E

Structure

Information

  • NT5E
  • Reversible Competitive Inhibitor
  • 200 nM
  • Reviewer recommended concentration: 0.4–4 nM

In Vitro Validations

Uniprot ID: P21589
Target Class: Other
Target SubClass: Membrane Protein
Potency: Ki, IC50
Potency Value: 5 pM, 43 pM
Potency Assay: AMP-Glo assay, Enzymatic reaction
PDB ID for probe-target interaction (3D structure): 6Z9D
Structure-activity relationship: yes
Target aliases:
5'-nucleotidase, NTE, NT5, NT5E, 5NTD_HUMAN, 5'-NT ...

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:
No off-target activity against the ecto-nucleotidases NTPDase-1 (CD39), -2, -3, and -8 up to 10 µM
Potency assay, off target (cells): CEREP
Probe Selectivity in Cell:
Screened against 60 targets in a wide ligand profile screen (CEREP) with no off-target activity observed up to 10 µM
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SERP ratings and comments


SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 10 Aug 2020 )

SERP Ratings

In Cell Rating
In Model Organisms

SERP Comments:

High levels of adenosine with the tumor microenvironment inhibit the activation of T cells and NK cells thereby suppressing the immune function. CD73 is ecto-nucleotidase which catalyses the conversion of adenosine monophosphate (AMP) to adenosine.  AB680 is a highly selective inhibitor of the ecto-nucleotidase CD73 however it is a triply charged molecule that requires iv delivery.  AB680 demonstrates excellent potency (Ki =5 pM). Furthermore, it shows a desirable slow clearance in several animal models including mouse, rat, dog, and monkey.

(last updated: 5 Sept 2020 )