Assay Detail

CHEMBL4668735

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Binding

Inhibition of human CD73 using AMP as substrate by Malachite green phosphate reagent-based assay

ChEMBL ↗

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Target

5'-nucleotidase (CHEMBL5957) ↗

Open DB target context

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5'-nucleotidase (CHEMBL5957) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target 5'-nucleotidase

CHEMBL5957

Anchored from Assay target.

Protein identity 5'-nucleotidase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

5'-nucleotidase (CHEMBL5957) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

Discovery of AB680: A Potent and Selective Inhibitor of CD73.

Lawson KV,Kalisiak J,Lindsey EA,Newcomb ET,Leleti MR,Debien L,Rosen BR,Miles DH,Sharif EU,Jeffrey JL,Tan JBL,Chen A,Zhao S,Xu G,Fu L,Jin L,Park TW,Berry W,Moschütz S,Scaletti E,Sträter N,Walker NP,Young SW,Walters MJ,Schindler U,Powers JP
J Med Chem (2020) 63 : 11448 -11468
PubMed 32614585 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	1	6.73	6.73
Ki	1	7.05	7.05

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL583969	PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER	—	2	7.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL583969	PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER	Ki	=	88.4	nM	7.05
CHEMBL583969	PHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER	IC50	=	187.0	nM	6.73