Assay Detail

CHEMBL3995072

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Binding

Displacement of [125I]ABOPX from human adenosine receptor A2b expressed in HEK293 cell membranes after 3 hrs by fluorescence assay

ChEMBL ↗

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Target

Adenosine receptor A2b (CHEMBL255) ↗

Open DB target context

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Adenosine receptor A2b (CHEMBL255) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Adenosine receptor A2b

CHEMBL255

Anchored from Assay target.

Protein identity Adenosine receptor A2b

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
Cell Type	HEK293
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

Adenosine receptor A2b (CHEMBL255) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

Publication

A2B adenosine receptor antagonists: Design, synthesis and biological evaluation of novel xanthine derivatives.

Basu S, Barawkar DA, Ramdas V, Waman Y, Patel M, Panmand A, Kumar S, Thorat S, Bonagiri R, Jadhav D, Mukhopadhyay P, Prasad V, Reddy BS, Goswami A, Chaturvedi S, Menon S, Quraishi A, Ghosh I, Dusange S, Paliwal S, Kulkarni A, Karande V, Thakre R, Bedse G, Rouduri S, Gundu J, Palle VP, Chugh A, Mookhtiar KA.
Eur J Med Chem (2017) 127 : 986 -996
PubMed 27842891 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	3	6.36	8.70

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL273807	—	—	1	8.70
CHEMBL279898	ENPROFYLLINE	2.0	1	5.33
CHEMBL1355736	THEOPHYLLINE	4.0	1	5.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL273807	—	Ki	=	2.0	nM	8.70
CHEMBL279898	ENPROFYLLINE	Ki	=	4700.0	nM	5.33
CHEMBL1355736	THEOPHYLLINE	Ki	=	9000.0	nM	5.05