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Assay Detail

CHEMBL3090422

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antagonist activity at human adenosine A2B receptor expressed in CHO cells assessed as inhibition of NECA-stimulated adenylyl cyclase activity
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

8-(2-Furyl)adenine derivatives as A₂A adenosine receptor ligands.
Dal Ben D, Buccioni M, Lambertucci C, Thomas A, Klotz KN, Federico S, Cacciari B, Spalluto G, Volpini R.
Eur J Med Chem (2013) 70 : 525 -535
PubMed 24189496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.96 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL506450 1 6.70
CHEMBL3087706 1 6.60
CHEMBL3087707 1 6.46
CHEMBL3087715 1 6.43
CHEMBL3087717 1 6.33
CHEMBL510288 1 6.14
CHEMBL3087716 1 6.11
CHEMBL3087710 1 6.10
CHEMBL468633 1 6.08
CHEMBL3087708 1 5.60
CHEMBL3087712 1 5.56
CHEMBL474058 1 5.55
CHEMBL475455 1 5.29
CHEMBL3087711 1 5.29
CHEMBL3087713 1 5.20
CHEMBL3087714 1 -
CHEMBL3087709 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL506450 Ki = 200.0 nM 6.70
CHEMBL3087706 Ki = 250.0 nM 6.60
CHEMBL3087707 Ki = 350.0 nM 6.46
CHEMBL3087715 Ki = 375.0 nM 6.43
CHEMBL3087717 Ki = 470.0 nM 6.33
CHEMBL510288 Ki = 720.0 nM 6.14
CHEMBL3087716 Ki = 786.0 nM 6.11
CHEMBL3087710 Ki = 792.0 nM 6.10
CHEMBL468633 Ki = 840.0 nM 6.08
CHEMBL3087708 Ki = 2510.0 nM 5.60
CHEMBL3087712 Ki = 2780.0 nM 5.56
CHEMBL474058 Ki = 2800.0 nM 5.55
CHEMBL475455 Ki = 5100.0 nM 5.29
CHEMBL3087711 Ki = 5070.0 nM 5.29
CHEMBL3087713 Ki = 6250.0 nM 5.20
CHEMBL3087714 Ki > 30000.0 nM -
CHEMBL3087709 Ki > 30000.0 nM -