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Assay Detail

CHEMBL1034142

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

Functional
Antagonist activity at adenosine A2B receptor in Wistar-Kyoto rat distal colon assessed as inhibition of bethanecol-induced contraction
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Colon
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2b (CHEMBL2592)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,3-Dialkyl-8-(hetero)aryl-9-OH-9-deazaxanthines as potent A2B adenosine receptor antagonists: design, synthesis, structure-affinity and structure-selectivity relationships.
Stefanachi A, Nicolotti O, Leonetti F, Cellamare S, Campagna F, Loza MI, Brea JM, Mazza F, Gavuzzo E, Carotti A.
Bioorg Med Chem (2008) 16 : 9780 -9789
PubMed 18938084 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 1 9.33 9.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL456125 1 9.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL456125 Kd = 0.4677 nM 9.33