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Assay Detail

CHEMBL4139731

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

Functional
Antagonist activity at Adenosine receptor subtype 2B in human RBC assessed as change in erythrocyte morphology incubated for 3 hrs with occasional gentle stirring for every 30 min measured for every 12 hrs by microscopic analysis
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Nanomolar anti-sickling compounds identified by ligand-based pharmacophore approach.
Paz OS, de Jesus Pinheiro M, do Espirito Santo RF, Villarreal CF, Castilho MS.
Eur J Med Chem (2017) 136 : 487 -496
PubMed 28528302 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 7.55 7.77
Ki 5 8.78 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL513681 1 9.10
CHEMBL4160732 1 8.98
CHEMBL4175851 1 8.88
CHEMBL4175454 1 8.74
CHEMBL404168 1 8.22
CHEMBL4168653 1 7.77
CHEMBL4165135 1 7.63
CHEMBL273807 1 7.63
CHEMBL4167064 1 7.46
CHEMBL4163380 1 7.46
CHEMBL4173768 1 7.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL513681 Ki = 0.7943 nM 9.10
CHEMBL4160732 Ki = 1.047 nM 8.98
CHEMBL4175851 Ki = 1.318 nM 8.88
CHEMBL4175454 Ki = 1.82 nM 8.74
CHEMBL404168 Ki = 6.026 nM 8.22
CHEMBL4168653 EC50 = 16.98 nM 7.77
CHEMBL4165135 EC50 = 23.44 nM 7.63
CHEMBL273807 EC50 = 23.44 nM 7.63
CHEMBL4167064 EC50 = 34.67 nM 7.46
CHEMBL4163380 EC50 = 34.67 nM 7.46
CHEMBL4173768 EC50 = 46.77 nM 7.33