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Assay Detail

CHEMBL901887

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

Binding
Displacement of [3H]ZM-241385 from adenosine A2A receptor expressed in PC12 cell membrane
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PC-12
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of adenosines with heterocyclic N6-substituents.
Ashton TD, Aumann KM, Baker SP, Schiesser CH, Scammells PJ.
Bioorg Med Chem Lett (2007) 17 : 6779 -6784
PubMed 17967536 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.36 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 6.96
CHEMBL240065 1 5.26
CHEMBL391031 1 5.11
CHEMBL391029 1 5.01
CHEMBL240279 1 4.46
CHEMBL392149 TECADENOSON 2.0 1 -
CHEMBL430374 1 -
CHEMBL392720 1 -
CHEMBL240487 1 -
CHEMBL240278 1 -
CHEMBL391030 1 -
CHEMBL240277 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 110.0 nM 6.96
CHEMBL240065 Ki = 5500.0 nM 5.26
CHEMBL391031 Ki = 7800.0 nM 5.11
CHEMBL391029 Ki = 9700.0 nM 5.01
CHEMBL240279 Ki = 34700.0 nM 4.46
CHEMBL392149 TECADENOSON Ki > 100000.0 nM -
CHEMBL430374 Ki > 100000.0 nM -
CHEMBL392720 Ki > 100000.0 nM -
CHEMBL240487 Ki > 100000.0 nM -
CHEMBL240278 Ki > 100000.0 nM -
CHEMBL391030 Ki > 100000.0 nM -
CHEMBL240277 Ki > 100000.0 nM -