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Assay Detail

CHEMBL935759

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

Binding
Displacement of radioligand from human adenosine A2A receptor expressed in HEK293 cells
10
Total Activities
10
Compounds Tested
1
Activity Types
0
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 A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of (N)-methanocarba adenosine 5'-uronamides as species-independent A3 receptor-selective agonists.
Melman A, Gao ZG, Kumar D, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.
Bioorg Med Chem Lett (2008) 18 : 2813 -2819
PubMed 18424135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.67 7.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL119709 IB-MECA 1 7.03
CHEMBL27376 1 6.11
CHEMBL2368455 1 5.89
CHEMBL2368366 1 5.80
CHEMBL175543 1 5.64
CHEMBL2112163 1 5.32
CHEMBL431733 NAMODENOSON 3.0 1 5.27
CHEMBL2112161 1 5.00
CHEMBL2112157 1 5.00
CHEMBL2368367 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL119709 IB-MECA Ki = 93.1 nM 7.03
CHEMBL27376 Ki = 784.0 nM 6.11
CHEMBL2368455 Ki = 1300.0 nM 5.89
CHEMBL2368366 Ki = 1600.0 nM 5.80
CHEMBL175543 Ki = 2300.0 nM 5.64
CHEMBL2112163 Ki = 4800.0 nM 5.32
CHEMBL431733 NAMODENOSON Ki = 5400.0 nM 5.27
CHEMBL2112161 Ki = 10000.0 nM 5.00
CHEMBL2112157 Ki = 10000.0 nM 5.00
CHEMBL2368367 Ki > 10000.0 nM -