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Assay Detail

CHEMBL2438814

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

Binding
Displacement of [125I]AB-MECA from human adenosine A3 receptor expressed in CHO cell membrane after 90 mins
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulation of A2B adenosine receptor by 1-Benzyl-3-ketoindole derivatives.
Taliani S, Trincavelli ML, Cosimelli B, Laneri S, Severi E, Barresi E, Pugliesi I, Daniele S, Giacomelli C, Greco G, Novellino E, Martini C, Da Settimo F.
Eur J Med Chem (2013) 69 : 331 -337
PubMed 24077183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.40 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431733 NAMODENOSON 3.0 1 9.66
CHEMBL464859 NECA 1 7.14
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 -
CHEMBL2435540 1 -
CHEMBL2435539 1 -
CHEMBL2435538 1 -
CHEMBL2435537 1 -
CHEMBL2435536 1 -
CHEMBL2435535 1 -
CHEMBL2435534 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431733 NAMODENOSON Ki = 0.22 nM 9.66
CHEMBL464859 NECA Ki = 73.0 nM 7.14
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki > 1000.0 nM -
CHEMBL2435540 Ki > 1000.0 nM -
CHEMBL2435539 Ki > 1000.0 nM -
CHEMBL2435538 Ki > 1000.0 nM -
CHEMBL2435537 Ki > 1000.0 nM -
CHEMBL2435536 Ki > 1000.0 nM -
CHEMBL2435535 Ki > 1000.0 nM -
CHEMBL2435534 Ki > 1000.0 nM -