Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL860280

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

Binding
Displacement of [3H]NECA from human adenosine A2A receptor expressed in CHO cells
27
Total Activities
27
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 Expert

Target

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

Publication

2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
Novellino E, Cosimelli B, Ehlardo M, Greco G, Iadanza M, Lavecchia A, Rimoli MG, Sala A, Da Settimo A, Primofiore G, Da Settimo F, Taliani S, La Motta C, Klotz KN, Tuscano D, Trincavelli ML, Martini C.
J Med Chem (2005) 48 : 8253 -8260
PubMed 16366607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.28 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.80
CHEMBL372580 1 6.48
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.47
CHEMBL200636 1 6.25
CHEMBL198461 1 6.14
CHEMBL198779 1 6.08
CHEMBL198054 1 5.52
CHEMBL198008 1 5.46
CHEMBL198959 1 -
CHEMBL197427 1 -
CHEMBL382935 1 -
CHEMBL445664 1 -
CHEMBL426297 1 -
CHEMBL260311 1 -
CHEMBL198060 1 -
CHEMBL197326 1 -
CHEMBL198460 1 -
CHEMBL197963 1 -
CHEMBL197634 1 -
CHEMBL198441 1 -
CHEMBL197743 1 -
CHEMBL198561 1 -
CHEMBL380770 1 -
CHEMBL197962 1 -
CHEMBL200480 1 -
CHEMBL403521 1 -
CHEMBL198673 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 16.0 nM 7.80
CHEMBL372580 Ki = 329.0 nM 6.48
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 337.0 nM 6.47
CHEMBL200636 Ki = 561.0 nM 6.25
CHEMBL198461 Ki = 720.0 nM 6.14
CHEMBL198779 Ki = 833.0 nM 6.08
CHEMBL198054 Ki = 3000.0 nM 5.52
CHEMBL198008 Ki = 3440.0 nM 5.46
CHEMBL198959 Ki > 10000.0 nM -
CHEMBL197427 Ki > 10000.0 nM -
CHEMBL382935 Ki > 10000.0 nM -
CHEMBL445664 Ki > 10000.0 nM -
CHEMBL426297 Ki > 10000.0 nM -
CHEMBL260311 Ki > 10000.0 nM -
CHEMBL198060 Ki > 10000.0 nM -
CHEMBL197326 Ki > 10000.0 nM -
CHEMBL198460 Ki > 10000.0 nM -
CHEMBL197963 Ki > 10000.0 nM -
CHEMBL197634 Ki > 10000.0 nM -
CHEMBL198441 Ki > 10000.0 nM -
CHEMBL197743 Ki > 10000.0 nM -
CHEMBL198561 Ki > 10000.0 nM -
CHEMBL380770 Ki > 10000.0 nM -
CHEMBL197962 Ki > 10000.0 nM -
CHEMBL200480 Ki > 10000.0 nM -
CHEMBL403521 Ki > 10000.0 nM -
CHEMBL198673 Ki > 10000.0 nM -