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

CHEMBL919033

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

Binding
Displacement of [3h]DPCPX from adenosine A receptor in rat cerebral cortex membrane
ChEMBL ↗
79
Total Activities
79
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Novel bicyclic piperazine derivatives of triazolotriazine and triazolopyrimidines as highly potent and selective adenosine A2A receptor antagonists.
Peng H, Kumaravel G, Yao G, Sha L, Wang J, Van Vlijmen H, Bohnert T, Huang C, Vu CB, Ensinger CL, Chang H, Engber TM, Whalley ET, Petter RC.
J Med Chem (2004) 47 : 6218 -6229
PubMed 15566292 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 79 5.84 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222731 — — 1 6.68
CHEMBL17127 SCH-58261 — 1 6.41
CHEMBL173672 — — 1 6.37
CHEMBL376712 — — 1 6.18
CHEMBL222783 — — 1 6.15
CHEMBL439141 — — 1 6.07
CHEMBL221772 — — 1 6.02
CHEMBL189192 — — 1 5.96
CHEMBL426738 — — 1 5.96
CHEMBL222097 — — 1 5.96
CHEMBL2096850 — — 1 5.92
CHEMBL373560 — — 1 5.92
CHEMBL221615 — — 1 5.89
CHEMBL222784 — — 1 5.85
CHEMBL222145 — — 1 5.82
CHEMBL222868 — — 1 5.80
CHEMBL373700 — — 1 5.48
CHEMBL222590 — — 1 5.46
CHEMBL374881 — — 1 5.46
CHEMBL222589 — — 1 5.46
CHEMBL221573 — — 1 5.22
CHEMBL222266 — — 1 5.21
CHEMBL222478 — — 1 5.11
CHEMBL387328 — — 1 -
CHEMBL426906 — — 1 -
CHEMBL376436 — — 1 -
CHEMBL386501 — — 1 -
CHEMBL375772 — — 1 -
CHEMBL222641 — — 1 -
CHEMBL387319 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222731 — Ki = 210.0 nM 6.68
CHEMBL17127 SCH-58261 Ki = 390.0 nM 6.41
CHEMBL173672 — Ki = 427.0 nM 6.37
CHEMBL376712 — Ki = 660.0 nM 6.18
CHEMBL222783 — Ki = 710.0 nM 6.15
CHEMBL439141 — Ki = 860.0 nM 6.07
CHEMBL221772 — Ki = 960.0 nM 6.02
CHEMBL222097 — Ki = 1100.0 nM 5.96
CHEMBL426738 — Ki = 1100.0 nM 5.96
CHEMBL189192 — Ki = 1100.0 nM 5.96
CHEMBL2096850 — Ki = 1200.0 nM 5.92
CHEMBL373560 — Ki = 1200.0 nM 5.92
CHEMBL221615 — Ki = 1300.0 nM 5.89
CHEMBL222784 — Ki = 1400.0 nM 5.85
CHEMBL222145 — Ki = 1500.0 nM 5.82
CHEMBL222868 — Ki = 1600.0 nM 5.80
CHEMBL373700 — Ki = 3300.0 nM 5.48
CHEMBL374881 — Ki = 3500.0 nM 5.46
CHEMBL222589 — Ki = 3500.0 nM 5.46
CHEMBL222590 — Ki = 3500.0 nM 5.46
CHEMBL221573 — Ki = 6000.0 nM 5.22
CHEMBL222266 — Ki = 6100.0 nM 5.21
CHEMBL222478 — Ki = 7800.0 nM 5.11
CHEMBL374800 — Ki > 500.0 nM -
CHEMBL223035 — Ki > 1000.0 nM -
CHEMBL223887 — Ki > 500.0 nM -
CHEMBL223883 — Ki > 1000.0 nM -
CHEMBL221352 — Ki > 500.0 nM -
CHEMBL222374 — Ki > 500.0 nM -
CHEMBL2096851 — Ki > 500.0 nM -
CHEMBL222901 — Ki > 500.0 nM -
CHEMBL221947 — Ki > 1000.0 nM -
CHEMBL223976 — Ki > 1000.0 nM -
CHEMBL375846 — Ki > 500.0 nM -
CHEMBL222855 — Ki > 500.0 nM -
CHEMBL425349 — Ki - — -
CHEMBL225462 — Ki > 500.0 nM -
CHEMBL223419 — Ki > 500.0 nM -
CHEMBL387352 — Ki > 500.0 nM -
CHEMBL222131 — Ki > 500.0 nM -
CHEMBL375436 — Ki > 500.0 nM -
CHEMBL222921 — Ki > 500.0 nM -
CHEMBL222481 — Ki > 1000.0 nM -
CHEMBL387319 — Ki > 500.0 nM -
CHEMBL222641 — Ki > 500.0 nM -
CHEMBL375772 — Ki > 500.0 nM -
CHEMBL386501 — Ki > 1000.0 nM -
CHEMBL376436 — Ki > 1000.0 nM -
CHEMBL426906 — Ki > 500.0 nM -
CHEMBL387328 — Ki > 500.0 nM -