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Assay Detail

CHEMBL2034747

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

Binding
Displacement of [3H]DPCPX from human A1 adenosine receptor expressed in CHO cell membrane
17
Total Activities
17
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 A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.
Taliani S, Pugliesi I, Barresi E, Simorini F, Salerno S, La Motta C, Marini AM, Cosimelli B, Cosconati S, Di Maro S, Marinelli L, Daniele S, Trincavelli ML, Greco G, Novellino E, Martini C, Da Settimo F.
J Med Chem (2012) 55 : 1490 -1499
PubMed 22257095 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.03 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.30
CHEMBL464859 NECA 1 7.85
CHEMBL7608 1 7.60
CHEMBL7909 1 7.21
CHEMBL112756 1 7.08
CHEMBL7098 1 6.68
CHEMBL326752 1 6.52
CHEMBL7113 1 6.14
CHEMBL431733 NAMODENOSON 3.0 1 6.05
CHEMBL2030703 1 5.87
CHEMBL113518 1 -
CHEMBL2030704 1 -
CHEMBL324100 1 -
CHEMBL2030705 1 -
CHEMBL2030706 1 -
CHEMBL2030707 1 -
CHEMBL2030708 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.5 nM 9.30
CHEMBL464859 NECA Ki = 14.0 nM 7.85
CHEMBL7608 Ki = 25.0 nM 7.60
CHEMBL7909 Ki = 62.0 nM 7.21
CHEMBL112756 Ki = 83.0 nM 7.08
CHEMBL7098 Ki = 211.0 nM 6.68
CHEMBL326752 Ki = 299.0 nM 6.52
CHEMBL7113 Ki = 728.0 nM 6.14
CHEMBL431733 NAMODENOSON Ki = 890.0 nM 6.05
CHEMBL2030703 Ki = 1357.0 nM 5.87
CHEMBL113518 Ki > 10000.0 nM -
CHEMBL2030704 Ki > 10000.0 nM -
CHEMBL324100 Ki > 10000.0 nM -
CHEMBL2030705 Ki > 10000.0 nM -
CHEMBL2030706 Ki > 10000.0 nM -
CHEMBL2030707 Ki > 10000.0 nM -
CHEMBL2030708 Ki > 10000.0 nM -