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Assay Detail

CHEMBL642332

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Binding
Binding affinity against adenosine A2 receptor in human striatal membranes using [3H]CGS-21680 as radioligand
ChEMBL ↗
53
Total Activities
53
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Study on affinity profile toward native human and bovine adenosine receptors of a series of 1,8-naphthyridine derivatives.
Ferrarini PL, Betti L, Cavallini T, Giannaccini G, Lucacchini A, Manera C, Martinelli A, Ortore G, Saccomanni G, Tuccinardi T.
J Med Chem (2004) 47 : 3019 -3031
PubMed 15163184 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 53 6.11 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL17127 SCH-58261 — 1 8.49
CHEMBL95384 — — 1 7.40
CHEMBL97687 — — 1 7.00
CHEMBL104999 — — 1 6.96
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] — 1 6.84
CHEMBL105000 — — 1 6.68
CHEMBL97337 — — 1 6.68
CHEMBL329293 — — 1 6.64
CHEMBL313864 — — 1 6.36
CHEMBL97760 — — 1 6.35
CHEMBL329294 — — 1 6.31
CHEMBL97624 — — 1 6.31
CHEMBL97549 — — 1 6.26
CHEMBL316630 — — 1 6.19
CHEMBL103559 — — 1 6.01
CHEMBL103150 — — 1 6.00
CHEMBL323303 — — 1 5.89
CHEMBL102429 — — 1 5.89
CHEMBL102753 — — 1 5.85
CHEMBL97895 — — 1 5.82
CHEMBL104998 — — 1 5.80
CHEMBL418797 — — 1 5.77
CHEMBL103553 — — 1 5.75
CHEMBL97037 — — 1 5.70
CHEMBL97757 — — 1 5.57
CHEMBL321769 — — 1 5.47
CHEMBL323288 — — 1 5.42
CHEMBL94538 — — 1 5.39
CHEMBL97896 — — 1 5.32
CHEMBL328214 — — 1 5.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL17127 SCH-58261 Ki = 3.25 nM 8.49
CHEMBL95384 — Ki = 40.0 nM 7.40
CHEMBL97687 — Ki = 100.0 nM 7.00
CHEMBL104999 — Ki = 110.0 nM 6.96
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 144.0 nM 6.84
CHEMBL105000 — Ki = 210.0 nM 6.68
CHEMBL97337 — Ki = 210.0 nM 6.68
CHEMBL329293 — Ki = 230.0 nM 6.64
CHEMBL313864 — Ki = 440.0 nM 6.36
CHEMBL97760 — Ki = 450.0 nM 6.35
CHEMBL329294 — Ki = 490.0 nM 6.31
CHEMBL97624 — Ki = 490.0 nM 6.31
CHEMBL97549 — Ki = 550.0 nM 6.26
CHEMBL316630 — Ki = 640.0 nM 6.19
CHEMBL103559 — Ki = 970.0 nM 6.01
CHEMBL103150 — Ki = 1000.0 nM 6.00
CHEMBL323303 — Ki = 1300.0 nM 5.89
CHEMBL102429 — Ki = 1300.0 nM 5.89
CHEMBL102753 — Ki = 1400.0 nM 5.85
CHEMBL97895 — Ki = 1500.0 nM 5.82
CHEMBL104998 — Ki = 1600.0 nM 5.80
CHEMBL418797 — Ki = 1700.0 nM 5.77
CHEMBL103553 — Ki = 1800.0 nM 5.75
CHEMBL97037 — Ki = 2000.0 nM 5.70
CHEMBL97757 — Ki = 2700.0 nM 5.57
CHEMBL321769 — Ki = 3400.0 nM 5.47
CHEMBL323288 — Ki = 3800.0 nM 5.42
CHEMBL94538 — Ki = 4100.0 nM 5.39
CHEMBL97896 — Ki = 4800.0 nM 5.32
CHEMBL328214 — Ki = 6500.0 nM 5.19
CHEMBL321330 — Ki = 7500.0 nM 5.12
CHEMBL102430 — Ki = 9000.0 nM 5.05
CHEMBL102491 — Ki > 10000.0 nM -
CHEMBL102017 — Ki > 10000.0 nM -
CHEMBL328334 — Ki > 10000.0 nM -
CHEMBL102974 — Ki > 10000.0 nM -
CHEMBL97778 — Ki > 10000.0 nM -
CHEMBL102126 — Ki > 10000.0 nM -
CHEMBL102178 — Ki > 10000.0 nM -
CHEMBL103278 — Ki > 10000.0 nM -
CHEMBL441815 — Ki > 10000.0 nM -
CHEMBL317411 — Ki > 10000.0 nM -
CHEMBL97665 — Ki > 10000.0 nM -
CHEMBL100121 — Ki > 10000.0 nM -
CHEMBL319580 — Ki > 10000.0 nM -
CHEMBL97904 — Ki > 10000.0 nM -
CHEMBL97344 — Ki > 10000.0 nM -
CHEMBL415697 — Ki > 10000.0 nM -
CHEMBL96617 — Ki > 10000.0 nM -
CHEMBL103588 — Ki > 10000.0 nM -