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Assay Detail

CHEMBL3096080

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

Binding
Displacement of [3H]MSX-2 from adenosine A2A receptor in rat brain striatum
ChEMBL ↗
59
Total Activities
59
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2a (CHEMBL302) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

1,3-Dialkyl-substituted tetrahydropyrimido[1,2-f]purine-2,4-diones as multiple target drugs for the potential treatment of neurodegenerative diseases.
Koch P, Akkari R, Brunschweiger A, Borrmann T, Schlenk M, Küppers P, Köse M, Radjainia H, Hockemeyer J, Drabczyńska A, Kieć-Kononowicz K, Müller CE.
Bioorg Med Chem (2013) 21 : 7435 -7452
PubMed 24139167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 59 5.85 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL413079 — — 1 8.10
CHEMBL3093328 — — 1 6.83
CHEMBL3093238 — — 1 6.78
CHEMBL3093315 — — 1 6.59
CHEMBL3093317 — — 1 6.56
CHEMBL3093318 — — 1 6.54
CHEMBL3093321 — — 1 6.44
CHEMBL3091482 — — 1 6.42
CHEMBL3093323 — — 1 6.30
CHEMBL239230 — — 1 6.29
CHEMBL3093310 — — 1 6.27
CHEMBL3093227 — — 1 6.21
CHEMBL3093311 — — 1 6.19
CHEMBL3093312 — — 1 6.16
CHEMBL3093320 — — 1 6.15
CHEMBL3093319 — — 1 6.14
CHEMBL3093239 — — 1 6.11
CHEMBL241618 — — 1 6.10
CHEMBL3093316 — — 1 6.08
CHEMBL3093326 — — 1 6.05
CHEMBL3093331 — — 1 6.03
CHEMBL3093233 — — 1 5.92
CHEMBL3093322 — — 1 5.84
CHEMBL3093333 — — 1 5.83
CHEMBL3093237 — — 1 5.79
CHEMBL3093230 — — 1 5.77
CHEMBL3093225 — — 1 5.74
CHEMBL3093228 — — 1 5.73
CHEMBL3093325 — — 1 5.73
CHEMBL3093329 — — 1 5.71

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL413079 — Ki = 8.04 nM 8.10
CHEMBL3093328 — Ki = 147.0 nM 6.83
CHEMBL3093238 — Ki = 166.0 nM 6.78
CHEMBL3093315 — Ki = 259.0 nM 6.59
CHEMBL3093317 — Ki = 276.0 nM 6.56
CHEMBL3093318 — Ki = 288.0 nM 6.54
CHEMBL3093321 — Ki = 361.0 nM 6.44
CHEMBL3091482 — Ki = 380.0 nM 6.42
CHEMBL3093323 — Ki = 498.0 nM 6.30
CHEMBL239230 — Ki = 515.0 nM 6.29
CHEMBL3093310 — Ki = 533.0 nM 6.27
CHEMBL3093227 — Ki = 624.0 nM 6.21
CHEMBL3093311 — Ki = 641.0 nM 6.19
CHEMBL3093312 — Ki = 696.0 nM 6.16
CHEMBL3093320 — Ki = 710.0 nM 6.15
CHEMBL3093319 — Ki = 723.0 nM 6.14
CHEMBL3093239 — Ki = 780.0 nM 6.11
CHEMBL241618 — Ki = 802.0 nM 6.10
CHEMBL3093316 — Ki = 827.0 nM 6.08
CHEMBL3093326 — Ki = 900.0 nM 6.05
CHEMBL3093331 — Ki = 932.0 nM 6.03
CHEMBL3093233 — Ki = 1210.0 nM 5.92
CHEMBL3093322 — Ki = 1430.0 nM 5.84
CHEMBL3093333 — Ki = 1480.0 nM 5.83
CHEMBL3093237 — Ki = 1640.0 nM 5.79
CHEMBL3093230 — Ki = 1700.0 nM 5.77
CHEMBL3093225 — Ki = 1830.0 nM 5.74
CHEMBL3093228 — Ki = 1880.0 nM 5.73
CHEMBL3093325 — Ki = 1880.0 nM 5.73
CHEMBL3093329 — Ki = 1940.0 nM 5.71
CHEMBL3093332 — Ki = 2040.0 nM 5.69
CHEMBL3093324 — Ki = 2470.0 nM 5.61
CHEMBL3093226 — Ki = 2650.0 nM 5.58
CHEMBL3093313 — Ki = 3030.0 nM 5.52
CHEMBL3093330 — Ki = 3030.0 nM 5.52
CHEMBL3093236 — Ki = 3690.0 nM 5.43
CHEMBL3093232 — Ki = 3760.0 nM 5.42
CHEMBL3093229 — Ki = 3870.0 nM 5.41
CHEMBL3093234 — Ki = 4700.0 nM 5.33
CHEMBL3093224 — Ki = 5370.0 nM 5.27
CHEMBL3093235 — Ki = 5540.0 nM 5.26
CHEMBL282038 — Ki = 5600.0 nM 5.25
CHEMBL3093314 — Ki = 6220.0 nM 5.21
CHEMBL3093221 — Ki = 7310.0 nM 5.14
CHEMBL241617 — Ki = 7230.0 nM 5.14
CHEMBL3093220 — Ki = 8220.0 nM 5.08
CHEMBL3093215 — Ki = 9420.0 nM 5.03
CHEMBL3093214 — Ki = 14000.0 nM 4.85
CHEMBL113 CAFFEINE Ki = 32500.0 nM 4.49
CHEMBL3093231 — Ki > 10000.0 nM -