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Assay Detail

CHEMBL3096083

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

Binding
Displacement of [3H]CCPA from adenosine A1 receptor in rat brain cortex
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 A1 (CHEMBL318)
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 6.04 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3093315 1 6.94
CHEMBL3093310 1 6.87
CHEMBL3093237 1 6.78
CHEMBL3093322 1 6.77
CHEMBL3093323 1 6.66
CHEMBL3093332 1 6.64
CHEMBL3093312 1 6.64
CHEMBL3093331 1 6.50
CHEMBL3093230 1 6.49
CHEMBL241618 1 6.37
CHEMBL3093330 1 6.33
CHEMBL3093225 1 6.30
CHEMBL3093317 1 6.30
CHEMBL3093321 1 6.29
CHEMBL3093325 1 6.26
CHEMBL3093313 1 6.26
CHEMBL3093316 1 6.20
CHEMBL413079 1 6.05
CHEMBL3093320 1 6.00
CHEMBL3091482 1 5.97
CHEMBL3093231 1 5.97
CHEMBL3093311 1 5.97
CHEMBL3093329 1 5.92
CHEMBL3093224 1 5.91
CHEMBL3093238 1 5.75
CHEMBL3093314 1 5.74
CHEMBL239230 1 5.52
CHEMBL3093318 1 5.50
CHEMBL3093236 1 5.40
CHEMBL3093232 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3093315 Ki = 114.0 nM 6.94
CHEMBL3093310 Ki = 135.0 nM 6.87
CHEMBL3093237 Ki = 165.0 nM 6.78
CHEMBL3093322 Ki = 169.0 nM 6.77
CHEMBL3093323 Ki = 219.0 nM 6.66
CHEMBL3093332 Ki = 228.0 nM 6.64
CHEMBL3093312 Ki = 227.0 nM 6.64
CHEMBL3093331 Ki = 313.0 nM 6.50
CHEMBL3093230 Ki = 321.0 nM 6.49
CHEMBL241618 Ki = 432.0 nM 6.37
CHEMBL3093330 Ki = 469.0 nM 6.33
CHEMBL3093225 Ki = 506.0 nM 6.30
CHEMBL3093317 Ki = 501.0 nM 6.30
CHEMBL3093321 Ki = 515.0 nM 6.29
CHEMBL3093313 Ki = 555.0 nM 6.26
CHEMBL3093325 Ki = 545.0 nM 6.26
CHEMBL3093316 Ki = 632.0 nM 6.20
CHEMBL413079 Ki = 900.0 nM 6.05
CHEMBL3093320 Ki = 990.0 nM 6.00
CHEMBL3091482 Ki = 1070.0 nM 5.97
CHEMBL3093231 Ki = 1070.0 nM 5.97
CHEMBL3093311 Ki = 1060.0 nM 5.97
CHEMBL3093329 Ki = 1190.0 nM 5.92
CHEMBL3093224 Ki = 1240.0 nM 5.91
CHEMBL3093238 Ki = 1760.0 nM 5.75
CHEMBL3093314 Ki = 1830.0 nM 5.74
CHEMBL239230 Ki = 3030.0 nM 5.52
CHEMBL3093318 Ki = 3140.0 nM 5.50
CHEMBL3093236 Ki = 4010.0 nM 5.40
CHEMBL3093232 Ki = 4420.0 nM 5.36
CHEMBL3093333 Ki = 5220.0 nM 5.28
CHEMBL3093239 Ki = 7240.0 nM 5.14
CHEMBL282038 Ki = 11000.0 nM 4.96
CHEMBL113 CAFFEINE Ki = 41000.0 nM 4.39
CHEMBL3093240 Ki > 1500.0 nM -
CHEMBL3093324 Ki > 10000.0 nM -
CHEMBL3093214 Ki > 1500.0 nM -
CHEMBL3093215 Ki > 1500.0 nM -
CHEMBL3093216 Ki > 1500.0 nM -
CHEMBL3093217 Ki > 1500.0 nM -
CHEMBL3093218 Ki > 1500.0 nM -
CHEMBL3093219 Ki > 1500.0 nM -
CHEMBL3093220 Ki > 1500.0 nM -
CHEMBL3093221 Ki > 1500.0 nM -
CHEMBL3091481 Ki > 1500.0 nM -
CHEMBL3093222 Ki > 1500.0 nM -
CHEMBL3093241 Ki > 1500.0 nM -
CHEMBL3093226 Ki > 10000.0 nM -
CHEMBL3093328 Ki > 25000.0 nM -
CHEMBL3093319 Ki > 10000.0 nM -