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Assay Detail

CHEMBL3830977

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

Binding
Displacement of [3H]CCPA from adenosine receptor A1 in rat brain cortical membranes
37
Total Activities
37
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

Similarities and differences in affinity and binding modes of tricyclic pyrimido- and pyrazinoxanthines at human and rat adenosine receptors.
Szymańska E, Drabczyńska A, Karcz T, Müller CE, Köse M, Karolak-Wojciechowska J, Fruziński A, Schabikowski J, Doroz-Płonka A, Handzlik J, Kieć-Kononowicz K.
Bioorg Med Chem (2016) 24 : 4347 -4362
PubMed 27485602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 37 6.64 7.25

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827598 1 7.25
CHEMBL3827074 1 7.14
CHEMBL3827331 1 7.10
CHEMBL3827201 1 6.90
CHEMBL3827187 1 6.86
CHEMBL3828555 1 6.76
CHEMBL3827623 1 6.76
CHEMBL3827301 1 6.76
CHEMBL3827267 1 6.75
CHEMBL3828002 1 6.74
CHEMBL3827298 1 6.59
CHEMBL3827922 1 6.57
CHEMBL3827716 1 6.53
CHEMBL3828401 1 6.46
CHEMBL3828658 1 6.43
CHEMBL3827653 1 6.25
CHEMBL3827216 1 5.86
CHEMBL3827628 1 5.76
CHEMBL3827973 1 -
CHEMBL3828530 1 -
CHEMBL3828477 1 -
CHEMBL3828341 1 -
CHEMBL3827127 1 -
CHEMBL3827704 1 -
CHEMBL3093326 1 -
CHEMBL3827031 1 -
CHEMBL3828044 1 -
CHEMBL3827075 1 -
CHEMBL3828237 1 -
CHEMBL3827920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827598 Ki = 56.0 nM 7.25
CHEMBL3827074 Ki = 72.0 nM 7.14
CHEMBL3827331 Ki = 80.0 nM 7.10
CHEMBL3827201 Ki = 127.0 nM 6.90
CHEMBL3827187 Ki = 137.0 nM 6.86
CHEMBL3828555 Ki = 172.0 nM 6.76
CHEMBL3827623 Ki = 175.0 nM 6.76
CHEMBL3827301 Ki = 174.0 nM 6.76
CHEMBL3827267 Ki = 180.0 nM 6.75
CHEMBL3828002 Ki = 184.0 nM 6.74
CHEMBL3827298 Ki = 254.0 nM 6.59
CHEMBL3827922 Ki = 268.0 nM 6.57
CHEMBL3827716 Ki = 297.0 nM 6.53
CHEMBL3828401 Ki = 347.0 nM 6.46
CHEMBL3828658 Ki = 370.0 nM 6.43
CHEMBL3827653 Ki = 567.0 nM 6.25
CHEMBL3827216 Ki = 1370.0 nM 5.86
CHEMBL3827628 Ki = 1740.0 nM 5.76
CHEMBL3827859 Ki > 1000.0 nM -
CHEMBL3827544 Ki > 1000.0 nM -
CHEMBL3828343 Ki > 1000.0 nM -
CHEMBL3827016 Ki > 1000.0 nM -
CHEMBL3827583 Ki > 1000.0 nM -
CHEMBL3827175 Ki > 1000.0 nM -
CHEMBL3827365 Ki > 1000.0 nM -
CHEMBL3827920 Ki > 500.0 nM -
CHEMBL3828237 Ki > 1000.0 nM -
CHEMBL3827075 Ki > 10000.0 nM -
CHEMBL3828044 Ki > 500.0 nM -
CHEMBL3827031 Ki > 10000.0 nM -
CHEMBL3093326 Ki > 1000.0 nM -
CHEMBL3827704 Ki > 1000.0 nM -
CHEMBL3827127 Ki > 1000.0 nM -
CHEMBL3828341 Ki > 1000.0 nM -
CHEMBL3828477 Ki > 1000.0 nM -
CHEMBL3828530 Ki > 1000.0 nM -
CHEMBL3827973 Ki > 1000.0 nM -