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Assay Detail

CHEMBL976201

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

Binding
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO cells by beta scintillation counter
20
Total Activities
20
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

1,3-dialkyl-8-N-substituted benzyloxycarbonylamino-9-deazaxanthines as potent adenosine receptor ligands: Design, synthesis, structure-affinity and structure-selectivity relationships.
Fernández F, Caamaño O, Isabel Nieto M, López C, García-Mera X, Stefanachi A, Nicolotti O, Isabel Loza M, Brea J, Esteve C, Segarra V, Vidal B, Carotti A.
Bioorg Med Chem (2009) 17 : 3618 -3629
PubMed 19398343 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 8.30 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL512276 1 9.40
CHEMBL512290 1 8.66
CHEMBL513681 1 8.00
CHEMBL469119 1 7.75
CHEMBL466021 1 7.69
CHEMBL468920 1 -
CHEMBL466828 1 -
CHEMBL452454 1 -
CHEMBL466652 1 -
CHEMBL466453 1 -
CHEMBL466035 1 -
CHEMBL467271 1 -
CHEMBL467270 1 -
CHEMBL468306 1 -
CHEMBL468295 1 -
CHEMBL511714 1 -
CHEMBL469136 1 -
CHEMBL513135 1 -
CHEMBL468506 1 -
CHEMBL468296 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL512276 Ki = 0.4 nM 9.40
CHEMBL512290 Ki = 2.2 nM 8.66
CHEMBL513681 Ki = 10.0 nM 8.00
CHEMBL469119 Ki = 17.8 nM 7.75
CHEMBL466021 Ki = 20.4 nM 7.69
CHEMBL468920 Ki - -
CHEMBL466828 Ki - -
CHEMBL452454 Ki - -
CHEMBL466652 Ki - -
CHEMBL466453 Ki - -
CHEMBL466035 Ki - -
CHEMBL467271 Ki - -
CHEMBL467270 Ki - -
CHEMBL468306 Ki - -
CHEMBL468295 Ki - -
CHEMBL511714 Ki - -
CHEMBL469136 Ki - -
CHEMBL513135 Ki - -
CHEMBL468506 Ki - -
CHEMBL468296 Ki - -