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Assay Detail

CHEMBL4481769

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

Binding
Displacement of [3H]CCPA from recombinant human adenosine A1 receptor expressed in CHO cells
18
Total Activities
18
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

Novel multi-target directed ligands based on annelated xanthine scaffold with aromatic substituents acting on adenosine receptor and monoamine oxidase B. Synthesis, in vitro and in silico studies.
Załuski M, Schabikowski J, Schlenk M, Olejarz-Maciej A, Kubas B, Karcz T, Kuder K, Latacz G, Zygmunt M, Synak D, Hinz S, Müller CE, Kieć-Kononowicz K.
Bioorg Med Chem (2019) 27 : 1195 -1210
PubMed 30808606 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.76 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563397 1 6.40
CHEMBL4579508 1 6.19
CHEMBL431770 ISTRADEFYLLINE 4.0 1 6.08
CHEMBL113 CAFFEINE 4.0 1 4.35
CHEMBL241618 1 -
CHEMBL4521398 1 -
CHEMBL4573517 1 -
CHEMBL4574378 1 -
CHEMBL4573063 1 -
CHEMBL4554404 1 -
CHEMBL4550899 1 -
CHEMBL4530654 1 -
CHEMBL4569183 1 -
CHEMBL4559410 1 -
CHEMBL4544530 1 -
CHEMBL4549927 1 -
CHEMBL4483563 1 -
CHEMBL4517303 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563397 Ki = 396.0 nM 6.40
CHEMBL4579508 Ki = 651.0 nM 6.19
CHEMBL431770 ISTRADEFYLLINE Ki = 841.0 nM 6.08
CHEMBL113 CAFFEINE Ki = 44900.0 nM 4.35
CHEMBL241618 Ki > 10000.0 nM -
CHEMBL4521398 Ki > 1000.0 nM -
CHEMBL4573517 Ki > 1000.0 nM -
CHEMBL4574378 Ki > 1000.0 nM -
CHEMBL4573063 Ki > 1000.0 nM -
CHEMBL4554404 Ki > 1000.0 nM -
CHEMBL4550899 Ki > 1000.0 nM -
CHEMBL4530654 Ki > 1000.0 nM -
CHEMBL4569183 Ki > 1000.0 nM -
CHEMBL4559410 Ki > 1000.0 nM -
CHEMBL4544530 Ki > 1000.0 nM -
CHEMBL4549927 Ki > 1000.0 nM -
CHEMBL4483563 Ki > 1000.0 nM -
CHEMBL4517303 Ki > 1000.0 nM -