Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4481771

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 cortical membranes
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 25 5.75 6.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL431770 ISTRADEFYLLINE 4.0 1 6.64
CHEMBL241618 1 6.37
CHEMBL4531455 1 6.31
CHEMBL4560961 1 6.03
CHEMBL4570974 1 6.03
CHEMBL4537668 1 6.01
CHEMBL4558859 1 5.85
CHEMBL4521517 1 5.81
CHEMBL4540760 1 5.75
CHEMBL4563999 1 5.72
CHEMBL4535750 1 5.63
CHEMBL4574105 1 5.58
CHEMBL4592888 1 5.52
CHEMBL4569201 1 5.38
CHEMBL4533073 1 5.36
CHEMBL4517925 1 5.31
CHEMBL113 CAFFEINE 4.0 1 4.39
CHEMBL4574192 1 -
CHEMBL4580206 1 -
CHEMBL4554986 1 -
CHEMBL4576786 1 -
CHEMBL4566592 1 -
CHEMBL4579395 1 -
CHEMBL4565406 1 -
CHEMBL4546819 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL431770 ISTRADEFYLLINE Ki = 230.0 nM 6.64
CHEMBL241618 Ki = 432.0 nM 6.37
CHEMBL4531455 Ki = 486.0 nM 6.31
CHEMBL4560961 Ki = 931.0 nM 6.03
CHEMBL4570974 Ki = 927.0 nM 6.03
CHEMBL4537668 Ki = 965.0 nM 6.01
CHEMBL4558859 Ki = 1410.0 nM 5.85
CHEMBL4521517 Ki = 1550.0 nM 5.81
CHEMBL4540760 Ki = 1780.0 nM 5.75
CHEMBL4563999 Ki = 1910.0 nM 5.72
CHEMBL4535750 Ki = 2320.0 nM 5.63
CHEMBL4574105 Ki = 2650.0 nM 5.58
CHEMBL4592888 Ki = 3020.0 nM 5.52
CHEMBL4569201 Ki = 4130.0 nM 5.38
CHEMBL4533073 Ki = 4360.0 nM 5.36
CHEMBL4517925 Ki = 4900.0 nM 5.31
CHEMBL113 CAFFEINE Ki = 41000.0 nM 4.39
CHEMBL4574192 Ki > 1000.0 nM -
CHEMBL4580206 Ki > 1000.0 nM -
CHEMBL4554986 Ki > 1000.0 nM -
CHEMBL4576786 Ki > 1000.0 nM -
CHEMBL4566592 Ki > 1000.0 nM -
CHEMBL4579395 Ki > 1000.0 nM -
CHEMBL4565406 Ki > 1000.0 nM -
CHEMBL4546819 Ki > 1000.0 nM -