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Assay Detail

CHEMBL4329059

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Binding
Displacement of [3H]-N-alpha-methylhistamine from human H3 receptor expressed in CHO-K1 cell membranes after 60 mins by microbeta2 scintillation counting analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

4-tert-Pentylphenoxyalkyl derivatives - Histamine H<sub>3</sub> receptor ligands and monoamine oxidase B inhibitors.
Łażewska D, Olejarz-Maciej A, Kaleta M, Bajda M, Siwek A, Karcz T, Doroz-Płonka A, Cichoń U, Kuder K, Kieć-Kononowicz K.
Bioorg Med Chem Lett (2018) 28 : 3596 -3600
PubMed 30404719 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.79 7.43

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4173079 1 7.43
CHEMBL4561401 1 7.20
CHEMBL4560631 1 7.00
CHEMBL4449671 1 6.85
CHEMBL4473751 1 6.83
CHEMBL4522715 1 6.53
CHEMBL4435585 1 6.36
CHEMBL4530407 1 6.12
CHEMBL4557594 1 -
CHEMBL887 RASAGILINE 4.0 1 -
CHEMBL396778 SAFINAMIDE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4173079 Ki = 37.0 nM 7.43
CHEMBL4561401 Ki = 63.0 nM 7.20
CHEMBL4560631 Ki = 100.0 nM 7.00
CHEMBL4449671 Ki = 140.0 nM 6.85
CHEMBL4473751 Ki = 147.0 nM 6.83
CHEMBL4522715 Ki = 298.0 nM 6.53
CHEMBL4435585 Ki = 437.0 nM 6.36
CHEMBL4530407 Ki = 753.0 nM 6.12
CHEMBL4557594 Ki > 1000.0 nM -
CHEMBL887 RASAGILINE Ki - -
CHEMBL396778 SAFINAMIDE Ki - -