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Assay Detail

CHEMBL4197754

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

Binding
Displacement of [3H]-N-alpha-methylhistamine from human H3R expressed in HEK293 cell membranes after 90 mins by liquid scintillation counting method
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel indanone derivatives as MAO B/H3R dual-targeting ligands for treatment of Parkinson's disease.
Affini A, Hagenow S, Zivkovic A, Marco-Contelles J, Stark H.
Eur J Med Chem (2018) 148 : 487 -497
PubMed 29477889 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.34 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4209497 1 8.68
CHEMBL4218833 1 8.66
CHEMBL4212330 1 8.41
CHEMBL4205653 1 8.19
CHEMBL4214411 1 7.96
CHEMBL2297871 1 7.96
CHEMBL4217355 1 7.50
CHEMBL4204965 1 7.48
CHEMBL4216392 1 7.41
CHEMBL4215163 1 6.80
CHEMBL4204031 1 6.69
CHEMBL4207429 1 6.52
CHEMBL4208908 1 6.46
CHEMBL4216240 1 6.16
CHEMBL4212333 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4209497 Ki = 2.1 nM 8.68
CHEMBL4218833 Ki = 2.2 nM 8.66
CHEMBL4212330 Ki = 3.9 nM 8.41
CHEMBL4205653 Ki = 6.5 nM 8.19
CHEMBL4214411 Ki = 11.0 nM 7.96
CHEMBL2297871 Ki = 11.0 nM 7.96
CHEMBL4217355 Ki = 32.0 nM 7.50
CHEMBL4204965 Ki = 33.0 nM 7.48
CHEMBL4216392 Ki = 39.0 nM 7.41
CHEMBL4215163 Ki = 159.0 nM 6.80
CHEMBL4204031 Ki = 205.0 nM 6.69
CHEMBL4207429 Ki = 304.0 nM 6.52
CHEMBL4208908 Ki = 345.0 nM 6.46
CHEMBL4216240 Ki = 696.0 nM 6.16
CHEMBL4212333 Ki = 6118.0 nM 5.21