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

CHEMBL692575

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

Binding
Histamine H3 receptor competition binding using [3H]Na-methylhistamine
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

A selective human H(4)-receptor agonist: (-)-2-cyano-1-methyl-3-[(2R,5R)-5- [1H-imidazol-4(5)-yl]tetrahydrofuran-2-y] methylguanidine.
Hashimoto T, Harusawa S, Araki L, Zuiderveld OP, Smit MJ, Imazu T, Takashima S, Yamamoto Y, Sakamoto Y, Kurihara T, Leurs R, Bakker RA, Yamatodani A.
J Med Chem (2003) 46 : 3162 -3165
PubMed 12825954 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 5.84 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90 HISTAMINE 4.0 1 7.47
CHEMBL106931 1 6.66
CHEMBL106612 IMIFURAMINE 1 6.64
CHEMBL105803 1 6.61
CHEMBL320331 1 6.48
CHEMBL109130 1 5.99
CHEMBL106913 1 5.77
CHEMBL321920 1 5.69
CHEMBL321860 1 5.66
CHEMBL319658 1 5.60
CHEMBL1632410 1 5.16
CHEMBL106158 1 5.15
CHEMBL108649 1 5.09
CHEMBL320279 1 4.94
CHEMBL106570 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90 HISTAMINE Ki = 33.88 nM 7.47
CHEMBL106931 Ki = 218.78 nM 6.66
CHEMBL106612 IMIFURAMINE Ki = 229.09 nM 6.64
CHEMBL105803 Ki = 245.47 nM 6.61
CHEMBL320331 Ki = 331.13 nM 6.48
CHEMBL109130 Ki = 1023.29 nM 5.99
CHEMBL106913 Ki = 1698.24 nM 5.77
CHEMBL321920 Ki = 2041.74 nM 5.69
CHEMBL321860 Ki = 2187.76 nM 5.66
CHEMBL319658 Ki = 2511.89 nM 5.60
CHEMBL1632410 Ki = 6918.31 nM 5.16
CHEMBL106158 Ki = 7079.46 nM 5.15
CHEMBL108649 Ki = 8128.31 nM 5.09
CHEMBL320279 Ki = 11481.54 nM 4.94
CHEMBL106570 Ki = 18620.87 nM 4.73