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Assay Detail

CHEMBL696447

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

Binding
Histamine H4 receptor competition binding using [3H]Na-methylhistamine
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H4 receptor (CHEMBL3759)
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 16 5.43 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL321860 1 6.90
CHEMBL106158 1 6.65
CHEMBL320331 1 6.36
CHEMBL106612 IMIFURAMINE 1 6.05
CHEMBL105803 1 5.98
CHEMBL321920 1 5.60
CHEMBL106913 1 5.19
CHEMBL108649 1 5.09
CHEMBL109130 1 4.93
CHEMBL107877 1 4.92
CHEMBL106931 1 4.89
CHEMBL1632410 1 4.87
CHEMBL106570 1 4.69
CHEMBL322256 1 4.67
CHEMBL320279 1 4.66
CHEMBL319658 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL321860 Ki = 125.89 nM 6.90
CHEMBL106158 Ki = 223.87 nM 6.65
CHEMBL320331 Ki = 436.52 nM 6.36
CHEMBL106612 IMIFURAMINE Ki = 891.25 nM 6.05
CHEMBL105803 Ki = 1047.13 nM 5.98
CHEMBL321920 Ki = 2511.89 nM 5.60
CHEMBL106913 Ki = 6456.54 nM 5.19
CHEMBL108649 Ki = 8128.31 nM 5.09
CHEMBL109130 Ki = 11748.98 nM 4.93
CHEMBL107877 Ki = 12022.64 nM 4.92
CHEMBL106931 Ki = 12882.5 nM 4.89
CHEMBL1632410 Ki = 13489.63 nM 4.87
CHEMBL106570 Ki = 20417.38 nM 4.69
CHEMBL322256 Ki = 21379.62 nM 4.67
CHEMBL320279 Ki = 21877.62 nM 4.66
CHEMBL319658 Ki < 100000.0 nM -