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Assay Detail

CHEMBL1925258

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

Binding
Displacement of [3H]histamine from human H4 receptor T6.55M mutant expressed in HEK293 cells after 1 to 1.5 hrs by scintillation counting
2
Total Activities
2
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 H4 receptor (CHEMBL3759)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.
Istyastono EP, Nijmeijer S, Lim HD, van de Stolpe A, Roumen L, Kooistra AJ, Vischer HF, de Esch IJ, Leurs R, de Graaf C.
J Med Chem (2011) 54 : 8136 -8147
PubMed 22003888 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 8.35 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14690 CLOBENPROPIT 1 8.80
CHEMBL43934 1 7.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14690 CLOBENPROPIT Ki = 1.585 nM 8.80
CHEMBL43934 Ki = 12.59 nM 7.90