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Assay Detail

CHEMBL1826889

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

Binding
Displacement of [3H]histamine from human H4R receptor expressed in HEK293 cells at 10 uM after 1.5 hrs by liquid scintillation counting
9
Total Activities
9
Compounds Tested
2
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

Fragment library screening reveals remarkable similarities between the G protein-coupled receptor histamine H₄ and the ion channel serotonin 5-HT₃A.
Verheij MH, de Graaf C, de Kloe GE, Nijmeijer S, Vischer HF, Smits RA, Zuiderveld OP, Hulscher S, Silvestri L, Thompson AJ, van Muijlwijk-Koezen JE, Lummis SC, Leurs R, de Esch IJ.
Bioorg Med Chem Lett (2011) 21 : 5460 -5464
PubMed 21782429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.92 8.20
pKi 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL492884 1 8.20
CHEMBL414183 1 7.20
CHEMBL78838 1 7.00
CHEMBL1824046 1 6.70
CHEMBL17740 1 6.20
CHEMBL260565 1 6.20
CHEMBL27453 1 -
CHEMBL148204 1 -
CHEMBL1824047 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL492884 Ki = 6.31 nM 8.20
CHEMBL414183 Ki = 63.1 nM 7.20
CHEMBL78838 Ki = 100.0 nM 7.00
CHEMBL1824046 Ki = 199.53 nM 6.70
CHEMBL17740 Ki = 630.96 nM 6.20
CHEMBL260565 Ki = 630.96 nM 6.20
CHEMBL27453 pKi - -
CHEMBL148204 pKi - -
CHEMBL1824047 pKi - -