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Assay Detail

CHEMBL1936679

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

Binding
Displacement of [3H]histamine from human H1 receptor expressed in HEK cell membranes
4
Total Activities
4
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 H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.
Smits RA, Lim HD, van der Meer T, Kuhne S, Bessembinder K, Zuiderveld OP, Wijtmans M, de Esch IJ, Leurs R.
Bioorg Med Chem Lett (2012) 22 : 461 -467
PubMed 22153663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.21 5.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1935572 1 5.55
CHEMBL1935573 1 5.19
CHEMBL1935571 1 5.13
CHEMBL1935574 1 4.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1935572 Ki = 2800.0 nM 5.55
CHEMBL1935573 Ki = 6422.0 nM 5.19
CHEMBL1935571 Ki = 7373.0 nM 5.13
CHEMBL1935574 Ki = 10500.0 nM 4.98