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Assay Detail

CHEMBL5350658

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

Binding
Displacement of [3H] mepyramine from human FLAG-tagged histamine H1 receptor stably expressed in HEK293T cells assessed as inhibition constant by competitive binding based radioligand depletion assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Dual Piperidine-Based Histamine H<sub>3</sub> and Sigma-1 Receptor Ligands in the Treatment of Nociceptive and Neuropathic Pain.
Szczepańska K, Karcz T, Dichiara M, Mogilski S, Kalinowska-Tłuścik J, Pilarski B, Leniak A, Pietruś W, Podlewska S, Popiołek-Barczyk K, Humphrys LJ, Ruiz-Cantero MC, Reiner-Link D, Leitzbach L, Łażewska D, Pockes S, Górka M, Zmysłowski A, Calmels T, Cobos EJ, Marrazzo A, Stark H, Bojarski AJ, Amata E, Kieć-Kononowicz K.
J Med Chem (2023) 66 : 9658 -9683
PubMed 37418295 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.65 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5433976 1 6.18
CHEMBL5421122 1 5.12
CHEMBL5413694 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5433976 Ki = 653.0 nM 6.18
CHEMBL5421122 Ki = 7615.0 nM 5.12
CHEMBL5413694 Ki > 10000.0 nM -