Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4337378

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

Binding
Displacement of 3 nM [3H]Nalpha-methylhistamine from human H3R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type Sf9
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

[<sup>3</sup>H]UR-DEBa176: A 2,4-Diaminopyrimidine-Type Radioligand Enabling Binding Studies at the Human, Mouse, and Rat Histamine H<sub>4</sub> Receptors.
Bartole E, Littmann T, Tanaka M, Ozawa T, Buschauer A, Bernhardt G.
J Med Chem (2019) 62 : 8338 -8356
PubMed 31469288 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 6.30 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454158 1 8.48
CHEMBL4455324 1 7.86
CHEMBL4443126 1 7.56
CHEMBL4439142 1 6.84
CHEMBL4543928 1 6.69
CHEMBL4586599 1 6.16
CHEMBL4445423 1 5.95
CHEMBL4543119 1 5.62
CHEMBL4538671 1 5.52
CHEMBL4513421 1 5.46
CHEMBL4534254 1 5.26
CHEMBL4437371 1 5.25
CHEMBL4576393 1 5.22
CHEMBL4466349 1 -
CHEMBL4471442 1 -
CHEMBL4563834 1 -
CHEMBL4513989 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454158 Ki = 3.311 nM 8.48
CHEMBL4455324 Ki = 13.8 nM 7.86
CHEMBL4443126 Ki = 27.54 nM 7.56
CHEMBL4439142 Ki = 144.54 nM 6.84
CHEMBL4543928 Ki = 204.17 nM 6.69
CHEMBL4586599 Ki = 691.83 nM 6.16
CHEMBL4445423 Ki = 1122.02 nM 5.95
CHEMBL4543119 Ki = 2398.83 nM 5.62
CHEMBL4538671 Ki = 3019.95 nM 5.52
CHEMBL4513421 Ki = 3467.37 nM 5.46
CHEMBL4534254 Ki = 5495.41 nM 5.26
CHEMBL4437371 Ki = 5623.41 nM 5.25
CHEMBL4576393 Ki = 6025.6 nM 5.22
CHEMBL4466349 Ki > 10000.0 nM -
CHEMBL4471442 Ki > 10000.0 nM -
CHEMBL4563834 Ki > 10000.0 nM -
CHEMBL4513989 Ki > 10000.0 nM -