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Assay Detail

CHEMBL4337392

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

Binding
Displacement of 20 nM [3H]UR-DE257 from human H2R expressed in Sf9 cell membranes co-expressing GsalphaS by competition binding assay
20
Total Activities
20
Compounds Tested
2
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 H2 receptor (CHEMBL1941)
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 18 6.25 6.25
pKi 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4466349 1 6.25
CHEMBL4455324 1 -
CHEMBL4513989 1 -
CHEMBL4518374 1 -
CHEMBL4563834 1 -
CHEMBL4586599 1 -
CHEMBL4437371 1 -
CHEMBL4543928 1 -
CHEMBL4513421 1 -
CHEMBL4473753 1 -
CHEMBL4470527 1 -
CHEMBL4443126 1 -
CHEMBL4439142 1 -
CHEMBL4534254 1 -
CHEMBL4543119 1 -
CHEMBL4445423 1 -
CHEMBL4576393 1 -
CHEMBL4471442 1 -
CHEMBL4538671 1 -
CHEMBL4454158 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4466349 Ki = 562.34 nM 6.25
CHEMBL4455324 Ki > 10000.0 nM -
CHEMBL4513989 Ki > 10000.0 nM -
CHEMBL4518374 Ki > 10000.0 nM -
CHEMBL4563834 Ki > 10000.0 nM -
CHEMBL4586599 Ki > 10000.0 nM -
CHEMBL4437371 Ki > 1000.0 nM -
CHEMBL4543928 Ki > 1000.0 nM -
CHEMBL4513421 Ki > 10000.0 nM -
CHEMBL4473753 pKi - -
CHEMBL4470527 pKi - -
CHEMBL4443126 Ki > 10000.0 nM -
CHEMBL4439142 Ki > 1000.0 nM -
CHEMBL4534254 Ki > 10000.0 nM -
CHEMBL4543119 Ki > 1000.0 nM -
CHEMBL4445423 Ki > 1000.0 nM -
CHEMBL4576393 Ki > 10000.0 nM -
CHEMBL4471442 Ki > 10000.0 nM -
CHEMBL4538671 Ki > 10000.0 nM -
CHEMBL4454158 Ki > 10000.0 nM -