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Assay Detail

CHEMBL4337389

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Binding
Displacement of 10 nM [3H]-histamine from human H4R expressed in Sf9 cell membranes co-expressing Gia2 and beta1gamma2 by competition binding assay
12
Total Activities
12
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 H4 receptor (CHEMBL3759)
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 12 7.08 8.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4454158 1 8.29
CHEMBL4455324 1 8.07
CHEMBL4439142 1 7.93
CHEMBL4543119 1 7.20
CHEMBL4445423 1 7.16
CHEMBL4534254 1 6.94
CHEMBL4513989 1 6.73
CHEMBL4586599 1 6.69
CHEMBL4576393 1 6.21
CHEMBL4471442 1 5.57
CHEMBL4563834 1 -
CHEMBL4466349 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4454158 Ki = 5.129 nM 8.29
CHEMBL4455324 Ki = 8.511 nM 8.07
CHEMBL4439142 Ki = 11.75 nM 7.93
CHEMBL4543119 Ki = 63.1 nM 7.20
CHEMBL4445423 Ki = 69.18 nM 7.16
CHEMBL4534254 Ki = 114.82 nM 6.94
CHEMBL4513989 Ki = 186.21 nM 6.73
CHEMBL4586599 Ki = 204.17 nM 6.69
CHEMBL4576393 Ki = 616.6 nM 6.21
CHEMBL4471442 Ki = 2691.53 nM 5.57
CHEMBL4563834 Ki > 10000.0 nM -
CHEMBL4466349 Ki > 10000.0 nM -