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Assay Detail

CHEMBL4369180

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

Binding
Displacement of [3H]Cimetidine from human H2 receptor expressed in HEK cells after 90 mins by scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H2 receptor (CHEMBL1941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationship of 2-arylalkynyl-adenine derivatives as human A<sub>3</sub> adenosine receptor antagonists.
Yu J, Mannes P, Jung YH, Ciancetta A, Bitant A, Lieberman DI, Khaznadar S, Auchampach JA, Gao ZG, Jacobson KA.
Medchemcomm (2018) 9 : 1920 -1932
PubMed 30568760 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 5.86 6.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4546937 1 6.28
CHEMBL4439593 1 5.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4546937 Ki = 520.0 nM 6.28
CHEMBL4439593 Ki = 3640.0 nM 5.44