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Assay Detail

CHEMBL973671

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

Binding
Displacement of [3H]NAMH from rat full length histamine H3 receptor expressed in rat C6 cells
8
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type C6
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL4124)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

The alkaloid conessine and analogues as potent histamine H3 receptor antagonists.
Zhao C, Sun M, Bennani YL, Gopalakrishnan SM, Witte DG, Miller TR, Krueger KM, Browman KE, Thiffault C, Wetter J, Marsh KC, Hancock AA, Esbenshade TA, Cowart MD.
J Med Chem (2008) 51 : 5423 -5430
PubMed 18683917 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.81 9.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14638 CIPROXIFAN 1 9.29
CHEMBL451821 1 8.59
CHEMBL260374 THIOPERAMIDE 1 8.44
CHEMBL488891 1 8.10
CHEMBL191703 CONESSINE 2.0 2 7.91
CHEMBL461024 CARCININE 1 6.53
CHEMBL519889 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14638 CIPROXIFAN Ki = 0.5129 nM 9.29
CHEMBL451821 Ki = 2.57 nM 8.59
CHEMBL260374 THIOPERAMIDE Ki = 3.631 nM 8.44
CHEMBL488891 Ki = 7.91 nM 8.10
CHEMBL191703 CONESSINE Ki = 12.3 nM 7.91
CHEMBL191703 CONESSINE Ki = 24.5 nM 7.61
CHEMBL461024 CARCININE Ki = 294.0 nM 6.53
CHEMBL519889 Ki = 1000.0 nM 6.00