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Assay Detail

CHEMBL697099

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

Binding
Displacement of [3H]mepyramine bound to membranes of CHO cells expressing guinea pig H1 receptors
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Expert

Target

Histamine H1 receptor (CHEMBL3943)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

New analogs of burimamide as potent and selective histamine H3 receptor antagonists: the effect of chain length variation of the alkyl spacer and modifications of the N-thiourea substituent.
Vollinga RC, Menge WM, Leurs R, Timmerman H.
J Med Chem (1995) 38 : 2244 -2250
PubMed 7783156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.26 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL72372 1 5.80
CHEMBL310087 1 5.60
CHEMBL308717 1 5.50
CHEMBL305929 1 5.50
CHEMBL70811 1 5.40
CHEMBL72571 1 5.10
CHEMBL70603 1 4.90
CHEMBL72424 1 4.80
CHEMBL44220 1 4.70
CHEMBL12160 BURIMAMIDE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL72372 Ki = 1584.89 nM 5.80
CHEMBL310087 Ki = 2511.89 nM 5.60
CHEMBL308717 Ki = 3162.28 nM 5.50
CHEMBL305929 Ki = 3162.28 nM 5.50
CHEMBL70811 Ki = 3981.07 nM 5.40
CHEMBL72571 Ki = 7943.28 nM 5.10
CHEMBL70603 Ki = 12589.25 nM 4.90
CHEMBL72424 Ki = 15848.93 nM 4.80
CHEMBL44220 Ki = 19952.62 nM 4.70
CHEMBL12160 BURIMAMIDE Ki = 316227.77 nM -