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Assay Detail

CHEMBL696935

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

Binding
Binding affinity against H1 receptor of guinea pig by the displacement of [3H]mepyramine, bound to membranes of CHO cells
7
Total Activities
7
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 Intermediate

Target

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

Publication

Homologs of histamine as histamine H3 receptor antagonists: a new potent and selective H3 antagonist, 4(5)-(5-aminopentyl)-1H-imidazole.
Vollinga RC, Menge WM, Leurs R, Timmerman H.
J Med Chem (1995) 38 : 266 -271
PubMed 7830269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.57 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL94249 1 6.20
CHEMBL90063 1 5.60
CHEMBL90 HISTAMINE 4.0 1 4.90
CHEMBL417096 IMPENTAMINE 1 -
CHEMBL554031 1 -
CHEMBL92694 1 -
CHEMBL91353 HOMOHISTAMINE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL94249 Ki = 630.96 nM 6.20
CHEMBL90063 Ki = 2511.89 nM 5.60
CHEMBL90 HISTAMINE Ki = 12589.25 nM 4.90
CHEMBL417096 IMPENTAMINE Ki = 125892.54 nM -
CHEMBL554031 Ki = 125892.54 nM -
CHEMBL92694 Ki > 1000000.0 nM -
CHEMBL91353 HOMOHISTAMINE Ki > 1000000.0 nM -