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Assay Detail

CHEMBL693572

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

Binding
Inhibition of [3H]N-alpha-methylhistamine binding to guinea pig brain Histamine H3 receptor
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Histamine H3 receptor (CHEMBL5076)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

Trans-4-methyl-3-imidazoyl pyrrolidine as a potent, highly selective histamine H3 receptor agonist in vivo.
Shih NY, Aslanian R, Lupo AT, Orlando S, Piwinski JJ, Green MJ, Ganguly AK, West R, Tozzi S, Kreutner W, Hey JA.
Bioorg Med Chem Lett (1998) 8 : 243 -248
PubMed 9871662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.88 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL79983 1 8.70
CHEMBL313127 1 8.64
CHEMBL18735 1 8.52
CHEMBL83271 1 8.52
CHEMBL83917 1 8.30
CHEMBL79271 1 8.15
CHEMBL81888 1 7.23
CHEMBL83862 1 7.12
CHEMBL83325 1 6.82
CHEMBL315572 1 6.77
CHEMBL312664 1 -
CHEMBL312613 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL79983 Ki = 2.0 nM 8.70
CHEMBL313127 Ki = 2.3 nM 8.64
CHEMBL18735 Ki = 3.0 nM 8.52
CHEMBL83271 Ki = 3.0 nM 8.52
CHEMBL83917 Ki = 5.0 nM 8.30
CHEMBL79271 Ki = 7.0 nM 8.15
CHEMBL81888 Ki = 59.0 nM 7.23
CHEMBL83862 Ki = 76.0 nM 7.12
CHEMBL83325 Ki = 150.0 nM 6.82
CHEMBL315572 Ki = 170.0 nM 6.77
CHEMBL312664 Ki > 2000.0 nM -
CHEMBL312613 Ki > 2000.0 nM -