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Assay Detail

CHEMBL1007534

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

Binding
Antagonist activity at human histamine H3 receptor expressed in HEK293 cells by [35S]gammaS binding assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Histamine H3 receptor (CHEMBL264)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-hydroxyindole-2-carboxylic acid amides: novel histamine-3 receptor inverse agonists for the treatment of obesity.
Pierson PD, Fettes A, Freichel C, Gatti-McArthur S, Hertel C, Huwyler J, Mohr P, Nakagawa T, Nettekoven M, Plancher JM, Raab S, Richter H, Roche O, Rodríguez Sarmiento RM, Schmitt M, Schuler F, Takahashi T, Taylor S, Ullmer C, Wiegand R.
J Med Chem (2009) 52 : 3855 -3868
PubMed 19456097 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 9.80 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL462605 PITOLISANT 4.0 1 9.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL462605 PITOLISANT Ki = 0.16 nM 9.80