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Assay Detail

CHEMBL3097144

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Binding
Binding affinity to human histamine H1 receptor
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Histamine H1 receptor (CHEMBL231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of clinical candidates from the benzazepine class of histamine H3 receptor antagonists.
Wilson DM, Apps J, Bailey N, Bamford MJ, Beresford IJ, Brackenborough K, Briggs MA, Brough S, Calver AR, Crook B, Davis RK, Davis RP, Davis S, Dean DK, Harris L, Heslop T, Holland V, Jeffrey P, Panchal TA, Parr CA, Quashie N, Schogger J, Sehmi SS, Stean TO, Steadman JG, Trail B, Wald J, Worby A, Takle AK, Witherington J, Medhurst AD.
Bioorg Med Chem Lett (2013) 23 : 6890 -6896
PubMed 24269482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.70 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1783890 1 5.80
CHEMBL3092650 GSK239512 2.0 1 5.60
CHEMBL517140 GSK189254 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1783890 Ki = 1584.89 nM 5.80
CHEMBL3092650 GSK239512 Ki = 2511.89 nM 5.60
CHEMBL517140 GSK189254 Ki > 2511.89 nM -