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Assay Detail

CHEMBL897805

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Functional
Antagonist activity at human histamine H3 receptor
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Benzylamine histamine H(3) antagonists and serotonin reuptake inhibitors.
Letavic MA, Stocking EM, Barbier AJ, Bonaventure P, Boggs JD, Lord B, Miller KL, Wilson SJ, Carruthers NI.
Bioorg Med Chem Lett (2007) 17 : 4799 -4803
PubMed 17616397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 8.32 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL237512 1 9.10
CHEMBL397577 1 8.78
CHEMBL393036 1 8.61
CHEMBL397575 1 8.58
CHEMBL236674 1 8.45
CHEMBL428024 1 8.14
CHEMBL391074 1 8.12
CHEMBL236475 1 7.97
CHEMBL236046 1 7.95
CHEMBL236675 1 7.90
CHEMBL236676 1 7.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL237512 Kd = 0.7943 nM 9.10
CHEMBL397577 Kd = 1.66 nM 8.78
CHEMBL393036 Kd = 2.455 nM 8.61
CHEMBL397575 Kd = 2.63 nM 8.58
CHEMBL236674 Kd = 3.548 nM 8.45
CHEMBL428024 Kd = 7.244 nM 8.14
CHEMBL391074 Kd = 7.586 nM 8.12
CHEMBL236475 Kd = 10.72 nM 7.97
CHEMBL236046 Kd = 11.22 nM 7.95
CHEMBL236675 Kd = 12.59 nM 7.90
CHEMBL236676 Kd = 12.88 nM 7.89