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Assay Detail

CHEMBL693105

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Binding
Inhibition of [125I]iodoproxyfan binding to human histamine H3 receptor of CHO-K1 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Different antagonist binding properties of human and rat histamine H3 receptors.
Stark H, Sippl W, Ligneau X, Arrang JM, Ganellin CR, Schwartz JC, Schunack W.
Bioorg Med Chem Lett (2001) 11 : 951 -954
PubMed 11294398 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.86 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367117 1 8.96
CHEMBL296450 1 8.68
CHEMBL14690 CLOBENPROPIT 1 8.62
CHEMBL19173 PROXYFAN 1 8.57
CHEMBL424365 1 7.75
CHEMBL368948 1 7.72
CHEMBL112951 1 7.57
CHEMBL19010 IODOPROXYFAN 1 7.39
CHEMBL124270 1 7.38
CHEMBL14638 CIPROXIFAN 1 7.34
CHEMBL369714 1 7.33
CHEMBL114129 1 7.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367117 Ki = 1.1 nM 8.96
CHEMBL296450 Ki = 2.1 nM 8.68
CHEMBL14690 CLOBENPROPIT Ki = 2.4 nM 8.62
CHEMBL19173 PROXYFAN Ki = 2.7 nM 8.57
CHEMBL424365 Ki = 18.0 nM 7.75
CHEMBL368948 Ki = 19.0 nM 7.72
CHEMBL112951 Ki = 27.0 nM 7.57
CHEMBL19010 IODOPROXYFAN Ki = 41.0 nM 7.39
CHEMBL124270 Ki = 42.0 nM 7.38
CHEMBL14638 CIPROXIFAN Ki = 46.0 nM 7.34
CHEMBL369714 Ki = 47.0 nM 7.33
CHEMBL114129 Ki = 87.0 nM 7.06