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Assay Detail

CHEMBL694894

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

Binding
Activity at Histamine H3 receptor expressed in CHO cells using [125I]iodoproxyfan binding assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of a new class of nonimidazole histamine H(3) receptor ligands with combined inhibitory histamine N-methyltransferase activity.
Apelt J, Ligneau X, Pertz HH, Arrang JM, Ganellin CR, Schwartz JC, Schunack W, Stark H.
J Med Chem (2002) 45 : 1128 -1141
PubMed 11855993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 9.33 10.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14364 1 10.10
CHEMBL15153 1 10.00
CHEMBL15056 1 9.50
CHEMBL14587 1 9.30
CHEMBL276938 1 9.30
CHEMBL14754 1 8.90
CHEMBL14484 1 8.80
CHEMBL14868 1 8.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14364 Ki = 0.07943 nM 10.10
CHEMBL15153 Ki = 0.1 nM 10.00
CHEMBL15056 Ki = 0.3162 nM 9.50
CHEMBL14587 Ki = 0.5012 nM 9.30
CHEMBL276938 Ki = 0.5012 nM 9.30
CHEMBL14754 Ki = 1.259 nM 8.90
CHEMBL14484 Ki = 1.585 nM 8.80
CHEMBL14868 Ki = 1.995 nM 8.70