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Assay Detail

CHEMBL1099708

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

Binding
Displacement of [125I]Iodoproxyfan from human histamine H3 receptor expressed in HEK293 cells after 60 mins by scintillation counting
9
Total Activities
9
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

Acidic elements in histamine H(3) receptor antagonists.
Sander K, von Coburg Y, Camelin JC, Ligneau X, Rau O, Schubert-Zsilavecz M, Schwartz JC, Stark H.
Bioorg Med Chem Lett (2010) 20 : 1581 -1584
PubMed 20138762 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.40 9.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL459350 1 9.50
CHEMBL129542 JNJ-5207852 1 9.20
CHEMBL1076567 1 8.70
CHEMBL1202099 1 8.40
CHEMBL1081073 1 8.30
CHEMBL1082147 1 8.10
CHEMBL1080906 1 8.10
CHEMBL1082149 1 8.00
CHEMBL1076599 1 7.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL459350 Ki = 0.3162 nM 9.50
CHEMBL129542 JNJ-5207852 Ki = 0.631 nM 9.20
CHEMBL1076567 Ki = 1.995 nM 8.70
CHEMBL1202099 Ki = 3.981 nM 8.40
CHEMBL1081073 Ki = 5.012 nM 8.30
CHEMBL1082147 Ki = 7.943 nM 8.10
CHEMBL1080906 Ki = 7.943 nM 8.10
CHEMBL1082149 Ki = 10.0 nM 8.00
CHEMBL1076599 Ki = 50.12 nM 7.30