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Assay Detail

CHEMBL694889

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

Functional
Histamine-induced inhibition of forskolin- stimulated cAMP accumulation in SK-N-MC cells overexpressing the human Histamine H3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type SK-N-MC
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

A new class of diamine-based human histamine H3 receptor antagonists: 4-(aminoalkoxy)benzylamines.
Apodaca R, Dvorak CA, Xiao W, Barbier AJ, Boggs JD, Wilson SJ, Lovenberg TW, Carruthers NI.
J Med Chem (2003) 46 : 3938 -3944
PubMed 12930154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 6 9.08 9.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129542 JNJ-5207852 1 9.84
CHEMBL129411 1 9.71
CHEMBL129306 1 9.64
CHEMBL339867 1 9.27
CHEMBL126904 1 8.05
CHEMBL337942 1 7.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129542 JNJ-5207852 Kd = 0.1445 nM 9.84
CHEMBL129411 Kd = 0.195 nM 9.71
CHEMBL129306 Kd = 0.2291 nM 9.64
CHEMBL339867 Kd = 0.537 nM 9.27
CHEMBL126904 Kd = 8.913 nM 8.05
CHEMBL337942 Kd = 10.47 nM 7.98