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Assay Detail

CHEMBL940222

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Binding
Inhibition of histamine H3 receptor
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
Bembenek SD, Keith JM, Letavic MA, Apodaca R, Barbier AJ, Dvorak L, Aluisio L, Miller KL, Lovenberg TW, Carruthers NI.
Bioorg Med Chem (2008) 16 : 2968 -2973
PubMed 18249544 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.15 9.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129542 JNJ-5207852 1 9.28
CHEMBL129306 1 9.14
CHEMBL259264 1 9.01
CHEMBL259482 1 8.89
CHEMBL502 DONEPEZIL 4.0 1 6.46
CHEMBL1190 DECAMETHONIUM 4.0 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129542 JNJ-5207852 IC50 = 0.53 nM 9.28
CHEMBL129306 IC50 = 0.72 nM 9.14
CHEMBL259264 IC50 = 0.98 nM 9.01
CHEMBL259482 IC50 = 1.3 nM 8.89
CHEMBL502 DONEPEZIL IC50 = 350.0 nM 6.46
CHEMBL1190 DECAMETHONIUM IC50 = 820.0 nM 6.09