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Assay Detail

CHEMBL784317

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

Functional
Inhibitory activity against nAChR mediated nicotine-evoked [3H]DA overflow using rat striatal slices
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Subtype-selective nicotinic receptor antagonists: potential as tobacco use cessation agents.
Dwoskin LP, Sumithran SP, Zhu J, Deaciuc AG, Ayers JT, Crooks PA.
Bioorg Med Chem Lett (2004) 14 : 1863 -1867
PubMed 15050617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.71 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54331 1 8.30
CHEMBL55181 1 7.52
CHEMBL55006 1 7.52
CHEMBL416496 1 6.52
CHEMBL52918 1 6.21
CHEMBL55795 1 6.00
CHEMBL53780 1 5.82
CHEMBL54117 1 5.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54331 IC50 = 5.0 nM 8.30
CHEMBL55181 IC50 = 30.0 nM 7.52
CHEMBL55006 IC50 = 30.0 nM 7.52
CHEMBL416496 IC50 = 300.0 nM 6.52
CHEMBL52918 IC50 = 610.0 nM 6.21
CHEMBL55795 IC50 = 1000.0 nM 6.00
CHEMBL53780 IC50 = 1520.0 nM 5.82
CHEMBL54117 IC50 = 1660.0 nM 5.78