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Assay Detail

CHEMBL902064

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

Functional
Antagonist activity at nAChR in rat striatal slices assessed as inhibition of nicotine-evoked [3H]dopamine release
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tris-azaaromatic quaternary ammonium salts: Novel templates as antagonists at nicotinic receptors mediating nicotine-evoked dopamine release.
Zheng G, Sumithran SP, Deaciuc AG, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2007) 17 : 6701 -6706
PubMed 17977723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.60 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239844 1 9.70
CHEMBL269243 1 8.70
CHEMBL54331 1 8.70
CHEMBL397306 1 8.40
CHEMBL55006 1 7.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239844 IC50 = 0.2 nM 9.70
CHEMBL269243 IC50 = 2.0 nM 8.70
CHEMBL54331 IC50 = 2.0 nM 8.70
CHEMBL397306 IC50 = 4.0 nM 8.40
CHEMBL55006 IC50 = 30.0 nM 7.52