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Assay Detail

CHEMBL1006200

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

Binding
Inhibition of nAChR-mediated nicotine-evoked [3H]DA release in superfused rat striatal slices
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Tetrakis-azaaromatic quaternary ammonium salts: novel subtype-selective antagonists at neuronal nicotinic receptors that mediate nicotine-evoked dopamine release.
Zhang Z, Zheng G, Pivavarchyk M, Deaciuc AG, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2008) 18 : 5753 -5753
PubMed 18851914 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.33 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239844 1 9.70
CHEMBL54331 1 8.70
CHEMBL451671 1 8.47
CHEMBL445002 1 7.55
CHEMBL499947 1 7.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239844 IC50 = 0.2 nM 9.70
CHEMBL54331 IC50 = 2.0 nM 8.70
CHEMBL451671 IC50 = 3.38 nM 8.47
CHEMBL445002 IC50 = 28.0 nM 7.55
CHEMBL499947 IC50 = 56.0 nM 7.25