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Assay Detail

CHEMBL1068974

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

Functional
Antagonist activity at nicotinic acetylcholine receptor in rat striatal slices assessed as inhibition of S-(-)-nicotine-induced [3H]dopamine release
10
Total Activities
10
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

Novel bis-2,2,6,6-tetramethylpiperidine (bis-TMP) and bis-mecamylamine antagonists at neuronal nicotinic receptors mediating nicotine-evoked dopamine release.
Zhang Z, Pivavarchyk M, Subramanian KL, Deaciuc AG, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2010) 20 : 1420 -1423
PubMed 20079634 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 7.98 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL239844 1 9.70
CHEMBL54331 1 8.70
CHEMBL600214 1 8.66
CHEMBL605784 1 7.34
CHEMBL589476 1 6.97
CHEMBL600418 1 6.50
CHEMBL602685 1 -
CHEMBL602686 1 -
CHEMBL601877 1 -
CHEMBL601446 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL239844 IC50 = 0.2 nM 9.70
CHEMBL54331 IC50 = 2.0 nM 8.70
CHEMBL600214 IC50 = 2.2 nM 8.66
CHEMBL605784 IC50 = 46.0 nM 7.34
CHEMBL589476 IC50 = 107.0 nM 6.97
CHEMBL600418 IC50 = 319.0 nM 6.50
CHEMBL602685 IC50 - -
CHEMBL602686 IC50 - -
CHEMBL601877 IC50 - -
CHEMBL601446 IC50 - -