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Assay Detail

CHEMBL2185176

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

Functional
Agonist activity at human nAChR alpha6/alpha3beta2beta3 V273S mutant expressed in HEK293T cells by FLIPR
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK-293T
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity studies of 7-heteroaryl-3-azabicyclo[3.3.1]non-6-enes: a novel class of highly potent nicotinic receptor ligands.
Breining SR, Melvin M, Bhatti BS, Byrd GD, Kiser MN, Hepler CD, Hooker DN, Zhang J, Reynolds LA, Benson LR, Fedorov NB, Sidach SS, Mitchener JP, Lucero LM, Lukas RJ, Whiteaker P, Yohannes D.
J Med Chem (2012) 55 : 9929 -9945
PubMed 23025891 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.84 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2177538 1 7.85
CHEMBL2177537 1 7.82
CHEMBL2177545 1 -
CHEMBL2177544 1 -
CHEMBL2177543 1 -
CHEMBL2177540 1 -
CHEMBL2177539 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2177538 EC50 = 14.0 nM 7.85
CHEMBL2177537 EC50 = 15.0 nM 7.82
CHEMBL2177545 EC50 > 10000.0 nM -
CHEMBL2177544 EC50 > 10000.0 nM -
CHEMBL2177543 EC50 > 10000.0 nM -
CHEMBL2177540 EC50 > 10000.0 nM -
CHEMBL2177539 EC50 > 10000.0 nM -