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Assay Detail

CHEMBL1785124

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ADMET
Activity at alpha3beta4* nAChR in mouse interpeduncular nucleus assessed as [3H]ACh release by scintillation counting relative to control
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Mus musculus
Tissue Interpeduncular nucleus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Publication

Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Breining SR, Bencherif M, Grady SR, Whiteaker P, Marks MJ, Wageman CR, Lester HA, Yohannes D.
Bioorg Med Chem Lett (2009) 19 : 4359 -4363
PubMed 19560354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 12 5.07 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217150 1 6.40
CHEMBL1783886 1 5.62
CHEMBL1783881 1 5.48
CHEMBL1782074 1 5.25
CHEMBL1783880 1 5.02
CHEMBL1783883 1 4.80
CHEMBL3215819 1 4.68
CHEMBL1783882 1 4.55
CHEMBL1783878 1 4.47
CHEMBL1783888 1 4.39
CHEMBL1783879 1 -
CHEMBL1783884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217150 EC50 = 400.0 nM 6.40
CHEMBL1783886 EC50 = 2400.0 nM 5.62
CHEMBL1783881 EC50 = 3300.0 nM 5.48
CHEMBL1782074 EC50 = 5600.0 nM 5.25
CHEMBL1783880 EC50 = 9500.0 nM 5.02
CHEMBL1783883 EC50 = 16000.0 nM 4.80
CHEMBL3215819 EC50 = 21000.0 nM 4.68
CHEMBL1783882 EC50 = 28000.0 nM 4.55
CHEMBL1783878 EC50 = 34000.0 nM 4.47
CHEMBL1783888 EC50 = 41000.0 nM 4.39
CHEMBL1783879 EC50 = 218000.0 nM -
CHEMBL1783884 EC50 = 161000.0 nM -