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Assay Detail

CHEMBL747859

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

Binding
Inhibitory concentration required for in vitro binding affinity to cholinergic central Nicotinic acetylcholine receptor on rat brain cortex by using [3H]MCC
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor (CHEMBL2094110)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Identification of novel (isoxazole)methylene-1-azabicyclic compounds with high affinity for the central nicotinic cholinergic receptor
Olesen P, Swedberg M, Eskesen K, Judge M, Egebjerg J, Tnder J, Rasmussen T, Sheardown M, Rimvall K
Bioorg Med Chem Lett (1997) 7 : 1963 -1968
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 7.44 8.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL58416 1 8.47
CHEMBL3 NICOTINE 4.0 1 8.40
CHEMBL291780 1 7.64
CHEMBL291442 1 7.58
CHEMBL274525 ABT-418 1 7.28
CHEMBL144540 1 7.07
CHEMBL60656 1 6.77
CHEMBL293142 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL58416 IC50 = 3.4 nM 8.47
CHEMBL3 NICOTINE IC50 = 4.0 nM 8.40
CHEMBL291780 IC50 = 23.0 nM 7.64
CHEMBL291442 IC50 = 26.0 nM 7.58
CHEMBL274525 ABT-418 IC50 = 53.0 nM 7.28
CHEMBL144540 IC50 = 85.0 nM 7.07
CHEMBL60656 IC50 = 170.0 nM 6.77
CHEMBL293142 IC50 = 500.0 nM 6.30