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Assay Detail

CHEMBL919235

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

Binding
Displacement of [125I]iodoMLA from alpha-7 nAChR in rat cerebral cortex
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs.
Ivy Carroll F, Ma W, Navarro HA, Abraham P, Wolckenhauer SA, Damaj MI, Martin BR.
Bioorg Med Chem (2007) 15 : 678 -685
PubMed 17098430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 8.57 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL510275 METHYLLYCACONITINE 1 9.06
CHEMBL413306 PHENYLLYCACONITINE 1 8.78
CHEMBL387363 1 8.75
CHEMBL3349999 1 8.67
CHEMBL442048 1 8.61
CHEMBL267682 CYCLOHEXYLLYCACONITINE 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL510275 METHYLLYCACONITINE Ki = 0.87 nM 9.06
CHEMBL413306 PHENYLLYCACONITINE Ki = 1.67 nM 8.78
CHEMBL387363 Ki = 1.78 nM 8.75
CHEMBL3349999 Ki = 2.12 nM 8.67
CHEMBL442048 Ki = 2.46 nM 8.61
CHEMBL267682 CYCLOHEXYLLYCACONITINE Ki = 26.8 nM 7.57