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Assay Detail

CHEMBL3767207

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

Binding
Displacement of [3H]methyllycaconitine from Sprague-Dawley rat brain alpha7* nAChR incubated for 2.5 hrs by liquid scintillation counting analysis
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

New quinoline derivatives as nicotinic receptor modulators.
Manetti D, Bellucci C, Dei S, Teodori E, Varani K, Spirova E, Kudryavtsev D, Shelukhina I, Tsetlin V, Romanelli MN.
Eur J Med Chem (2016) 110 : 246 -258
PubMed 26840365 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.51 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3764582 1 8.85
CHEMBL2151572 ENCENICLINE 3.0 1 8.00
CHEMBL2151442 1 7.96
CHEMBL604798 1 7.87
CHEMBL559478 SSR180711 2.0 1 7.66
CHEMBL177611 PNU-282987 1 7.62
CHEMBL3763220 1 7.02
CHEMBL3764496 1 6.93
CHEMBL3764445 1 6.61
CHEMBL3765305 1 6.54
CHEMBL3764287 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3764582 Ki = 1.4 nM 8.85
CHEMBL2151572 ENCENICLINE Ki = 9.98 nM 8.00
CHEMBL2151442 Ki = 11.0 nM 7.96
CHEMBL604798 Ki = 13.5 nM 7.87
CHEMBL559478 SSR180711 Ki = 22.0 nM 7.66
CHEMBL177611 PNU-282987 Ki = 24.0 nM 7.62
CHEMBL3763220 Ki = 96.0 nM 7.02
CHEMBL3764496 Ki = 117.0 nM 6.93
CHEMBL3764445 Ki = 248.0 nM 6.61
CHEMBL3765305 Ki = 287.0 nM 6.54
CHEMBL3764287 Ki > 1000.0 nM -