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Assay Detail

CHEMBL748707

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Binding
Evaluated for its binding affinity towards Nicotinic acetylcholine receptor in rat brain homogenate
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Lobeline: structure-affinity investigation of nicotinic acetylcholinergic receptor binding.
Flammia D, Dukat M, Damaj MI, Martin B, Glennon RA.
J Med Chem (1999) 42 : 3726 -3731
PubMed 10479304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 6.34 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122270 LOBELINE 2.0 1 8.40
CHEMBL333898 1 8.30
CHEMBL122425 1 6.96
CHEMBL122317 1 6.63
CHEMBL122676 1 6.52
CHEMBL125511 8R-hydroxylobelane 1 6.47
CHEMBL339402 1 5.96
CHEMBL124219 1 5.88
CHEMBL433194 1 5.69
CHEMBL332074 1 5.66
CHEMBL121876 1 5.60
CHEMBL50115 1 5.23
CHEMBL331161 1 5.11
CHEMBL122636 1 -
CHEMBL122723 1 -
CHEMBL120990 1 -
CHEMBL122314 1 -
CHEMBL333465 LOBELANE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122270 LOBELINE Ki = 4.0 nM 8.40
CHEMBL333898 Ki = 5.0 nM 8.30
CHEMBL122425 Ki = 110.0 nM 6.96
CHEMBL122317 Ki = 235.0 nM 6.63
CHEMBL122676 Ki = 300.0 nM 6.52
CHEMBL125511 8R-hydroxylobelane Ki = 340.0 nM 6.47
CHEMBL339402 Ki = 1085.0 nM 5.96
CHEMBL124219 Ki = 1315.0 nM 5.88
CHEMBL433194 Ki = 2035.0 nM 5.69
CHEMBL332074 Ki = 2200.0 nM 5.66
CHEMBL121876 Ki = 2490.0 nM 5.60
CHEMBL50115 Ki = 5900.0 nM 5.23
CHEMBL331161 Ki = 7800.0 nM 5.11
CHEMBL122636 Ki > 10000.0 nM -
CHEMBL122723 Ki > 10000.0 nM -
CHEMBL120990 Ki > 10000.0 nM -
CHEMBL122314 Ki > 10000.0 nM -
CHEMBL333465 LOBELANE Ki > 10000.0 nM -