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Assay Detail

CHEMBL830139

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

Binding
Inhibition of 3 nM [3H]-MLA binding to Nicotinic acetylcholine receptor alpha7 of rat brain membranes
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Defunctionalized lobeline analogues: structure-activity of novel ligands for the vesicular monoamine transporter.
Zheng G, Dwoskin LP, Deaciuc AG, Norrholm SD, Crooks PA.
J Med Chem (2005) 48 : 5551 -5560
PubMed 16107155 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 4.77 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL188912 1 5.62
CHEMBL122270 LOBELINE 2.0 1 5.20
CHEMBL190113 1 5.02
CHEMBL187455 1 4.82
CHEMBL191947 1 4.60
CHEMBL333465 LOBELANE 1 4.58
CHEMBL193292 1 4.47
CHEMBL190870 1 4.40
CHEMBL189788 1 4.26
CHEMBL372435 1 -
CHEMBL193224 1 -
CHEMBL194053 1 -
CHEMBL372892 1 -
CHEMBL192910 1 -
CHEMBL190555 1 -
CHEMBL193782 1 -
CHEMBL193571 1 -
CHEMBL192329 1 -
CHEMBL1794918 1 -
CHEMBL193079 1 -
CHEMBL424816 1 -
CHEMBL190691 1 -
CHEMBL192502 1 -
CHEMBL190319 1 -
CHEMBL190725 1 -
CHEMBL192574 1 -
CHEMBL192573 1 -
CHEMBL122636 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL188912 Ki = 2390.0 nM 5.62
CHEMBL122270 LOBELINE Ki = 6260.0 nM 5.20
CHEMBL190113 Ki = 9630.0 nM 5.02
CHEMBL187455 Ki = 15100.0 nM 4.82
CHEMBL191947 Ki = 25300.0 nM 4.60
CHEMBL333465 LOBELANE Ki = 26000.0 nM 4.58
CHEMBL193292 Ki = 33800.0 nM 4.47
CHEMBL190870 Ki = 40000.0 nM 4.40
CHEMBL189788 Ki = 55100.0 nM 4.26
CHEMBL372435 Ki > 100000.0 nM -
CHEMBL193224 Ki > 100000.0 nM -
CHEMBL194053 Ki > 100000.0 nM -
CHEMBL372892 Ki > 100000.0 nM -
CHEMBL192910 Ki > 100000.0 nM -
CHEMBL190555 Ki > 25200.0 nM -
CHEMBL193782 Ki > 100000.0 nM -
CHEMBL193571 Ki > 100000.0 nM -
CHEMBL192329 Ki > 100000.0 nM -
CHEMBL1794918 Ki > 100000.0 nM -
CHEMBL193079 Ki > 100000.0 nM -
CHEMBL424816 Ki > 100000.0 nM -
CHEMBL190691 Ki > 100000.0 nM -
CHEMBL192502 Ki > 100000.0 nM -
CHEMBL190319 Ki > 100000.0 nM -
CHEMBL190725 Ki > 100000.0 nM -
CHEMBL192574 Ki > 100000.0 nM -
CHEMBL192573 Ki > 100000.0 nM -
CHEMBL122636 Ki > 100000.0 nM -