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Assay Detail

CHEMBL1068124

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

Binding
Displacement of [3HDTBZ from VMAT2 in rat whole brain vesicles by liquid scintillation spectrophotometry
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Synaptic vesicular amine transporter (CHEMBL4828)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters.
Hojahmat M, Horton DB, Norrholm SD, Miller DK, Grinevich VP, Deaciuc AG, Dwoskin LP, Crooks PA.
Bioorg Med Chem (2010) 18 : 640 -649
PubMed 20036131 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.45 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL603692 1 5.70
CHEMBL599268 1 5.68
CHEMBL599267 1 5.61
CHEMBL597298 1 5.52
CHEMBL597297 1 5.49
CHEMBL596683 1 5.46
CHEMBL604306 1 5.40
CHEMBL605420 1 5.38
CHEMBL605748 1 5.37
CHEMBL597299 1 5.37
CHEMBL597085 1 4.97

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL603692 Ki = 1980.0 nM 5.70
CHEMBL599268 Ki = 2090.0 nM 5.68
CHEMBL599267 Ki = 2480.0 nM 5.61
CHEMBL597298 Ki = 3000.0 nM 5.52
CHEMBL597297 Ki = 3240.0 nM 5.49
CHEMBL596683 Ki = 3500.0 nM 5.46
CHEMBL604306 Ki = 3980.0 nM 5.40
CHEMBL605420 Ki = 4120.0 nM 5.38
CHEMBL605748 Ki = 4230.0 nM 5.37
CHEMBL597299 Ki = 4230.0 nM 5.37
CHEMBL597085 Ki = 10800.0 nM 4.97