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Assay Detail

CHEMBL829602

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

Binding
Displacement of [3H]-nisoxetine from norepinephrine transporter of rat cerebral corticex homogenate
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and amine transporter affinities of novel phenyltropane derivatives as potential positron emission tomography (PET) imaging agents.
Peng X, Zhang A, Kula NS, Baldessarini RJ, Neumeyer JL.
Bioorg Med Chem Lett (2004) 14 : 5635 -5639
PubMed 15482938 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.38 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365623 1 8.99
CHEMBL184123 1 8.69
CHEMBL184807 1 8.05
CHEMBL186119 1 7.82
CHEMBL97887 1 7.82
CHEMBL318961 1 6.94
CHEMBL433159 1 6.71
CHEMBL362565 1 6.65
CHEMBL365649 1 6.61
CHEMBL185608 1 6.55
CHEMBL187299 1 6.38
CHEMBL183259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365623 Ki = 1.02 nM 8.99
CHEMBL184123 Ki = 2.03 nM 8.69
CHEMBL184807 Ki = 8.85 nM 8.05
CHEMBL186119 Ki = 15.2 nM 7.82
CHEMBL97887 Ki = 15.3 nM 7.82
CHEMBL318961 Ki = 116.0 nM 6.94
CHEMBL433159 Ki = 196.0 nM 6.71
CHEMBL362565 Ki = 225.0 nM 6.65
CHEMBL365649 Ki = 244.0 nM 6.61
CHEMBL185608 Ki = 280.0 nM 6.55
CHEMBL187299 Ki = 413.0 nM 6.38
CHEMBL183259 Ki > 10000.0 nM -