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Assay Detail

CHEMBL747096

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

Binding
Tested for the binding affinity towards Norepinephrine transporter in rat cerebral cortex by displacing [3H]nisoxetine radioligand
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebral cortex
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and transporter binding properties of 3beta-[4'-(phenylalkyl, -phenylalkenyl, and -phenylalkynyl)phenyl]tropane-2beta-carboxylic acid methyl esters: evidence of a remote phenyl binding domain on the dopamine transporter.
Blough BE, Keverline KI, Nie Z, Navarro H, Kuhar MJ, Carroll FI.
J Med Chem (2002) 45 : 4029 -4037
PubMed 12190324 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 6.46 8.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2310877 1 8.19
CHEMBL2310867 1 7.90
CHEMBL2310871 1 7.78
CHEMBL2373962 1 7.44
CHEMBL2310874 1 7.37
CHEMBL2310868 1 7.33
CHEMBL3350431 1 7.30
CHEMBL1790051 1 7.26
CHEMBL2310872 1 6.68
CHEMBL84680 1 6.65
CHEMBL2310869 1 6.31
CHEMBL2310880 1 6.22
CHEMBL2310881 1 6.12
CHEMBL2310873 1 6.05
CHEMBL2310876 1 6.05
CHEMBL2310884 1 6.02
CHEMBL2310883 1 5.93
CHEMBL2310865 1 5.86
CHEMBL50157 1 5.63
CHEMBL2310866 1 5.63
CHEMBL2310875 1 5.57
CHEMBL2310879 1 5.37
CHEMBL2310870 1 5.24
CHEMBL2310878 1 5.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2310877 Ki = 6.5 nM 8.19
CHEMBL2310867 Ki = 12.7 nM 7.90
CHEMBL2310871 Ki = 16.5 nM 7.78
CHEMBL2373962 Ki = 36.0 nM 7.44
CHEMBL2310874 Ki = 42.3 nM 7.37
CHEMBL2310868 Ki = 47.0 nM 7.33
CHEMBL3350431 Ki = 50.1 nM 7.30
CHEMBL1790051 Ki = 55.0 nM 7.26
CHEMBL2310872 Ki = 209.0 nM 6.68
CHEMBL84680 Ki = 224.0 nM 6.65
CHEMBL2310869 Ki = 494.0 nM 6.31
CHEMBL2310880 Ki = 606.0 nM 6.22
CHEMBL2310881 Ki = 759.0 nM 6.12
CHEMBL2310873 Ki = 885.0 nM 6.05
CHEMBL2310876 Ki = 892.0 nM 6.05
CHEMBL2310884 Ki = 958.0 nM 6.02
CHEMBL2310883 Ki = 1180.0 nM 5.93
CHEMBL2310865 Ki = 1390.0 nM 5.86
CHEMBL50157 Ki = 2360.0 nM 5.63
CHEMBL2310866 Ki = 2360.0 nM 5.63
CHEMBL2310875 Ki = 2680.0 nM 5.57
CHEMBL2310879 Ki = 4260.0 nM 5.37
CHEMBL2310870 Ki = 5720.0 nM 5.24
CHEMBL2310878 Ki = 8500.0 nM 5.07