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Assay Detail

CHEMBL950332

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

Binding
Inhibition of [3H]Nisoxetine uptake in human noradrenaline transporter transfected HEK293 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent noradrenaline transporter (CHEMBL222)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

[4-(Phenoxy)pyridin-3-yl]methylamines: a new class of selective noradrenaline reuptake inhibitors.
Fish PV, Ryckmans T, Stobie A, Wakenhut F.
Bioorg Med Chem Lett (2008) 18 : 1795 -1798
PubMed 18313294 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.00 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14370 REBOXETINE 4.0 1 8.30
CHEMBL270791 1 8.00
CHEMBL273208 1 8.00
CHEMBL403363 1 7.89
CHEMBL256293 1 7.66
CHEMBL436673 1 7.57
CHEMBL405017 1 7.24
CHEMBL403251 1 7.13
CHEMBL401651 1 7.09
CHEMBL401550 1 6.88
CHEMBL258291 1 6.80
CHEMBL429759 1 6.75
CHEMBL404885 1 6.71
CHEMBL403956 1 6.63
CHEMBL440584 1 6.59
CHEMBL265951 1 6.53
CHEMBL261465 1 6.44
CHEMBL258292 1 6.36
CHEMBL408329 1 6.34
CHEMBL262357 1 6.04
CHEMBL270366 1 6.02

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14370 REBOXETINE Ki = 5.0 nM 8.30
CHEMBL270791 Ki = 10.0 nM 8.00
CHEMBL273208 Ki = 10.0 nM 8.00
CHEMBL403363 Ki = 13.0 nM 7.89
CHEMBL256293 Ki = 22.0 nM 7.66
CHEMBL436673 Ki = 27.0 nM 7.57
CHEMBL405017 Ki = 58.0 nM 7.24
CHEMBL403251 Ki = 74.0 nM 7.13
CHEMBL401651 Ki = 82.0 nM 7.09
CHEMBL401550 Ki = 131.0 nM 6.88
CHEMBL258291 Ki = 159.0 nM 6.80
CHEMBL429759 Ki = 179.0 nM 6.75
CHEMBL404885 Ki = 194.0 nM 6.71
CHEMBL403956 Ki = 232.0 nM 6.63
CHEMBL440584 Ki = 255.0 nM 6.59
CHEMBL265951 Ki = 296.0 nM 6.53
CHEMBL261465 Ki = 366.0 nM 6.44
CHEMBL258292 Ki = 438.0 nM 6.36
CHEMBL408329 Ki = 461.0 nM 6.34
CHEMBL262357 Ki = 921.0 nM 6.04
CHEMBL270366 Ki = 951.0 nM 6.02