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Assay Detail

CHEMBL1012269

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

Binding
Inhibition of [3H]NA reuptake in human noradrenaline transporter expressed in HEK293 cells
46
Total Activities
46
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

Designing rapid onset selective serotonin re-uptake inhibitors. 2: structure-activity relationships of substituted (aryl)benzylamines.
Middleton DS, Andrews M, Glossop P, Gymer G, Hepworth D, Jessiman A, Johnson PS, Mackenny M, Pitcher MJ, Rooker T, Stobie A, Tang K, Morgan P.
Bioorg Med Chem Lett (2008) 18 : 4018 -4021
PubMed 18571404 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 46 5.97 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL493263 1 7.30
CHEMBL257424 1 7.30
CHEMBL451165 1 7.30
CHEMBL479783 1 7.16
CHEMBL481306 1 6.89
CHEMBL257423 1 6.75
CHEMBL493040 1 6.70
CHEMBL443922 1 6.54
CHEMBL479999 1 6.37
CHEMBL502129 1 6.29
CHEMBL449015 1 6.28
CHEMBL446481 1 6.20
CHEMBL493264 1 6.19
CHEMBL474922 1 6.17
CHEMBL479410 1 6.16
CHEMBL452376 1 6.12
CHEMBL383706 1 6.11
CHEMBL482292 1 5.98
CHEMBL492842 1 5.89
CHEMBL491268 1 5.89
CHEMBL507422 1 5.85
CHEMBL481526 1 5.82
CHEMBL493057 1 5.70
CHEMBL479411 1 5.70
CHEMBL481124 1 5.57
CHEMBL481696 1 5.54
CHEMBL482293 1 5.52
CHEMBL493476 1 5.51
CHEMBL481695 1 5.38
CHEMBL448689 1 5.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL493263 IC50 = 50.0 nM 7.30
CHEMBL451165 IC50 = 50.0 nM 7.30
CHEMBL257424 IC50 = 50.0 nM 7.30
CHEMBL479783 IC50 = 70.0 nM 7.16
CHEMBL481306 IC50 = 130.0 nM 6.89
CHEMBL257423 IC50 = 180.0 nM 6.75
CHEMBL493040 IC50 = 200.0 nM 6.70
CHEMBL443922 IC50 = 290.0 nM 6.54
CHEMBL479999 IC50 = 430.0 nM 6.37
CHEMBL502129 IC50 = 510.0 nM 6.29
CHEMBL449015 IC50 = 530.0 nM 6.28
CHEMBL446481 IC50 = 630.0 nM 6.20
CHEMBL493264 IC50 = 640.0 nM 6.19
CHEMBL474922 IC50 = 680.0 nM 6.17
CHEMBL479410 IC50 = 700.0 nM 6.16
CHEMBL452376 IC50 = 760.0 nM 6.12
CHEMBL383706 IC50 = 770.0 nM 6.11
CHEMBL482292 IC50 = 1050.0 nM 5.98
CHEMBL492842 IC50 = 1300.0 nM 5.89
CHEMBL491268 IC50 = 1300.0 nM 5.89
CHEMBL507422 IC50 = 1400.0 nM 5.85
CHEMBL481526 IC50 = 1500.0 nM 5.82
CHEMBL479411 IC50 = 2000.0 nM 5.70
CHEMBL493057 IC50 = 2000.0 nM 5.70
CHEMBL481124 IC50 = 2700.0 nM 5.57
CHEMBL481696 IC50 = 2900.0 nM 5.54
CHEMBL482293 IC50 = 3000.0 nM 5.52
CHEMBL493476 IC50 = 3100.0 nM 5.51
CHEMBL481695 IC50 = 4200.0 nM 5.38
CHEMBL448689 IC50 = 4900.0 nM 5.31
CHEMBL481697 IC50 = 5600.0 nM 5.25
CHEMBL493056 IC50 = 6000.0 nM 5.22
CHEMBL482295 IC50 = 6400.0 nM 5.19
CHEMBL481353 IC50 = 6700.0 nM 5.17
CHEMBL492841 IC50 = 7300.0 nM 5.14
CHEMBL451120 IC50 = 7900.0 nM 5.10
CHEMBL453493 IC50 = 8600.0 nM 5.07
CHEMBL493027 IC50 = 9200.0 nM 5.04
CHEMBL493058 IC50 - -
CHEMBL493667 IC50 - -
CHEMBL500629 IC50 > 10000.0 nM -
CHEMBL479409 IC50 > 10000.0 nM -
CHEMBL520760 IC50 - -
CHEMBL482294 IC50 > 10000.0 nM -
CHEMBL481527 IC50 > 10000.0 nM -
CHEMBL481941 IC50 - -