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Assay Detail

CHEMBL783715

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Functional
Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine
ChEMBL ↗
65
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Hypothalamus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304) ↗
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Nontricyclic antidepressant agents derived from cis- and trans-1-amino-4-aryltetralins.
Welch WM, Kraska AR, Sarges R, Koe BK.
J Med Chem (1984) 27 : 1508 -1515
PubMed 6492080 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.18 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284994 — — 2 8.00
CHEMBL38120 TAMETRALINE 2.0 2 7.75
CHEMBL37714 — — 2 7.72
CHEMBL1788361 — — 1 7.70
CHEMBL273575 NOMIFENSINE 4.0 1 7.70
CHEMBL1788366 — — 1 7.52
CHEMBL1743844 — — 1 7.52
CHEMBL1743855 — — 1 7.52
CHEMBL1743845 — — 1 7.40
CHEMBL1788368 TAMETRALINE HYDROCHLORIDE -1.0 1 7.40
CHEMBL1743854 — — 1 7.22
CHEMBL11 IMIPRAMINE 4.0 1 7.22
CHEMBL1743860 — — 1 6.89
CHEMBL1743859 — — 1 6.85
CHEMBL1743851 — — 1 6.82
CHEMBL1743864 — — 1 6.60
CHEMBL39591 — — 1 6.58
CHEMBL809 SERTRALINE 4.0 2 6.52
CHEMBL1743873 — — 1 6.51
CHEMBL1743874 — — 1 6.51
CHEMBL287499 — — 1 6.47
CHEMBL39354 — — 1 6.40
CHEMBL1743857 — — 1 6.32
CHEMBL1743849 — — 1 6.16
CHEMBL1709 SERTRALINE HYDROCHLORIDE 4.0 1 6.14
CHEMBL1743861 — — 1 6.05
CHEMBL39405 — — 1 6.05
CHEMBL1743869 — — 1 6.03
CHEMBL1743858 — — 1 6.01
CHEMBL36714 — — 2 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284994 — IC50 = 10.0 nM 8.00
CHEMBL38120 TAMETRALINE IC50 = 18.0 nM 7.75
CHEMBL37714 — IC50 = 19.0 nM 7.72
CHEMBL1788361 — IC50 = 20.0 nM 7.70
CHEMBL273575 NOMIFENSINE IC50 = 20.0 nM 7.70
CHEMBL1788366 — IC50 = 30.0 nM 7.52
CHEMBL1743844 — IC50 = 30.0 nM 7.52
CHEMBL1743855 — IC50 = 30.0 nM 7.52
CHEMBL1743845 — IC50 = 40.0 nM 7.40
CHEMBL1788368 TAMETRALINE HYDROCHLORIDE IC50 = 40.0 nM 7.40
CHEMBL284994 — IC50 = 44.0 nM 7.36
CHEMBL1743854 — IC50 = 60.0 nM 7.22
CHEMBL11 IMIPRAMINE IC50 = 60.0 nM 7.22
CHEMBL1743860 — IC50 = 130.0 nM 6.89
CHEMBL1743859 — IC50 = 140.0 nM 6.85
CHEMBL1743851 — IC50 = 150.0 nM 6.82
CHEMBL1743864 — IC50 = 250.0 nM 6.60
CHEMBL39591 — IC50 = 260.0 nM 6.58
CHEMBL809 SERTRALINE IC50 = 300.0 nM 6.52
CHEMBL1743873 — IC50 = 310.0 nM 6.51
CHEMBL1743874 — IC50 = 310.0 nM 6.51
CHEMBL287499 — IC50 = 340.0 nM 6.47
CHEMBL38120 TAMETRALINE IC50 = 370.0 nM 6.43
CHEMBL39354 — IC50 = 400.0 nM 6.40
CHEMBL37714 — IC50 = 460.0 nM 6.34
CHEMBL1743857 — IC50 = 480.0 nM 6.32
CHEMBL1743849 — IC50 = 690.0 nM 6.16
CHEMBL1709 SERTRALINE HYDROCHLORIDE IC50 = 720.0 nM 6.14
CHEMBL39405 — IC50 = 890.0 nM 6.05
CHEMBL1743861 — IC50 = 890.0 nM 6.05
CHEMBL1743869 — IC50 = 940.0 nM 6.03
CHEMBL1743858 — IC50 = 970.0 nM 6.01
CHEMBL36714 — IC50 = 1050.0 nM 5.98
CHEMBL1743856 — IC50 = 1150.0 nM 5.94
CHEMBL1743872 — IC50 = 1160.0 nM 5.94
CHEMBL809 SERTRALINE IC50 = 1200.0 nM 5.92
CHEMBL1788370 — IC50 = 1410.0 nM 5.85
CHEMBL1743865 — IC50 = 1400.0 nM 5.85
CHEMBL1743852 — IC50 = 1400.0 nM 5.85
CHEMBL290359 — IC50 = 1400.0 nM 5.85
CHEMBL36260 — IC50 = 1800.0 nM 5.75
CHEMBL1788365 — IC50 = 1860.0 nM 5.73
CHEMBL814 FLUVOXAMINE IC50 = 1900.0 nM 5.72
CHEMBL1743846 — IC50 = 2300.0 nM 5.64
CHEMBL1743870 — IC50 = 2300.0 nM 5.64
CHEMBL36050 — IC50 = 2300.0 nM 5.64
CHEMBL1743853 — IC50 = 2300.0 nM 5.64
CHEMBL1788367 — IC50 = 2550.0 nM 5.59
CHEMBL38369 — IC50 = 2700.0 nM 5.57
CHEMBL1743848 — IC50 = 3000.0 nM 5.52