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Assay Detail

CHEMBL782596

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

Functional
Inhibition of 5-HT uptake in synaptosomal preparation from rat corpus striatum, using [3H]5-HT
65
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
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 6.15 7.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL284994 2 7.41
CHEMBL1743845 1 7.40
CHEMBL1788361 1 7.30
CHEMBL809 SERTRALINE 4.0 2 7.22
CHEMBL1709 SERTRALINE HYDROCHLORIDE 4.0 1 7.16
CHEMBL39354 1 7.16
CHEMBL37714 2 7.08
CHEMBL1743855 1 7.05
CHEMBL1788366 1 6.92
CHEMBL1743860 1 6.92
CHEMBL1743865 1 6.72
CHEMBL39405 1 6.72
CHEMBL38369 2 6.70
CHEMBL1788364 1 6.66
CHEMBL290359 1 6.66
CHEMBL1743872 1 6.62
CHEMBL1788367 1 6.60
CHEMBL1788370 1 6.58
CHEMBL1743854 1 6.47
CHEMBL417704 1 6.46
CHEMBL36050 2 6.43
CHEMBL1743868 1 6.42
CHEMBL1743851 1 6.42
CHEMBL39591 1 6.41
CHEMBL1743864 1 6.40
CHEMBL1743849 1 6.37
CHEMBL1743859 1 6.34
CHEMBL38340 1 6.31
CHEMBL1743874 1 6.30
CHEMBL36714 2 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL284994 IC50 = 39.0 nM 7.41
CHEMBL1743845 IC50 = 40.0 nM 7.40
CHEMBL1788361 IC50 = 50.0 nM 7.30
CHEMBL809 SERTRALINE IC50 = 60.0 nM 7.22
CHEMBL1709 SERTRALINE HYDROCHLORIDE IC50 = 70.0 nM 7.16
CHEMBL39354 IC50 = 70.0 nM 7.16
CHEMBL37714 IC50 = 84.0 nM 7.08
CHEMBL1743855 IC50 = 90.0 nM 7.05
CHEMBL1788366 IC50 = 120.0 nM 6.92
CHEMBL1743860 IC50 = 120.0 nM 6.92
CHEMBL1743865 IC50 = 190.0 nM 6.72
CHEMBL39405 IC50 = 190.0 nM 6.72
CHEMBL38369 IC50 = 200.0 nM 6.70
CHEMBL290359 IC50 = 220.0 nM 6.66
CHEMBL1788364 IC50 = 220.0 nM 6.66
CHEMBL1743872 IC50 = 240.0 nM 6.62
CHEMBL1788367 IC50 = 250.0 nM 6.60
CHEMBL1788370 IC50 = 260.0 nM 6.58
CHEMBL1743854 IC50 = 340.0 nM 6.47
CHEMBL417704 IC50 = 350.0 nM 6.46
CHEMBL36050 IC50 = 370.0 nM 6.43
CHEMBL1743868 IC50 = 380.0 nM 6.42
CHEMBL1743851 IC50 = 380.0 nM 6.42
CHEMBL39591 IC50 = 390.0 nM 6.41
CHEMBL1743864 IC50 = 400.0 nM 6.40
CHEMBL1743849 IC50 = 430.0 nM 6.37
CHEMBL809 SERTRALINE IC50 = 460.0 nM 6.34
CHEMBL1743859 IC50 = 460.0 nM 6.34
CHEMBL284994 IC50 = 470.0 nM 6.33
CHEMBL38340 IC50 = 490.0 nM 6.31
CHEMBL1743874 IC50 = 500.0 nM 6.30
CHEMBL36714 IC50 = 500.0 nM 6.30
CHEMBL814 FLUVOXAMINE IC50 = 540.0 nM 6.27
CHEMBL1743844 IC50 = 580.0 nM 6.24
CHEMBL287499 IC50 = 600.0 nM 6.22
CHEMBL1743848 IC50 = 700.0 nM 6.16
CHEMBL1743852 IC50 = 760.0 nM 6.12
CHEMBL1788369 IC50 = 820.0 nM 6.09
CHEMBL11 IMIPRAMINE IC50 = 810.0 nM 6.09
CHEMBL38120 TAMETRALINE IC50 = 840.0 nM 6.08
CHEMBL1743858 IC50 = 1050.0 nM 5.98
CHEMBL39856 IC50 = 1100.0 nM 5.96
CHEMBL36050 IC50 = 1220.0 nM 5.91
CHEMBL1743861 IC50 = 1400.0 nM 5.85
CHEMBL1788368 TAMETRALINE HYDROCHLORIDE IC50 = 1480.0 nM 5.83
CHEMBL1743873 IC50 = 1600.0 nM 5.80
CHEMBL1743846 IC50 = 1700.0 nM 5.77
CHEMBL39856 IC50 = 2200.0 nM 5.66
CHEMBL36714 IC50 = 2300.0 nM 5.64
CHEMBL38369 IC50 = 3100.0 nM 5.51