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Assay Detail

CHEMBL805322

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Binding
Binding affinity to the serotonin transporter (SERT) measured by displacement of [3H]paroxetine in male wistar rats
80
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters.
Orjales A, Mosquera R, Toledo A, Pumar MC, García N, Cortizo L, Labeaga L, Innerárity A.
J Med Chem (2003) 46 : 5512 -5532
PubMed 14640559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 80 8.05 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152254 3 9.40
CHEMBL149971 3 9.22
CHEMBL490 PAROXETINE 4.0 1 9.15
CHEMBL357051 1 9.05
CHEMBL150442 1 9.05
CHEMBL153093 3 9.00
CHEMBL152935 3 9.00
CHEMBL348704 3 8.85
CHEMBL356400 3 8.82
CHEMBL358168 1 8.72
CHEMBL149697 1 8.70
CHEMBL357565 3 8.70
CHEMBL447188 1 8.64
CHEMBL356849 1 8.59
CHEMBL152141 3 8.55
CHEMBL149970 1 8.43
CHEMBL436069 1 8.41
CHEMBL149641 3 8.38
CHEMBL151140 1 8.38
CHEMBL345277 3 8.37
CHEMBL153504 1 8.28
CHEMBL356403 1 8.24
CHEMBL153185 1 8.12
CHEMBL356482 1 8.09
CHEMBL150932 3 8.08
CHEMBL153127 1 8.05
CHEMBL152930 1 8.00
CHEMBL151010 1 8.00
CHEMBL153533 1 7.91
CHEMBL153735 1 7.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152254 Ki = 0.4 nM 9.40
CHEMBL149971 Ki = 0.6 nM 9.22
CHEMBL490 PAROXETINE Ki = 0.7 nM 9.15
CHEMBL357051 Ki = 0.9 nM 9.05
CHEMBL150442 Ki = 0.9 nM 9.05
CHEMBL153093 Ki = 1.0 nM 9.00
CHEMBL152935 Ki = 1.0 nM 9.00
CHEMBL152254 Ki = 1.1 nM 8.96
CHEMBL153093 Ki = 1.4 nM 8.85
CHEMBL153093 Ki = 1.4 nM 8.85
CHEMBL348704 Ki = 1.4 nM 8.85
CHEMBL356400 Ki = 1.5 nM 8.82
CHEMBL358168 Ki = 1.9 nM 8.72
CHEMBL152935 Ki = 1.9 nM 8.72
CHEMBL149697 Ki = 2.0 nM 8.70
CHEMBL357565 Ki = 2.0 nM 8.70
CHEMBL447188 Ki = 2.3 nM 8.64
CHEMBL149971 Ki = 2.4 nM 8.62
CHEMBL356400 Ki = 2.6 nM 8.59
CHEMBL356849 Ki = 2.6 nM 8.59
CHEMBL152141 Ki = 2.8 nM 8.55
CHEMBL356400 Ki = 3.0 nM 8.52
CHEMBL348704 Ki = 3.4 nM 8.47
CHEMBL149970 Ki = 3.7 nM 8.43
CHEMBL436069 Ki = 3.9 nM 8.41
CHEMBL151140 Ki = 4.2 nM 8.38
CHEMBL149641 Ki = 4.2 nM 8.38
CHEMBL345277 Ki = 4.3 nM 8.37
CHEMBL153504 Ki = 5.3 nM 8.28
CHEMBL357565 Ki = 5.7 nM 8.24
CHEMBL356403 Ki = 5.8 nM 8.24
CHEMBL149641 Ki = 6.3 nM 8.20
CHEMBL348704 Ki = 7.1 nM 8.15
CHEMBL152935 Ki = 7.3 nM 8.14
CHEMBL153185 Ki = 7.5 nM 8.12
CHEMBL356482 Ki = 8.2 nM 8.09
CHEMBL150932 Ki = 8.3 nM 8.08
CHEMBL153127 Ki = 9.0 nM 8.05
CHEMBL345277 Ki = 9.3 nM 8.03
CHEMBL152930 Ki = 9.9 nM 8.00
CHEMBL151010 Ki = 10.0 nM 8.00
CHEMBL152141 Ki = 10.0 nM 8.00
CHEMBL153533 Ki = 12.2 nM 7.91
CHEMBL153735 Ki = 13.9 nM 7.86
CHEMBL359345 Ki = 14.1 nM 7.85
CHEMBL346882 Ki = 14.9 nM 7.83
CHEMBL149971 Ki = 15.1 nM 7.82
CHEMBL153532 Ki = 15.6 nM 7.81
CHEMBL153676 Ki = 15.5 nM 7.81
CHEMBL152141 Ki = 16.1 nM 7.79