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Assay Detail

CHEMBL1013151

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

Binding
Displacement of [3H]paroxetine from rat cortical 5HTT reuptake site
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Studies toward the discovery of the next generation of antidepressants. Part 6: Dual 5-HT1A receptor and serotonin transporter affinity within a class of arylpiperazinyl-cyclohexyl indole derivatives.
Zhou D, Zhou P, Evrard DA, Meagher K, Webb M, Harrison BL, Huryn DM, Golembieski J, Hornby GA, Schechter LE, Smith DL, Andree TH, Mewshaw RE.
Bioorg Med Chem (2008) 16 : 6707 -6723
PubMed 18571421 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 35 7.69 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL481113 1 8.96
CHEMBL481754 1 8.89
CHEMBL494276 1 8.80
CHEMBL41 FLUOXETINE 4.0 1 8.57
CHEMBL494484 1 8.48
CHEMBL480932 1 8.46
CHEMBL481747 1 8.34
CHEMBL520753 1 8.31
CHEMBL359495 1 8.28
CHEMBL494483 1 8.07
CHEMBL522529 1 7.94
CHEMBL522671 1 7.90
CHEMBL517996 1 7.89
CHEMBL518946 1 7.87
CHEMBL493684 1 7.87
CHEMBL481108 1 7.86
CHEMBL481914 1 7.70
CHEMBL481940 1 7.57
CHEMBL480935 1 7.42
CHEMBL493037 1 7.42
CHEMBL481753 1 7.41
CHEMBL178267 1 7.31
CHEMBL481112 1 7.24
CHEMBL481523 1 7.21
CHEMBL521110 1 7.20
CHEMBL493455 1 7.17
CHEMBL481109 1 7.14
CHEMBL481337 1 7.12
CHEMBL520265 1 7.12
CHEMBL494688 1 6.99

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL481113 Ki = 1.1 nM 8.96
CHEMBL481754 Ki = 1.3 nM 8.89
CHEMBL494276 Ki = 1.6 nM 8.80
CHEMBL41 FLUOXETINE Ki = 2.7 nM 8.57
CHEMBL494484 Ki = 3.3 nM 8.48
CHEMBL480932 Ki = 3.5 nM 8.46
CHEMBL481747 Ki = 4.6 nM 8.34
CHEMBL520753 Ki = 4.9 nM 8.31
CHEMBL359495 Ki = 5.3 nM 8.28
CHEMBL494483 Ki = 8.5 nM 8.07
CHEMBL522529 Ki = 11.6 nM 7.94
CHEMBL522671 Ki = 12.7 nM 7.90
CHEMBL517996 Ki = 13.0 nM 7.89
CHEMBL518946 Ki = 13.6 nM 7.87
CHEMBL493684 Ki = 13.4 nM 7.87
CHEMBL481108 Ki = 13.8 nM 7.86
CHEMBL481914 Ki = 20.0 nM 7.70
CHEMBL481940 Ki = 26.7 nM 7.57
CHEMBL493037 Ki = 38.0 nM 7.42
CHEMBL480935 Ki = 38.5 nM 7.42
CHEMBL481753 Ki = 39.3 nM 7.41
CHEMBL178267 Ki = 48.5 nM 7.31
CHEMBL481112 Ki = 58.2 nM 7.24
CHEMBL481523 Ki = 61.0 nM 7.21
CHEMBL521110 Ki = 62.5 nM 7.20
CHEMBL493455 Ki = 67.5 nM 7.17
CHEMBL481109 Ki = 73.0 nM 7.14
CHEMBL481337 Ki = 75.0 nM 7.12
CHEMBL520265 Ki = 75.0 nM 7.12
CHEMBL494688 Ki = 102.0 nM 6.99
CHEMBL481524 Ki = 105.0 nM 6.98
CHEMBL519616 Ki = 115.0 nM 6.94
CHEMBL494468 Ki = 155.0 nM 6.81
CHEMBL482266 Ki = 640.0 nM 6.19
CHEMBL31354 WAY-100,635 Ki - -