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Assay Detail

CHEMBL804187

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

Binding
Inhibition of [3H]peroxitine binding to rat cortical membranes as measure of inhibitory activity towards 5-HT uptake
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

New indole derivatives as potent and selective serotonin uptake inhibitors.
Malleron JL, Guérémy C, Mignani S, Peyronel JF, Truchon A, Blanchard JC, Doble A, Laduron P, Piot O, Zundel JL.
J Med Chem (1993) 36 : 1194 -1202
PubMed 8487257 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 8.56 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL19613 1 9.70
CHEMBL18224 1 9.52
CHEMBL19267 1 9.52
CHEMBL18512 1 9.40
CHEMBL19347 1 9.40
CHEMBL19111 1 9.22
CHEMBL274517 1 9.22
CHEMBL19203 1 9.10
CHEMBL19051 1 8.96
CHEMBL274728 RP-68303 1 8.92
CHEMBL18501 1 8.85
CHEMBL429768 1 8.85
CHEMBL278080 1 8.80
CHEMBL18625 1 8.77
CHEMBL276920 1 8.70
CHEMBL19270 1 8.40
CHEMBL276922 1 8.30
CHEMBL416544 1 8.30
CHEMBL275354 1 8.22
CHEMBL18212 1 8.00
CHEMBL276565 1 8.00
CHEMBL279414 1 8.00
CHEMBL281808 1 7.96
CHEMBL41 FLUOXETINE 4.0 1 7.82
CHEMBL19228 1 7.66
CHEMBL19652 1 7.60
CHEMBL19226 1 7.46
CHEMBL19335 1 7.00
CHEMBL414187 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL19613 IC50 = 0.2 nM 9.70
CHEMBL18224 IC50 = 0.3 nM 9.52
CHEMBL19267 IC50 = 0.3 nM 9.52
CHEMBL18512 IC50 = 0.4 nM 9.40
CHEMBL19347 IC50 = 0.4 nM 9.40
CHEMBL19111 IC50 = 0.6 nM 9.22
CHEMBL274517 IC50 = 0.6 nM 9.22
CHEMBL19203 IC50 = 0.8 nM 9.10
CHEMBL19051 IC50 = 1.1 nM 8.96
CHEMBL274728 RP-68303 IC50 = 1.2 nM 8.92
CHEMBL18501 IC50 = 1.4 nM 8.85
CHEMBL429768 IC50 = 1.4 nM 8.85
CHEMBL278080 IC50 = 1.6 nM 8.80
CHEMBL18625 IC50 = 1.7 nM 8.77
CHEMBL276920 IC50 = 2.0 nM 8.70
CHEMBL19270 IC50 = 4.0 nM 8.40
CHEMBL276922 IC50 = 5.0 nM 8.30
CHEMBL416544 IC50 = 5.0 nM 8.30
CHEMBL275354 IC50 = 6.0 nM 8.22
CHEMBL18212 IC50 = 10.0 nM 8.00
CHEMBL276565 IC50 = 10.0 nM 8.00
CHEMBL279414 IC50 = 10.0 nM 8.00
CHEMBL281808 IC50 = 11.0 nM 7.96
CHEMBL41 FLUOXETINE IC50 = 15.0 nM 7.82
CHEMBL19228 IC50 = 22.0 nM 7.66
CHEMBL19652 IC50 = 25.0 nM 7.60
CHEMBL19226 IC50 = 35.0 nM 7.46
CHEMBL19335 IC50 = 100.0 nM 7.00
CHEMBL414187 IC50 > 100.0 nM -