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Assay Detail

CHEMBL873467

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

Binding
Binding affinity against Serotonin transporter in rat cerebral cortex using [3H]paroxetine binding assay.
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Dual NK(1) antagonists--serotonin reuptake inhibitors as potential antidepressants. Part 2: SAR and activity of benzyloxyphenethyl piperazine derivatives.
Ryckmans T, Berton O, Grimée R, Kogej T, Lamberty Y, Pasau P, Talaga P, Genicot C.
Bioorg Med Chem Lett (2002) 12 : 3195 -3198
PubMed 12372532 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.29 9.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL111303 1 9.10
CHEMBL107941 1 8.60
CHEMBL41 FLUOXETINE 4.0 1 8.20
CHEMBL432627 1 8.20
CHEMBL111244 1 8.10
CHEMBL108667 1 8.00
CHEMBL107831 1 7.90
CHEMBL320535 1 7.80
CHEMBL111176 1 7.60
CHEMBL107829 1 7.50
CHEMBL320544 1 7.00
CHEMBL109514 1 6.80
CHEMBL109183 1 6.70
CHEMBL108200 1 6.70
CHEMBL108889 1 6.70
CHEMBL321892 1 6.70
CHEMBL108422 1 6.60
CHEMBL419742 1 6.60
CHEMBL109937 1 6.60
CHEMBL107875 1 6.50
CHEMBL110086 1 6.50
CHEMBL111304 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL111303 IC50 = 0.7943 nM 9.10
CHEMBL107941 IC50 = 2.512 nM 8.60
CHEMBL41 FLUOXETINE IC50 = 6.31 nM 8.20
CHEMBL432627 IC50 = 6.31 nM 8.20
CHEMBL111244 IC50 = 7.943 nM 8.10
CHEMBL108667 IC50 = 10.0 nM 8.00
CHEMBL107831 IC50 = 12.59 nM 7.90
CHEMBL320535 IC50 = 15.85 nM 7.80
CHEMBL111176 IC50 = 25.12 nM 7.60
CHEMBL107829 IC50 = 31.62 nM 7.50
CHEMBL320544 IC50 = 100.0 nM 7.00
CHEMBL109514 IC50 = 158.49 nM 6.80
CHEMBL109183 IC50 = 199.53 nM 6.70
CHEMBL108200 IC50 = 199.53 nM 6.70
CHEMBL108889 IC50 = 199.53 nM 6.70
CHEMBL321892 IC50 = 199.53 nM 6.70
CHEMBL108422 IC50 = 251.19 nM 6.60
CHEMBL419742 IC50 = 251.19 nM 6.60
CHEMBL109937 IC50 = 251.19 nM 6.60
CHEMBL107875 IC50 = 316.23 nM 6.50
CHEMBL110086 IC50 = 316.23 nM 6.50
CHEMBL111304 IC50 = 1000.0 nM 6.00