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Assay Detail

CHEMBL806555

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

Binding
Inhibition of [3H]paroxetine binding to serotonin transporter in rat frontal cortex
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and transporter binding properties of 3 beta-(4'-alkyl-, 4'-alkenyl-, and 4'-alkynylphenyl)nortropane-2 beta-carboxylic acid methyl esters: serotonin transporter selective analogs.
Blough BE, Abraham P, Lewin AH, Kuhar MJ, Boja JW, Carroll FI.
J Med Chem (1996) 39 : 4027 -4035
PubMed 8831768 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.97 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL334877 1 9.22
CHEMBL132499 1 8.94
CHEMBL340447 1 8.89
CHEMBL442763 1 8.80
CHEMBL132513 1 8.65
CHEMBL128186 1 8.50
CHEMBL336190 1 8.50
CHEMBL131662 1 8.36
CHEMBL337507 1 8.21
CHEMBL335001 1 8.15
CHEMBL340523 1 8.09
CHEMBL129608 1 8.02
CHEMBL132329 1 7.94
CHEMBL335868 1 7.82
CHEMBL127557 1 7.80
CHEMBL131354 1 7.58
CHEMBL130750 1 7.55
CHEMBL334546 1 7.55
CHEMBL129662 1 7.15
CHEMBL301281 1 6.90
CHEMBL337980 1 6.72
CHEMBL370805 COCAINE 4.0 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL334877 IC50 = 0.6 nM 9.22
CHEMBL132499 IC50 = 1.15 nM 8.94
CHEMBL340447 IC50 = 1.3 nM 8.89
CHEMBL442763 IC50 = 1.59 nM 8.80
CHEMBL132513 IC50 = 2.25 nM 8.65
CHEMBL128186 IC50 = 3.13 nM 8.50
CHEMBL336190 IC50 = 3.16 nM 8.50
CHEMBL131662 IC50 = 4.4 nM 8.36
CHEMBL337507 IC50 = 6.2 nM 8.21
CHEMBL335001 IC50 = 7.09 nM 8.15
CHEMBL340523 IC50 = 8.13 nM 8.09
CHEMBL129608 IC50 = 9.5 nM 8.02
CHEMBL132329 IC50 = 11.4 nM 7.94
CHEMBL335868 IC50 = 15.1 nM 7.82
CHEMBL127557 IC50 = 15.7 nM 7.80
CHEMBL131354 IC50 = 26.0 nM 7.58
CHEMBL130750 IC50 = 28.4 nM 7.55
CHEMBL334546 IC50 = 28.4 nM 7.55
CHEMBL129662 IC50 = 70.4 nM 7.15
CHEMBL301281 IC50 = 127.0 nM 6.90
CHEMBL337980 IC50 = 191.0 nM 6.72
CHEMBL370805 COCAINE IC50 = 1045.0 nM 5.98