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Assay Detail

CHEMBL806802

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

Binding
Affinity for the displacement of [3H]paroxetine binding to serotonin transporter (SERT) in rat frontal cortex membranes
23
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of 2beta-acyl-3beta-(substituted naphthyl)-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites.
Davies HM, Gilliatt V, Kuhn LA, Saikali E, Ren P, Hammond PS, Sexton T, Childers SR.
J Med Chem (2001) 44 : 1509 -1515
PubMed 11334561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 8.15 9.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL36720 1 9.64
CHEMBL287945 1 9.43
CHEMBL34243 1 9.42
CHEMBL418190 2 9.41
CHEMBL435371 1 9.33
CHEMBL22930 1 8.97
CHEMBL416058 1 8.71
CHEMBL39589 1 8.68
CHEMBL39990 1 8.65
CHEMBL290412 1 8.64
CHEMBL287940 1 8.12
CHEMBL39340 1 8.05
CHEMBL39330 1 7.82
CHEMBL289849 1 7.80
CHEMBL278572 1 7.68
CHEMBL23672 2 7.58
CHEMBL278122 1 7.44
CHEMBL39764 1 7.06
CHEMBL23142 1 6.88
CHEMBL290662 1 6.87
CHEMBL285039 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL36720 Ki = 0.23 nM 9.64
CHEMBL287945 Ki = 0.37 nM 9.43
CHEMBL34243 Ki = 0.38 nM 9.42
CHEMBL418190 Ki = 0.39 nM 9.41
CHEMBL435371 Ki = 0.47 nM 9.33
CHEMBL22930 Ki = 1.06 nM 8.97
CHEMBL416058 Ki = 1.97 nM 8.71
CHEMBL39589 Ki = 2.08 nM 8.68
CHEMBL39990 Ki = 2.24 nM 8.65
CHEMBL290412 Ki = 2.27 nM 8.64
CHEMBL287940 Ki = 7.55 nM 8.12
CHEMBL39340 Ki = 8.99 nM 8.05
CHEMBL39330 Ki = 15.0 nM 7.82
CHEMBL289849 Ki = 15.8 nM 7.80
CHEMBL418190 Ki = 16.4 nM 7.79
CHEMBL278572 Ki = 21.0 nM 7.68
CHEMBL23672 Ki = 26.0 nM 7.58
CHEMBL278122 Ki = 36.0 nM 7.44
CHEMBL39764 Ki = 88.0 nM 7.06
CHEMBL23142 Ki = 131.0 nM 6.88
CHEMBL290662 Ki = 136.0 nM 6.87
CHEMBL285039 Ki = 175.0 nM 6.76
CHEMBL23672 Ki = 217.0 nM 6.66