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Assay Detail

CHEMBL809425

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

Binding
Inhibition of [3H]paroxetine binding to serotonin transport sites in rat frontal cortex membranes.
21
Total Activities
17
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 2 beta-acyl-3 beta-aryl-8-azabicyclo[3.2.1]octanes and their binding affinities at dopamine and serotonin transport sites in rat striatum and frontal cortex.
Davies HM, Saikali E, Huby NJ, Gilliatt VJ, Matasi JJ, Sexton T, Childers SR.
J Med Chem (1994) 37 : 1262 -1268
PubMed 8176704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.27 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418190 3 9.92
CHEMBL22930 1 8.97
CHEMBL22518 1 8.37
CHEMBL278572 1 7.68
CHEMBL23672 1 7.59
CHEMBL278122 1 7.45
CHEMBL23142 3 7.13
CHEMBL23974 1 7.11
CHEMBL23141 1 6.91
CHEMBL23655 1 6.20
CHEMBL22665 1 6.07
CHEMBL23875 1 6.00
CHEMBL416007 1 5.87
CHEMBL22377 1 5.75
CHEMBL281413 1 -
CHEMBL280382 1 -
CHEMBL277200 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418190 Ki = 0.121 nM 9.92
CHEMBL418190 Ki = 0.394 nM 9.40
CHEMBL22930 Ki = 1.06 nM 8.97
CHEMBL22518 Ki = 4.31 nM 8.37
CHEMBL278572 Ki = 20.9 nM 7.68
CHEMBL23672 Ki = 25.6 nM 7.59
CHEMBL278122 Ki = 35.8 nM 7.45
CHEMBL23142 Ki = 74.0 nM 7.13
CHEMBL23974 Ki = 78.2 nM 7.11
CHEMBL23141 Ki = 122.0 nM 6.91
CHEMBL23142 Ki = 131.0 nM 6.88
CHEMBL418190 Ki = 484.0 nM 6.32
CHEMBL23655 Ki = 630.0 nM 6.20
CHEMBL22665 Ki = 857.0 nM 6.07
CHEMBL23875 Ki = 1005.0 nM 6.00
CHEMBL416007 Ki = 1364.0 nM 5.87
CHEMBL22377 Ki = 1771.0 nM 5.75
CHEMBL281413 Ki > 10000.0 nM -
CHEMBL280382 Ki > 10000.0 nM -
CHEMBL23142 Ki > 10000.0 nM -
CHEMBL277200 Ki > 10000.0 nM -