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Assay Detail

CHEMBL890738

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

Binding
Displacement of [3H]paroxetine from SERT in Sprague-Dawley rat brain
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Synthesis, monoamine transporter binding, properties, and functional monoamine uptake activity of 3beta-[4-methylphenyl and 4-chlorophenyl]-2 beta-[5-(substituted phenyl)thiazol-2-yl]tropanes.
Gong PK, Blough BE, Brieaddy LE, Huang X, Kuhar MJ, Navarro HA, Carroll FI.
J Med Chem (2007) 50 : 3686 -3695
PubMed 17602602 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.08 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL376113 1 6.72
CHEMBL227231 1 6.55
CHEMBL388760 1 6.52
CHEMBL436132 1 6.51
CHEMBL390743 1 6.43
CHEMBL388612 1 6.42
CHEMBL227233 1 6.10
CHEMBL388759 1 6.08
CHEMBL227180 1 6.04
CHEMBL227232 1 6.01
CHEMBL229381 1 5.96
CHEMBL388832 1 5.82
CHEMBL229436 1 5.77
CHEMBL390742 TROPARIL 1 5.72
CHEMBL229699 1 5.65
CHEMBL226984 1 5.00
CHEMBL227179 1 -
CHEMBL226933 1 -
CHEMBL2113279 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL376113 Ki = 190.0 nM 6.72
CHEMBL227231 Ki = 280.0 nM 6.55
CHEMBL388760 Ki = 301.0 nM 6.52
CHEMBL436132 Ki = 312.0 nM 6.51
CHEMBL390743 Ki = 371.0 nM 6.43
CHEMBL388612 Ki = 380.0 nM 6.42
CHEMBL227233 Ki = 800.0 nM 6.10
CHEMBL388759 Ki = 840.0 nM 6.08
CHEMBL227180 Ki = 903.0 nM 6.04
CHEMBL227232 Ki = 980.0 nM 6.01
CHEMBL229381 Ki = 1110.0 nM 5.96
CHEMBL388832 Ki = 1510.0 nM 5.82
CHEMBL229436 Ki = 1690.0 nM 5.77
CHEMBL390742 TROPARIL Ki = 1900.0 nM 5.72
CHEMBL229699 Ki = 2240.0 nM 5.65
CHEMBL226984 Ki = 10000.0 nM 5.00
CHEMBL227179 Ki > 2000.0 nM -
CHEMBL226933 Ki > 2000.0 nM -
CHEMBL2113279 Ki > 2000.0 nM -