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Assay Detail

CHEMBL808124

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Binding
Tested for the ability to displace [3H]- paroxetine binding in rat frontal cortex membrane against Serotonin transporter
15
Total Activities
15
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 iodinated 3beta-aryltropanes with selective binding to either the dopamine or serotonin transporters.
Davies HM, Ren P, Kong NX, Sexton T, Childers SR.
Bioorg Med Chem Lett (2002) 12 : 845 -847
PubMed 11958976 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.50 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL355259 1 9.89
CHEMBL423275 1 9.24
CHEMBL352913 1 9.21
CHEMBL169117 1 8.97
CHEMBL168455 1 8.94
CHEMBL352698 1 8.73
CHEMBL354725 1 8.61
CHEMBL169361 1 8.55
CHEMBL355734 1 8.14
CHEMBL355650 1 8.04
CHEMBL355733 1 7.88
CHEMBL171565 1 7.80
CHEMBL168305 1 7.71
CHEMBL169320 1 7.29
CHEMBL2112943 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL355259 Ki = 0.13 nM 9.89
CHEMBL423275 Ki = 0.57 nM 9.24
CHEMBL352913 Ki = 0.62 nM 9.21
CHEMBL169117 Ki = 1.08 nM 8.97
CHEMBL168455 Ki = 1.14 nM 8.94
CHEMBL352698 Ki = 1.88 nM 8.73
CHEMBL354725 Ki = 2.44 nM 8.61
CHEMBL169361 Ki = 2.82 nM 8.55
CHEMBL355734 Ki = 7.26 nM 8.14
CHEMBL355650 Ki = 9.07 nM 8.04
CHEMBL355733 Ki = 13.1 nM 7.88
CHEMBL171565 Ki = 15.7 nM 7.80
CHEMBL168305 Ki = 19.7 nM 7.71
CHEMBL169320 Ki = 50.8 nM 7.29
CHEMBL2112943 Ki > 1100.0 nM -