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Assay Detail

CHEMBL751450

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

Binding
Displacement of [3H]-nisoxatine from Norepinephrine transporter of rat forebrain membrane
14
Total Activities
14
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

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of 3 beta-aryl-8-azabicyclo[3.2.1]octanes with high binding affinities and selectivities for the serotonin transporter site.
Davies HM, Kuhn LA, Thornley C, Matasi JJ, Sexton T, Childers SR.
J Med Chem (1996) 39 : 2554 -2558
PubMed 8691453 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.88 8.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418190 1 8.54
CHEMBL87983 1 8.26
CHEMBL85492 1 7.96
CHEMBL314361 1 7.11
CHEMBL85877 1 7.03
CHEMBL85256 1 6.82
CHEMBL23142 1 6.80
CHEMBL36720 1 6.36
CHEMBL82807 1 6.10
CHEMBL84899 1 5.37
CHEMBL87678 1 5.29
CHEMBL278122 1 -
CHEMBL314919 1 -
CHEMBL87739 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418190 Ki = 2.9 nM 8.54
CHEMBL87983 Ki = 5.5 nM 8.26
CHEMBL85492 Ki = 10.9 nM 7.96
CHEMBL314361 Ki = 78.0 nM 7.11
CHEMBL85877 Ki = 94.0 nM 7.03
CHEMBL85256 Ki = 150.0 nM 6.82
CHEMBL23142 Ki = 160.0 nM 6.80
CHEMBL36720 Ki = 440.0 nM 6.36
CHEMBL82807 Ki = 794.0 nM 6.10
CHEMBL84899 Ki = 4300.0 nM 5.37
CHEMBL87678 Ki = 5100.0 nM 5.29
CHEMBL278122 Ki > 10000.0 nM -
CHEMBL314919 Ki > 10000.0 nM -
CHEMBL87739 Ki > 10000.0 nM -