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Assay Detail

CHEMBL839753

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

Binding
Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat cerebral cortex
20
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and monoamine transporter binding properties of 3alpha-(substituted phenyl)nortropane-2beta-carboxylic acid methyl esters. Norepinephrine transporter selective compounds.
Carroll FI, Tyagi S, Blough BE, Kuhar MJ, Navarro HA.
J Med Chem (2005) 48 : 3852 -3857
PubMed 15916437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.79 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL365738 1 9.37
CHEMBL371607 1 8.69
CHEMBL195738 1 8.67
CHEMBL366159 1 8.59
CHEMBL81525 2 8.51
CHEMBL192924 1 8.40
CHEMBL80262 2 8.36
CHEMBL80515 2 8.23
CHEMBL306208 2 7.66
CHEMBL192195 1 7.65
CHEMBL82027 2 7.44
CHEMBL192035 1 7.13
CHEMBL2079586 2 6.30
CHEMBL370805 COCAINE 4.0 1 5.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL365738 Ki = 0.43 nM 9.37
CHEMBL371607 Ki = 2.05 nM 8.69
CHEMBL195738 Ki = 2.12 nM 8.67
CHEMBL366159 Ki = 2.6 nM 8.59
CHEMBL81525 Ki = 3.1 nM 8.51
CHEMBL81525 Ki = 3.28 nM 8.48
CHEMBL192924 Ki = 4.0 nM 8.40
CHEMBL80262 Ki = 4.4 nM 8.36
CHEMBL80262 Ki = 5.2 nM 8.28
CHEMBL80515 Ki = 5.9 nM 8.23
CHEMBL80515 Ki = 11.3 nM 7.95
CHEMBL306208 Ki = 22.0 nM 7.66
CHEMBL192195 Ki = 22.4 nM 7.65
CHEMBL306208 Ki = 36.0 nM 7.44
CHEMBL82027 Ki = 36.0 nM 7.44
CHEMBL192035 Ki = 74.0 nM 7.13
CHEMBL82027 Ki = 160.0 nM 6.80
CHEMBL2079586 Ki = 503.0 nM 6.30
CHEMBL2079586 Ki = 741.0 nM 6.13
CHEMBL370805 COCAINE Ki = 1900.0 nM 5.72