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Assay Detail

CHEMBL749361

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

Binding
Binding affinity towards norepinephrine transporter was determined using [3H]nisoxetine radioligand.
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes.
Carroll FI, Pawlush N, Kuhar MJ, Pollard GT, Howard JL.
J Med Chem (2004) 47 : 296 -302
PubMed 14711303 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.34 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL317905 1 7.58
CHEMBL103523 1 7.28
CHEMBL103227 1 7.14
CHEMBL316528 1 6.96
CHEMBL103228 1 6.82
CHEMBL317904 1 6.75
CHEMBL14144 1 6.67
CHEMBL298580 1 6.66
CHEMBL316585 1 6.62
CHEMBL320627 1 6.34
CHEMBL322856 1 6.34
CHEMBL102279 1 6.26
CHEMBL1790051 1 6.26
CHEMBL329517 1 6.26
CHEMBL321806 1 6.26
CHEMBL321780 1 6.24
CHEMBL322385 1 5.99
CHEMBL322400 1 5.81
CHEMBL317909 1 5.74
CHEMBL370805 COCAINE 4.0 1 5.70
CHEMBL100652 1 5.42
CHEMBL103223 1 5.42
CHEMBL328415 1 5.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL317905 Ki = 26.0 nM 7.58
CHEMBL103523 Ki = 52.0 nM 7.28
CHEMBL103227 Ki = 72.0 nM 7.14
CHEMBL316528 Ki = 109.0 nM 6.96
CHEMBL103228 Ki = 153.0 nM 6.82
CHEMBL317904 Ki = 180.0 nM 6.75
CHEMBL14144 Ki = 213.0 nM 6.67
CHEMBL298580 Ki = 220.0 nM 6.66
CHEMBL316585 Ki = 239.0 nM 6.62
CHEMBL320627 Ki = 454.0 nM 6.34
CHEMBL322856 Ki = 455.0 nM 6.34
CHEMBL102279 Ki = 552.0 nM 6.26
CHEMBL1790051 Ki = 550.0 nM 6.26
CHEMBL329517 Ki = 553.0 nM 6.26
CHEMBL321806 Ki = 554.0 nM 6.26
CHEMBL321780 Ki = 575.0 nM 6.24
CHEMBL322385 Ki = 1030.0 nM 5.99
CHEMBL322400 Ki = 1550.0 nM 5.81
CHEMBL317909 Ki = 1825.0 nM 5.74
CHEMBL370805 COCAINE Ki = 1990.0 nM 5.70
CHEMBL100652 Ki = 3807.0 nM 5.42
CHEMBL103223 Ki = 3790.0 nM 5.42
CHEMBL328415 Ki = 3990.0 nM 5.40