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Assay Detail

CHEMBL755919

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

Binding
Affinity for norepinephrine transporter determined by [3H]nisoxetine displacement.
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

2002 Medicinal Chemistry Division Award address: monoamine transporters and opioid receptors. Targets for addiction therapy.
Carroll FI.
J Med Chem (2003) 46 : 1775 -1794
PubMed 12723940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 23 6.90 9.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL301938 1 9.37
CHEMBL50858 1 8.55
CHEMBL51617 1 8.27
CHEMBL2373961 1 7.97
CHEMBL300226 1 7.67
CHEMBL610897 1 7.66
CHEMBL2310929 1 7.64
CHEMBL2373962 1 7.44
CHEMBL301562 1 7.13
CHEMBL51154 1 7.06
CHEMBL297507 1 7.05
CHEMBL51771 1 6.54
CHEMBL298580 1 6.52
CHEMBL1790051 1 6.26
CHEMBL52324 1 6.25
CHEMBL1643896 1 6.22
CHEMBL2310926 1 6.07
CHEMBL300220 1 6.02
CHEMBL432878 1 5.99
CHEMBL298703 1 5.94
CHEMBL14144 1 5.75
CHEMBL50157 1 5.63
CHEMBL51355 1 5.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL301938 Ki = 0.43 nM 9.37
CHEMBL50858 Ki = 2.8 nM 8.55
CHEMBL51617 Ki = 5.4 nM 8.27
CHEMBL2373961 Ki = 10.8 nM 7.97
CHEMBL300226 Ki = 21.6 nM 7.67
CHEMBL610897 Ki = 22.0 nM 7.66
CHEMBL2310929 Ki = 23.0 nM 7.64
CHEMBL2373962 Ki = 36.0 nM 7.44
CHEMBL301562 Ki = 74.0 nM 7.13
CHEMBL51154 Ki = 87.0 nM 7.06
CHEMBL297507 Ki = 89.0 nM 7.05
CHEMBL51771 Ki = 289.0 nM 6.54
CHEMBL298580 Ki = 304.0 nM 6.52
CHEMBL1790051 Ki = 554.0 nM 6.26
CHEMBL52324 Ki = 566.0 nM 6.25
CHEMBL1643896 Ki = 596.0 nM 6.22
CHEMBL2310926 Ki = 843.0 nM 6.07
CHEMBL300220 Ki = 964.0 nM 6.02
CHEMBL432878 Ki = 1030.0 nM 5.99
CHEMBL298703 Ki = 1160.0 nM 5.94
CHEMBL14144 Ki = 1780.0 nM 5.75
CHEMBL50157 Ki = 2353.0 nM 5.63
CHEMBL51355 Ki = 2370.0 nM 5.62