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Assay Detail

CHEMBL828882

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

Binding
Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of new tetracyclic tetrahydrofuran derivatives as potential broad-spectrum psychotropic agents.
Fernández J, Alonso JM, Andrés JI, Cid JM, Díaz A, Iturrino L, Gil P, Megens A, Sipido VK, Trabanco AA.
J Med Chem (2005) 48 : 1709 -1712
PubMed 15771415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.44 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL193639 2 8.80
CHEMBL363581 1 8.57
CHEMBL194659 1 8.44
CHEMBL329566 1 8.11
CHEMBL435301 1 8.03
CHEMBL195706 1 7.70
CHEMBL366164 1 7.40
CHEMBL364270 1 7.06
CHEMBL6437 MIANSERIN 4.0 1 7.00
CHEMBL193435 1 6.42
CHEMBL42 CLOZAPINE 4.0 1 6.16
CHEMBL715 OLANZAPINE 4.0 1 6.02
CHEMBL654 MIRTAZAPINE 4.0 1 5.79
CHEMBL85 RISPERIDONE 4.0 1 -
CHEMBL195856 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL193639 Ki = 1.6 nM 8.80
CHEMBL193639 Ki = 2.0 nM 8.70
CHEMBL363581 Ki = 2.7 nM 8.57
CHEMBL194659 Ki = 3.6 nM 8.44
CHEMBL329566 Ki = 7.8 nM 8.11
CHEMBL435301 Ki = 9.4 nM 8.03
CHEMBL195706 Ki = 20.0 nM 7.70
CHEMBL366164 Ki = 40.0 nM 7.40
CHEMBL364270 Ki = 88.0 nM 7.06
CHEMBL6437 MIANSERIN Ki = 101.0 nM 7.00
CHEMBL193435 Ki = 382.0 nM 6.42
CHEMBL42 CLOZAPINE Ki = 697.0 nM 6.16
CHEMBL715 OLANZAPINE Ki = 958.0 nM 6.02
CHEMBL654 MIRTAZAPINE Ki = 1640.0 nM 5.79
CHEMBL85 RISPERIDONE Ki > 5454.0 nM -
CHEMBL195856 Ki > 5454.0 nM -