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Assay Detail

CHEMBL748007

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

Binding
Binding affinity for norepinephrine transporter (NET) labeled with [3H]nisoxetine
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Norepinephrine transporter (CHEMBL304)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline.
Gu XH, Yu H, Jacobson AE, Rothman RB, Dersch CM, George C, Flippen-Anderson JL, Rice KC.
J Med Chem (2000) 43 : 4868 -4876
PubMed 11123996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.18 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL296602 INDATRALINE 2.0 1 8.24
CHEMBL543688 1 7.82
CHEMBL542500 1 7.57
CHEMBL543449 1 7.12
CHEMBL541602 1 7.03
CHEMBL541605 1 6.99
CHEMBL545559 1 6.91
CHEMBL554033 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL296602 INDATRALINE Ki = 5.8 nM 8.24
CHEMBL543688 Ki = 15.0 nM 7.82
CHEMBL542500 Ki = 27.0 nM 7.57
CHEMBL543449 Ki = 76.5 nM 7.12
CHEMBL541602 Ki = 93.0 nM 7.03
CHEMBL541605 Ki = 102.0 nM 6.99
CHEMBL545559 Ki = 122.0 nM 6.91
CHEMBL554033 Ki = 1686.0 nM 5.77