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Assay Detail

CHEMBL901476

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

Binding
Displacement of [3H]GBR from DAT in rat brain membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
Subcellular Brain membranes
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Sodium-dependent dopamine transporter (CHEMBL338)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Development of SPECT imaging agents for the norepinephrine transporters: [123I]INER.
Tamagnan GD, Brenner E, Alagille D, Staley JK, Haile C, Koren A, Early M, Baldwin RM, Tarazi FI, Baldessarini RJ, Jarkas N, Goodman MM, Seibyl JP.
Bioorg Med Chem Lett (2007) 17 : 533 -537
PubMed 17095215 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.42 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL247284 1 7.85
CHEMBL245638 1 6.73
CHEMBL245639 1 6.68
CHEMBL393236 1 6.64
CHEMBL396328 1 6.39
CHEMBL245637 1 6.14
CHEMBL439030 1 6.13
CHEMBL429658 1 5.73
CHEMBL394965 1 5.50
CHEMBL247687 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL247284 Ki = 14.2 nM 7.85
CHEMBL245638 Ki = 186.0 nM 6.73
CHEMBL245639 Ki = 210.0 nM 6.68
CHEMBL393236 Ki = 228.0 nM 6.64
CHEMBL396328 Ki = 410.0 nM 6.39
CHEMBL245637 Ki = 716.0 nM 6.14
CHEMBL439030 Ki = 740.0 nM 6.13
CHEMBL429658 Ki = 1871.0 nM 5.73
CHEMBL394965 Ki = 3139.0 nM 5.50
CHEMBL247687 Ki > 10000.0 nM -