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Assay Detail

CHEMBL948194

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Binding
Binding affinity to human DAT
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Sodium-dependent dopamine transporter (CHEMBL238)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of piperazine and diazepane amides that are histamine H3 antagonists and serotonin reuptake inhibitors.
Ly KS, Letavic MA, Keith JM, Miller JM, Stocking EM, Barbier AJ, Bonaventure P, Lord B, Jiang X, Boggs JD, Dvorak L, Miller KL, Nepomuceno D, Wilson SJ, Carruthers NI.
Bioorg Med Chem Lett (2008) 18 : 39 -43
PubMed 18060777 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.50 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257738 1 6.48
CHEMBL408206 1 6.48
CHEMBL402644 1 6.31
CHEMBL257909 1 6.11
CHEMBL272699 1 5.60
CHEMBL404247 1 5.52
CHEMBL273157 1 5.40
CHEMBL270607 1 5.16
CHEMBL403148 1 5.16
CHEMBL409877 1 5.16
CHEMBL270625 1 5.14
CHEMBL401683 1 5.14
CHEMBL257221 1 5.11
CHEMBL401867 1 5.10
CHEMBL270165 1 5.08
CHEMBL403377 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257738 Ki = 330.0 nM 6.48
CHEMBL408206 Ki = 330.0 nM 6.48
CHEMBL402644 Ki = 490.0 nM 6.31
CHEMBL257909 Ki = 770.0 nM 6.11
CHEMBL272699 Ki = 2500.0 nM 5.60
CHEMBL404247 Ki = 3000.0 nM 5.52
CHEMBL273157 Ki = 4000.0 nM 5.40
CHEMBL270607 Ki = 7000.0 nM 5.16
CHEMBL403148 Ki = 7000.0 nM 5.16
CHEMBL409877 Ki = 7000.0 nM 5.16
CHEMBL270625 Ki = 7300.0 nM 5.14
CHEMBL401683 Ki = 7300.0 nM 5.14
CHEMBL257221 Ki = 7700.0 nM 5.11
CHEMBL401867 Ki = 8000.0 nM 5.10
CHEMBL270165 Ki = 8300.0 nM 5.08
CHEMBL403377 Ki = 9000.0 nM 5.05