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Assay Detail

CHEMBL948191

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Binding
Inhibition of rat SERT
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL313)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 40 7.88 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267267 1 9.00
CHEMBL272077 1 8.85
CHEMBL270625 1 8.74
CHEMBL272503 1 8.72
CHEMBL257434 1 8.66
CHEMBL257909 1 8.42
CHEMBL270165 1 8.40
CHEMBL409877 1 8.38
CHEMBL273136 1 8.35
CHEMBL408206 1 8.31
CHEMBL273157 1 8.24
CHEMBL258349 1 8.17
CHEMBL272698 1 8.10
CHEMBL256044 1 8.09
CHEMBL256390 1 8.09
CHEMBL272917 1 8.07
CHEMBL257738 1 8.04
CHEMBL402644 1 8.03
CHEMBL257221 1 8.02
CHEMBL404247 1 8.01
CHEMBL272699 1 8.01
CHEMBL257743 1 8.00
CHEMBL402590 1 7.96
CHEMBL403377 1 7.96
CHEMBL402286 1 7.96
CHEMBL258153 1 7.92
CHEMBL257208 1 7.89
CHEMBL272289 1 7.85
CHEMBL269966 1 7.80
CHEMBL403148 1 7.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267267 Ki = 1.0 nM 9.00
CHEMBL272077 Ki = 1.4 nM 8.85
CHEMBL270625 Ki = 1.8 nM 8.74
CHEMBL272503 Ki = 1.9 nM 8.72
CHEMBL257434 Ki = 2.2 nM 8.66
CHEMBL257909 Ki = 3.8 nM 8.42
CHEMBL270165 Ki = 4.0 nM 8.40
CHEMBL409877 Ki = 4.2 nM 8.38
CHEMBL273136 Ki = 4.5 nM 8.35
CHEMBL408206 Ki = 4.9 nM 8.31
CHEMBL273157 Ki = 5.8 nM 8.24
CHEMBL258349 Ki = 6.7 nM 8.17
CHEMBL272698 Ki = 7.9 nM 8.10
CHEMBL256044 Ki = 8.2 nM 8.09
CHEMBL256390 Ki = 8.1 nM 8.09
CHEMBL272917 Ki = 8.5 nM 8.07
CHEMBL257738 Ki = 9.1 nM 8.04
CHEMBL402644 Ki = 9.3 nM 8.03
CHEMBL257221 Ki = 9.5 nM 8.02
CHEMBL272699 Ki = 9.7 nM 8.01
CHEMBL404247 Ki = 9.7 nM 8.01
CHEMBL257743 Ki = 10.0 nM 8.00
CHEMBL402590 Ki = 11.0 nM 7.96
CHEMBL403377 Ki = 11.0 nM 7.96
CHEMBL402286 Ki = 11.0 nM 7.96
CHEMBL258153 Ki = 12.0 nM 7.92
CHEMBL257208 Ki = 13.0 nM 7.89
CHEMBL272289 Ki = 14.0 nM 7.85
CHEMBL269966 Ki = 16.0 nM 7.80
CHEMBL403148 Ki = 18.0 nM 7.75
CHEMBL404572 Ki = 24.0 nM 7.62
CHEMBL401683 Ki = 37.0 nM 7.43
CHEMBL401867 Ki = 39.0 nM 7.41
CHEMBL270411 Ki = 102.0 nM 6.99
CHEMBL270607 Ki = 113.0 nM 6.95
CHEMBL402949 Ki = 117.0 nM 6.93
CHEMBL270396 Ki = 186.0 nM 6.73
CHEMBL257009 Ki = 238.0 nM 6.62
CHEMBL255127 Ki = 299.0 nM 6.52
CHEMBL439246 Ki = 900.0 nM 6.05