Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL885432

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

Binding
Binding affinity at human SERT
30
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Sodium-dependent serotonin transporter (CHEMBL228)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel tetrahydroisoquinolines are histamine H3 antagonists and serotonin reuptake inhibitors.
Letavic MA, Keith JM, Jablonowski JA, Stocking EM, Gomez LA, Ly KS, Miller JM, Barbier AJ, Bonaventure P, Boggs JD, Wilson SJ, Miller KL, Lord B, McAllister HM, Tognarelli DJ, Wu J, Abad MC, Schubert C, Lovenberg TW, Carruthers NI.
Bioorg Med Chem Lett (2007) 17 : 1047 -1051
PubMed 17127059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 8.02 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL395368 3 8.70
CHEMBL41 FLUOXETINE 4.0 1 8.66
CHEMBL233054 3 8.57
CHEMBL246955 3 8.42
CHEMBL397299 1 8.37
CHEMBL246954 1 8.37
CHEMBL246127 1 8.33
CHEMBL394861 1 8.29
CHEMBL246331 1 8.24
CHEMBL233053 1 8.19
CHEMBL246542 1 8.07
CHEMBL246332 1 7.96
CHEMBL246749 1 7.89
CHEMBL247161 1 7.89
CHEMBL395609 1 7.89
CHEMBL246747 1 7.82
CHEMBL246748 1 7.80
CHEMBL246333 1 7.75
CHEMBL246540 1 7.68
CHEMBL397300 1 7.62
CHEMBL246953 1 7.47
CHEMBL397065 1 7.34
CHEMBL246541 1 6.97
CHEMBL395608 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL395368 Ki = 2.0 nM 8.70
CHEMBL41 FLUOXETINE Ki = 2.2 nM 8.66
CHEMBL233054 Ki = 2.7 nM 8.57
CHEMBL233054 Ki = 2.9 nM 8.54
CHEMBL246955 Ki = 3.8 nM 8.42
CHEMBL395368 Ki = 4.2 nM 8.38
CHEMBL397299 Ki = 4.3 nM 8.37
CHEMBL246954 Ki = 4.3 nM 8.37
CHEMBL246127 Ki = 4.7 nM 8.33
CHEMBL394861 Ki = 5.1 nM 8.29
CHEMBL246955 Ki = 5.2 nM 8.28
CHEMBL246331 Ki = 5.7 nM 8.24
CHEMBL246955 Ki = 6.2 nM 8.21
CHEMBL233053 Ki = 6.5 nM 8.19
CHEMBL246542 Ki = 8.6 nM 8.07
CHEMBL395368 Ki = 8.8 nM 8.06
CHEMBL233054 Ki = 9.3 nM 8.03
CHEMBL246332 Ki = 11.0 nM 7.96
CHEMBL246749 Ki = 13.0 nM 7.89
CHEMBL247161 Ki = 13.0 nM 7.89
CHEMBL395609 Ki = 13.0 nM 7.89
CHEMBL246747 Ki = 15.0 nM 7.82
CHEMBL246748 Ki = 16.0 nM 7.80
CHEMBL246333 Ki = 18.0 nM 7.75
CHEMBL246540 Ki = 21.0 nM 7.68
CHEMBL397300 Ki = 24.0 nM 7.62
CHEMBL246953 Ki = 34.0 nM 7.47
CHEMBL397065 Ki = 46.0 nM 7.34
CHEMBL246541 Ki = 107.0 nM 6.97
CHEMBL395608 Ki = 135.0 nM 6.87