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Assay Detail

CHEMBL886655

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

Binding
Binding affinity to human SERT
27
Total Activities
27
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 naphthyridines are histamine H3 antagonists and serotonin reuptake transporter inhibitors.
Letavic MA, Keith JM, Ly KS, Barbier AJ, Boggs JD, Wilson SJ, Lord B, Lovenberg TW, Carruthers NI.
Bioorg Med Chem Lett (2007) 17 : 2566 -2569
PubMed 17307358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 27 6.78 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41 FLUOXETINE 4.0 1 8.66
CHEMBL247265 1 7.58
CHEMBL236252 1 7.52
CHEMBL392933 1 7.51
CHEMBL394732 1 7.50
CHEMBL247669 1 7.43
CHEMBL247671 1 7.21
CHEMBL247267 1 7.18
CHEMBL247472 1 7.16
CHEMBL247670 1 7.03
CHEMBL246874 1 6.97
CHEMBL238052 1 6.97
CHEMBL247683 1 6.92
CHEMBL246873 1 6.85
CHEMBL241706 1 6.83
CHEMBL247094 1 6.83
CHEMBL247470 1 6.72
CHEMBL247266 1 6.65
CHEMBL241705 1 6.52
CHEMBL241712 1 6.44
CHEMBL247063 1 6.12
CHEMBL392429 1 6.08
CHEMBL247061 1 5.94
CHEMBL247076 1 5.88
CHEMBL247268 1 5.70
CHEMBL247062 1 5.63
CHEMBL391605 1 5.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41 FLUOXETINE Ki = 2.2 nM 8.66
CHEMBL247265 Ki = 26.0 nM 7.58
CHEMBL236252 Ki = 30.0 nM 7.52
CHEMBL392933 Ki = 31.0 nM 7.51
CHEMBL394732 Ki = 32.0 nM 7.50
CHEMBL247669 Ki = 37.0 nM 7.43
CHEMBL247671 Ki = 62.0 nM 7.21
CHEMBL247267 Ki = 66.0 nM 7.18
CHEMBL247472 Ki = 70.0 nM 7.16
CHEMBL247670 Ki = 93.0 nM 7.03
CHEMBL246874 Ki = 106.0 nM 6.97
CHEMBL238052 Ki = 107.0 nM 6.97
CHEMBL247683 Ki = 120.0 nM 6.92
CHEMBL246873 Ki = 141.0 nM 6.85
CHEMBL241706 Ki = 147.0 nM 6.83
CHEMBL247094 Ki = 147.0 nM 6.83
CHEMBL247470 Ki = 189.0 nM 6.72
CHEMBL247266 Ki = 226.0 nM 6.65
CHEMBL241705 Ki = 302.0 nM 6.52
CHEMBL241712 Ki = 362.0 nM 6.44
CHEMBL247063 Ki = 768.0 nM 6.12
CHEMBL392429 Ki = 826.0 nM 6.08
CHEMBL247061 Ki = 1137.0 nM 5.94
CHEMBL247076 Ki = 1333.0 nM 5.88
CHEMBL247268 Ki = 2000.0 nM 5.70
CHEMBL247062 Ki = 2333.0 nM 5.63
CHEMBL391605 Ki = 4767.0 nM 5.32