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Assay Detail

CHEMBL884752

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

Binding
Binding inhibition towards human serotonin transporter
24
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Conformationally restricted homotryptamines. 2. Indole cyclopropylmethylamines as selective serotonin reuptake inhibitors.
Mattson RJ, Catt JD, Denhart DJ, Deskus JA, Ditta JL, Higgins MA, Marcin LR, Sloan CP, Beno BR, Gao Q, Cunningham MA, Mattson GK, Molski TF, Taber MT, Lodge NJ.
J Med Chem (2005) 48 : 6023 -6034
PubMed 16162005 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 24 8.16 10.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL490 PAROXETINE 4.0 1 10.40
CHEMBL196468 1 9.25
CHEMBL197354 1 9.24
CHEMBL198019 2 9.17
CHEMBL41 FLUOXETINE 4.0 1 9.14
CHEMBL199054 1 8.74
CHEMBL180630 1 8.70
CHEMBL361949 1 8.40
CHEMBL373211 1 8.24
CHEMBL199053 1 8.19
CHEMBL1162965 1 8.15
CHEMBL197966 1 8.13
CHEMBL195774 1 8.05
CHEMBL364050 1 8.00
CHEMBL196513 2 7.85
CHEMBL194910 1 7.77
CHEMBL194960 1 7.42
CHEMBL197315 1 7.39
CHEMBL194909 1 7.23
CHEMBL383347 1 7.00
CHEMBL198018 2 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL490 PAROXETINE Ki = 0.04 nM 10.40
CHEMBL196468 Ki = 0.56 nM 9.25
CHEMBL197354 Ki = 0.58 nM 9.24
CHEMBL198019 Ki = 0.68 nM 9.17
CHEMBL41 FLUOXETINE Ki = 0.72 nM 9.14
CHEMBL199054 Ki = 1.8 nM 8.74
CHEMBL180630 Ki = 2.0 nM 8.70
CHEMBL198019 Ki = 2.1 nM 8.68
CHEMBL361949 Ki = 4.0 nM 8.40
CHEMBL373211 Ki = 5.7 nM 8.24
CHEMBL199053 Ki = 6.5 nM 8.19
CHEMBL1162965 Ki = 7.1 nM 8.15
CHEMBL197966 Ki = 7.4 nM 8.13
CHEMBL195774 Ki = 8.9 nM 8.05
CHEMBL364050 Ki = 10.0 nM 8.00
CHEMBL196513 Ki = 14.0 nM 7.85
CHEMBL194910 Ki = 17.0 nM 7.77
CHEMBL196513 Ki = 24.0 nM 7.62
CHEMBL194960 Ki = 38.0 nM 7.42
CHEMBL197315 Ki = 41.0 nM 7.39
CHEMBL194909 Ki = 59.0 nM 7.23
CHEMBL383347 Ki = 100.0 nM 7.00
CHEMBL198018 Ki = 230.0 nM 6.64
CHEMBL198018 Ki = 420.0 nM 6.38