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Assay Detail

CHEMBL783341

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Functional
Inhibition of uptake of 5-HT in rat brain cortex
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

3-(4-Piperidinylalkyl)indoles, selective inhibitors of neuronal 5-hydroxytryptamine uptake.
Gueremy C, Audiau F, Champseix, Uzan A, Le Fur G, Rataud J.
J Med Chem (1980) 23 : 1306 -1310
PubMed 7452682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 19 6.47 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276520 INDALPINE 4.0 1 8.00
CHEMBL415 CLOMIPRAMINE 4.0 1 7.70
CHEMBL24042 1 7.40
CHEMBL429771 1 7.30
CHEMBL278080 1 7.00
CHEMBL25428 1 6.89
CHEMBL24731 1 6.85
CHEMBL543980 1 6.40
CHEMBL284004 1 6.35
CHEMBL1159866 1 6.22
CHEMBL25416 1 6.16
CHEMBL1159870 1 6.16
CHEMBL24075 1 6.00
CHEMBL1159861 1 6.00
CHEMBL1159865 1 5.82
CHEMBL544216 1 5.77
CHEMBL557413 1 5.72
CHEMBL24783 1 5.66
CHEMBL278816 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276520 INDALPINE IC50 = 10.0 nM 8.00
CHEMBL415 CLOMIPRAMINE IC50 = 20.0 nM 7.70
CHEMBL24042 IC50 = 40.0 nM 7.40
CHEMBL429771 IC50 = 50.0 nM 7.30
CHEMBL278080 IC50 = 100.0 nM 7.00
CHEMBL25428 IC50 = 130.0 nM 6.89
CHEMBL24731 IC50 = 140.0 nM 6.85
CHEMBL543980 IC50 = 400.0 nM 6.40
CHEMBL284004 IC50 = 450.0 nM 6.35
CHEMBL1159866 IC50 = 600.0 nM 6.22
CHEMBL25416 IC50 = 700.0 nM 6.16
CHEMBL1159870 IC50 = 700.0 nM 6.16
CHEMBL24075 IC50 = 1000.0 nM 6.00
CHEMBL1159861 IC50 = 1000.0 nM 6.00
CHEMBL1159865 IC50 = 1500.0 nM 5.82
CHEMBL544216 IC50 = 1700.0 nM 5.77
CHEMBL557413 IC50 = 1900.0 nM 5.72
CHEMBL24783 IC50 = 2200.0 nM 5.66
CHEMBL278816 IC50 = 2500.0 nM 5.60