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Assay Detail

CHEMBL884710

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

Binding
Inhibition of 5-hydroxytryptamine reuptake
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

New selective and potent 5-HT(1B/1D) antagonists: chemistry and pharmacological evaluation of N-piperazinylphenyl biphenylcarboxamides and biphenylsulfonamides.
Liao Y, Böttcher H, Harting J, Greiner H, van Amsterdam C, Cremers T, Sundell S, März J, Rautenberg W, Wikström H.
J Med Chem (2000) 43 : 517 -525
PubMed 10669578 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.75 6.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147503 1 6.39
CHEMBL151420 1 6.05
CHEMBL15928 GR-127935 1 6.00
CHEMBL443762 1 5.42
CHEMBL359447 1 5.33
CHEMBL281350 SB-224289 1 5.33
CHEMBL151894 1 -
CHEMBL147071 1 -
CHEMBL151695 1 -
CHEMBL146735 1 -
CHEMBL422504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147503 IC50 = 407.0 nM 6.39
CHEMBL151420 IC50 = 900.0 nM 6.05
CHEMBL15928 GR-127935 IC50 = 1000.0 nM 6.00
CHEMBL443762 IC50 = 3800.0 nM 5.42
CHEMBL359447 IC50 = 4700.0 nM 5.33
CHEMBL281350 SB-224289 IC50 = 4700.0 nM 5.33
CHEMBL151894 IC50 > 1000.0 nM -
CHEMBL147071 IC50 > 1000.0 nM -
CHEMBL151695 IC50 > 1000.0 nM -
CHEMBL146735 IC50 > 1000.0 nM -
CHEMBL422504 IC50 > 1000.0 nM -