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Assay Detail

CHEMBL616409

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Binding
Inhibition activity against 5-hydroxytryptamine 1A receptor in rat hippocampus membranes using radio binding assays
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Hippocampus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

5-hydroxytryptamine receptor 1A (CHEMBL273)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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 6.31 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL147503 1 7.64
CHEMBL147071 1 7.24
CHEMBL15928 GR-127935 1 6.37
CHEMBL151894 1 6.16
CHEMBL151420 1 5.30
CHEMBL443762 1 5.16
CHEMBL359447 1 -
CHEMBL151695 1 -
CHEMBL281350 SB-224289 1 -
CHEMBL146735 1 -
CHEMBL422504 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL147503 IC50 = 23.0 nM 7.64
CHEMBL147071 IC50 = 57.0 nM 7.24
CHEMBL15928 GR-127935 IC50 = 425.0 nM 6.37
CHEMBL151894 IC50 = 700.0 nM 6.16
CHEMBL151420 IC50 = 5000.0 nM 5.30
CHEMBL443762 IC50 = 7000.0 nM 5.16
CHEMBL359447 IC50 > 100.0 nM -
CHEMBL151695 IC50 > 10000.0 nM -
CHEMBL281350 SB-224289 IC50 > 1000.0 nM -
CHEMBL146735 IC50 > 1000.0 nM -
CHEMBL422504 IC50 > 1000.0 nM -