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Assay Detail

CHEMBL884525

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

Binding
Compound was evaluated for binding affinity towards 5-hydroxytryptamine 1A receptor in rat cortex using [3H]-8-OH-DPAT as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-(2-Aminoethyl)-3-methyl-8,9-dihydropyrano[3,2-e]indole: a rotationally restricted phenolic analog of the neurotransmitter serotonin and agonist selective for serotonin (5-HT2-type) receptors.
Macor JE, Fox CB, Johnson C, Koe BK, Lebel LA, Zorn SH.
J Med Chem (1992) 35 : 3625 -3632
PubMed 1433172 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.06 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7257 MEBUFOTENIN 2.0 1 7.96
CHEMBL27173 1 6.21
CHEMBL122860 1 5.92
CHEMBL412876 1 5.72
CHEMBL25800 1 5.28
CHEMBL26427 1 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7257 MEBUFOTENIN IC50 = 11.0 nM 7.96
CHEMBL27173 IC50 = 610.0 nM 6.21
CHEMBL122860 IC50 = 1200.0 nM 5.92
CHEMBL412876 IC50 = 1900.0 nM 5.72
CHEMBL25800 IC50 = 5300.0 nM 5.28
CHEMBL26427 IC50 = 5400.0 nM 5.27