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Assay Detail

CHEMBL616494

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

Binding
Compound was evaluated for binding affinity towards 5-hydroxytryptamine 2 receptor in rat anterior cortex using [125I]DOI as radioligand
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Serotonin 2 (5-HT2) receptor (CHEMBL2093870)
Type PROTEIN FAMILY
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 7.15 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27173 1 7.85
CHEMBL25800 1 7.85
CHEMBL412876 1 7.20
CHEMBL26427 1 7.09
CHEMBL7257 MEBUFOTENIN 2.0 1 6.89
CHEMBL122860 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27173 IC50 = 14.0 nM 7.85
CHEMBL25800 IC50 = 14.0 nM 7.85
CHEMBL412876 IC50 = 63.0 nM 7.20
CHEMBL26427 IC50 = 81.0 nM 7.09
CHEMBL7257 MEBUFOTENIN IC50 = 130.0 nM 6.89
CHEMBL122860 IC50 = 920.0 nM 6.04