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Assay Detail

CHEMBL798398

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

Functional
The ability to inhibit the 5-HT-induced contraction of isolated rat fundus muscle was determined
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Structure-activity relationships for hallucinogenic N,N-dialkyltryptamines: photoelectron spectra and serotonin receptor affinities of methylthio and methylenedioxy derivatives.
Kline TB, Benington F, Morin RD, Beaton JM, Glennon RA, Domelsmith LN, Houk KN, Rozeboom MD.
J Med Chem (1982) 25 : 1381 -1383
PubMed 6815326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 9 6.26 7.08

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7257 MEBUFOTENIN 2.0 1 7.08
CHEMBL31783 1 6.84
CHEMBL28354 1 6.40
CHEMBL285355 1 6.21
CHEMBL32029 1 6.17
CHEMBL12420 N,N-DIMETHYLTRYPTAMINE 2.0 1 6.00
CHEMBL283686 1 5.99
CHEMBL417480 1 5.92
CHEMBL281408 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7257 MEBUFOTENIN Kd = 83.18 nM 7.08
CHEMBL31783 Kd = 144.54 nM 6.84
CHEMBL28354 Kd = 398.11 nM 6.40
CHEMBL285355 Kd = 616.6 nM 6.21
CHEMBL32029 Kd = 676.08 nM 6.17
CHEMBL12420 N,N-DIMETHYLTRYPTAMINE Kd = 1000.0 nM 6.00
CHEMBL283686 Kd = 1023.29 nM 5.99
CHEMBL417480 Kd = 1202.26 nM 5.92
CHEMBL281408 Kd = 1698.24 nM 5.77