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Assay Detail

CHEMBL4186933

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

Functional
Antagonist activity at 5-HT1A receptor in Sprague-Dawley rat hippocampal membranes assessed as inhibition of 8-OH-DPAT-induced receptor activation after 90 mins by microbeta scintillation counting based [35S]GTPgammaS binding assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

5-HT1A and 5-HT2A receptors affinity, docking studies and pharmacological evaluation of a series of 8-acetyl-7-hydroxy-4-methylcoumarin derivatives.
Ostrowska K, Grzeszczuk D, Głuch-Lutwin M, Gryboś A, Siwek A, Leśniak A, Sacharczuk M, Trzaskowski B.
Bioorg Med Chem (2018) 26 : 527 -535
PubMed 29269256 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.55 6.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4218720 1 6.90
CHEMBL4215022 1 6.20

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4218720 EC50 = 125.89 nM 6.90
CHEMBL4215022 EC50 = 630.96 nM 6.20