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Assay Detail

CHEMBL4009977

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

Binding
Displacement of [3H]-8-OH-DPAT from 5-HT1A receptor in rat hippocampal membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The "Phenylalkylaminome" with a Focus on Selected Drugs of Abuse.
Glennon RA.
J Med Chem (2017) 60 : 2605 -2628
PubMed 28244748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 8.52 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56 8-OH-DPAT 1 8.92
CHEMBL11760 1 8.89
CHEMBL285351 1 8.72
CHEMBL27937 1 8.70
CHEMBL28111 1 8.68
CHEMBL27019 1 8.64
CHEMBL27609 1 8.60
CHEMBL27252 1 8.25
CHEMBL26688 1 7.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56 8-OH-DPAT Ki = 1.2 nM 8.92
CHEMBL11760 Ki = 1.3 nM 8.89
CHEMBL285351 Ki = 1.9 nM 8.72
CHEMBL27937 Ki = 2.0 nM 8.70
CHEMBL28111 Ki = 2.1 nM 8.68
CHEMBL27019 Ki = 2.3 nM 8.64
CHEMBL27609 Ki = 2.5 nM 8.60
CHEMBL27252 Ki = 5.6 nM 8.25
CHEMBL26688 Ki = 53.0 nM 7.28