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Assay Detail

CHEMBL1948477

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

Binding
Displacement of [3H]-OH-DPAT from human recombinant 5HT1A receptor expressed in HeLa cells after 30 mins by liquid scintillation counting
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HeLa
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

5-hydroxytryptamine receptor 1A (CHEMBL214)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis, biological evaluation, and docking studies of tetrahydrofuran- cyclopentanone- and cyclopentanol-based ligands acting at adrenergic α₁- and serotonine 5-HT1A receptors.
Prandi A, Franchini S, Manasieva LI, Fossa P, Cichero E, Marucci G, Buccioni M, Cilia A, Pirona L, Brasili L.
J Med Chem (2012) 55 : 23 -36
PubMed 22145629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.65 9.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946786 1 9.49
CHEMBL514874 1 9.48
CHEMBL1946787 1 9.25
CHEMBL286003 1 9.22
CHEMBL1946788 1 9.10
CHEMBL1946779 1 9.08
CHEMBL13647 BMY-7378 1 8.90
CHEMBL1946778 1 8.70
CHEMBL1946782 1 8.46
CHEMBL1946783 1 8.46
CHEMBL37883 1 8.45
CHEMBL56 8-OH-DPAT 1 8.43
CHEMBL1946780 1 8.36
CHEMBL1946784 1 8.03
CHEMBL1946785 1 8.02
CHEMBL1946781 1 7.98
CHEMBL1946777 1 7.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946786 Ki = 0.3236 nM 9.49
CHEMBL514874 Ki = 0.3311 nM 9.48
CHEMBL1946787 Ki = 0.5623 nM 9.25
CHEMBL286003 Ki = 0.6026 nM 9.22
CHEMBL1946788 Ki = 0.7943 nM 9.10
CHEMBL1946779 Ki = 0.8318 nM 9.08
CHEMBL13647 BMY-7378 Ki = 1.259 nM 8.90
CHEMBL1946778 Ki = 1.995 nM 8.70
CHEMBL1946782 Ki = 3.467 nM 8.46
CHEMBL1946783 Ki = 3.467 nM 8.46
CHEMBL37883 Ki = 3.548 nM 8.45
CHEMBL56 8-OH-DPAT Ki = 3.715 nM 8.43
CHEMBL1946780 Ki = 4.365 nM 8.36
CHEMBL1946784 Ki = 9.333 nM 8.03
CHEMBL1946785 Ki = 9.55 nM 8.02
CHEMBL1946781 Ki = 10.47 nM 7.98
CHEMBL1946777 Ki = 22.91 nM 7.64