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Assay Detail

CHEMBL1246632

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

Binding
Displacement [3H]8-OH-DPAT of human cloned 5HT1A receptor expressed in human HeLa cells by rapid filtration technique
15
Total Activities
15
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

1,3-Dioxolane-based ligands incorporating a lactam or imide moiety: structure-affinity/activity relationship at alpha1-adrenoceptor subtypes and at 5-HT1A receptors.
Franchini S, Prandi A, Baraldi A, Sorbi C, Tait A, Buccioni M, Marucci G, Cilia A, Pirona L, Fossa P, Cichero E, Brasili L.
Eur J Med Chem (2010) 45 : 3740 -3751
PubMed 20605276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.29 9.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31354 WAY-100,635 1 9.48
CHEMBL1241557 1 8.90
CHEMBL13647 BMY-7378 1 8.90
CHEMBL1242912 1 8.58
CHEMBL1242818 1 8.50
CHEMBL1242542 1 8.29
CHEMBL1242724 1 8.29
CHEMBL1242541 1 8.28
CHEMBL1242632 1 8.25
CHEMBL1242444 1 8.16
CHEMBL1242633 1 8.14
CHEMBL1242445 1 7.95
CHEMBL1242352 1 7.64
CHEMBL1242725 1 7.59
CHEMBL1242819 1 7.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31354 WAY-100,635 Ki = 0.3311 nM 9.48
CHEMBL1241557 Ki = 1.259 nM 8.90
CHEMBL13647 BMY-7378 Ki = 1.259 nM 8.90
CHEMBL1242912 Ki = 2.63 nM 8.58
CHEMBL1242818 Ki = 3.162 nM 8.50
CHEMBL1242542 Ki = 5.129 nM 8.29
CHEMBL1242724 Ki = 5.129 nM 8.29
CHEMBL1242541 Ki = 5.248 nM 8.28
CHEMBL1242632 Ki = 5.623 nM 8.25
CHEMBL1242444 Ki = 6.918 nM 8.16
CHEMBL1242633 Ki = 7.244 nM 8.14
CHEMBL1242445 Ki = 11.22 nM 7.95
CHEMBL1242352 Ki = 22.91 nM 7.64
CHEMBL1242725 Ki = 25.7 nM 7.59
CHEMBL1242819 Ki = 44.67 nM 7.35