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Assay Detail

CHEMBL1251069

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

Binding
Displacement of [3H]8-OH-DPAT from human adrenergic 5HT1A expressed in human HeLa cells cells
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

Structure-activity relationships in 1,4-benzodioxan-related compounds. 10. Novel α1-adrenoreceptor antagonists related to openphendioxan: synthesis, biological evaluation, and α1d computational study.
Carrieri A, Piergentili A, Del Bello F, Giannella M, Pigini M, Leonardi A, Fanelli F, Quaglia W.
Bioorg Med Chem (2010) 18 : 7065 -7077
PubMed 20801662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 8.06 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25554 1 8.68
CHEMBL1254659 1 8.60
CHEMBL1254915 1 8.60
CHEMBL1254660 1 8.50
CHEMBL1254829 1 8.40
CHEMBL1254914 1 8.30
CHEMBL1255086 1 8.10
CHEMBL43116 1 7.93
CHEMBL1255085 1 7.90
CHEMBL1254582 1 7.80
CHEMBL1254743 1 7.80
CHEMBL1255003 1 7.80
CHEMBL1254742 1 7.50
CHEMBL1254828 1 7.50
CHEMBL1255002 1 7.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25554 Ki = 2.089 nM 8.68
CHEMBL1254659 Ki = 2.512 nM 8.60
CHEMBL1254915 Ki = 2.512 nM 8.60
CHEMBL1254660 Ki = 3.162 nM 8.50
CHEMBL1254829 Ki = 3.981 nM 8.40
CHEMBL1254914 Ki = 5.012 nM 8.30
CHEMBL1255086 Ki = 7.943 nM 8.10
CHEMBL43116 Ki = 11.75 nM 7.93
CHEMBL1255085 Ki = 12.59 nM 7.90
CHEMBL1254582 Ki = 15.85 nM 7.80
CHEMBL1254743 Ki = 15.85 nM 7.80
CHEMBL1255003 Ki = 15.85 nM 7.80
CHEMBL1254742 Ki = 31.62 nM 7.50
CHEMBL1254828 Ki = 31.62 nM 7.50
CHEMBL1255002 Ki = 31.62 nM 7.50