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Assay Detail

CHEMBL619203

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

Binding
Affinity constant on CHO cells expressing Human recombinant 5-hydroxytryptamine receptor 1A
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.
Quaglia W, Pigini M, Piergentili A, Giannella M, Gentili F, Marucci G, Carrieri A, Carotti A, Poggesi E, Leonardi A, Melchiorre C.
J Med Chem (2002) 45 : 1633 -1643
PubMed 11931617 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 8.47 10.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL43116 1 10.17
CHEMBL13647 BMY-7378 1 9.43
CHEMBL42231 1 8.20
CHEMBL42472 1 8.19
CHEMBL40325 1 7.99
CHEMBL42558 1 7.97
CHEMBL44403 1 7.96
CHEMBL43905 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL43116 Ki = 0.06761 nM 10.17
CHEMBL13647 BMY-7378 Ki = 0.3715 nM 9.43
CHEMBL42231 Ki = 6.31 nM 8.20
CHEMBL42472 Ki = 6.457 nM 8.19
CHEMBL40325 Ki = 10.23 nM 7.99
CHEMBL42558 Ki = 10.72 nM 7.97
CHEMBL44403 Ki = 10.96 nM 7.96
CHEMBL43905 Ki = 15.14 nM 7.82