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Assay Detail

CHEMBL4353357

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

Binding
Displacement of [3H] prazosin from human cloned adrenoceptor alpha 1D expressed in CHO cell membrane incubated for 30 mins by liquid scintillation counter
21
Total Activities
21
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 Autocuration

Target

Alpha-1D adrenergic receptor (CHEMBL223)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

1,3-Dioxane as a scaffold for potent and selective 5-HT1AR agonist with in-vivo anxiolytic, anti-depressant and anti-nociceptive activity.
Franchini S, Sorbi C, Linciano P, Carnevale G, Tait A, Ronsisvalle S, Buccioni M, Del Bello F, Cilia A, Pirona L, Denora N, Iacobazzi RM, Brasili L.
Eur J Med Chem (2019) 176 : 310 -325
PubMed 31112892 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 21 7.85 8.99

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4467585 1 8.99
CHEMBL4462600 1 8.92
CHEMBL4526865 1 8.36
CHEMBL31354 WAY-100,635 1 8.34
CHEMBL4582160 1 8.30
CHEMBL4458714 1 8.24
CHEMBL4439658 1 8.23
CHEMBL4570387 1 8.15
CHEMBL286003 1 8.03
CHEMBL4468507 1 8.00
CHEMBL37883 1 7.94
CHEMBL4551941 1 7.80
CHEMBL4579802 1 7.78
CHEMBL4588223 1 7.60
CHEMBL4462768 1 7.53
CHEMBL4520390 1 7.52
CHEMBL4558985 1 7.24
CHEMBL4473623 1 7.12
CHEMBL4457585 1 7.06
CHEMBL4580335 1 7.02
CHEMBL4544457 1 6.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4467585 Ki = 1.023 nM 8.99
CHEMBL4462600 Ki = 1.202 nM 8.92
CHEMBL4526865 Ki = 4.365 nM 8.36
CHEMBL31354 WAY-100,635 Ki = 4.571 nM 8.34
CHEMBL4582160 Ki = 5.012 nM 8.30
CHEMBL4458714 Ki = 5.754 nM 8.24
CHEMBL4439658 Ki = 5.888 nM 8.23
CHEMBL4570387 Ki = 7.079 nM 8.15
CHEMBL286003 Ki = 9.333 nM 8.03
CHEMBL4468507 Ki = 10.0 nM 8.00
CHEMBL37883 Ki = 11.48 nM 7.94
CHEMBL4551941 Ki = 15.85 nM 7.80
CHEMBL4579802 Ki = 16.6 nM 7.78
CHEMBL4588223 Ki = 25.12 nM 7.60
CHEMBL4462768 Ki = 29.51 nM 7.53
CHEMBL4520390 Ki = 30.2 nM 7.52
CHEMBL4558985 Ki = 57.54 nM 7.24
CHEMBL4473623 Ki = 75.86 nM 7.12
CHEMBL4457585 Ki = 87.1 nM 7.06
CHEMBL4580335 Ki = 95.5 nM 7.02
CHEMBL4544457 Ki = 177.83 nM 6.75