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Assay Detail

CHEMBL3878028

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

Binding
Displacement of [3H]prazosin from recombinant human alpha1d adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
12
Total Activities
12
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

Synthesis, biological evaluation and molecular modeling of 1-oxa-4-thiaspiro- and 1,4-dithiaspiro[4.5]decane derivatives as potent and selective 5-HT1A receptor agonists.
Franchini S, Manasieva LI, Sorbi C, Battisti UM, Fossa P, Cichero E, Denora N, Iacobazzi RM, Cilia A, Pirona L, Ronsisvalle S, Aricò G, Brasili L.
Eur J Med Chem (2017) 125 : 435 -452
PubMed 27689727 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 7.27 9.09

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1963046 1 9.09
CHEMBL13647 BMY-7378 1 8.89
CHEMBL3901382 1 7.49
CHEMBL3938383 1 7.46
CHEMBL3892434 1 7.41
CHEMBL3981480 1 7.02
CHEMBL3929328 1 7.00
CHEMBL3917316 1 6.91
CHEMBL3970754 1 6.67
CHEMBL1183249 1 6.26
CHEMBL3911497 1 5.75
CHEMBL2234448 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1963046 Ki = 0.8128 nM 9.09
CHEMBL13647 BMY-7378 Ki = 1.288 nM 8.89
CHEMBL3901382 Ki = 32.36 nM 7.49
CHEMBL3938383 Ki = 34.67 nM 7.46
CHEMBL3892434 Ki = 38.9 nM 7.41
CHEMBL3981480 Ki = 95.5 nM 7.02
CHEMBL3929328 Ki = 100.0 nM 7.00
CHEMBL3917316 Ki = 123.03 nM 6.91
CHEMBL3970754 Ki = 213.8 nM 6.67
CHEMBL1183249 Ki = 549.54 nM 6.26
CHEMBL3911497 Ki = 1778.28 nM 5.75
CHEMBL2234448 Ki > 1000.0 nM -