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Assay Detail

CHEMBL3878026

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

Binding
Displacement of [3H]prazosin from recombinant human alpha1a adrenergic receptor expressed in CHO cell membranes after 30 mins by TopCount liquid scintillation counting method
11
Total Activities
11
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-1A adrenergic receptor (CHEMBL229)
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 11 6.76 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3892434 1 7.24
CHEMBL2234448 1 7.04
CHEMBL3938383 1 6.73
CHEMBL3929328 1 6.70
CHEMBL3981480 1 6.64
CHEMBL3901382 1 6.57
CHEMBL13647 BMY-7378 1 6.41
CHEMBL1183249 1 -
CHEMBL3911497 1 -
CHEMBL3970754 1 -
CHEMBL3917316 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3892434 Ki = 57.54 nM 7.24
CHEMBL2234448 Ki = 91.2 nM 7.04
CHEMBL3938383 Ki = 186.21 nM 6.73
CHEMBL3929328 Ki = 199.53 nM 6.70
CHEMBL3981480 Ki = 229.09 nM 6.64
CHEMBL3901382 Ki = 269.15 nM 6.57
CHEMBL13647 BMY-7378 Ki = 389.05 nM 6.41
CHEMBL1183249 Ki > 1000.0 nM -
CHEMBL3911497 Ki > 1000.0 nM -
CHEMBL3970754 Ki > 1000.0 nM -
CHEMBL3917316 Ki > 1000.0 nM -