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Assay Detail

CHEMBL4047797

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

Binding
Displacement of [3H]prazosin from rat salivary gland adrenergic alpha1a receptor
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Alpha-1A adrenergic receptor (CHEMBL319)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Identification of selective 8-(piperidin-4-yloxy)quinoline sulfone and sulfonamide histamine H1 receptor antagonists for use in allergic rhinitis.
Procopiou PA, Ford AJ, Gore PM, Hancock AP, Hodgson ST, Holmes DS, Looker BE, Vile S, Clark KL, Saunders KA, Slack RJ, Watts CJ.
Bioorg Med Chem Lett (2017) 27 : 4914 -4919
PubMed 28958623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 6.50 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL639 AZELASTINE 4.0 1 7.30
CHEMBL4088036 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL639 AZELASTINE Ki = 50.12 nM 7.30
CHEMBL4088036 Ki = 1995.26 nM 5.70