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Assay Detail

CHEMBL3744664

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

Binding
Displacement of [3H]-Prazosin from alpha-1 adrenergic receptor in rat cerebral cortex after 1 hr by microplate reader based assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Adrenergic receptor alpha-1 (CHEMBL1907610)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Arylsulfonamide derivatives of (aryloxy)ethylpiperidines as selective 5-HT7receptor antagonists and their psychotropic properties
Zajdel P, Canale V, Partyka A, Marciniec K, Kurczab R, Sataa G, Siwek A, Jastrzebska-Wiesek M, Wesoowska A, Kos T, Popik P, Bojarski AJ
Medchemcomm (2015) 6 : 1272 -1277
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.04 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3739745 1 6.41
CHEMBL3740235 1 6.23
CHEMBL3742076 1 6.20
CHEMBL3739680 1 6.15
CHEMBL3740054 1 6.01
CHEMBL3740055 1 5.70
CHEMBL2159466 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3739745 Ki = 389.0 nM 6.41
CHEMBL3740235 Ki = 589.0 nM 6.23
CHEMBL3742076 Ki = 629.0 nM 6.20
CHEMBL3739680 Ki = 712.0 nM 6.15
CHEMBL3740054 Ki = 979.0 nM 6.01
CHEMBL3740055 Ki = 2019.0 nM 5.70
CHEMBL2159466 Ki = 2541.0 nM 5.59