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Assay Detail

CHEMBL648585

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

Binding
In vitro radioligand binding assay on adrenaline Alpha-1 adrenergic receptor of rat cortex using [3H]- prazosin
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

N-[2-[(substituted chroman-8-yl)oxy]ethyl]-4-(4-methoxyphenyl)butylamines: synthesis and wide range of antagonism at the human 5-HT1A receptor.
Yasunaga T, Naito R, Kontani T, Tsukamoto S, Nomura T, Yamaguchi T, Mase T.
J Med Chem (1997) 40 : 1252 -1257
PubMed 9111299 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.19 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25213 1 8.57
CHEMBL25215 1 8.29
CHEMBL278806 1 8.06
CHEMBL22682 1 7.84
CHEMBL25663 1 7.55
CHEMBL21475 1 7.46
CHEMBL22328 1 7.15
CHEMBL22802 1 7.01
CHEMBL38288 1 6.05
CHEMBL283968 1 5.90
CHEMBL22778 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25213 Ki = 2.71 nM 8.57
CHEMBL25215 Ki = 5.19 nM 8.29
CHEMBL278806 Ki = 8.77 nM 8.06
CHEMBL22682 Ki = 14.3 nM 7.84
CHEMBL25663 Ki = 27.9 nM 7.55
CHEMBL21475 Ki = 35.1 nM 7.46
CHEMBL22328 Ki = 71.5 nM 7.15
CHEMBL22802 Ki = 98.4 nM 7.01
CHEMBL38288 Ki = 897.0 nM 6.05
CHEMBL283968 Ki = 1260.0 nM 5.90
CHEMBL22778 Ki = 6080.0 nM 5.22