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Assay Detail

CHEMBL648029

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor from rat whole brain using [3H]prazosin (18.1 Ci/mmol,0.9nanoM)as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Novel indolodioxanes with antihypertensive effects: potent ligands for the 5-HT1A receptor.
Ennis MD, Baze ME, Smith MW, Lawson CF, McCall RB, Lahti RA, Piercey MF.
J Med Chem (1992) 35 : 3058 -3066
PubMed 1323682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 8.02 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318374 1 9.22
CHEMBL418802 1 8.74
CHEMBL101535 1 8.22
CHEMBL323088 1 8.06
CHEMBL103983 1 7.94
CHEMBL319023 1 7.91
CHEMBL101483 1 7.70
CHEMBL320880 1 7.53
CHEMBL318166 1 7.52
CHEMBL102175 1 7.40
CHEMBL106283 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318374 Ki = 0.6 nM 9.22
CHEMBL418802 Ki = 1.8 nM 8.74
CHEMBL101535 Ki = 6.0 nM 8.22
CHEMBL323088 Ki = 8.8 nM 8.06
CHEMBL103983 Ki = 11.4 nM 7.94
CHEMBL319023 Ki = 12.3 nM 7.91
CHEMBL101483 Ki = 19.8 nM 7.70
CHEMBL320880 Ki = 29.4 nM 7.53
CHEMBL318166 Ki = 30.4 nM 7.52
CHEMBL102175 Ki = 39.6 nM 7.40
CHEMBL106283 Ki > 862.0 nM -