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Assay Detail

CHEMBL645550

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

Binding
Binding affinity towards Alpha-1 adrenergic receptor of rat brain
9
Total Activities
9
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

Conformational effects on the activity of drugs. 13. A revision of previously proposed models for the activation of alpha- and beta-adrenergic receptors.
Macchia B, Balsamo A, Breschi MC, Lapucci A, Lucacchini A, Macchia F, Manera C, Martinelli A, Martini C, Martinotti E.
J Med Chem (1992) 35 : 1009 -1018
PubMed 1313109 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.48 6.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL7185 1 6.52
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.35
CHEMBL6898 1 5.92
CHEMBL268881 1 5.17
CHEMBL7681 1 5.13
CHEMBL7278 1 4.82
CHEMBL266290 1 4.44
CHEMBL7160 1 -
CHEMBL6913 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL7185 Ki = 300.0 nM 6.52
CHEMBL1437 NOREPINEPHRINE Ki = 450.0 nM 6.35
CHEMBL6898 Ki = 1200.0 nM 5.92
CHEMBL268881 Ki = 6700.0 nM 5.17
CHEMBL7681 Ki = 7400.0 nM 5.13
CHEMBL7278 Ki = 15000.0 nM 4.82
CHEMBL266290 Ki = 36000.0 nM 4.44
CHEMBL7160 Ki > 100000.0 nM -
CHEMBL6913 Ki > 100000.0 nM -