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Assay Detail

CHEMBL645693

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

Binding
The compound was evaluated for the inhibition of [3H]prazosin binding to alpha-1 adrenergic receptor from rat liver
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Conformationally defined adrenergic agents. 2. Catechol imidazoline derivatives: biological effects at alpha 1 and alpha 2 adrenergic receptors.
DeBernardis JF, Kyncl JJ, Basha FZ, Arendsen DL, Martin YC, Winn M, Kerkman DJ.
J Med Chem (1986) 29 : 463 -467
PubMed 2870187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.02 6.46

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL545092 1 6.46
CHEMBL1437 NOREPINEPHRINE 4.0 1 6.41
CHEMBL543684 1 6.40
CHEMBL544627 1 5.96
CHEMBL554004 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL545092 Ki = 350.0 nM 6.46
CHEMBL1437 NOREPINEPHRINE Ki = 390.0 nM 6.41
CHEMBL543684 Ki = 400.0 nM 6.40
CHEMBL544627 Ki = 1100.0 nM 5.96
CHEMBL554004 Ki = 13000.0 nM 4.89