Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL652747

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

Binding
Alpha-1 adrenergic receptor binding affinity in rat brain membranes
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Medetomidine analogs as alpha 2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine.
Zhang X, Yao XT, Dalton JT, Shams G, Lei L, Patil PN, Feller DR, Hsu FL, George C, Miller DD.
J Med Chem (1996) 39 : 3001 -3013
PubMed 8709134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.30 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105328 1 7.26
CHEMBL322844 1 7.24
CHEMBL306751 1 6.65
CHEMBL102669 1 6.41
CHEMBL102076 1 6.24
CHEMBL420652 1 6.18
CHEMBL77921 MEDETOMIDINE 3.0 1 5.96
CHEMBL105487 1 5.76
CHEMBL677 LEVONORDEFRIN 4.0 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105328 Ki = 55.0 nM 7.26
CHEMBL322844 Ki = 57.0 nM 7.24
CHEMBL306751 Ki = 224.0 nM 6.65
CHEMBL102669 Ki = 387.0 nM 6.41
CHEMBL102076 Ki = 574.0 nM 6.24
CHEMBL420652 Ki = 655.0 nM 6.18
CHEMBL77921 MEDETOMIDINE Ki = 1109.0 nM 5.96
CHEMBL105487 Ki = 1734.0 nM 5.76
CHEMBL677 LEVONORDEFRIN Ki = 9221.0 nM 5.04