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Assay Detail

CHEMBL643405

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

Binding
in vitro alpha-1 adrenergic receptor binding assay from rats, using RX 821002 as the displaceable ligand
7
Total Activities
7
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

Alpha(2) adrenoceptor agonists as potential analgesic agents. 2. Discovery of 4-(4-imidazo)-1,3-dimethyl-6,7-dihydro-thianaphthene as a high-affinity ligand for the alpha(2D) adrenergic receptor.
Ross TM, Jetter MC, McDonnell ME, Boyd RE, Connelly CD, Martinez RP, Lewis MA, Codd EE, Raffa RB, Reitz AB.
J Med Chem (2000) 43 : 1423 -1426
PubMed 10753480 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 6.87 7.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL30739 1 7.32
CHEMBL286269 1 7.04
CHEMBL284213 1 6.96
CHEMBL284795 1 6.96
CHEMBL134 CLONIDINE 4.0 1 6.94
CHEMBL30534 1 6.46
CHEMBL30955 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL30739 Ki = 48.0 nM 7.32
CHEMBL286269 Ki = 91.0 nM 7.04
CHEMBL284213 Ki = 110.0 nM 6.96
CHEMBL284795 Ki = 110.0 nM 6.96
CHEMBL134 CLONIDINE Ki = 116.0 nM 6.94
CHEMBL30534 Ki = 343.0 nM 6.46
CHEMBL30955 Ki = 399.0 nM 6.40