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Assay Detail

CHEMBL645792

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

Binding
Compound was tested for binding affinity based on dissociation constant of Alpha-1 adrenergic receptor
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 (CHEMBL2094251)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Synthesis and evaluation of 2-[(5-methylbenz-1-ox-4-azin-6-yl)imino]imidazoline, a potent, peripherally acting alpha 2 adrenoceptor agonist.
Munk SA, Harcourt D, Ambrus G, Denys L, Gluchowski C, Burke JA, Kharlamb AB, Manlapaz CA, Padillo EU, Runde E, Williams L, Wheeler LA, Garst ME.
J Med Chem (1996) 39 : 3533 -3538
PubMed 8784451 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.06 6.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL647 APRACLONIDINE 4.0 1 6.75
CHEMBL298936 1 6.33
CHEMBL134 CLONIDINE 4.0 1 6.29
CHEMBL49137 1 5.85
CHEMBL49284 1 5.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL647 APRACLONIDINE Ki = 180.0 nM 6.75
CHEMBL298936 Ki = 470.0 nM 6.33
CHEMBL134 CLONIDINE Ki = 510.0 nM 6.29
CHEMBL49137 Ki = 1400.0 nM 5.85
CHEMBL49284 Ki = 8700.0 nM 5.06