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Assay Detail

CHEMBL643926

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

Binding
Binding affinity towards Alpha-2 adrenergic receptor
11
Total Activities
11
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-2 (CHEMBL2093864)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Novel pyridazino[4,5-b][1,5]oxazepines and -thiazepines as 5-HT1A receptor ligands
Matyus P, Varga I, Zara E, Mezei A, Behr A, Simay A, Haider N, Boros S, Bakonyi A, Horvath E, Horvath K
Bioorg Med Chem Lett (1997) 7 : 2857 -2862
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.51 6.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL316490 1 6.57
CHEMBL99523 1 6.27
CHEMBL318857 1 6.07
CHEMBL95832 1 5.75
CHEMBL95837 1 5.63
CHEMBL95310 1 5.51
CHEMBL319937 1 5.41
CHEMBL97618 1 5.34
CHEMBL100260 1 5.02
CHEMBL97711 1 4.68
CHEMBL319600 1 4.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL316490 IC50 = 270.0 nM 6.57
CHEMBL99523 IC50 = 540.0 nM 6.27
CHEMBL318857 IC50 = 860.0 nM 6.07
CHEMBL95832 IC50 = 1800.0 nM 5.75
CHEMBL95837 IC50 = 2330.0 nM 5.63
CHEMBL95310 IC50 = 3100.0 nM 5.51
CHEMBL319937 IC50 = 3900.0 nM 5.41
CHEMBL97618 IC50 = 4600.0 nM 5.34
CHEMBL100260 IC50 = 9500.0 nM 5.02
CHEMBL97711 IC50 = 21000.0 nM 4.68
CHEMBL319600 IC50 = 47000.0 nM 4.33