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Assay Detail

CHEMBL644381

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

Binding
In vitro affinity for alpha adrenergic receptor by displacement of 3[H]clonidine in calf cerebral cortex
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Tissue Cerebral cortex
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Cerebral cortex alpha adrenergic receptor (CHEMBL2111420)
Type PROTEIN FAMILY
Organism Bos taurus

Publication

Synthesis of (7R)-7H-indolo[3,4-gh][1,4]benzoxazines, a new class of D-heteroergolines with dopamine agonist activity.
Anderson PS, Baldwin JJ, McClure DE, Lundell GF, Jones JH, Randall WC, Martin GE, Williams M, Hirshfield JM, Clineschmidt BV, Lumma PK, Remy DC.
J Med Chem (1983) 26 : 363 -367
PubMed 6298427 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 7.21 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333794 4 8.15
CHEMBL330997 1 7.57
CHEMBL333795 1 7.51
CHEMBL531 PERGOLIDE 4.0 1 7.39
CHEMBL332337 1 7.34
CHEMBL121653 1 7.26
CHEMBL332546 1 6.69
CHEMBL493 BROMOCRIPTINE 4.0 1 6.29

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333794 IC50 = 7.0 nM 8.15
CHEMBL333794 IC50 = 15.0 nM 7.82
CHEMBL330997 IC50 = 27.0 nM 7.57
CHEMBL333795 IC50 = 31.0 nM 7.51
CHEMBL333794 IC50 = 34.0 nM 7.47
CHEMBL531 PERGOLIDE IC50 = 41.0 nM 7.39
CHEMBL332337 IC50 = 46.0 nM 7.34
CHEMBL121653 IC50 = 55.0 nM 7.26
CHEMBL332546 IC50 = 206.0 nM 6.69
CHEMBL493 BROMOCRIPTINE IC50 = 514.0 nM 6.29
CHEMBL333794 IC50 = 1354.0 nM 5.87