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Assay Detail

CHEMBL644077

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

Binding
Binding affinity against adrenergic beta 2 receptor versus 1 nM [3H]dihydroalprenolol in rat cerebral cerebellar membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Cerebellum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Beta-2 adrenergic receptor (CHEMBL3754)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Syntheses of 2,5- and 2,6-difluoronorepinephrine, 2,5-difluoroepinephrine, and 2,6-difluorophenylephrine: effect of disubstitution with fluorine on adrenergic activity.
Chen GT, King M, Gusovsky F, Creveling CR, Daly JW, Chen BH, Nie JY, Kirk KL.
J Med Chem (1993) 36 : 3947 -3955
PubMed 8254623 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.55 6.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL126347 1 6.15
CHEMBL679 EPINEPHRINE 4.0 1 6.14
CHEMBL287587 1 5.82
CHEMBL1437 NOREPINEPHRINE 4.0 1 5.38
CHEMBL129190 1 5.26
CHEMBL281232 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL126347 Ki = 710.0 nM 6.15
CHEMBL679 EPINEPHRINE Ki = 720.0 nM 6.14
CHEMBL287587 Ki = 1500.0 nM 5.82
CHEMBL1437 NOREPINEPHRINE Ki = 4200.0 nM 5.38
CHEMBL129190 Ki = 5500.0 nM 5.26
CHEMBL281232 Ki = 29000.0 nM 4.54