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Assay Detail

CHEMBL4312088

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

Binding
Antagonist activity at human recombinant beta2 adrenoreceptor expressed in CHOK1 cells incubated for 30 mins by HTRF
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Beta-2 adrenergic receptor (CHEMBL210)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Controlling cellular distribution of drugs with permeability modifying moieties.
Richardson PL, Marin VL, Koeniger SL, Baranczak A, Wilsbacher JL, Kovar PJ, Bacon-Trusk PE, Cheng M, Hopkins TA, Haman ST, Vasudevan A.
Medchemcomm (2019) 10 : 974 -984
PubMed 31303996 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.28 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL266195 ALPRENOLOL 2.0 1 8.48
CHEMBL4466532 1 8.16
CHEMBL4458797 1 7.72
CHEMBL4542960 1 7.66
CHEMBL4459696 1 7.14
CHEMBL4545079 1 7.08
CHEMBL4475573 1 7.07
CHEMBL4452249 1 7.02
CHEMBL4587648 1 7.00
CHEMBL4454523 1 6.42
CHEMBL4527905 1 6.30
CHEMBL4440189 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL266195 ALPRENOLOL IC50 = 3.3 nM 8.48
CHEMBL4466532 IC50 = 6.9 nM 8.16
CHEMBL4458797 IC50 = 19.0 nM 7.72
CHEMBL4542960 IC50 = 22.0 nM 7.66
CHEMBL4459696 IC50 = 72.0 nM 7.14
CHEMBL4545079 IC50 = 83.4 nM 7.08
CHEMBL4475573 IC50 = 86.0 nM 7.07
CHEMBL4452249 IC50 = 96.0 nM 7.02
CHEMBL4587648 IC50 = 100.0 nM 7.00
CHEMBL4454523 IC50 = 380.0 nM 6.42
CHEMBL4527905 IC50 = 500.0 nM 6.30
CHEMBL4440189 IC50 > 1000.0 nM -