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Assay Detail

CHEMBL648171

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

Binding
Binding affinity was evaluated on chinese hamster ovary (CHO) cells expressing the cloned human beta-3 adrenergic receptor in the presence of [125I]- iodocyanopindolol.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Beta-3 adrenergic receptor (CHEMBL246)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a potent, orally bioavailable beta(3) adrenergic receptor agonist, (R)-N-[4-[2-[[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4 -[4-(trifluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide.
Mathvink RJ, Tolman JS, Chitty D, Candelore MR, Cascieri MA, Colwell LF, Deng L, Feeney WP, Forrest MJ, Hom GJ, MacIntyre DE, Miller RR, Stearns RA, Tota L, Wyvratt MJ, Fisher MH, Weber AE.
J Med Chem (2000) 43 : 3832 -3836
PubMed 11052788 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.52 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL293994 1 7.70
CHEMBL331744 1 7.52
CHEMBL111201 1 7.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL293994 IC50 = 20.0 nM 7.70
CHEMBL331744 IC50 = 30.0 nM 7.52
CHEMBL111201 IC50 = 46.0 nM 7.34