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Assay Detail

CHEMBL3379944

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Functional
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type A-431
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

The identification of 7-[(R)-2-((1S,2S)-2-benzyloxycyclopentylamino)-1-hydroxyethyl]-4-hydroxybenzothiazolone as an inhaled long-acting β2-adrenoceptor agonist.
Arnold N, Beattie D, Bradley M, Brearley A, Brown L, Charlton SJ, Fairhurst RA, Farr D, Fozard J, Fullerton J, Gosling M, Hatto J, Janus D, Jones D, Jordan L, Lewis C, Maas J, McCarthy C, Mercer M, Oakman H, Press N, Profit R, Schuerch F, Sykes D, Taylor RJ, Trifilieff A, Tuffnell A.
Bioorg Med Chem Lett (2014) 24 : 4341 -4347
PubMed 25065493 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 9.21 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1221681 1 9.60
CHEMBL1095777 INDACATEROL 4.0 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1221681 EC50 = 0.25 nM 9.60
CHEMBL1095777 INDACATEROL EC50 = 1.5 nM 8.82