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Assay Detail

CHEMBL4610312

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Functional
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL ↗
35
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Design, synthesis and biological evaluation of 8-(2-amino-1-hydroxyethyl)-6-hydroxy-1,4-benzoxazine-3(4H)-one derivatives as potent β<sub>2</sub>-adrenoceptor agonists.
Yi C, Xing G, Wang S, Li X, Liu Y, Li J, Lin B, Woo AY, Zhang Y, Pan L, Cheng M.
Bioorg Med Chem (2020) 28 : 115178 -115178
PubMed 31753798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 35 9.72 10.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4634131 — — 1 10.79
CHEMBL4635163 — — 1 10.62
CHEMBL4646881 — — 1 10.59
CHEMBL4641262 — — 1 10.56
CHEMBL4642770 — — 1 10.54
CHEMBL4636255 — — 1 10.51
CHEMBL4638864 — — 1 10.49
CHEMBL4645203 — — 1 10.45
CHEMBL4644638 — — 1 10.40
CHEMBL1263 SALMETEROL 4.0 1 10.35
CHEMBL4645694 — — 1 10.31
CHEMBL4649233 — — 1 10.31
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE 4.0 1 10.26
CHEMBL4639822 — — 1 9.89
CHEMBL4648525 — — 1 9.85
CHEMBL4640925 — — 1 9.76
CHEMBL4648663 — — 1 9.76
CHEMBL4636111 — — 1 9.67
CHEMBL4643148 — — 1 9.60
CHEMBL4648975 — — 1 9.50
CHEMBL4645720 — — 1 9.42
CHEMBL4632876 — — 1 9.37
CHEMBL4632435 — — 1 9.21
CHEMBL4648695 — — 1 9.16
CHEMBL4645932 — — 1 9.13
CHEMBL4648440 — — 1 9.10
CHEMBL4643561 — — 1 9.05
CHEMBL4632700 — — 1 9.03
CHEMBL4647449 — — 1 8.87
CHEMBL4642893 — — 1 8.79

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4634131 — EC50 = 0.01622 nM 10.79
CHEMBL4635163 — EC50 = 0.02399 nM 10.62
CHEMBL4646881 — EC50 = 0.0257 nM 10.59
CHEMBL4641262 — EC50 = 0.02754 nM 10.56
CHEMBL4642770 — EC50 = 0.02884 nM 10.54
CHEMBL4636255 — EC50 = 0.0309 nM 10.51
CHEMBL4638864 — EC50 = 0.03236 nM 10.49
CHEMBL4645203 — EC50 = 0.03548 nM 10.45
CHEMBL4644638 — EC50 = 0.03981 nM 10.40
CHEMBL1263 SALMETEROL EC50 = 0.04467 nM 10.35
CHEMBL4645694 — EC50 = 0.04898 nM 10.31
CHEMBL4649233 — EC50 = 0.04898 nM 10.31
CHEMBL1711 ISOPROTERENOL HYDROCHLORIDE EC50 = 0.05495 nM 10.26
CHEMBL4639822 — EC50 = 0.1288 nM 9.89
CHEMBL4648525 — EC50 = 0.1413 nM 9.85
CHEMBL4640925 — EC50 = 0.1738 nM 9.76
CHEMBL4648663 — EC50 = 0.1738 nM 9.76
CHEMBL4636111 — EC50 = 0.2138 nM 9.67
CHEMBL4643148 — EC50 = 0.2512 nM 9.60
CHEMBL4648975 — EC50 = 0.3162 nM 9.50
CHEMBL4645720 — EC50 = 0.3802 nM 9.42
CHEMBL4632876 — EC50 = 0.4266 nM 9.37
CHEMBL4632435 — EC50 = 0.6166 nM 9.21
CHEMBL4648695 — EC50 = 0.6918 nM 9.16
CHEMBL4645932 — EC50 = 0.7413 nM 9.13
CHEMBL4648440 — EC50 = 0.7943 nM 9.10
CHEMBL4643561 — EC50 = 0.8913 nM 9.05
CHEMBL4632700 — EC50 = 0.9333 nM 9.03
CHEMBL4647449 — EC50 = 1.349 nM 8.87
CHEMBL4642893 — EC50 = 1.622 nM 8.79
CHEMBL4636080 — EC50 = 2.239 nM 8.65
CHEMBL4641339 — EC50 = 2.399 nM 8.62
CHEMBL4649718 — EC50 = 4.898 nM 8.31
CHEMBL4645927 — EC50 = 0.00912 nM -
CHEMBL2105743 OLODATEROL HYDROCHLORIDE EC50 = 0.008511 nM -