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Assay Detail

CHEMBL5530376

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Functional
Agonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as induction of accumulation of cAMP by HTRF assay
ChEMBL ↗
44
Total Activities
44
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

Discovery and Identification of Novel 5-Hydroxy-4<i>H</i>-benzo[1,4]oxazin-3-one Derivatives as Potent β<sub>2</sub>-Adrenoceptor Agonists through Structure-Based Design, Synthesis, and Biological Evaluation.
Xing G, Li Z, Zhi Z, Yi C, Zhang R, Yang H, Zhang Y, Lin B, Liu Y, Pan L, Cheng M.
J Med Chem (2024) 67 : 2986 -3003
PubMed 38347756 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 44 10.40 10.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5570917 — — 1 10.94
CHEMBL5574011 — — 1 10.88
CHEMBL5571865 — — 1 10.88
CHEMBL5571445 — — 1 10.80
CHEMBL5573592 — — 1 10.65
CHEMBL5574770 — — 1 10.65
CHEMBL5565495 — — 1 10.62
CHEMBL5572643 — — 1 10.59
CHEMBL5571279 — — 1 10.57
CHEMBL5594851 — — 1 10.55
CHEMBL5592612 — — 1 10.52
CHEMBL5571660 — — 1 10.51
CHEMBL5532178 — — 1 10.50
CHEMBL5594574 — — 1 10.37
CHEMBL5566587 — — 1 10.33
CHEMBL5574906 — — 1 10.27
CHEMBL605846 OLODATEROL 4.0 1 10.26
CHEMBL1263 SALMETEROL 4.0 1 10.14
CHEMBL5571981 — — 1 10.06
CHEMBL434 ISOPROTERENOL 4.0 1 9.33
CHEMBL5593074 — — 1 8.88
CHEMBL5571785 — — 1 -
CHEMBL5575290 — — 1 -
CHEMBL5573953 — — 1 -
CHEMBL5575873 — — 1 -
CHEMBL5567636 — — 1 -
CHEMBL5572781 — — 1 -
CHEMBL5565088 — — 1 -
CHEMBL5564275 — — 1 -
CHEMBL5568704 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5570917 — EC50 = 0.01148 nM 10.94
CHEMBL5574011 — EC50 = 0.01318 nM 10.88
CHEMBL5571865 — EC50 = 0.01318 nM 10.88
CHEMBL5571445 — EC50 = 0.01585 nM 10.80
CHEMBL5573592 — EC50 = 0.02239 nM 10.65
CHEMBL5574770 — EC50 = 0.02239 nM 10.65
CHEMBL5565495 — EC50 = 0.02399 nM 10.62
CHEMBL5572643 — EC50 = 0.0257 nM 10.59
CHEMBL5571279 — EC50 = 0.02692 nM 10.57
CHEMBL5594851 — EC50 = 0.02818 nM 10.55
CHEMBL5592612 — EC50 = 0.0302 nM 10.52
CHEMBL5571660 — EC50 = 0.0309 nM 10.51
CHEMBL5532178 — EC50 = 0.03162 nM 10.50
CHEMBL5594574 — EC50 = 0.04266 nM 10.37
CHEMBL5566587 — EC50 = 0.04677 nM 10.33
CHEMBL5574906 — EC50 = 0.0537 nM 10.27
CHEMBL605846 OLODATEROL EC50 = 0.05495 nM 10.26
CHEMBL1263 SALMETEROL EC50 = 0.07244 nM 10.14
CHEMBL5571981 — EC50 = 0.0871 nM 10.06
CHEMBL434 ISOPROTERENOL EC50 = 0.4677 nM 9.33
CHEMBL5593074 — EC50 = 1.318 nM 8.88
CHEMBL5571651 — EC50 = 0.003715 nM -
CHEMBL5590155 — EC50 = 0.00537 nM -
CHEMBL5562809 — EC50 = 0.005888 nM -
CHEMBL5573712 — EC50 = 0.00912 nM -
CHEMBL5570658 — EC50 = 0.007244 nM -
CHEMBL5569415 — EC50 = 0.003802 nM -
CHEMBL5563982 — EC50 = 0.004677 nM -
CHEMBL5550060 — EC50 = 0.004786 nM -
CHEMBL5574456 — EC50 = 0.002399 nM -
CHEMBL5555646 — EC50 = 0.005495 nM -
CHEMBL5570025 — EC50 = 0.007586 nM -
CHEMBL5555612 — EC50 = 0.00871 nM -
CHEMBL5595588 — EC50 = 0.004365 nM -
CHEMBL5570271 — EC50 = 0.006166 nM -
CHEMBL5568704 — EC50 = 0.003802 nM -
CHEMBL5564275 — EC50 = 0.007943 nM -
CHEMBL5565088 — EC50 = 0.004571 nM -
CHEMBL5572781 — EC50 = 0.005754 nM -
CHEMBL5567636 — EC50 = 0.004365 nM -
CHEMBL5575873 — EC50 = 0.00631 nM -
CHEMBL5573953 — EC50 = 0.006166 nM -
CHEMBL5575290 — EC50 = 0.003802 nM -
CHEMBL5571785 — EC50 = 0.007586 nM -