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Assay Detail

CHEMBL5530377

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Functional
Agonist activity at human beta1 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-1 adrenergic receptor (CHEMBL213) ↗
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 8.85 9.98

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5574456 — — 1 9.98
CHEMBL5572781 — — 1 9.92
CHEMBL5575873 — — 1 9.89
CHEMBL5567636 — — 1 9.86
CHEMBL5563982 — — 1 9.82
CHEMBL5550060 — — 1 9.77
CHEMBL5565088 — — 1 9.75
CHEMBL5573953 — — 1 9.63
CHEMBL5569415 — — 1 9.61
CHEMBL5595588 — — 1 9.61
CHEMBL5562809 — — 1 9.59
CHEMBL5574770 — — 1 9.51
CHEMBL5570271 — — 1 9.49
CHEMBL5564275 — — 1 9.40
CHEMBL5568704 — — 1 9.29
CHEMBL5592612 — — 1 9.29
CHEMBL5571785 — — 1 9.13
CHEMBL5594851 — — 1 9.04
CHEMBL5570658 — — 1 9.00
CHEMBL5555646 — — 1 8.92
CHEMBL5573592 — — 1 8.88
CHEMBL5565495 — — 1 8.86
CHEMBL5574906 — — 1 8.80
CHEMBL5571651 — — 1 8.77
CHEMBL5571445 — — 1 8.77
CHEMBL434 ISOPROTERENOL 4.0 1 8.75
CHEMBL5570025 — — 1 8.74
CHEMBL5573712 — — 1 8.72
CHEMBL5555612 — — 1 8.70
CHEMBL5575290 — — 1 8.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5574456 — EC50 = 0.1047 nM 9.98
CHEMBL5572781 — EC50 = 0.1202 nM 9.92
CHEMBL5575873 — EC50 = 0.1288 nM 9.89
CHEMBL5567636 — EC50 = 0.138 nM 9.86
CHEMBL5563982 — EC50 = 0.1514 nM 9.82
CHEMBL5550060 — EC50 = 0.1698 nM 9.77
CHEMBL5565088 — EC50 = 0.1778 nM 9.75
CHEMBL5573953 — EC50 = 0.2344 nM 9.63
CHEMBL5569415 — EC50 = 0.2455 nM 9.61
CHEMBL5595588 — EC50 = 0.2455 nM 9.61
CHEMBL5562809 — EC50 = 0.257 nM 9.59
CHEMBL5574770 — EC50 = 0.309 nM 9.51
CHEMBL5570271 — EC50 = 0.3236 nM 9.49
CHEMBL5564275 — EC50 = 0.3981 nM 9.40
CHEMBL5592612 — EC50 = 0.5129 nM 9.29
CHEMBL5568704 — EC50 = 0.5129 nM 9.29
CHEMBL5571785 — EC50 = 0.7413 nM 9.13
CHEMBL5594851 — EC50 = 0.912 nM 9.04
CHEMBL5570658 — EC50 = 1.0 nM 9.00
CHEMBL5555646 — EC50 = 1.202 nM 8.92
CHEMBL5573592 — EC50 = 1.318 nM 8.88
CHEMBL5565495 — EC50 = 1.38 nM 8.86
CHEMBL5574906 — EC50 = 1.585 nM 8.80
CHEMBL5571445 — EC50 = 1.698 nM 8.77
CHEMBL5571651 — EC50 = 1.698 nM 8.77
CHEMBL434 ISOPROTERENOL EC50 = 1.778 nM 8.75
CHEMBL5570025 — EC50 = 1.82 nM 8.74
CHEMBL5573712 — EC50 = 1.905 nM 8.72
CHEMBL5555612 — EC50 = 1.995 nM 8.70
CHEMBL5575290 — EC50 = 2.138 nM 8.67
CHEMBL5574011 — EC50 = 2.188 nM 8.66
CHEMBL5571660 — EC50 = 2.188 nM 8.66
CHEMBL5566587 — EC50 = 2.239 nM 8.65
CHEMBL5571279 — EC50 = 3.715 nM 8.43
CHEMBL5590155 — EC50 = 3.715 nM 8.43
CHEMBL5570917 — EC50 = 4.074 nM 8.39
CHEMBL5594574 — EC50 = 5.129 nM 8.29
CHEMBL5571865 — EC50 = 5.37 nM 8.27
CHEMBL5532178 — EC50 = 14.45 nM 7.84
CHEMBL5572643 — EC50 = 16.6 nM 7.78
CHEMBL1263 SALMETEROL EC50 = 29.51 nM 7.53
CHEMBL605846 OLODATEROL EC50 = 33.88 nM 7.47
CHEMBL5571981 — EC50 = 109.65 nM 6.96
CHEMBL5593074 — EC50 = 1000.0 nM 6.00