Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
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DOI

11504295 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
11504295.0 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
4814 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
7543 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
CHEMBL605846 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
DB09080 2923 None 40 Human Functional pAC50 = 8.8 8.8 416 8
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1038/s41467-023-40064-9
12582 950 None 27 Human Functional pAC50 = 7.9 7.9 -2 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
2783 950 None 27 Human Functional pAC50 = 7.9 7.9 -2 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
2783.0 950 None 27 Human Functional pAC50 = 7.9 7.9 -2 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
CHEMBL49080 950 None 27 Human Functional pAC50 = 7.9 7.9 -2 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
DB01407 950 None 27 Human Functional pAC50 = 7.9 7.9 -2 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1038/s41467-023-40064-9
1499 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
3779 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
3779.0 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
536 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
CHEMBL434 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
DB01064 2091 None 34 Human Functional pAC50 = 7.7 7.7 -102 38
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
1028 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
139148732 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
479 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
5816.0 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL679 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00668 291 None 40 Human Functional pAC50 = 7.7 7.7 -7 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
105 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
2083 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
2083.0 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
558 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
CHEMBL714 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
DB01001 3461 None 54 Human Functional pAC50 = 6.6 6.6 -13 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1038/s41467-023-40064-9
1155 1629 None 38 Human Functional pAC50 = 7.6 7.6 1 11
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
3343 1629 None 38 Human Functional pAC50 = 7.6 7.6 1 11
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
557 1629 None 38 Human Functional pAC50 = 7.6 7.6 1 11
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL32800 1629 None 38 Human Functional pAC50 = 7.6 7.6 1 11
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
DB01288 1629 None 38 Human Functional pAC50 = 7.6 7.6 1 11
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
2419 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5152 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
5152.0 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
559 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL1263 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
DB00938 3463 None 53 Human Functional pAC50 = 7.5 7.5 8 19
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
643976 14524 None 29 Human Functional pAC50 = 5.5 5.5 2 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 456 7 6 10 -1.6 Cc1cc2nc3c(=O)[nH]c(=O)nc-3n(C[C@H](O)[C@H](O)[C@H](O)COP(=O)(O)O)c2cc1C 10.1038/s41467-023-40064-9
CHEMBL1201794 14524 None 29 Human Functional pAC50 = 5.5 5.5 2 3
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 456 7 6 10 -1.6 Cc1cc2nc3c(=O)[nH]c(=O)nc-3n(C[C@H](O)[C@H](O)[C@H](O)COP(=O)(O)O)c2cc1C 10.1038/s41467-023-40064-9
2146 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
485 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
6041.0 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL1215 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
DB00388 3100 None 45 Human Functional pAC50 = 5.4 5.4 -691 14
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
10184665 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
10184665.0 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
4799 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
7353 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
CHEMBL1198857 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
DB09082 3991 None 42 Human Functional pAC50 = 8.2 8.2 40 10
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
5606 10195 None 41 Human Functional pAC50 = 6.3 6.3 3 2
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1038/s41467-023-40064-9
5606.0 10195 None 41 Human Functional pAC50 = 6.3 6.3 3 2
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1159717 10195 None 41 Human Functional pAC50 = 6.3 6.3 3 2
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1038/s41467-023-40064-9
DB12248 10195 None 41 Human Functional pAC50 = 6.3 6.3 3 2
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 227 3 2 2 2.8 CC(C)(C)NCC(O)c1ccccc1Cl 10.1038/s41467-023-40064-9
4567 9950 None 29 Human Functional pAC50 = 7.1 7.1 -2 12
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL114655 9950 None 29 Human Functional pAC50 = 7.1 7.1 -2 12
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
6083 207273 None 55 Human Functional pAC50 = 5.0 5.0 -19 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL1315633 207273 None 55 Human Functional pAC50 = 5.0 5.0 -19 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL752 207273 None 55 Human Functional pAC50 = 5.0 5.0 -19 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 347 4 5 10 -1.9 Nc1ncnc2c1ncn2[C@@H]1O[C@H](COP(=O)(O)O)[C@@H](O)[C@H]1O 10.1038/s41467-023-40064-9
68555 103167 None 14 Human Functional pAC50 = 5 5.0 -229 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 7 1 5 2.6 CNCCc1ccc(OC(=O)C(C)C)c(OC(=O)C(C)C)c1 10.1038/s41467-023-40064-9
CHEMBL307739 103167 None 14 Human Functional pAC50 = 5 5.0 -229 7
Agonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer methodAgonist activity at human ADRB2 in an in vitro cell-based assay measured by time-resolved fluorescence resonance energy transfer method
ChEMBL 307 7 1 5 2.6 CNCCc1ccc(OC(=O)C(C)C)c(OC(=O)C(C)C)c1 10.1038/s41467-023-40064-9
164617688 188629 None 0 Human Functional pEC50 = 11.0 11.0 416 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4847536 188629 None 0 Human Functional pEC50 = 11.0 11.0 416 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028449 188629 None 0 Human Functional pEC50 = 11.0 11.0 416 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164622954 188673 None 0 Human Functional pEC50 = 10.9 10.9 245 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4871708 188673 None 0 Human Functional pEC50 = 10.9 10.9 245 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028726 188673 None 0 Human Functional pEC50 = 10.9 10.9 245 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164625303 188696 None 0 Human Functional pEC50 = 10.9 10.9 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4873082 188696 None 0 Human Functional pEC50 = 10.9 10.9 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028871 188696 None 0 Human Functional pEC50 = 10.9 10.9 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
164617772 188631 None 0 Human Functional pEC50 = 10.9 10.9 173 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848793 188631 None 0 Human Functional pEC50 = 10.9 10.9 173 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028458 188631 None 0 Human Functional pEC50 = 10.9 10.9 173 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 368 7 5 5 2.6 CC(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164615126 188611 None 0 Human Functional pEC50 = 10.8 10.8 104 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4854569 188611 None 0 Human Functional pEC50 = 10.8 10.8 104 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028293 188611 None 0 Human Functional pEC50 = 10.8 10.8 104 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156010908 178438 None 0 Human Functional pEC50 = 10.8 10.8 2238 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4634131 178438 None 0 Human Functional pEC50 = 10.8 10.8 2238 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651173 178438 None 0 Human Functional pEC50 = 10.8 10.8 2238 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164623230 188678 None 0 Human Functional pEC50 = 10.8 10.8 1479 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4865710 188678 None 0 Human Functional pEC50 = 10.8 10.8 1479 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028744 188678 None 0 Human Functional pEC50 = 10.8 10.8 1479 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164618278 188634 None 0 Human Functional pEC50 = 10.8 10.8 389 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848018 188634 None 0 Human Functional pEC50 = 10.8 10.8 389 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028489 188634 None 0 Human Functional pEC50 = 10.8 10.8 389 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccccc1CCC(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164615492 188616 None 0 Human Functional pEC50 = 10.8 10.8 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848704 188616 None 0 Human Functional pEC50 = 10.8 10.8 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028319 188616 None 0 Human Functional pEC50 = 10.8 10.8 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164623105 188675 None 0 Human Functional pEC50 = 10.8 10.8 47 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4862449 188675 None 0 Human Functional pEC50 = 10.8 10.8 47 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028738 188675 None 0 Human Functional pEC50 = 10.8 10.8 47 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccc(Cl)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164611794 188582 None 0 Human Functional pEC50 = 10.7 10.7 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4854261 188582 None 0 Human Functional pEC50 = 10.7 10.7 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028104 188582 None 0 Human Functional pEC50 = 10.7 10.7 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1cccc(O)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164612025 188584 None 0 Human Functional pEC50 = 10.7 10.7 2454 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4860454 188584 None 0 Human Functional pEC50 = 10.7 10.7 2454 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028117 188584 None 0 Human Functional pEC50 = 10.7 10.7 2454 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164618895 188642 None 0 Human Functional pEC50 = 10.7 10.7 95 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868938 188642 None 0 Human Functional pEC50 = 10.7 10.7 95 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028525 188642 None 0 Human Functional pEC50 = 10.7 10.7 95 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164610792 188575 None 0 Human Functional pEC50 = 10.7 10.7 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4855974 188575 None 0 Human Functional pEC50 = 10.7 10.7 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028040 188575 None 0 Human Functional pEC50 = 10.7 10.7 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 380 7 4 4 3.6 Cc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
11504295 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
11504295.0 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
4814 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
7543 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
CHEMBL605846 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
DB09080 2923 None 40 Human Functional pEC50 = 10.7 10.7 416 8
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1021/acs.jmedchem.0c01195
9957764 88741 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 503 11 6 6 3.6 COc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL236039 88741 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 503 11 6 6 3.6 COc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
11259765 86044 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 462 11 5 5 3.4 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
CHEMBL230486 86044 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 462 11 5 5 3.4 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
11621158 16709 None 1 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(O)cc2Cl)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1242943 16709 None 1 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(O)cc2Cl)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155517986 170310 None 0 Human Functional pEC50 = 10.7 10.7 478630 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4445289 170310 None 0 Human Functional pEC50 = 10.7 10.7 478630 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155517986 170310 None 0 Human Functional pEC50 = 10.7 10.7 478630 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4445289 170310 None 0 Human Functional pEC50 = 10.7 10.7 478630 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164621302 188658 None 0 Human Functional pEC50 = 10.7 10.7 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4863282 188658 None 0 Human Functional pEC50 = 10.7 10.7 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028641 188658 None 0 Human Functional pEC50 = 10.7 10.7 120 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1cccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
164623918 188685 None 0 Human Functional pEC50 = 10.7 10.7 199 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4872480 188685 None 0 Human Functional pEC50 = 10.7 10.7 199 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028793 188685 None 0 Human Functional pEC50 = 10.7 10.7 199 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 374 7 4 4 2.8 O=c1ccc2c(C(O)CNCCCc3cc(F)cc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
44434130 88744 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 5 5 3.9 C[C@H](Cc1ccc2[nH]c(C(=O)N(C)Cc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236041 88744 None 0 Human Functional pEC50 = 10.7 10.7 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 5 5 3.9 C[C@H](Cc1ccc2[nH]c(C(=O)N(C)Cc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
164615222 188613 None 0 Human Functional pEC50 = 10.7 10.7 91 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4857267 188613 None 0 Human Functional pEC50 = 10.7 10.7 91 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028301 188613 None 0 Human Functional pEC50 = 10.7 10.7 91 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccccc1CCC(C)(C)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164622827 188671 None 0 Human Functional pEC50 = 10.7 10.7 26 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868585 188671 None 0 Human Functional pEC50 = 10.7 10.7 26 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028721 188671 None 0 Human Functional pEC50 = 10.7 10.7 26 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 400 7 4 4 3.9 CC(C)(CCc1cccc(Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
11455274 16731 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 12 5 6 3.3 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243189 16731 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 12 5 6 3.3 CC(C)(Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
164624634 188692 None 0 Human Functional pEC50 = 10.6 10.6 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868684 188692 None 0 Human Functional pEC50 = 10.6 10.6 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028836 188692 None 0 Human Functional pEC50 = 10.6 10.6 131 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1cccc(F)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014115 178395 None 0 Human Functional pEC50 = 10.6 10.6 58 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4635163 178395 None 0 Human Functional pEC50 = 10.6 10.6 58 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650951 178395 None 0 Human Functional pEC50 = 10.6 10.6 58 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
11214499 86046 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
CHEMBL230490 86046 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
164608750 188565 None 0 Human Functional pEC50 = 10.6 10.6 181 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4846631 188565 None 0 Human Functional pEC50 = 10.6 10.6 181 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5027923 188565 None 0 Human Functional pEC50 = 10.6 10.6 181 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3cccc(F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
156015148 178390 None 0 Human Functional pEC50 = 10.6 10.6 208 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4646881 178390 None 0 Human Functional pEC50 = 10.6 10.6 208 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650929 178390 None 0 Human Functional pEC50 = 10.6 10.6 208 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164620479 188651 None 0 Human Functional pEC50 = 10.6 10.6 288 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4863847 188651 None 0 Human Functional pEC50 = 10.6 10.6 288 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028596 188651 None 0 Human Functional pEC50 = 10.6 10.6 288 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1cccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
11249243 16728 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 511 12 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243158 16728 None 0 Human Functional pEC50 = 10.6 10.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 511 12 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
156015482 178357 None 0 Human Functional pEC50 = 10.6 10.6 204 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4641262 178357 None 0 Human Functional pEC50 = 10.6 10.6 204 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650664 178357 None 0 Human Functional pEC50 = 10.6 10.6 204 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
164619360 188645 None 0 Human Functional pEC50 = 10.6 10.6 371 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4868763 188645 None 0 Human Functional pEC50 = 10.6 10.6 371 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028547 188645 None 0 Human Functional pEC50 = 10.6 10.6 371 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 370 7 4 4 3.0 CC(CCc1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164623544 188681 None 0 Human Functional pEC50 = 10.6 10.6 2754 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4872653 188681 None 0 Human Functional pEC50 = 10.6 10.6 2754 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028764 188681 None 0 Human Functional pEC50 = 10.6 10.6 2754 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 406 7 4 4 3.5 O=c1ccc2c(C(O)CNCCCc3cccc(C(F)(F)F)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
164612078 188585 None 0 Human Functional pEC50 = 10.5 10.5 64 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4848617 188585 None 0 Human Functional pEC50 = 10.5 10.5 64 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028119 188585 None 0 Human Functional pEC50 = 10.5 10.5 64 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 8 4 5 2.9 COc1ccccc1CC[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014817 178409 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4642770 178409 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650993 178409 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164617235 188626 None 0 Human Functional pEC50 = 10.5 10.5 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4848775 188626 None 0 Human Functional pEC50 = 10.5 10.5 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028422 188626 None 0 Human Functional pEC50 = 10.5 10.5 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 396 8 4 5 3.3 COc1ccc(CCC(C)(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
156013777 178453 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4636255 178453 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651241 178453 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1cccc(O)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
10390417 167868 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 480 10 6 7 3.0 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3nccs3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL430361 167868 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 480 10 6 7 3.0 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3nccs3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
49864395 15644 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
CHEMBL1221680 15644 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulationAgonist activity at beta 2 in human A431 cells adrenoceptor assessed as cAMP accumulation
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@@H]3CCC[C@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2010.06.136
11477877 16754 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 517 12 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCC2CCCCC2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243348 16754 None 0 Human Functional pEC50 = 10.5 10.5 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 517 12 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCC2CCCCC2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
13121366 177560 None 0 Human Functional pEC50 = 10.5 10.5 457 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4638864 177560 None 0 Human Functional pEC50 = 10.5 10.5 457 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
164612262 188586 None 0 Human Functional pEC50 = 10.5 10.5 190 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4853372 188586 None 0 Human Functional pEC50 = 10.5 10.5 190 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028127 188586 None 0 Human Functional pEC50 = 10.5 10.5 190 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccc(Cl)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
164614743 188606 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4860764 188606 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028269 188606 None 0 Human Functional pEC50 = 10.5 10.5 134 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1ccccc1Cl)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
156014962 178355 None 0 Human Functional pEC50 = 10.5 10.5 229 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4645203 178355 None 0 Human Functional pEC50 = 10.5 10.5 229 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650644 178355 None 0 Human Functional pEC50 = 10.5 10.5 229 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NC[C@H](O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
155536314 172278 None 0 Human Functional pEC50 = 10.4 10.4 6025 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4473515 172278 None 0 Human Functional pEC50 = 10.4 10.4 6025 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
155536314 172278 None 0 Human Functional pEC50 = 10.4 10.4 6025 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4473515 172278 None 0 Human Functional pEC50 = 10.4 10.4 6025 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
164620585 188652 None 0 Human Functional pEC50 = 10.4 10.4 616 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4866766 188652 None 0 Human Functional pEC50 = 10.4 10.4 616 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028602 188652 None 0 Human Functional pEC50 = 10.4 10.4 616 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 382 7 5 5 3.0 CC(C)(CCc1ccc(O)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
44434126 88743 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 519 11 6 6 4.3 CSc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL236040 88743 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 519 11 6 6 4.3 CSc1ccccc1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
10027868 144980 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 474 10 6 6 2.9 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccn3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391006 144980 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 474 10 6 6 2.9 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccn3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
164618813 188641 None 0 Human Functional pEC50 = 10.4 10.4 275 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4865833 188641 None 0 Human Functional pEC50 = 10.4 10.4 275 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028523 188641 None 0 Human Functional pEC50 = 10.4 10.4 275 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 366 7 4 4 3.2 Cc1ccc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
164623433 188679 None 0 Human Functional pEC50 = 10.4 10.4 380 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL4870623 188679 None 0 Human Functional pEC50 = 10.4 10.4 380 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
CHEMBL5028756 188679 None 0 Human Functional pEC50 = 10.4 10.4 380 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2021.113697
156014983 178435 None 0 Human Functional pEC50 = 10.4 10.4 724 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4644638 178435 None 0 Human Functional pEC50 = 10.4 10.4 724 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651152 178435 None 0 Human Functional pEC50 = 10.4 10.4 724 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 386 7 5 6 2.5 CC(C)(CCc1ccc(O)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
11261001 16732 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 13 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243190 16732 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 525 13 5 6 2.9 C[C@H](Cc1cccc(CC(=O)NCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
11489605 16739 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 541 13 5 7 2.9 COc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243256 16739 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 541 13 5 7 2.9 COc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
155533625 171980 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4469364 171980 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155564766 175593 None 0 Human Functional pEC50 = 10.4 10.4 181 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4577508 175593 None 0 Human Functional pEC50 = 10.4 10.4 181 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
11489574 16736 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 14 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243222 16736 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 14 5 6 3.3 C[C@H](Cc1cccc(CC(=O)NCCCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155536813 172309 None 0 Human Functional pEC50 = 10.4 10.4 263 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4473790 172309 None 0 Human Functional pEC50 = 10.4 10.4 263 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164624092 188688 None 0 Human Functional pEC50 = 10.4 10.4 794 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL4865514 188688 None 0 Human Functional pEC50 = 10.4 10.4 794 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL5028807 188688 None 0 Human Functional pEC50 = 10.4 10.4 794 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 442 10 4 7 2.9 COc1cc(CCC(C)NCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
2419 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
5152 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
5152.0 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
559 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
CHEMBL1263 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
DB00938 3463 None 53 Human Functional pEC50 = 10.4 10.4 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2019.115178
11699773 16723 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 569 12 6 7 3.6 Cc1cc(O)cc(C)c1CNC(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243101 16723 None 0 Human Functional pEC50 = 10.4 10.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 569 12 6 7 3.6 Cc1cc(O)cc(C)c1CNC(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
164626310 188702 None 0 Human Functional pEC50 = 10.3 10.3 346 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL4874945 188702 None 0 Human Functional pEC50 = 10.3 10.3 346 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
CHEMBL5028930 188702 None 0 Human Functional pEC50 = 10.3 10.3 346 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 356 7 4 4 2.6 O=c1ccc2c(C(O)CNCCCc3ccc(F)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2021.113697
11398811 16742 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 555 14 5 7 3.3 CCOc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1243285 16742 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 555 14 5 7 3.3 CCOc1ccccc1CNC(=O)Cc1cccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
155543358 174877 None 0 Human Functional pEC50 = 10.3 10.3 102 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4561253 174877 None 0 Human Functional pEC50 = 10.3 10.3 102 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
156015401 178376 None 0 Human Functional pEC50 = 10.3 10.3 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4645694 178376 None 0 Human Functional pEC50 = 10.3 10.3 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650809 178376 None 0 Human Functional pEC50 = 10.3 10.3 251 2
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
156015798 178383 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4649233 178383 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650858 178383 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
44434125 146199 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 473 10 6 5 3.6 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391946 146199 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 473 10 6 5 3.6 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
44237865 58248 None 0 Guinea pig Functional pEC50 = 10.3 10.3 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 500 11 6 5 3.9 O=C(NCCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682213 58248 None 0 Guinea pig Functional pEC50 = 10.3 10.3 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 500 11 6 5 3.9 O=C(NCCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
155557083 174645 None 0 Human Functional pEC50 = 10.3 10.3 724 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4556022 174645 None 0 Human Functional pEC50 = 10.3 10.3 724 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
10389119 88788 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 451 10 6 5 3.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCC3CCC3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236251 88788 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 451 10 6 5 3.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCC3CCC3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
155564340 175528 None 0 Human Functional pEC50 = 10.3 10.3 263 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
CHEMBL4576089 175528 None 0 Human Functional pEC50 = 10.3 10.3 263 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
44434127 88641 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 509 10 6 5 3.8 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(F)cccc3F)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL235612 88641 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 509 10 6 5 3.8 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(F)cccc3F)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
3466 4142 None 34 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
37990 4142 None 34 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
CHEMBL1243407 4142 None 34 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 378 8 4 5 2.4 OC(c1ccc(c(c1)NS(=O)(=O)C)O)CNC(Cc1ccccc1)(C)C 10.1021/jm1005989
1499 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
3779 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
3779.0 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
536 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
CHEMBL434 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
DB01064 2091 None 34 Human Functional pEC50 = 10.3 10.3 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
11376125 16747 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 12 5 6 3.5 Cc1ccc(CNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)cc1C 10.1021/jm1005989
CHEMBL1243317 16747 None 0 Human Functional pEC50 = 10.3 10.3 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 539 12 5 6 3.5 Cc1ccc(CNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)cc1C 10.1021/jm1005989
164614249 188601 None 0 Human Functional pEC50 = 10.2 10.2 295 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4859591 188601 None 0 Human Functional pEC50 = 10.2 10.2 295 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028241 188601 None 0 Human Functional pEC50 = 10.2 10.2 295 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
10324803 89629 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 533 12 6 7 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
CHEMBL237501 89629 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 533 12 6 7 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2[nH]1 10.1016/j.bmcl.2007.09.031
10390752 146344 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 6 5 4.1 C[C@H](Cc1ccc2[nH]c(C(=O)N[C@H](C)c3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL392056 146344 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 487 10 6 5 4.1 C[C@H](Cc1ccc2[nH]c(C(=O)N[C@H](C)c3ccccc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
16049087 64104 None 0 Human Functional pEC50 = 10.2 10.2 125 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807817 64104 None 0 Human Functional pEC50 = 10.2 10.2 125 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
9892481 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
90645347 112576 None 0 Human Functional pEC50 = 10.2 10.2 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 112576 None 0 Human Functional pEC50 = 10.2 10.2 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
9892481 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL1940832 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
9892481 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940832 70257 None 12 Human Functional pEC50 = 10.2 10.2 -3 4
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
11420492 155290 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 492 10 5 5 3.8 C[C@H](Cc1cccc(CC(=O)NC23CC4CC(CC(C4)C2)C3)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
CHEMBL402501 155290 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 492 10 5 5 3.8 C[C@H](Cc1cccc(CC(=O)NC23CC4CC(CC(C4)C2)C3)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm1005989
155564079 175515 None 0 Human Functional pEC50 = 10.2 10.2 97 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4575759 175515 None 0 Human Functional pEC50 = 10.2 10.2 97 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
11456127 16753 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 593 12 5 6 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243347 16753 None 0 Human Functional pEC50 = 10.2 10.2 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 593 12 5 6 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
44237667 58245 None 0 Guinea pig Functional pEC50 = 10.2 10.2 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 458 8 6 5 3.7 O=C(Nc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682210 58245 None 0 Guinea pig Functional pEC50 = 10.2 10.2 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 458 8 6 5 3.7 O=C(Nc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
2419 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
5152 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
5152.0 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
559 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
CHEMBL1263 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
DB00938 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.09.031
2419 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
5152 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
5152.0 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
559 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
CHEMBL1263 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
DB00938 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2007.04.081
2419 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
5152 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
5152.0 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
559 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
CHEMBL1263 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
DB00938 3463 None 53 Human Functional pEC50 = 10.2 10.2 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm1005989
45269924 197904 None 0 Guinea pig Functional pEC50 = 10.1 10.1 - 1
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
CHEMBL552398 197904 None 0 Guinea pig Functional pEC50 = 10.1 10.1 - 1
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
164615474 188615 None 0 Human Functional pEC50 = 10.1 10.1 61 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL4847767 188615 None 0 Human Functional pEC50 = 10.1 10.1 61 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
CHEMBL5028315 188615 None 0 Human Functional pEC50 = 10.1 10.1 61 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 4 3.5 CC(CCc1cccc(Cl)c1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.ejmech.2021.113697
155548071 173853 None 0 Human Functional pEC50 = 10.1 10.1 131 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(O)CNCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4536813 173853 None 0 Human Functional pEC50 = 10.1 10.1 131 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(O)CNCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
155567283 176074 None 0 Human Functional pEC50 = 10.1 10.1 588 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
CHEMBL4588479 176074 None 0 Human Functional pEC50 = 10.1 10.1 588 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
155548668 173887 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4537644 173887 None 0 Human Functional pEC50 = 10.1 10.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
2419 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
5152 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
5152.0 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
559 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
CHEMBL1263 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
DB00938 3463 None 53 Human Functional pEC50 = 10.1 10.1 8 19
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
16049088 64105 None 0 Human Functional pEC50 = 10.1 10.1 100 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807818 64105 None 0 Human Functional pEC50 = 10.1 10.1 100 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 448 13 4 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
16049028 64106 None 0 Human Functional pEC50 = 10.1 10.1 50 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 462 14 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807819 64106 None 0 Human Functional pEC50 = 10.1 10.1 50 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 462 14 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
11592062 112520 None 0 Human Functional pEC50 = 10.1 10.1 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 112520 None 0 Human Functional pEC50 = 10.1 10.1 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
11169365 112575 None 0 Human Functional pEC50 = 10.1 10.1 22 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 112575 None 0 Human Functional pEC50 = 10.1 10.1 22 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
155513474 169843 None 0 Human Functional pEC50 = 10.1 10.1 83 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4438531 169843 None 0 Human Functional pEC50 = 10.1 10.1 83 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 478 8 4 4 5.1 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
164622775 188670 None 0 Human Functional pEC50 = 10.1 10.1 120226 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL4867311 188670 None 0 Human Functional pEC50 = 10.1 10.1 120226 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
CHEMBL5028718 188670 None 0 Human Functional pEC50 = 10.1 10.1 120226 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 428 10 4 7 2.5 COc1cc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc(OC)c1OC 10.1016/j.ejmech.2021.113697
11504295 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
11504295.0 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
4814 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
7543 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
CHEMBL605846 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
DB09080 2923 None 40 Human Functional pEC50 = 10.1 10.1 416 8
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(cc1)CC(NC[C@@H](c1cc(O)cc2c1OCC(=O)N2)O)(C)C 10.1016/j.ejmech.2021.113697
44237615 58247 None 0 Guinea pig Functional pEC50 = 10.1 10.1 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 486 10 6 5 3.5 O=C(NCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682212 58247 None 0 Guinea pig Functional pEC50 = 10.1 10.1 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 486 10 6 5 3.5 O=C(NCCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
11707090 16719 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)c(O)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243068 16719 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)c(O)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
164623583 188683 None 0 Human Functional pEC50 = 10.0 10.0 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL4873280 188683 None 0 Human Functional pEC50 = 10.0 10.0 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
CHEMBL5028767 188683 None 0 Human Functional pEC50 = 10.0 10.0 316 2
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 352 7 4 4 2.8 Cc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2021.113697
11247541 85998 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 434 11 5 5 2.6 O=C(Cc1cccc(CCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NCc1ccccc1 10.1016/j.bmcl.2007.04.081
CHEMBL230203 85998 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 434 11 5 5 2.6 O=C(Cc1cccc(CCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NCc1ccccc1 10.1016/j.bmcl.2007.04.081
44425580 86045 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 448 11 5 5 3.0 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
CHEMBL230487 86045 None 0 Human Functional pEC50 = 10.0 10.0 - 1
Agonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMPAgonist activity at human recombinant beta-2 adrenoceptor expressed in CHO cells assessed as elevation of cAMP
ChEMBL 448 11 5 5 3.0 C[C@H](Cc1cccc(CC(=O)NCc2ccccc2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.04.081
57334265 70882 None 0 Guinea pig Functional pEC50 = 10 10.0 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951067 70882 None 0 Guinea pig Functional pEC50 = 10 10.0 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
12065 628 None 28 Human Functional pEC50 = 10 10.0 6 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
45483813 628 None 28 Human Functional pEC50 = 10 10.0 6 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
CHEMBL579394 628 None 28 Human Functional pEC50 = 10 10.0 6 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
13345218 199677 None 0 Human Functional pEC50 = 10 10.0 8 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568272 199677 None 0 Human Functional pEC50 = 10 10.0 8 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
16049024 64107 None 0 Human Functional pEC50 = 10 10.0 79 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 498 13 4 7 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807820 64107 None 0 Human Functional pEC50 = 10 10.0 79 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 498 13 4 7 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
118737358 119129 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
CHEMBL3426706 119129 None 0 Human Functional pEC50 = 10 10.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 13 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1021/jm501915g
10239722 112521 None 0 Human Functional pEC50 = 10 10.0 11 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 112521 None 0 Human Functional pEC50 = 10 10.0 11 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
66796015 112523 None 0 Human Functional pEC50 = 10 10.0 35 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 112523 None 0 Human Functional pEC50 = 10 10.0 35 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
10180590 70255 None 0 Human Functional pEC50 = 10 10.0 707 2
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940830 70255 None 0 Human Functional pEC50 = 10 10.0 707 2
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
105 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
2083 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
2083.0 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
558 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
CHEMBL714 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
DB01001 3461 None 54 Human Functional pEC50 = 10.0 10.0 -13 3
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.1c02006
10392857 88693 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 552 11 7 7 2.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(S(N)(=O)=O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL235818 88693 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 552 11 7 7 2.2 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(S(N)(=O)=O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
3083544 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
3083544.0 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
CHEMBL1200811 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
CHEMBL1363 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
CHEMBL1951071 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
CHEMBL605993 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
DB00983 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
DB01274 26817 None 34 Guinea pig Functional pEC50 = 9.9 9.9 2 6
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2012.01.013
16049026 64108 None 0 Human Functional pEC50 = 9.9 9.9 25 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 432 13 4 7 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807821 64108 None 0 Human Functional pEC50 = 9.9 9.9 25 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 432 13 4 7 2.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
16049029 64109 None 0 Human Functional pEC50 = 9.9 9.9 25 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 482 13 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807822 64109 None 0 Human Functional pEC50 = 9.9 9.9 25 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 482 13 4 7 3.7 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCOCCc3cccc4ccccc34)c2s1 10.1016/j.bmcl.2011.05.097
10461973 119120 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426697 119120 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 655 15 6 8 4.9 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)NCCCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
9871386 112334 None 3 Human Functional pEC50 = 9.9 9.9 8 4
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 112334 None 3 Human Functional pEC50 = 9.9 9.9 8 4
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
90645344 112519 None 0 Human Functional pEC50 = 9.9 9.9 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 112519 None 0 Human Functional pEC50 = 9.9 9.9 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
56943545 112525 None 0 Human Functional pEC50 = 9.9 9.9 28 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 112525 None 0 Human Functional pEC50 = 9.9 9.9 28 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
11180293 112571 None 0 Human Functional pEC50 = 9.9 9.9 22 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 112571 None 0 Human Functional pEC50 = 9.9 9.9 22 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
46832232 14220 None 0 Human Functional pEC50 = 9.9 9.9 39 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1085837 14220 None 0 Human Functional pEC50 = 9.9 9.9 39 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1198923 14220 None 0 Human Functional pEC50 = 9.9 9.9 39 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
10217757 112333 None 0 Human Functional pEC50 = 9.9 9.9 10 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 112333 None 0 Human Functional pEC50 = 9.9 9.9 10 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
9871386 112334 None 3 Human Functional pEC50 = 9.9 9.9 8 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 112334 None 3 Human Functional pEC50 = 9.9 9.9 8 4
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
57398384 70258 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
CHEMBL1940833 70258 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
156015656 178448 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4639822 178448 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651230 178448 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 378 7 4 5 2.3 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cc(F)cc(F)c2)N1 10.1016/j.bmc.2019.115178
53323515 58249 None 0 Guinea pig Functional pEC50 = 9.9 9.9 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 515 10 7 6 2.5 NC(=O)c1cccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682214 58249 None 0 Guinea pig Functional pEC50 = 9.9 9.9 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 515 10 7 6 2.5 NC(=O)c1cccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 10.1016/j.bmcl.2010.12.096
46938907 16716 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)cc(Cl)c2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243035 16716 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 609 12 6 7 4.3 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)cc(Cl)c2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
155524038 170994 None 0 Human Functional pEC50 = 9.9 9.9 120 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4454489 170994 None 0 Human Functional pEC50 = 9.9 9.9 120 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
2419 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
5152 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
5152.0 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
559 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
DB00938 3463 None 53 Human Functional pEC50 = 9.9 9.9 8 19
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.ejmech.2021.113697
156020412 178454 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4648525 178454 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651243 178454 None 0 Human Functional pEC50 = 9.9 9.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
155550964 174054 None 0 Human Functional pEC50 = 9.8 9.8 575 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(O)CNCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4541263 174054 None 0 Human Functional pEC50 = 9.8 9.8 575 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(O)CNCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
1499 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
3779 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
3779.0 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
536 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
DB01064 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
1499 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
3779 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
3779.0 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
536 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
DB01064 2091 None 34 Human Functional pEC50 = 9.8 9.8 -102 38
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
10394806 119121 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL3426698 119121 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 681 12 6 8 5.3 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)N[C@H]1CC[C@H](CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737354 119124 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426701 119124 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 703 12 6 8 5.8 Cc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
56943518 112524 None 0 Human Functional pEC50 = 9.8 9.8 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 112524 None 0 Human Functional pEC50 = 9.8 9.8 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 112541 None 0 Human Functional pEC50 = 9.8 9.8 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 112541 None 0 Human Functional pEC50 = 9.8 9.8 25 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901144 70353 None 0 Human Functional pEC50 = 9.8 9.8 -1 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944691 70353 None 0 Human Functional pEC50 = 9.8 9.8 -1 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
10288976 66601 None 0 Human Functional pEC50 = 9.8 9.8 10 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835862 66601 None 0 Human Functional pEC50 = 9.8 9.8 10 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852543 66601 None 0 Human Functional pEC50 = 9.8 9.8 10 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
9849126 12443 None 0 Human Functional pEC50 = 9.8 9.8 -3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL1185969 12443 None 0 Human Functional pEC50 = 9.8 9.8 -3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL443435 12443 None 0 Human Functional pEC50 = 9.8 9.8 -3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
9891927 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL446840 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483200 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483201 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
9891927 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL446840 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483200 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL483201 184303 None 9 Human Functional pEC50 = 9.8 9.8 5 4
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
155551133 174100 None 0 Human Functional pEC50 = 9.8 9.8 446 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 7 4 5 1.9 O=c1ccc2c(C(O)CNCCOc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4542430 174100 None 0 Human Functional pEC50 = 9.8 9.8 446 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 7 4 5 1.9 O=c1ccc2c(C(O)CNCCOc3ccccc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
44434128 149227 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 489 10 7 6 3.3 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL394339 149227 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 489 10 7 6 3.3 C[C@H](Cc1ccc2[nH]c(C(=O)NCc3ccc(O)cc3)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
11534330 16713 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)ccc2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1243000 16713 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 575 12 6 7 3.6 CC(C)(Cc1cccc(CC(=O)NCc2cc(Cl)ccc2O)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
156020206 178447 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4648663 178447 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651226 178447 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(O)c2)N1 10.1016/j.bmc.2019.115178
156015463 178456 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4640925 178456 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651254 178456 None 0 Human Functional pEC50 = 9.8 9.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
1239 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3410 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3410.0 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
3465 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
DB00983 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.01.043
56658246 64518 None 0 Guinea pig Functional pEC50 = 9.7 9.7 3 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814277 64518 None 0 Guinea pig Functional pEC50 = 9.7 9.7 3 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814278 64518 None 0 Guinea pig Functional pEC50 = 9.7 9.7 3 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
24901413 70380 None 0 Guinea pig Functional pEC50 = 9.7 9.7 3 4
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945032 70380 None 0 Guinea pig Functional pEC50 = 9.7 9.7 3 4
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
15981386 63571 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 459 12 4 7 2.0 CN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800472 63571 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 459 12 4 7 2.0 CN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
56663238 64123 None 0 Human Functional pEC50 = 9.7 9.7 251 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807872 64123 None 0 Human Functional pEC50 = 9.7 9.7 251 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
11857427 119116 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426693 119116 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
118737350 119117 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426694 119117 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 6 8 6.1 Cc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
1239 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410.0 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
16738927 70382 None 0 Human Functional pEC50 = 9.7 9.7 31 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945034 70382 None 0 Human Functional pEC50 = 9.7 9.7 31 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
42625823 12683 None 0 Human Functional pEC50 = 9.7 9.7 251 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187371 12683 None 0 Human Functional pEC50 = 9.7 9.7 251 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL500782 12683 None 0 Human Functional pEC50 = 9.7 9.7 251 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
1239 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410.0 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1677 None 37 Human Functional pEC50 = 9.7 9.7 -2 6
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
44237612 58246 None 0 Guinea pig Functional pEC50 = 9.7 9.7 4466 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 472 9 6 5 3.4 O=C(NCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682211 58246 None 0 Guinea pig Functional pEC50 = 9.7 9.7 4466 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 472 9 6 5 3.4 O=C(NCc1ccccc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237613 58250 None 0 Guinea pig Functional pEC50 = 9.7 9.7 2754 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 502 10 6 6 3.4 COc1ccccc1CNC(=O)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682215 58250 None 0 Guinea pig Functional pEC50 = 9.7 9.7 2754 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 502 10 6 6 3.4 COc1ccccc1CNC(=O)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237614 58251 None 0 Guinea pig Functional pEC50 = 9.7 9.7 31622 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 490 9 6 5 3.6 O=C(NCc1ccc(F)cc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682216 58251 None 0 Guinea pig Functional pEC50 = 9.7 9.7 31622 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 490 9 6 5 3.6 O=C(NCc1ccc(F)cc1)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237669 58252 None 0 Guinea pig Functional pEC50 = 9.7 9.7 7943 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682217 58252 None 0 Guinea pig Functional pEC50 = 9.7 9.7 7943 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
44237666 58253 None 0 Guinea pig Functional pEC50 = 9.7 9.7 44668 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 548 10 6 5 5.0 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682218 58253 None 0 Guinea pig Functional pEC50 = 9.7 9.7 44668 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 548 10 6 5 5.0 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)NC(c1ccccc1)c1ccccc1 10.1016/j.bmcl.2010.12.096
45483810 199600 None 0 Human Functional pEC50 = 9.7 9.7 3 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL567863 199600 None 0 Human Functional pEC50 = 9.7 9.7 3 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
1499 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
3779 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
3779.0 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
536 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
DB01064 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2013.11.030
11577915 16615 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 591 12 6 7 4.1 CC(C)(Cc1cccc(CC(=O)NCc2ccc3cc(O)ccc3c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240965 16615 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 591 12 6 7 4.1 CC(C)(Cc1cccc(CC(=O)NCc2ccc3cc(O)ccc3c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
1499 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
3779 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
3779.0 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
536 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
DB01064 2091 None 34 Human Functional pEC50 = 9.7 9.7 -102 38
Agonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulationAgonist activity at human beta2 adrenoreceptor overexpressed in HEK293 cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2021.113697
156014685 178451 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
CHEMBL4636111 178451 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
CHEMBL4651237 178451 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2O)N1 10.1016/j.bmc.2019.115178
155536173 172265 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4473349 172265 None 0 Human Functional pEC50 = 9.7 9.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 442 8 4 4 4.9 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
155527926 171356 None 0 Human Functional pEC50 = 9.7 9.7 8709 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4460095 171356 None 0 Human Functional pEC50 = 9.7 9.7 8709 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
11714238 16616 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(-c3ccc(O)cc3)cc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240966 16616 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2ccc(-c3ccc(O)cc3)cc2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
1155 1629 None 38 Human Functional pEC50 = 9.6 9.6 1 11
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.ejmech.2022.114961
3343 1629 None 38 Human Functional pEC50 = 9.6 9.6 1 11
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.ejmech.2022.114961
557 1629 None 38 Human Functional pEC50 = 9.6 9.6 1 11
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.ejmech.2022.114961
CHEMBL32800 1629 None 38 Human Functional pEC50 = 9.6 9.6 1 11
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.ejmech.2022.114961
DB01288 1629 None 38 Human Functional pEC50 = 9.6 9.6 1 11
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1016/j.ejmech.2022.114961
11647002 15645 None 0 Human Functional pEC50 = 9.6 9.6 8 2
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
CHEMBL1221681 15645 None 0 Human Functional pEC50 = 9.6 9.6 8 2
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 400 7 4 6 3.1 O=c1[nH]c2c(O)ccc([C@@H](O)CN[C@H]3CCC[C@@H]3OCc3ccccc3)c2s1 10.1016/j.bmcl.2014.06.014
164612026 185475 None 0 Human Functional pEC50 = 9.6 9.6 776 2
Agonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 237 4 3 4 1.3 CC(C)NC(CO)c1cc(F)c(N)c(C#N)c1 10.1021/acs.jmedchem.0c01195
CHEMBL4860455 185475 None 0 Human Functional pEC50 = 9.6 9.6 776 2
Agonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assayAgonist activity at human beta2 adrenoceptor expressed in HEK293 cells assessed as increase in cAMP accumulation measured after 60 mins by HTRF assay
ChEMBL 237 4 3 4 1.3 CC(C)NC(CO)c1cc(F)c(N)c(C#N)c1 10.1021/acs.jmedchem.0c01195
56672271 66562 None 0 Guinea pig Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835859 66562 None 0 Guinea pig Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852407 66562 None 0 Guinea pig Functional pEC50 = 9.6 9.6 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
24901144 70353 None 0 Guinea pig Functional pEC50 = 9.6 9.6 1 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944691 70353 None 0 Guinea pig Functional pEC50 = 9.6 9.6 1 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
57393349 70557 None 0 Guinea pig Functional pEC50 = 9.6 9.6 3 2
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1947151 70557 None 0 Guinea pig Functional pEC50 = 9.6 9.6 3 2
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 523 11 4 5 6.2 C[C@@H](NCc1ccccc1-c1ccc(CCNCCc2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
2419 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
5152 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
5152.0 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
559 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
DB00938 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.05.064
56672116 66386 None 0 Human Functional pEC50 = 9.6 9.6 316 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814276 66386 None 0 Human Functional pEC50 = 9.6 9.6 316 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851624 66386 None 0 Human Functional pEC50 = 9.6 9.6 316 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
10372836 102452 None 36 Human Functional pEC50 = 9.6 9.6 -1 3
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3039518 102452 None 36 Human Functional pEC50 = 9.6 9.6 -1 3
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
10372344 119110 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426687 119110 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.8 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
10327462 119111 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
CHEMBL3426688 119111 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1Cl 10.1021/jm501915g
118737348 119114 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426691 119114 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737351 119118 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
CHEMBL3426695 119118 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1C 10.1021/jm501915g
118737355 119125 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
CHEMBL3426702 119125 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 689 12 5 8 5.5 CN(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)C(=O)c1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm501915g
56943515 112507 None 0 Human Functional pEC50 = 9.6 9.6 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298213 112507 None 0 Human Functional pEC50 = 9.6 9.6 7 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 478 13 6 7 3.7 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1 10.1016/j.bmcl.2014.04.095
10173878 112522 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298327 112522 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901210 70352 None 0 Human Functional pEC50 = 9.6 9.6 125 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944690 70352 None 0 Human Functional pEC50 = 9.6 9.6 125 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 11 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901347 70357 None 0 Human Functional pEC50 = 9.6 9.6 17 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944695 70357 None 0 Human Functional pEC50 = 9.6 9.6 17 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 463 11 5 6 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901413 70380 None 0 Human Functional pEC50 = 9.6 9.6 -3 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945032 70380 None 0 Human Functional pEC50 = 9.6 9.6 -3 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)cc3)c[nH]c12 10.1016/j.bmcl.2011.10.049
2419 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
5152 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
5152.0 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
559 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
DB00938 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm401532g
156016062 178430 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4643148 178430 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4651124 178430 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 8 4 5 2.4 O=C1COc2c(cc(O)cc2C(O)CNCCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
2419 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
5152 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
5152.0 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
559 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
DB00938 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2011.08.043
56672271 66562 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835859 66562 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852407 66562 None 0 Human Functional pEC50 = 9.6 9.6 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 19 7 7 2.7 NC(=O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
2419 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
5152 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
5152.0 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
559 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
DB00938 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm801016j
2419 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
5152 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
5152.0 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
559 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
DB00938 3463 None 53 Human Functional pEC50 = 9.6 9.6 8 19
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100326d
46832509 14217 None 0 Human Functional pEC50 = 9.6 9.6 50 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085399 14217 None 0 Human Functional pEC50 = 9.6 9.6 50 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198908 14217 None 0 Human Functional pEC50 = 9.6 9.6 50 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
10006800 88745 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 517 12 6 6 3.6 COc1cccc(CCNC(=O)c2cc3cc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(CO)c4)ccc3[nH]2)c1 10.1016/j.bmcl.2007.09.031
CHEMBL236042 88745 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 517 12 6 6 3.6 COc1cccc(CCNC(=O)c2cc3cc(C[C@@H](C)NC[C@H](O)c4ccc(O)c(CO)c4)ccc3[nH]2)c1 10.1016/j.bmcl.2007.09.031
10256921 145383 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 13 6 7 4.0 CC[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(OC)cccc3OC)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
CHEMBL391308 145383 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 13 6 7 4.0 CC[C@H](Cc1ccc2[nH]c(C(=O)NCc3c(OC)cccc3OC)cc2c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2007.09.031
11505444 16617 None 20 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2cccc(-c3ccc(O)cc3)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
CHEMBL1240967 16617 None 20 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 617 13 6 7 4.6 CC(C)(Cc1cccc(CC(=O)NCc2cccc(-c3ccc(O)cc3)c2)c1)NC[C@H](O)c1ccc(O)c(NS(C)(=O)=O)c1 10.1021/jm1005989
11625619 77648 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
CHEMBL2088201 77648 None 0 Human Functional pEC50 = 9.6 9.6 - 1
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 406 6 4 4 3.5 CCc1cc2c(cc1CC)CC(C)(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1016/j.bmcl.2012.07.096
16735257 85765 None 0 Human Functional pEC50 = 9.5 9.5 812 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228992 85765 None 0 Human Functional pEC50 = 9.5 9.5 812 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
688468 142419 None 7 Human Functional pEC50 = 9.5 9.5 346 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL388570 142419 None 7 Human Functional pEC50 = 9.5 9.5 346 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 303 6 5 5 2.1 C[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
16735257 85765 None 0 Human Functional pEC50 = 9.5 9.5 812 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228992 85765 None 0 Human Functional pEC50 = 9.5 9.5 812 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
155543518 175102 None 0 Human Functional pEC50 = 9.5 9.5 794 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
CHEMBL4566727 175102 None 0 Human Functional pEC50 = 9.5 9.5 794 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
1239 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410.0 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3465 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
CHEMBL1256786 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
DB00983 1677 None 37 Guinea pig Functional pEC50 = 9.5 9.5 -1 6
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3083544 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
3083544.0 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1200811 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1363 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1951071 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL605993 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
DB00983 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
DB01274 26817 None 34 Guinea pig Functional pEC50 = 9.5 9.5 2 6
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
24900685 70381 None 0 Guinea pig Functional pEC50 = 9.5 9.5 3 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945033 70381 None 0 Guinea pig Functional pEC50 = 9.5 9.5 3 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
3083544 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
3083544.0 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
CHEMBL1200811 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
CHEMBL1363 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
CHEMBL1951071 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
CHEMBL605993 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
DB00983 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
DB01274 26817 None 34 Human Functional pEC50 = 9.5 9.5 -2 6
Agonist activity at beta2-adrenergic receptor (unknown origin)Agonist activity at beta2-adrenergic receptor (unknown origin)
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmcl.2013.11.028
118737352 119119 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426696 119119 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 13 6 9 6.1 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
1499 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
1499 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
3779 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
3779 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
3779.0 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
3779.0 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
536 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
536 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
DB01064 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2018.10.043
DB01064 2091 None 34 Human Functional pEC50 = 9.5 9.5 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2018.04.041
2419 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152.0 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
56943485 112566 None 0 Human Functional pEC50 = 9.5 9.5 12 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 112566 None 0 Human Functional pEC50 = 9.5 9.5 12 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
11592062 112520 None 0 Human Functional pEC50 = 9.5 9.5 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
CHEMBL3298325 112520 None 0 Human Functional pEC50 = 9.5 9.5 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1cccc(CN)c1 10.1016/j.bmcl.2014.04.095
24901348 70351 None 0 Human Functional pEC50 = 9.5 9.5 70 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944689 70351 None 0 Human Functional pEC50 = 9.5 9.5 70 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
24901211 70355 None 0 Human Functional pEC50 = 9.5 9.5 158 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1944693 70355 None 0 Human Functional pEC50 = 9.5 9.5 158 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24901351 70356 None 0 Human Functional pEC50 = 9.5 9.5 10 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1944694 70356 None 0 Human Functional pEC50 = 9.5 9.5 10 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
24901209 70379 None 0 Human Functional pEC50 = 9.5 9.5 177 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
CHEMBL1945031 70379 None 0 Human Functional pEC50 = 9.5 9.5 177 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 516 11 6 6 4.3 Cc1cccc2c(CCNCc3cccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)sc45)c3)c[nH]c12 10.1016/j.bmcl.2011.10.049
24901143 70389 None 0 Human Functional pEC50 = 9.5 9.5 12 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945041 70389 None 0 Human Functional pEC50 = 9.5 9.5 12 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 483 10 5 6 4.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
156015043 178369 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4648975 178369 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650763 178369 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 342 7 4 5 2.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
56668796 66623 None 0 Human Functional pEC50 = 9.5 9.5 31 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835860 66623 None 0 Human Functional pEC50 = 9.5 9.5 31 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852632 66623 None 0 Human Functional pEC50 = 9.5 9.5 31 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
2419 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152.0 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
2419 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152.0 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
559 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
DB00938 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
9932018 70240 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940815 70240 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
57403562 70242 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 450 11 6 6 3.7 CC(C)(Cc1ccc(NCC(O)c2ccccc2)cc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2011.11.072
CHEMBL1940817 70242 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 450 11 6 6 3.7 CC(C)(Cc1ccc(NCC(O)c2ccccc2)cc1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2011.11.072
10202462 70256 None 0 Human Functional pEC50 = 9.5 9.5 223 2
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940831 70256 None 0 Human Functional pEC50 = 9.5 9.5 223 2
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
2419 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
5152 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
5152.0 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
559 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
DB00938 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/jm100068m
9986442 58554 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683933 58554 None 0 Human Functional pEC50 = 9.5 9.5 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 626 15 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
2419 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
5152 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
5152.0 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
559 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
DB00938 3463 None 53 Human Functional pEC50 = 9.5 9.5 8 19
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.01.043
9874175 58555 None 1 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683934 58555 None 1 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
46938906 16711 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 603 13 5 7 4.4 CCN(Cc1ccc(O)cc1Cl)C(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
CHEMBL1242969 16711 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate methodAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as elevation in cAMP level after 1 hr by flashplate method
ChEMBL 603 13 5 7 4.4 CCN(Cc1ccc(O)cc1Cl)C(=O)Cc1cccc(CC(C)(C)NC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)c1 10.1021/jm1005989
156019922 178449 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4645720 178449 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651233 178449 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccccc1CCCNCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
16049309 64121 None 0 Human Functional pEC50 = 9.4 9.4 100 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807870 64121 None 0 Human Functional pEC50 = 9.4 9.4 100 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
9874175 58555 None 1 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
CHEMBL1683934 58555 None 1 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1021/jm501915g
118737349 119115 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
CHEMBL3426692 119115 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 739 13 6 9 6.4 COc1c(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1Cl 10.1021/jm501915g
9871386 112334 None 3 Human Functional pEC50 = 9.4 9.4 8 4
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3290999 112334 None 3 Human Functional pEC50 = 9.4 9.4 8 4
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
24901349 70354 None 0 Human Functional pEC50 = 9.4 9.4 56 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1944692 70354 None 0 Human Functional pEC50 = 9.4 9.4 56 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(CNCCc4ccccc4F)cc3)c2s1 10.1016/j.bmcl.2011.10.049
57398562 70384 None 0 Human Functional pEC50 = 9.4 9.4 112 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945036 70384 None 0 Human Functional pEC50 = 9.4 9.4 112 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 11 5 6 4.1 CC(CNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1)c1ccccc1 10.1016/j.bmcl.2011.10.049
24900942 70413 None 0 Human Functional pEC50 = 9.4 9.4 31 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945299 70413 None 0 Human Functional pEC50 = 9.4 9.4 31 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 493 12 5 7 3.5 COc1ccccc1CNCCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
10184665 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
10184665.0 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
4799 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
7353 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
CHEMBL1198857 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
DB09082 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm401532g
10184665 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
10184665.0 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
4799 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
7353 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
CHEMBL1198857 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
DB09082 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1016/j.bmc.2011.08.043
9871386 112334 None 3 Human Functional pEC50 = 9.4 9.4 8 4
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290999 112334 None 3 Human Functional pEC50 = 9.4 9.4 8 4
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 521 10 5 6 5.5 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
10184665 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
10184665.0 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
4799 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
7353 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
CHEMBL1198857 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
DB09082 3991 None 42 Human Functional pEC50 = 9.4 9.4 40 10
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1021/jm100326d
46832798 14208 None 0 Human Functional pEC50 = 9.4 9.4 19 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1084648 14208 None 0 Human Functional pEC50 = 9.4 9.4 19 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1198879 14208 None 0 Human Functional pEC50 = 9.4 9.4 19 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
10225563 14214 None 0 Human Functional pEC50 = 9.4 9.4 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084891 14214 None 0 Human Functional pEC50 = 9.4 9.4 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198889 14214 None 0 Human Functional pEC50 = 9.4 9.4 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 445 16 4 6 3.9 Cc1cc(C)cc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
22712045 70241 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 423 11 5 6 2.9 OCc1cc(C(O)CNCCc2ccc(OCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940816 70241 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 423 11 5 6 2.9 OCc1cc(C(O)CNCCc2ccc(OCC(O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
12093446 70259 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 5 5 4.6 Nc1c(Cl)cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)cc1Cl 10.1016/j.bmcl.2011.11.072
CHEMBL1940834 70259 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 5 5 4.6 Nc1c(Cl)cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)cc1Cl 10.1016/j.bmcl.2011.11.072
1239 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
3410 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
3410.0 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
3465 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
DB00983 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.10.013
45483816 199592 None 0 Human Functional pEC50 = 9.4 9.4 12 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.10.013
CHEMBL567833 199592 None 0 Human Functional pEC50 = 9.4 9.4 12 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1cccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.10.013
45483864 201365 None 0 Human Functional pEC50 = 9.4 9.4 9 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL584498 201365 None 0 Human Functional pEC50 = 9.4 9.4 9 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
53379897 63667 None 0 Human Functional pEC50 = 9.4 9.4 151 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800961 63667 None 0 Human Functional pEC50 = 9.4 9.4 151 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
1239 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
3410 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
3410.0 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
3465 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
DB00983 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.06.104
1239 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
3410 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
3410.0 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
3465 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
DB00983 1677 None 37 Human Functional pEC50 = 9.4 9.4 -2 6
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2009.12.087
156009486 178368 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4632876 178368 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650738 178368 None 0 Human Functional pEC50 = 9.4 9.4 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
105 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083.0 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
558 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
CHEMBL714 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
DB01001 3461 None 54 Guinea pig Functional pEC50 = 9.3 9.3 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
45483852 199213 None 0 Human Functional pEC50 = 9.3 9.3 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565267 199213 None 0 Human Functional pEC50 = 9.3 9.3 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
45484568 200806 None 0 Human Functional pEC50 = 9.3 9.3 10 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 541 13 6 8 1.8 CN(C)CC(=O)NCCCC(=O)Nc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.06.104
CHEMBL576428 200806 None 0 Human Functional pEC50 = 9.3 9.3 10 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 541 13 6 8 1.8 CN(C)CC(=O)NCCCC(=O)Nc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.06.104
57401201 70881 None 0 Guinea pig Functional pEC50 = 9.3 9.3 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951066 70881 None 0 Guinea pig Functional pEC50 = 9.3 9.3 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
24900689 70387 None 0 Guinea pig Functional pEC50 = 9.3 9.3 3 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945039 70387 None 0 Guinea pig Functional pEC50 = 9.3 9.3 3 5
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
57393350 70558 None 0 Guinea pig Functional pEC50 = 9.3 9.3 63 2
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947152 70558 None 0 Guinea pig Functional pEC50 = 9.3 9.3 63 2
Agonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contractionAgonist activity at beta2 adrenoceptor in guinea pig trachea assessed as reduction in methacholine-induced contraction
ChEMBL 509 11 4 5 5.6 O=c1[nH]c2c(O)ccc(CCNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
2419 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
5152.0 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
559 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
DB00938 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.11.072
9892481 70257 None 12 Human Functional pEC50 = 9.3 9.3 -3 4
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940832 70257 None 12 Human Functional pEC50 = 9.3 9.3 -3 4
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
1239 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3410.0 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
3465 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
DB00983 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmc.2011.05.064
1239 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
3410 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
3410.0 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
3465 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
DB00983 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.04.135
19082200 110280 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 443 12 3 7 2.9 CN(CCNCCc1ccc(O)c2nc(O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL323776 110280 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 443 12 3 7 2.9 CN(CCNCCc1ccc(O)c2nc(O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
16049377 64119 None 0 Human Functional pEC50 = 9.3 9.3 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807832 64119 None 0 Human Functional pEC50 = 9.3 9.3 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 465 13 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
10484922 119112 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426689 119112 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.8 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
10327461 119113 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
CHEMBL3426690 119113 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 709 12 6 8 6.4 O=C(CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c(Cl)c1 10.1021/jm501915g
10439505 119122 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
CHEMBL3426699 119122 None 0 Human Functional pEC50 = 9.3 9.3 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 675 12 6 8 5.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCNC(=O)c2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)CC1 10.1021/jm501915g
155515718 170066 None 0 Human Functional pEC50 = 9.3 9.3 2884 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
CHEMBL4441752 170066 None 0 Human Functional pEC50 = 9.3 9.3 2884 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
155551006 174049 None 0 Human Functional pEC50 = 9.3 9.3 44 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4541169 174049 None 0 Human Functional pEC50 = 9.3 9.3 44 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
90645345 112542 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 112542 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
90645346 112558 None 0 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 112558 None 0 Human Functional pEC50 = 9.3 9.3 2 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
2419 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
5152.0 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
559 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
DB00938 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.095
9892481 70257 None 12 Human Functional pEC50 = 9.3 9.3 -3 4
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 70257 None 12 Human Functional pEC50 = 9.3 9.3 -3 4
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
10239722 112521 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 112521 None 0 Human Functional pEC50 = 9.3 9.3 11 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
66796015 112523 None 0 Human Functional pEC50 = 9.3 9.3 35 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298328 112523 None 0 Human Functional pEC50 = 9.3 9.3 35 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 474 11 6 7 3.2 NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24900685 70381 None 0 Human Functional pEC50 = 9.3 9.3 -3 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945033 70381 None 0 Human Functional pEC50 = 9.3 9.3 -3 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 11 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900426 70385 None 0 Human Functional pEC50 = 9.3 9.3 31 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945037 70385 None 0 Human Functional pEC50 = 9.3 9.3 31 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 477 12 5 6 3.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccc4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24901141 70563 None 0 Human Functional pEC50 = 9.3 9.3 39 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947157 70563 None 0 Human Functional pEC50 = 9.3 9.3 39 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 531 11 5 6 4.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
3083544 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
3083544.0 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1200811 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1363 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL1951071 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
CHEMBL605993 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
DB00983 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
DB01274 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm401532g
10482960 106445 None 0 Human Functional pEC50 = 9.3 9.3 316 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3126383 106445 None 0 Human Functional pEC50 = 9.3 9.3 316 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3139365 106445 None 0 Human Functional pEC50 = 9.3 9.3 316 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
3083544 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
3083544.0 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1200811 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1363 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1951071 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL605993 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
DB00983 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
DB01274 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1016/j.bmc.2011.08.043
56658405 66609 None 0 Human Functional pEC50 = 9.3 9.3 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1835856 66609 None 0 Human Functional pEC50 = 9.3 9.3 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
CHEMBL1852565 66609 None 0 Human Functional pEC50 = 9.3 9.3 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.08.043
56658407 66659 None 0 Human Functional pEC50 = 9.3 9.3 15 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835857 66659 None 0 Human Functional pEC50 = 9.3 9.3 15 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852796 66659 None 0 Human Functional pEC50 = 9.3 9.3 15 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 487 18 6 6 3.3 NC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
2419 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
5152.0 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
559 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
DB00938 3463 None 53 Human Functional pEC50 = 9.3 9.3 8 19
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2014.04.069
1239 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3410 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3410.0 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3465 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
DB00983 1677 None 37 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
42625513 12563 None 0 Human Functional pEC50 = 9.3 9.3 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL1186722 12563 None 0 Human Functional pEC50 = 9.3 9.3 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL475389 12563 None 0 Human Functional pEC50 = 9.3 9.3 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
42625517 12725 None 0 Human Functional pEC50 = 9.3 9.3 19 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187654 12725 None 0 Human Functional pEC50 = 9.3 9.3 19 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL514032 12725 None 0 Human Functional pEC50 = 9.3 9.3 19 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
3083544 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
3083544.0 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1200811 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1363 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL1951071 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
CHEMBL605993 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
DB00983 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
DB01274 26817 None 34 Human Functional pEC50 = 9.3 9.3 -2 6
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/jm100326d
10128077 112332 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290997 112332 None 0 Human Functional pEC50 = 9.3 9.3 1 2
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
45483843 199492 None 0 Human Functional pEC50 = 9.2 9.2 9 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL567192 199492 None 0 Human Functional pEC50 = 9.2 9.2 9 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
45483868 199678 None 0 Human Functional pEC50 = 9.2 9.2 6 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568273 199678 None 0 Human Functional pEC50 = 9.2 9.2 6 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
156010782 178375 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4632435 178375 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650800 178375 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 446 8 4 5 4.3 CC(C)(CC(c1ccccc1)c1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
56678847 66398 None 0 Human Functional pEC50 = 9.2 9.2 99 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814274 66398 None 0 Human Functional pEC50 = 9.2 9.2 99 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851691 66398 None 0 Human Functional pEC50 = 9.2 9.2 99 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CN(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
9871096 66671 None 0 Human Functional pEC50 = 9.2 9.2 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814268 66671 None 0 Human Functional pEC50 = 9.2 9.2 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1852860 66671 None 0 Human Functional pEC50 = 9.2 9.2 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
16049234 64115 None 0 Human Functional pEC50 = 9.2 9.2 177 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807828 64115 None 0 Human Functional pEC50 = 9.2 9.2 177 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
56673674 64118 None 0 Human Functional pEC50 = 9.2 9.2 1258 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 513 13 5 8 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCS(=O)(=O)CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807831 64118 None 0 Human Functional pEC50 = 9.2 9.2 1258 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 513 13 5 8 2.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCS(=O)(=O)CCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
183812 208197 None 20 Human Functional pEC50 = 9.2 9.2 15 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.05.097
CHEMBL82663 208197 None 20 Human Functional pEC50 = 9.2 9.2 15 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.05.097
56943517 112567 None 0 Human Functional pEC50 = 9.2 9.2 3 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
CHEMBL3298832 112567 None 0 Human Functional pEC50 = 9.2 9.2 3 3
Agonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 621 13 5 9 2.8 CS(=O)(=O)N1CCN(CCOc2ccc(Nc3ccc(CCNC[C@H](O)c4ccc(O)c5[nH]c(=O)ccc45)cc3)cc2)CC1 10.1016/j.bmcl.2014.04.095
56943518 112524 None 0 Human Functional pEC50 = 9.2 9.2 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298329 112524 None 0 Human Functional pEC50 = 9.2 9.2 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 488 12 6 7 3.6 NCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943545 112525 None 0 Human Functional pEC50 = 9.2 9.2 28 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298330 112525 None 0 Human Functional pEC50 = 9.2 9.2 28 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 13 6 7 4.0 NCCCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943546 112541 None 0 Human Functional pEC50 = 9.2 9.2 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298691 112541 None 0 Human Functional pEC50 = 9.2 9.2 25 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 518 14 6 8 3.2 NCCOCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
90645347 112576 None 0 Human Functional pEC50 = 9.2 9.2 7 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 112576 None 0 Human Functional pEC50 = 9.2 9.2 7 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
24900689 70387 None 0 Human Functional pEC50 = 9.2 9.2 -3 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945039 70387 None 0 Human Functional pEC50 = 9.2 9.2 -3 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccccc1CNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
24900813 70390 None 0 Human Functional pEC50 = 9.2 9.2 7 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945042 70390 None 0 Human Functional pEC50 = 9.2 9.2 7 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 467 10 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900812 70391 None 0 Human Functional pEC50 = 9.2 9.2 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945043 70391 None 0 Human Functional pEC50 = 9.2 9.2 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 450 10 5 7 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900937 70408 None 0 Human Functional pEC50 = 9.2 9.2 199 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945294 70408 None 0 Human Functional pEC50 = 9.2 9.2 199 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 413 8 4 6 2.8 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCCC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
24900424 70562 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947156 70562 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 525 11 5 6 5.1 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(-c4cccc(CNCc5ccccc5)c4)c3)c2s1 10.1016/j.bmcl.2011.10.049
183812 208197 None 20 Human Functional pEC50 = 9.2 9.2 15 2
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.10.049
CHEMBL82663 208197 None 20 Human Functional pEC50 = 9.2 9.2 15 2
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 464 13 3 8 2.9 O=S(=O)(CCCOCCc1ccccc1)CCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.10.049
56672269 66608 None 0 Human Functional pEC50 = 9.2 9.2 50 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835858 66608 None 0 Human Functional pEC50 = 9.2 9.2 50 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852564 66608 None 0 Human Functional pEC50 = 9.2 9.2 50 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 515 19 6 6 3.9 CCNC(=O)NCc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
42625515 12734 None 0 Human Functional pEC50 = 9.2 9.2 794 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187711 12734 None 0 Human Functional pEC50 = 9.2 9.2 794 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL516056 12734 None 0 Human Functional pEC50 = 9.2 9.2 794 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 3.0 CNS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
10077662 90272 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 623 14 5 8 5.1 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2007.09.031
CHEMBL238347 90272 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 623 14 5 8 5.1 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1Cc1ccccc1 10.1016/j.bmcl.2007.09.031
156015718 178361 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4648695 178361 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650694 178361 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1cccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
44237670 58254 None 0 Guinea pig Functional pEC50 = 9.2 9.2 8128 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 534 9 6 5 5.4 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682219 58254 None 0 Guinea pig Functional pEC50 = 9.2 9.2 8128 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 534 9 6 5 5.4 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1ccccc1-c1ccccc1 10.1016/j.bmcl.2010.12.096
45483814 199728 None 0 Human Functional pEC50 = 9.2 9.2 5 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568531 199728 None 0 Human Functional pEC50 = 9.2 9.2 5 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
1499 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
3779 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
3779.0 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
536 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
DB01064 2091 None 34 Human Functional pEC50 = 9.2 9.2 -102 38
Agonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assayAgonist activity at human beta2-AR expressed in CHOK1 cells co-expressing Galpha15 measured after 21 secs to 120 secs by Calcium-4 dye based FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.7b00762
46232769 203297 None 0 Human Functional pEC50 = 9.2 9.2 6 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601036 203297 None 0 Human Functional pEC50 = 9.2 9.2 6 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44434116 166690 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 12 5 8 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1C 10.1016/j.bmcl.2007.09.031
CHEMBL428027 166690 None 0 Human Functional pEC50 = 9.2 9.2 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 547 12 5 8 3.6 COc1cccc(OC)c1CNC(=O)c1cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc2n1C 10.1016/j.bmcl.2007.09.031
2419 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
5152 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
5152.0 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
559 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
DB00938 3463 None 53 Human Functional pEC50 = 9.2 9.2 8 19
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.0c01195
156014816 178408 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4645932 178408 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650992 178408 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 360 7 4 5 2.1 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(F)cc2)N1 10.1016/j.bmc.2019.115178
63952 8590 None 24 Human Functional pEC50 = 9.1 9.1 -2 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
86306667 8590 None 24 Human Functional pEC50 = 9.1 9.1 -2 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
CHEMBL1094785 8590 None 24 Human Functional pEC50 = 9.1 9.1 -2 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 368 7 4 5 2.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1021/jm100068m
4183 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
6918554 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
6918554.0 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
7455 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
CHEMBL1095777 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
DB05039 2025 None 43 Human Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/acs.jmedchem.0c01195
9871096 66671 None 0 Guinea pig Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814268 66671 None 0 Guinea pig Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1852860 66671 None 0 Guinea pig Functional pEC50 = 9.1 9.1 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
56658246 64518 None 0 Human Functional pEC50 = 9.1 9.1 -3 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814277 64518 None 0 Human Functional pEC50 = 9.1 9.1 -3 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814278 64518 None 0 Human Functional pEC50 = 9.1 9.1 -3 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1cc[nH]c(=O)n1-c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
53357712 66428 None 0 Human Functional pEC50 = 9.1 9.1 79 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814271 66428 None 0 Human Functional pEC50 = 9.1 9.1 79 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851848 66428 None 0 Human Functional pEC50 = 9.1 9.1 79 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
56678849 66647 None 0 Human Functional pEC50 = 9.1 9.1 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814275 66647 None 0 Human Functional pEC50 = 9.1 9.1 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1852744 66647 None 0 Human Functional pEC50 = 9.1 9.1 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 18 5 8 2.7 O=C1NC(=O)N(Cc2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
2419 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
5152 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
5152.0 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
559 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
DB00938 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.04.135
16049289 63586 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 501 15 4 7 3.2 CCCCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800660 63586 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 501 15 4 7 3.2 CCCCN(CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
2419 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
5152 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
5152.0 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
559 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
DB00938 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.05.097
16049090 64110 None 0 Human Functional pEC50 = 9.1 9.1 316 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 447 13 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807823 64110 None 0 Human Functional pEC50 = 9.1 9.1 316 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 447 13 5 7 2.9 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3)c2s1 10.1016/j.bmcl.2011.05.097
56673609 64124 None 0 Human Functional pEC50 = 9.1 9.1 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807873 64124 None 0 Human Functional pEC50 = 9.1 9.1 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
319 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
321 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
444031 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
444031.0 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
784 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
CHEMBL1346 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
DB00496 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1021/jm501915g
118737356 119126 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426703 119126 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 753 13 5 9 6.5 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
118737360 119131 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426708 119131 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1CCNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
90645344 112519 None 0 Human Functional pEC50 = 9.1 9.1 7 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 112519 None 0 Human Functional pEC50 = 9.1 9.1 7 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
2419 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
5152 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
5152.0 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
559 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
CHEMBL1263 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
DB00938 3463 None 53 Human Functional pEC50 = 9.1 9.1 8 19
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmcl.2011.10.049
24900750 70403 None 0 Human Functional pEC50 = 9.1 9.1 5 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945289 70403 None 0 Human Functional pEC50 = 9.1 9.1 5 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1ccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)cc1 10.1016/j.bmcl.2011.10.049
24901285 70411 None 0 Human Functional pEC50 = 9.1 9.1 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 11 5 6 5.2 CC(Cc1cccc(CNCCc2c(Cl)cccc2Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2011.10.049
CHEMBL1945297 70411 None 0 Human Functional pEC50 = 9.1 9.1 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 11 5 6 5.2 CC(Cc1cccc(CNCCc2c(Cl)cccc2Cl)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12 10.1016/j.bmcl.2011.10.049
156015629 178358 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4648440 178358 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650679 178358 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 482 8 4 5 4.6 CC(C)(CC(c1ccc(F)cc1)c1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
10238776 66497 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835853 66497 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852214 66497 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
10217757 112333 None 0 Human Functional pEC50 = 9.1 9.1 10 4
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 112333 None 0 Human Functional pEC50 = 9.1 9.1 10 4
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
42625511 12741 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL1187778 12741 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL520313 12741 None 0 Human Functional pEC50 = 9.1 9.1 3 4
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
10203169 14244 None 0 Human Functional pEC50 = 9.1 9.1 25 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1086536 14244 None 0 Human Functional pEC50 = 9.1 9.1 25 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1199300 14244 None 0 Human Functional pEC50 = 9.1 9.1 25 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
319 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
321 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
444031 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
444031.0 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
784 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
CHEMBL1346 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
DB00496 1324 None 32 Human Functional pEC50 = 9.1 9.1 -2 18
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.01.043
1499 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
3779 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
3779.0 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
536 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
CHEMBL434 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
DB01064 2091 None 34 Human Functional pEC50 = 9.1 9.1 -102 38
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2009.06.083
156014807 178335 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4643561 178335 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650530 178335 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 5 6 1.7 O=C1COc2c(cc(O)cc2C(O)CNCCCc2ccc(O)cc2)N1 10.1016/j.bmc.2019.115178
53316961 58277 None 0 Guinea pig Functional pEC50 = 9.1 9.1 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 528 9 6 5 4.7 CC(C)(C)c1ccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 10.1016/j.bmcl.2010.12.096
CHEMBL1682302 58277 None 0 Guinea pig Functional pEC50 = 9.1 9.1 - 1
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 528 9 6 5 4.7 CC(C)(C)c1ccc(CNC(=O)Nc2cccc(CCNCC(O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 10.1016/j.bmcl.2010.12.096
45484536 199670 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 527 13 7 8 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL568239 199670 None 0 Human Functional pEC50 = 9.1 9.1 5 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 527 13 7 8 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
53326837 58562 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
CHEMBL1683942 58562 None 0 Human Functional pEC50 = 9.1 9.1 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 722 17 5 10 5.3 C[N+]1(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)[C@@H]2C[C@H](OC(=O)C(O)(c3cccs3)c3cccs3)C[C@@H]1[C@H]1O[C@H]12 10.1016/j.bmcl.2011.01.043
155541614 173138 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 437 10 5 5 3.5 CC(C)CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4518961 173138 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 437 10 5 5 3.5 CC(C)CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
156010796 178406 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4632700 178406 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650979 178406 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 372 8 4 6 2.0 COc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
11091850 47245 None 0 Human Functional pEC50 = 9 9.0 25 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL154370 47245 None 0 Human Functional pEC50 = 9 9.0 25 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
53357711 64519 None 0 Guinea pig Functional pEC50 = 9 9.0 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 64519 None 0 Guinea pig Functional pEC50 = 9 9.0 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 64519 None 0 Guinea pig Functional pEC50 = 9 9.0 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
319 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
321 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
444031 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
444031.0 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
784 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
CHEMBL1346 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
DB00496 1324 None 32 Guinea pig Functional pEC50 = 9 9.0 2 18
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
44237766 58256 None 0 Guinea pig Functional pEC50 = 9 9.0 10000 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682221 58256 None 0 Guinea pig Functional pEC50 = 9 9.0 10000 2
Agonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxationAgonist activity at beta2 adrenoceptor in guinea pig tracheal rings assessed as vasorelaxation
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
53357711 64519 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 64519 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 64519 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
56673241 63581 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 13 3 6 2.9 CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800656 63581 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 457 13 3 6 2.9 CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
1239 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
3410 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
3410.0 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
3465 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
DB00983 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.05.097
16049450 64114 None 0 Human Functional pEC50 = 9 9.0 125 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807827 64114 None 0 Human Functional pEC50 = 9 9.0 125 2
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
11169365 112575 None 0 Human Functional pEC50 = 9 9.0 22 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298986 112575 None 0 Human Functional pEC50 = 9 9.0 22 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 502 11 6 7 4.0 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
45484585 14103 None 0 Human Functional pEC50 = 9 9.0 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL1197807 14103 None 0 Human Functional pEC50 = 9 9.0 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL587197 14103 None 0 Human Functional pEC50 = 9 9.0 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
45101519 200979 None 0 Human Functional pEC50 = 9 9.0 1 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL577917 200979 None 0 Human Functional pEC50 = 9 9.0 1 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
1239 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
3410 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
3410.0 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
3465 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
DB00983 1677 None 37 Human Functional pEC50 = 9 9.0 -2 6
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2011.10.049
24900872 70386 None 0 Human Functional pEC50 = 9 9.0 89 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945038 70386 None 0 Human Functional pEC50 = 9 9.0 89 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 478 12 5 7 3.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CNCCCc4ccccn4)c3)c2s1 10.1016/j.bmcl.2011.10.049
57391554 70392 None 0 Human Functional pEC50 = 9 9.0 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945044 70392 None 0 Human Functional pEC50 = 9 9.0 25 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 479 11 5 7 3.5 COc1cccc(CNCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)sc34)c2)c1 10.1016/j.bmcl.2011.10.049
24901140 70559 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947153 70559 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 503 9 4 6 4.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3cccc(CN4CCC(c5ccccc5)CC4)c3)c2s1 10.1016/j.bmcl.2011.10.049
10053159 106337 None 0 Human Functional pEC50 = 9 9.0 398 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3124955 106337 None 0 Human Functional pEC50 = 9 9.0 398 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
CHEMBL3139033 106337 None 0 Human Functional pEC50 = 9 9.0 398 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 545 18 4 7 4.6 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CC=CC1 10.1021/jm401532g
56665368 66480 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835854 66480 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852119 66480 None 0 Human Functional pEC50 = 9 9.0 1 4
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
56678973 66600 None 0 Human Functional pEC50 = 9 9.0 2 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835855 66600 None 0 Human Functional pEC50 = 9 9.0 2 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852541 66600 None 0 Human Functional pEC50 = 9 9.0 2 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 555 18 6 6 5.6 O=C(Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCCC1 10.1016/j.bmc.2011.08.043
56675663 66610 None 0 Human Functional pEC50 = 9 9.0 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835861 66610 None 0 Human Functional pEC50 = 9 9.0 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852575 66610 None 0 Human Functional pEC50 = 9 9.0 25 3
Agonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 6 6 4.6 NC(=O)Nc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(C(F)(F)F)c1 10.1016/j.bmc.2011.08.043
42625821 12548 None 0 Human Functional pEC50 = 9 9.0 630 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186678 12548 None 0 Human Functional pEC50 = 9 9.0 630 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL474393 12548 None 0 Human Functional pEC50 = 9 9.0 630 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 522 18 4 7 3.4 CN(C)S(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625587 12704 None 0 Human Functional pEC50 = 9 9.0 125 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL1187520 12704 None 0 Human Functional pEC50 = 9 9.0 125 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL506518 12704 None 0 Human Functional pEC50 = 9 9.0 125 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
9958539 103160 None 0 Human Functional pEC50 = 9 9.0 5 3
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
CHEMBL307647 103160 None 0 Human Functional pEC50 = 9 9.0 5 3
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
87142783 119127 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3426704 119127 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 719 13 5 9 5.8 COc1cc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548101 124466 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3639442 124466 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548063 125268 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645274 125268 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 16 6 9 6.3 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548134 125269 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645275 125269 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
66791483 125271 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645277 125271 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 16 6 9 6.6 Cc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548074 125272 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645278 125272 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 17 6 10 6.7 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548094 125274 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645280 125274 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.4 CC(Cc1cccc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548099 125275 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645281 125275 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 CC(Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
68057677 125276 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645282 125276 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548122 125277 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645283 125277 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 17 6 9 6.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548079 125278 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645284 125278 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)CCCCN(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548056 125279 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645285 125279 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 818 18 6 10 6.4 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548067 125280 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645286 125280 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 18 6 10 7.1 COc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548141 125281 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645287 125281 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)c1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548102 125282 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645288 125282 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 802 18 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
68057804 125283 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645289 125283 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 CC(Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548054 125284 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645290 125284 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548125 125285 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645291 125285 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 830 19 6 9 6.2 C[C@@H](Cc1cccc(CC(=O)NCCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548051 125286 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645292 125286 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548107 125287 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645293 125287 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 14 6 9 7.4 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548124 125288 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645294 125288 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1ccc(C)c(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548081 125289 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
CHEMBL3645295 125289 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 838 15 6 10 7.1 COc1cc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)ccc1NC(=O)c1cccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1 nan
59548120 125290 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645296 125290 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 14 6 9 7.7 Cc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548093 125292 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645298 125292 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 822 15 6 9 7.1 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548119 125293 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645299 125293 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548129 125296 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645301 125296 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843902 125297 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645302 125297 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 15 6 9 7.8 Cc1ccc(C(=O)Nc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548098 125298 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645303 125298 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548123 125299 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645304 125299 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1cccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548138 125300 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645305 125300 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 CC(Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548095 125302 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645307 125302 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548130 125303 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645308 125303 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.5 C[C@@H](Cc1ccc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548100 125304 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645309 125304 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1cccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548136 125305 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645310 125305 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 16 6 9 7.5 Cc1ccc(C(=O)NCc2cccc(CC(C)NC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
66791606 125306 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645311 125306 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 CC(Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843738 125308 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645313 125308 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843742 125309 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645314 125309 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1ccc(CNC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
70843734 125311 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645316 125311 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.2 C[C@@H](Cc1cccc(CNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548091 125312 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645317 125312 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.4 CC(Cc1cccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548132 125316 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645320 125316 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548118 125317 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645321 125317 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548139 125319 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645323 125319 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.2 C[C@@H](Cc1ccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548061 125322 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645326 125322 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 886 16 6 10 7.6 COc1cc(NC(=O)Cc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548066 125323 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
CHEMBL3645327 125323 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)c1 nan
59548076 125324 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
CHEMBL3645328 125324 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 7.0 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1cccc(CC(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)c1 nan
59548128 125325 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645329 125325 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548117 125326 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645330 125326 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CC(=O)NCc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548058 125327 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645331 125327 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548121 125328 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645332 125328 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548110 125329 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645333 125329 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548080 125330 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645334 125330 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548135 125331 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645335 125331 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 17 6 9 7.4 Cc1c(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cccc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548052 125333 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645337 125333 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548059 125337 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645340 125337 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 17 6 9 6.7 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548142 125338 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645341 125338 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548084 125339 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645342 125339 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548083 125340 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645343 125340 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 C[C@@H](Cc1cccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548114 125341 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645344 125341 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 864 17 6 9 7.1 CC(Cc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548140 125342 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645345 125342 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548050 125343 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645346 125343 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548069 125345 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645348 125345 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1cc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)ccc1F)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 125346 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 125346 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548115 125347 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645350 125347 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548103 125348 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645351 125348 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548057 125349 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645352 125349 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@@H](Cc1ccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548078 125350 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645353 125350 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 CC(Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548082 125351 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645354 125351 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548090 125353 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
CHEMBL3645356 125353 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(C)NC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1CC(=O)NCc1ccc(N(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)cc1 nan
59548137 125354 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645357 125354 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 882 17 6 9 7.2 CC(Cc1ccc(F)c(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548068 125356 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645359 125356 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.0 CN(CCCC(=O)Nc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
59548105 125358 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645361 125358 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 15 6 9 7.4 Cc1ccc(C(=O)Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
56953428 125360 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3645363 125360 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 788 17 6 9 6.4 CN(CCCCC(=O)Nc1ccc(CNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
49785227 125362 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645365 125362 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 C[C@H](Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785225 128534 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3666068 128534 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 17 6 9 7.0 Cc1cc(NC(=O)CCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
49785142 143359 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3896828 143359 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 816 18 6 9 5.8 C[C@@H](Cc1cccc(CC(=O)NCCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405092 150341 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
CHEMBL3952427 150341 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 15 5 8 8.9 Cc1ccc(C(=O)Nc2ccc(CC(C)NC[C@H](C)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1N(C)C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 nan
118405970 151894 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3965175 151894 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 848 17 5 8 7.6 CC(Cc1ccc(CNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1)NCCc1ccc(O)c2[nH]c(=O)ccc12 nan
118405900 153757 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3981221 153757 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 852 15 6 10 7.4 COc1cc(NC(=O)c2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)c(C)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
118405964 160873 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
CHEMBL4114219 160873 None 0 Human Functional pEC50 = 9 9.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 850 16 6 9 7.3 C[C@@H](NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12)c1cccc(CCNC(=O)c2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1 nan
11214499 86046 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2010.10.132
CHEMBL230490 86046 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 516 11 5 5 4.3 C[C@H](Cc1cccc(CC(=O)NCc2ccc(Cl)c(Cl)c2)c1)NC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2010.10.132
45484583 200948 None 0 Human Functional pEC50 = 9.0 9.0 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL577702 200948 None 0 Human Functional pEC50 = 9.0 9.0 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
10438748 58553 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683932 58553 None 0 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 612 14 5 7 6.2 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
10326800 58558 None 1 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683938 58558 None 1 Human Functional pEC50 = 9.0 9.0 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
1499 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
3779 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
3779.0 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
536 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
CHEMBL434 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
DB01064 2091 None 34 Human Functional pEC50 = 8.9 8.9 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assayAgonist activity at human beta2 adrenergic receptor expressed in CHOK1 cells co-expressing Galpha15 assessed as increase in calcium influx by measuring fluorescence intensity by FLIPR assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jnatprod.9b00418
45484569 200090 None 0 Human Functional pEC50 = 8.9 8.9 4 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 596 13 6 9 1.5 CN1CCN(CC(=O)NCCCC(=O)Nc2ccc(CC(C)(C)NCC(O)c3ccc(O)c4c3OCC(=O)N4)cc2)CC1 10.1016/j.bmcl.2009.06.104
CHEMBL570834 200090 None 0 Human Functional pEC50 = 8.9 8.9 4 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 596 13 6 9 1.5 CN1CCN(CC(=O)NCCCC(=O)Nc2ccc(CC(C)(C)NCC(O)c3ccc(O)c4c3OCC(=O)N4)cc2)CC1 10.1016/j.bmcl.2009.06.104
45101520 201240 None 0 Human Functional pEC50 = 8.9 8.9 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 513 12 7 8 1.2 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL583235 201240 None 0 Human Functional pEC50 = 8.9 8.9 3 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 513 12 7 8 1.2 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)CN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
44396736 66889 None 0 Human Functional pEC50 = 8.9 8.9 -11 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL186271 66889 None 0 Human Functional pEC50 = 8.9 8.9 -11 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
56665368 66480 None 0 Guinea pig Functional pEC50 = 8.9 8.9 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835854 66480 None 0 Guinea pig Functional pEC50 = 8.9 8.9 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852119 66480 None 0 Guinea pig Functional pEC50 = 8.9 8.9 -1 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 501 18 6 6 4.2 CCNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
10180590 70255 None 0 Human Functional pEC50 = 8.9 8.9 707 2
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940830 70255 None 0 Human Functional pEC50 = 8.9 8.9 707 2
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 422 11 6 6 2.9 OCc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
57398384 70258 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
CHEMBL1940833 70258 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at beta2-adrenoceptor endogenously expressed in human BEAS-2B cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 459 10 6 6 3.2 O=c1ccc2c([C@@H](O)CNCCc3ccc(NC[C@H](O)c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.11.072
9893058 66403 None 0 Human Functional pEC50 = 8.9 8.9 39 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1814267 66403 None 0 Human Functional pEC50 = 8.9 8.9 39 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
CHEMBL1851721 66403 None 0 Human Functional pEC50 = 8.9 8.9 39 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 525 17 5 8 2.9 O=c1ccn(-c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)c(=O)[nH]1 10.1016/j.bmc.2011.05.064
56675511 66430 None 0 Human Functional pEC50 = 8.9 8.9 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814273 66430 None 0 Human Functional pEC50 = 8.9 8.9 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1851850 66430 None 0 Human Functional pEC50 = 8.9 8.9 31 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
16049374 64120 None 0 Human Functional pEC50 = 8.9 8.9 89 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807869 64120 None 0 Human Functional pEC50 = 8.9 8.9 89 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
118737359 119130 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
CHEMBL3426707 119130 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 719 14 6 9 5.8 COc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)cc1NC(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1 10.1021/jm501915g
24901284 70410 None 0 Human Functional pEC50 = 8.9 8.9 2 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945296 70410 None 0 Human Functional pEC50 = 8.9 8.9 2 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 545 12 5 6 5.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCc3cccc(CNCCc4c(Cl)cccc4Cl)c3)c2s1 10.1016/j.bmcl.2011.10.049
42625897 12480 None 0 Human Functional pEC50 = 8.9 8.9 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL1186265 12480 None 0 Human Functional pEC50 = 8.9 8.9 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
CHEMBL456485 12480 None 0 Human Functional pEC50 = 8.9 8.9 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 564 18 4 8 3.1 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCOCC1 10.1021/jm801016j
10311070 112323 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290989 112323 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 484 11 5 6 5.2 COc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
10310047 112326 None 0 Human Functional pEC50 = 8.9 8.9 158 2
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290991 112326 None 0 Human Functional pEC50 = 8.9 8.9 158 2
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 422 11 5 6 3.9 CCOc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
145989945 166885 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4284146 166885 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c([C@@H](CO)NCCc3ccc(O)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
1239 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3410 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3410.0 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
3465 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
DB00983 1677 None 37 Human Functional pEC50 = 8.9 8.9 -2 6
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm100068m
53318455 58552 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683931 58552 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 556 10 5 7 4.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1016/j.bmcl.2011.01.043
11703823 203612 None 0 Human Functional pEC50 = 8.9 8.9 131 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL603274 203612 None 0 Human Functional pEC50 = 8.9 8.9 131 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44396715 67472 None 0 Human Functional pEC50 = 8.9 8.9 -20 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL189081 67472 None 0 Human Functional pEC50 = 8.9 8.9 -20 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
156015726 178381 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4647449 178381 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650846 178381 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 410 7 4 5 3.0 O=C1COc2c(cc(O)cc2C(O)CNCCCc2cccc(C(F)(F)F)c2)N1 10.1016/j.bmc.2019.115178
46232973 203244 None 0 Human Functional pEC50 = 8.9 8.9 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccccc1C(F)(F)F)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600617 203244 None 0 Human Functional pEC50 = 8.9 8.9 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccccc1C(F)(F)F)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
9800339 203610 None 9 Human Functional pEC50 = 8.9 8.9 251 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL603271 203610 None 9 Human Functional pEC50 = 8.9 8.9 251 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
4183 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
6918554 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
6918554.0 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
7455 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
CHEMBL1095777 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
DB05039 2025 None 43 Human Functional pEC50 = 8.8 8.8 -1 4
Agonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP levelAgonist activity at adrenergic beta2 receptor in human A431 cells assessed as elevation of cAMP level
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2014.06.014
45483844 200852 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL576848 200852 None 0 Human Functional pEC50 = 8.8 8.8 4 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2ccc(O)c3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.10.013
44392566 64849 None 0 Human Functional pEC50 = 8.8 8.8 11 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181964 64849 None 0 Human Functional pEC50 = 8.8 8.8 11 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C=C(C)CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
2233849 33360 None 5 Human Functional pEC50 = 8.8 8.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
CHEMBL1419122 33360 None 5 Human Functional pEC50 = 8.8 8.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
10288976 66601 None 0 Guinea pig Functional pEC50 = 8.8 8.8 -10 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835862 66601 None 0 Guinea pig Functional pEC50 = 8.8 8.8 -10 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852543 66601 None 0 Guinea pig Functional pEC50 = 8.8 8.8 -10 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 487 17 6 6 3.9 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(NC(N)=O)c1 10.1016/j.bmc.2011.08.043
44339091 9449 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 429 12 4 7 2.6 O=C(CCOCCc1ccccc1)NCCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.04.135
CHEMBL111775 9449 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 429 12 4 7 2.6 O=C(CCOCCc1ccccc1)NCCNCCc1ccc(O)c2nc(O)sc12 10.1016/j.bmcl.2011.04.135
53307432 63584 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800659 63584 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
16049448 64116 None 0 Human Functional pEC50 = 8.8 8.8 56 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807829 64116 None 0 Human Functional pEC50 = 8.8 8.8 56 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
16049376 64122 None 0 Human Functional pEC50 = 8.8 8.8 44 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807871 64122 None 0 Human Functional pEC50 = 8.8 8.8 44 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
53307432 63584 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL1800659 63584 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 485 15 3 6 3.7 CCCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
118737353 119123 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
CHEMBL3426700 119123 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation countingAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as cAMP accumulation using [125I]cAMP by scintillation counting
ChEMBL 705 13 6 9 5.2 COc1cc(C(=O)NCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/jm501915g
145989075 167188 None 0 Human Functional pEC50 = 8.8 8.8 524 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 324 6 4 4 2.1 O=c1ccc2c(C(CO)NCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4289813 167188 None 0 Human Functional pEC50 = 8.8 8.8 524 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 324 6 4 4 2.1 O=c1ccc2c(C(CO)NCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
90645346 112558 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 112558 None 0 Human Functional pEC50 = 8.8 8.8 2 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
11180293 112571 None 0 Human Functional pEC50 = 8.8 8.8 22 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 112571 None 0 Human Functional pEC50 = 8.8 8.8 22 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
24901416 70383 None 0 Human Functional pEC50 = 8.8 8.8 -2 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945035 70383 None 0 Human Functional pEC50 = 8.8 8.8 -2 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 481 11 5 6 3.6 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccccc3CNCCc3ccccc3F)c2s1 10.1016/j.bmcl.2011.10.049
10370605 106489 None 0 Human Functional pEC50 = 8.8 8.8 158 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3126385 106489 None 0 Human Functional pEC50 = 8.8 8.8 158 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
CHEMBL3139615 106489 None 0 Human Functional pEC50 = 8.8 8.8 158 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.2 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCCC1 10.1021/jm401532g
42625588 180532 None 0 Human Functional pEC50 = 8.8 8.8 630 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475237 180532 None 0 Human Functional pEC50 = 8.8 8.8 630 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46833102 14211 None 0 Human Functional pEC50 = 8.8 8.8 31 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1084656 14211 None 0 Human Functional pEC50 = 8.8 8.8 31 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198882 14211 None 0 Human Functional pEC50 = 8.8 8.8 31 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
46832507 14219 None 0 Human Functional pEC50 = 8.8 8.8 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085638 14219 None 0 Human Functional pEC50 = 8.8 8.8 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198915 14219 None 0 Human Functional pEC50 = 8.8 8.8 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
57400045 70245 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 456 11 6 6 3.5 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(Cl)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940820 70245 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 456 11 6 6 3.5 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(Cl)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
149373618 178354 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4642893 178354 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4650643 178354 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 358 7 4 6 1.6 COc1ccc(CCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
73056754 104331 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099659 104331 None 0 Human Functional pEC50 = 8.8 8.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
45483847 199268 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565686 199268 None 0 Human Functional pEC50 = 8.8 8.8 2 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
45101522 201473 None 0 Human Functional pEC50 = 8.7 8.7 5 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 578 15 7 9 2.0 CC(C)(Cc1ccc(NC(=O)CCCNCCCS(=O)(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL585751 201473 None 0 Human Functional pEC50 = 8.7 8.7 5 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 578 15 7 9 2.0 CC(C)(Cc1ccc(NC(=O)CCCNCCCS(=O)(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
11962616 221 None 18 Human Functional pEC50 = 8.7 8.7 40 3
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
9326 221 None 18 Human Functional pEC50 = 8.7 8.7 40 3
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
CHEMBL3039530 221 None 18 Human Functional pEC50 = 8.7 8.7 40 3
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
DB12100 221 None 18 Human Functional pEC50 = 8.7 8.7 40 3
Agonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxationAgonist activity at beta2 adrenoceptor human bronchi assessed as induction of maximum relaxation
ChEMBL 460 13 4 5 4.2 O=c1ccc2c([nH]1)c(O)ccc2[C@H](CNCCCCCCOCC(c1ccccc1)(F)F)O 10.1021/acs.jmedchem.0c01195
56678845 66427 None 0 Human Functional pEC50 = 8.7 8.7 15 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1814269 66427 None 0 Human Functional pEC50 = 8.7 8.7 15 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
CHEMBL1851839 66427 None 0 Human Functional pEC50 = 8.7 8.7 15 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmc.2011.05.064
145981405 166593 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccccc3Cl)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4278577 166593 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccccc3Cl)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
145987168 167311 None 0 Human Functional pEC50 = 8.7 8.7 316 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1cccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2018.04.041
CHEMBL4291941 167311 None 0 Human Functional pEC50 = 8.7 8.7 316 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1cccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.ejmech.2018.04.041
10173878 112522 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298327 112522 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 459 10 5 6 4.2 CCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
24901283 70406 None 0 Human Functional pEC50 = 8.7 8.7 -2 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
CHEMBL1945292 70406 None 0 Human Functional pEC50 = 8.7 8.7 -2 5
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1cccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)c1 10.1016/j.bmcl.2011.10.049
10076176 106491 None 0 Human Functional pEC50 = 8.7 8.7 50 5
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3126382 106491 None 0 Human Functional pEC50 = 8.7 8.7 50 5
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
CHEMBL3139683 106491 None 0 Human Functional pEC50 = 8.7 8.7 50 5
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)C1CCCC1 10.1021/jm401532g
46832804 6988 None 0 Human Functional pEC50 = 8.7 8.7 50 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084655 6988 None 0 Human Functional pEC50 = 8.7 8.7 50 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
10310564 112322 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290988 112322 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 454 10 5 5 5.2 OCc1cc(C(O)CNCCc2ccc(Nc3cccc(-c4ccccc4)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
57396615 70243 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 5 6 2.9 CN(CC(O)c1ccccc1)c1ccc(CCNCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940818 70243 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 5 6 2.9 CN(CC(O)c1ccccc1)c1ccc(CCNCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2011.11.072
57391344 70246 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 440 11 6 6 3.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940821 70246 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 440 11 6 6 3.0 OCc1cc(C(O)CNCCc2ccc(NCC(O)c3ccc(F)cc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
10902809 48091 None 0 Human Functional pEC50 = 8 8.0 -1 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL155072 48091 None 0 Human Functional pEC50 = 8 8.0 -1 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 304 7 3 3 3.5 C[C@H](CNc1ccccc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11005613 119863 None 0 Human Functional pEC50 = 8 8.0 1 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348269 119863 None 0 Human Functional pEC50 = 8 8.0 1 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
90655867 111327 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
CHEMBL3265164 111327 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 562 17 3 7 3.9 CCN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1cccc(Cl)c1 10.1021/ml4005232
16036676 111330 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccc2ccccc2c1 10.1021/ml4005232
CHEMBL3265168 111330 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 578 17 3 7 4.4 CCN(CC)CCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccc2ccccc2c1 10.1021/ml4005232
54586985 61833 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773262 61833 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 583 15 5 7 5.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
145981007 166688 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4280227 166688 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 340 6 5 5 1.8 O=c1ccc2c(C(CO)NCCc3ccccc3O)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
145994130 167477 None 0 Human Functional pEC50 = 8 8.0 83 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(CO)NCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4294937 167477 None 0 Human Functional pEC50 = 8 8.0 83 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 338 7 4 4 2.5 O=c1ccc2c(C(CO)NCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
24900423 70560 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1947154 70560 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 537 9 4 6 5.3 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCc3ccc(-c4cccc(CN5Cc6ccccc6C5)c4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
45271518 197331 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203999 197331 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL549689 197331 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 479 11 4 6 3.9 COC(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45272431 197481 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204002 197481 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549960 197481 None 0 Human Functional pEC50 = 8 8.0 6 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 547 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(I)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45271523 197584 None 0 Human Functional pEC50 = 8 8.0 10 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204000 197584 None 0 Human Functional pEC50 = 8 8.0 10 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550096 197584 None 0 Human Functional pEC50 = 8 8.0 10 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45270697 197626 None 0 Human Functional pEC50 = 8 8.0 20 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203995 197626 None 0 Human Functional pEC50 = 8 8.0 20 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550444 197626 None 0 Human Functional pEC50 = 8 8.0 20 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45272430 197900 None 0 Human Functional pEC50 = 8 8.0 8 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204001 197900 None 0 Human Functional pEC50 = 8 8.0 8 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552374 197900 None 0 Human Functional pEC50 = 8 8.0 8 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 439 10 4 4 4.2 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(F)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45269025 198603 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203991 198603 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL561173 198603 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 500 11 5 6 2.7 NS(=O)(=O)c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45267257 199138 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203987 199138 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL564648 199138 None 0 Human Functional pEC50 = 8 8.0 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 449 12 4 4 3.8 O[C@@H](CNCCc1ccc(NC(=S)NCCc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
11605652 12559 None 0 Human Functional pEC50 = 8 8.0 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186715 12559 None 0 Human Functional pEC50 = 8 8.0 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475236 12559 None 0 Human Functional pEC50 = 8 8.0 501 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
59119455 112325 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
CHEMBL3290990 112325 None 0 Human Functional pEC50 = 8 8.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 408 10 5 6 3.5 COc1cccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)c1 10.1016/j.bmcl.2014.04.069
44392457 166052 None 0 Human Functional pEC50 = 8 8.0 -34 3
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL425161 166052 None 0 Human Functional pEC50 = 8 8.0 -34 3
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
10121328 4439 None 0 Human Functional pEC50 = 8 8.0 4 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101606 4439 None 0 Human Functional pEC50 = 8 8.0 4 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
73056757 104329 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099657 104329 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
10372836 102452 None 36 Human Functional pEC50 = 8.0 8.0 -1 3
GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.6019/CHEMBL5442687
CHEMBL3039518 102452 None 36 Human Functional pEC50 = 8.0 8.0 -1 3
GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in agonist mode with target: ADRB2
ChEMBL 739 13 6 9 6.4 COc1cc(NC(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)c(Cl)cc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.6019/CHEMBL5442687
11539348 203243 None 0 Human Functional pEC50 = 8.0 8.0 9 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600616 203243 None 0 Human Functional pEC50 = 8.0 8.0 9 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
6852397 60253 None 0 Human Functional pEC50 = 8.0 8.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
CHEMBL1735137 60253 None 0 Human Functional pEC50 = 8.0 8.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
CHEMBL1740818 60253 None 0 Human Functional pEC50 = 8.0 8.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 330 8 4 5 2.4 COc1ccc([C@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 nan
44441226 93721 None 0 Human Functional pEC50 = 7 7.0 -7 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL246908 93721 None 0 Human Functional pEC50 = 7 7.0 -7 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441231 148142 None 0 Human Functional pEC50 = 7 7.0 -50 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393470 148142 None 0 Human Functional pEC50 = 7 7.0 -50 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
57397010 70520 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946761 70520 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 515 11 4 5 5.3 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4c(Cl)cccc4Cl)cc3)c2s1 10.1016/j.bmcl.2011.10.049
11124502 119772 None 0 Human Functional pEC50 = 6 6.0 -630 2
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL347400 119772 None 0 Human Functional pEC50 = 6 6.0 -630 2
Activity against human beta 2 adrenergic receptor (AR), expressed in CHO cellsActivity against human beta 2 adrenergic receptor (AR), expressed in CHO cells
ChEMBL 551 13 4 7 3.3 C[C@H](CNc1cccc(CCS(=O)(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
11647543 138323 None 0 Human Functional pEC50 = 6 6.0 -3981 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL377028 138323 None 0 Human Functional pEC50 = 6 6.0 -3981 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
44428083 92613 None 0 Guinea pig Functional pEC50 = 6 6.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 6 6.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
127045854 139651 None 0 Human Functional pEC50 = 6 6.0 -3 2
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3797205 139651 None 0 Human Functional pEC50 = 6 6.0 -3 2
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 492 12 4 7 3.6 COc1cc(CCNC[C@@H](O)c2ccc(O)c3c2OCC(=O)N3)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
1499 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779.0 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 2091 None 34 Human Functional pEC50 = 6 6.0 -102 38
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
90644152 112315 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 503 11 5 6 3.1 O=C(Cc1ccccc1)NC1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290981 112315 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 503 11 5 6 3.1 O=C(Cc1ccccc1)NC1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
44331425 4446 None 0 Human Functional pEC50 = 6 6.0 -100 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
CHEMBL101630 4446 None 0 Human Functional pEC50 = 6 6.0 -100 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
11718543 165927 None 0 Human Functional pEC50 = 5 5.0 -251 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
CHEMBL424866 165927 None 0 Human Functional pEC50 = 5 5.0 -251 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)n1 10.1021/jm0509445
168277791 192952 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
CHEMBL5176681 192952 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
CHEMBL5221722 192952 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 368 6 3 4 3.0 COc1ccc(CNC(CO)c2cc(F)c(N)c(Br)c2)cc1 10.1021/acs.jmedchem.1c02006
168294241 193113 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5205567 193113 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5222734 193113 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 338 5 3 3 3.0 Nc1c(F)cc(C(CO)NCc2ccccc2)cc1Br 10.1021/acs.jmedchem.1c02006
2685 890 None 19 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
541 890 None 19 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
CHEMBL280822 890 None 19 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 494 11 4 8 2.3 OC(COc1ccc(cc1)c1nc(cn1C)C(F)(F)F)CNCCOc1ccc(c(c1)C(=O)N)O 10.1021/jm400348g
12578 936 None 44 Human Functional pEC50 = 5 5.0 -154 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
2755 936 None 44 Human Functional pEC50 = 5 5.0 -154 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
CHEMBL1374751 936 None 44 Human Functional pEC50 = 5 5.0 -154 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 219 4 3 4 1.2 CC(C)NCC(C1=CC(=C(C=C1)N)C#N)O 10.1021/jm400348g
5311116 2334 None 9 Human Functional pEC50 = 5 5.0 -4365 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 2334 None 9 Human Functional pEC50 = 5 5.0 -4365 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 2334 None 9 Human Functional pEC50 = 5 5.0 -4365 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
66653268 88285 None 0 Human Functional pEC50 = 5 5.0 -3311 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
CHEMBL2348201 88285 None 0 Human Functional pEC50 = 5 5.0 -3311 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 491 14 4 6 3.8 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1cccc(Cl)c1 10.1021/jm400348g
56598967 88295 None 0 Human Functional pEC50 = 5 5.0 -2238 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
CHEMBL2348211 88295 None 0 Human Functional pEC50 = 5 5.0 -2238 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 457 14 4 6 3.2 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccccc1 10.1021/jm400348g
56598833 88301 None 0 Human Functional pEC50 = 5 5.0 -436 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
CHEMBL2348217 88301 None 0 Human Functional pEC50 = 5 5.0 -436 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
56598832 88302 None 0 Human Functional pEC50 = 5 5.0 -4365 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 88302 None 0 Human Functional pEC50 = 5 5.0 -4365 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56597179 88303 None 0 Human Functional pEC50 = 5 5.0 -2754 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348219 88303 None 0 Human Functional pEC50 = 5 5.0 -2754 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 473 14 5 7 2.9 O=C(NCCNCC(O)COc1ccc(OCCOC2CCCC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
56598831 89177 None 0 Human Functional pEC50 = 5 5.0 -1023 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348220 89177 None 0 Human Functional pEC50 = 5 5.0 -1023 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2365796 89177 None 0 Human Functional pEC50 = 5 5.0 -1023 3
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 459 15 5 7 2.3 O=C(NCCNCC(O)COc1ccc(OCCOCC2CC2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
10028830 2246 None 31 Human Functional pEC50 = 5 5.0 -4897 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2022.114961
3932 2246 None 31 Human Functional pEC50 = 5 5.0 -4897 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2022.114961
CHEMBL4238084 2246 None 31 Human Functional pEC50 = 5 5.0 -4897 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2022.114961
172447878 195770 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 413 8 2 7 2.7 CC1(C)CC(=O)c2ccc(OC[C@@H](O)CNCCc3ccc4c(c3)OCO4)cc2O1 10.1016/j.ejmech.2022.114961
CHEMBL5410388 195770 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 413 8 2 7 2.7 CC1(C)CC(=O)c2ccc(OC[C@@H](O)CNCCc3ccc4c(c3)OCO4)cc2O1 10.1016/j.ejmech.2022.114961
172461665 196598 None 0 Human Functional pEC50 = 5 5.0 -134 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 366 7 2 6 2.4 O[C@@H](CNCC1COc2ccccc2O1)COc1cccc2cnccc12 10.1016/j.ejmech.2022.114961
CHEMBL5427527 196598 None 0 Human Functional pEC50 = 5 5.0 -134 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 366 7 2 6 2.4 O[C@@H](CNCC1COc2ccccc2O1)COc1cccc2cnccc12 10.1016/j.ejmech.2022.114961
90644151 112314 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 413 8 4 6 1.4 CC(=O)N1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290980 112314 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 413 8 4 6 1.4 CC(=O)N1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
73056758 104332 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
CHEMBL3099660 104332 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 331 8 4 5 2.8 CC[C@@H](Cc1ccc(OC)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2013.11.030
90666108 109394 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219038 109394 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)cc(F)c3O)CC2)ccc1O 10.1039/C1MD00140J
89108753 192988 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5186069 192988 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221958 192988 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 310 6 3 3 3.4 CCCCNC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
16735272 85846 None 0 Rat Functional pEC50 = 7.0 7.0 -57 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229614 85846 None 0 Rat Functional pEC50 = 7.0 7.0 -57 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
2952103 29323 None 8 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 376 3 0 5 3.9 CCOC(=O)N1CCN(c2nnc(-c3ccc(C)cc3)c3ccccc23)CC1 nan
CHEMBL1383120 29323 None 8 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 376 3 0 5 3.9 CCOC(=O)N1CCN(c2nnc(-c3ccc(C)cc3)c3ccccc23)CC1 nan
2945777 31755 None 9 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 8 1 9 4.0 COc1cc(OC)nc(NC(=O)CSc2nnc(-c3ccccc3)n2C2CCCCC2)n1 nan
CHEMBL1405897 31755 None 9 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 454 8 1 9 4.0 COc1cc(OC)nc(NC(=O)CSc2nnc(-c3ccccc3)n2C2CCCCC2)n1 nan
10745501 110612 None 0 Human Functional pEC50 = 5.0 5.0 -288 2
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
CHEMBL32521 110612 None 0 Human Functional pEC50 = 5.0 5.0 -288 2
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 562 13 5 8 2.4 CCCCN(CC(=O)O)C(=O)c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1021/jm000544b
659759 47285 None 9 Human Functional pEC50 = 7.0 7.0 14 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 47285 None 9 Human Functional pEC50 = 7.0 7.0 14 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
18559738 35317 None 8 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 0 6 4.3 COc1cc2ncc(S(=O)(=O)c3ccccc3)c(N3CCCC(C)C3)c2cc1OC nan
CHEMBL1436649 35317 None 8 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 426 5 0 6 4.3 COc1cc2ncc(S(=O)(=O)c3ccccc3)c(N3CCCC(C)C3)c2cc1OC nan
664890 40410 None 5 Human Functional pEC50 = 6.0 6.0 9 3
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 431 8 1 7 5.0 Cc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
CHEMBL1482007 40410 None 5 Human Functional pEC50 = 6.0 6.0 9 3
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 431 8 1 7 5.0 Cc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
25023951 177058 None 0 Golden hamster Functional pEC50 = 6.0 6.0 - 1
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL462274 177058 None 0 Golden hamster Functional pEC50 = 6.0 6.0 - 1
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 489 11 8 13 -0.8 Nc1cc(C(O)CNCCCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
3759952 22490 None 6 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
4017821 22490 None 6 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
CHEMBL1325241 22490 None 6 Human Functional pEC50 = 6.0 6.0 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 368 5 3 6 2.8 CCOC(=O)C1(C)C=C(Nc2ccc(O)cc2)C(=O)N1c1ccc(O)cc1 nan
4183 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
6918554 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
6918554.0 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
7455 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
CHEMBL1095777 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
DB05039 2025 None 43 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1021/jm100068m
44392480 64600 None 0 Human Functional pEC50 = 8.0 8.0 -1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181603 64600 None 0 Human Functional pEC50 = 8.0 8.0 -1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 471 12 4 6 4.1 CC/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
59548053 125352 None 0 Human Functional pEC50 = 8.0 8.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645355 125352 None 0 Human Functional pEC50 = 8.0 8.0 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.5 C[C@@H](Cc1cccc(CCC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
45484538 14102 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL1197779 14102 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL585382 14102 None 0 Human Functional pEC50 = 7.9 7.9 2 2
Agonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta2 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 556 13 6 7 1.9 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C[N+](C)(C)C)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
1287365 37827 None 6 Human Functional pEC50 = 7.9 7.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
CHEMBL1458579 37827 None 6 Human Functional pEC50 = 7.9 7.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 373 5 2 3 5.3 Cc1ccc(SCC(=O)Nc2ccc(-c3nc4ccccc4[nH]3)cc2)cc1 nan
46232857 203214 None 0 Human Functional pEC50 = 7.9 7.9 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600400 203214 None 0 Human Functional pEC50 = 7.9 7.9 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44428083 92613 None 0 Guinea pig Functional pEC50 = 7.0 7.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 7.0 7.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
44428085 93314 None 0 Guinea pig Functional pEC50 = 7.0 7.0 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
CHEMBL244906 93314 None 0 Guinea pig Functional pEC50 = 7.0 7.0 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
1155 1629 None 38 Human Functional pEC50 = 7.0 7.0 1 11
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
3343 1629 None 38 Human Functional pEC50 = 7.0 7.0 1 11
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
557 1629 None 38 Human Functional pEC50 = 7.0 7.0 1 11
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
CHEMBL32800 1629 None 38 Human Functional pEC50 = 7.0 7.0 1 11
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
DB01288 1629 None 38 Human Functional pEC50 = 7.0 7.0 1 11
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O nan
44428083 92613 None 0 Guinea pig Functional pEC50 = 6.0 6.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 6.0 6.0 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
24895263 194658 None 0 Human Functional pEC50 = 6.0 6.0 -31622 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
CHEMBL529659 194658 None 0 Human Functional pEC50 = 6.0 6.0 -31622 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 475 10 4 6 4.6 Nc1ccc([C@@H](O)CNCCc2ccc(-c3ccc(C(=O)O)c(OC4CCCCC4)c3)cc2)cn1 10.1021/jm8000345
44591508 179101 None 0 Human Functional pEC50 = 6.0 6.0 -31622 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
CHEMBL470857 179101 None 0 Human Functional pEC50 = 6.0 6.0 -31622 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 475 10 4 6 4.6 Nc1ccncc1[C@@H](O)CNCCc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1 10.1021/jm9000709
172462257 196705 None 0 Human Functional pEC50 = 7.0 7.0 2 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 459 10 2 5 5.0 CC1(C)CC(=O)c2ccc(OC[C@@H](O)CNCCC(c3ccccc3)c3ccccc3)cc2O1 10.1016/j.ejmech.2022.114961
CHEMBL5430355 196705 None 0 Human Functional pEC50 = 7.0 7.0 2 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 459 10 2 5 5.0 CC1(C)CC(=O)c2ccc(OC[C@@H](O)CNCCC(c3ccccc3)c3ccccc3)cc2O1 10.1016/j.ejmech.2022.114961
1542103 22491 None 20 Human Functional pEC50 = 5.9 5.9 -3 3
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
CHEMBL1325250 22491 None 20 Human Functional pEC50 = 5.9 5.9 -3 3
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 418 4 0 6 4.2 Cc1ccccc1N1CCN(c2ncnc3c2cnn3Cc2ccc(Cl)cc2)CC1 nan
46221604 8559 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094487 8559 None 0 Human Functional pEC50 = 6.9 6.9 -1 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 392 6 4 4 3.1 CCc1ccc(CC)c2c1CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44589133 175948 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
CHEMBL458541 175948 None 0 Human Functional pEC50 = 5.9 5.9 -1 3
Agonist activity at adrenergic beta-2 receptorAgonist activity at adrenergic beta-2 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
54586986 61834 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773263 61834 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 780 27 6 8 8.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)CCCCCCCCCCNC[C@H](O)c2ccc(O)c(NS(C)(=O)=O)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44610361 124055 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629357 124055 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 14 5 9 4.9 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc(C(O)(c6ccccc6)c6ccccc6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
2488220 28837 None 1 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 0 6 1.1 CN(CC(=O)N1CCN(c2ncccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
CHEMBL1379002 28837 None 1 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 409 5 0 6 1.1 CN(CC(=O)N1CCN(c2ncccn2)CC1)S(=O)(=O)c1ccc(Cl)cc1 nan
145986105 165465 None 0 Human Functional pEC50 = 6.9 6.9 -83 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4237453 165465 None 0 Human Functional pEC50 = 6.9 6.9 -83 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 429 10 4 4 4.0 O=C(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
168289963 193071 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5195910 193071 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222469 193071 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 334 8 3 4 2.2 CCOCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
2560512 24067 None 2 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 335 4 2 9 1.7 Nc1cc(N)nc(SCc2cc([N+](=O)[O-])cc3c2OCOC3)n1 nan
CHEMBL1338286 24067 None 2 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 335 4 2 9 1.7 Nc1cc(N)nc(SCc2cc([N+](=O)[O-])cc3c2OCOC3)n1 nan
1267856 45959 None 7 Human Functional pEC50 = 5.9 5.9 31 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
CHEMBL1532219 45959 None 7 Human Functional pEC50 = 5.9 5.9 31 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
5182299 24941 None 8 Human Functional pEC50 = 6.9 6.9 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
CHEMBL1345891 24941 None 8 Human Functional pEC50 = 6.9 6.9 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
9871800 56504 None 0 Human Functional pEC50 = 5.9 5.9 -120 3
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL163262 56504 None 0 Human Functional pEC50 = 5.9 5.9 -120 3
Agonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptorAgonistic activity was assessed by measurement of cAMP accumulation levels in CHO cells expressing human beta-2-adrenergic receptor
ChEMBL 534 9 5 9 2.0 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
44396509 67320 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL188315 67320 None 0 Human Functional pEC50 = 7.9 7.9 -6 2
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 513 11 4 6 5.1 CC(C)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
44331444 4271 None 0 Human Functional pEC50 = 7.9 7.9 2 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
CHEMBL100589 4271 None 0 Human Functional pEC50 = 7.9 7.9 2 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 709 13 5 8 4.2 CC(C)N(Cc1cc(F)ccc1F)C(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(02)00608-x
10221081 124167 None 1 Rat Functional pEC50 = 7.9 7.9 18 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 124167 None 1 Rat Functional pEC50 = 7.9 7.9 18 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
16222317 203338 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601429 203338 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 392 6 4 5 2.6 CC(C)(Cc1cc(F)cc(F)c1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
11189433 203340 None 0 Human Functional pEC50 = 7.9 7.9 57 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601430 203340 None 0 Human Functional pEC50 = 7.9 7.9 57 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 424 6 4 5 3.4 CC(C)(Cc1ccc(C(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
16735495 85820 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229401 85820 None 0 Human Functional pEC50 = 7.9 7.9 3 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
16049160 64112 None 0 Human Functional pEC50 = 7.9 7.9 10 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 491 15 5 8 3.3 CCOc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807825 64112 None 0 Human Functional pEC50 = 7.9 7.9 10 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 491 15 5 8 3.3 CCOc1ccc(CCNCCCSCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.05.097
90655869 111329 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 15 3 7 4.0 O=C(CCOCCc1cccc(Cl)c1)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)CCN1CCCCC1 10.1021/ml4005232
CHEMBL3265166 111329 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 574 15 3 7 4.0 O=C(CCOCCc1cccc(Cl)c1)N(CCNCCc1ccc(O)c2[nH]c(=O)sc12)CCN1CCCCC1 10.1021/ml4005232
145992462 167037 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(CO)NCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4287029 167037 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 352 8 4 4 2.9 O=c1ccc2c(C(CO)NCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
76315639 85351 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260987 85351 None 0 Human Functional pEC50 = 6.9 6.9 -1 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(C(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
127045855 139751 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3797876 139751 None 0 Human Functional pEC50 = 6.9 6.9 -2 3
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
44428086 150167 None 0 Guinea pig Functional pEC50 = 5.9 5.9 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Guinea pig Functional pEC50 = 5.9 5.9 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
44565932 187117 None 0 Human Functional pEC50 = 5.9 5.9 -15135 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL490733 187117 None 0 Human Functional pEC50 = 5.9 5.9 -15135 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 528 11 4 8 3.4 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10221081 124167 None 1 Rat Functional pEC50 = 5.9 5.9 18 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 124167 None 1 Rat Functional pEC50 = 5.9 5.9 18 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
44428083 92613 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Rat Functional pEC50 = 5.9 5.9 -4 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
162386697 184856 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Antagonist activity at ADRB2 (unknown origin)Antagonist activity at ADRB2 (unknown origin)
ChEMBL 390 3 0 6 2.3 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc3nncn3n2)CC1 10.1021/acs.jmedchem.1c01136
CHEMBL4850904 184856 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Antagonist activity at ADRB2 (unknown origin)Antagonist activity at ADRB2 (unknown origin)
ChEMBL 390 3 0 6 2.3 O=C(Cc1ccc(Cl)c(Cl)c1)N1CCN(c2ccc3nncn3n2)CC1 10.1021/acs.jmedchem.1c01136
580005 44342 None 5 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 319 4 0 6 3.5 c1ccc(CSc2nnnn2-c2cccc3ccccc23)nc1 nan
CHEMBL1517798 44342 None 5 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 319 4 0 6 3.5 c1ccc(CSc2nnnn2-c2cccc3ccccc23)nc1 nan
651592 45916 None 4 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 6 4.0 CN(C)c1ccc(-c2noc(C3CCN(S(=O)(=O)c4cccc(Cl)c4)CC3)n2)cc1 nan
CHEMBL1531826 45916 None 4 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 6 4.0 CN(C)c1ccc(-c2noc(C3CCN(S(=O)(=O)c4cccc(Cl)c4)CC3)n2)cc1 nan
57399439 70883 None 0 Guinea pig Functional pEC50 = 6.9 6.9 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951068 70883 None 0 Guinea pig Functional pEC50 = 6.9 6.9 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 538 13 4 8 3.4 COc1ccc(C2=NN(CCCCNC[C@@H](O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
53307431 63573 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 499 15 2 6 4.0 CCCCN(CCN(C)CCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
CHEMBL1800475 63573 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 499 15 2 6 4.0 CCCCN(CCN(C)CCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1016/j.bmcl.2011.04.135
9888047 93434 None 0 Human Functional pEC50 = 6.9 6.9 -501 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245673 93434 None 0 Human Functional pEC50 = 6.9 6.9 -501 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441227 148137 None 0 Human Functional pEC50 = 6.9 6.9 -7 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393469 148137 None 0 Human Functional pEC50 = 6.9 6.9 -7 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
929341 27040 None 5 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nc(Oc2ccc(Cl)cc2)n1 nan
CHEMBL1364979 27040 None 5 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nc(Oc2ccc(Cl)cc2)n1 nan
1025603 28451 None 7 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
CHEMBL1375364 28451 None 7 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 430 8 1 4 3.4 CN(Cc1ccccc1)S(=O)(=O)c1ccc(NS(=O)(=O)Cc2ccccc2)cc1 nan
9512 3636 None 34 Human Functional pEC50 = 5.9 5.9 -380 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
9887812 3636 None 34 Human Functional pEC50 = 5.9 5.9 -380 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
CHEMBL208427 3636 None 34 Human Functional pEC50 = 5.9 5.9 -380 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
DB06190 3636 None 34 Human Functional pEC50 = 5.9 5.9 -380 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 410 9 4 4 4.4 Clc1cccc(c1)[C@H](CNCCNc1cccc(c1)c1cccc(c1)C(=O)O)O 10.1021/jm0509445
90644148 112310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
CHEMBL3290977 112310 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 474 10 4 6 3.9 O=C(c1ccccc1)C1CCN(c2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)CC1 10.1016/j.bmcl.2014.04.069
16013947 21692 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
CHEMBL1318405 21692 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 442 6 1 8 1.9 CC(=O)Nc1ccc(S(=O)(=O)N2CCC(Oc3ccc(-n4cnnn4)cc3)CC2)cc1 nan
2475524 23533 None 3 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 4 0 5 4.4 CN(Cc1cccs1)c1nc(-c2cccnc2)nc2ccccc12 nan
CHEMBL1333885 23533 None 3 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 332 4 0 5 4.4 CN(Cc1cccs1)c1nc(-c2cccnc2)nc2ccccc12 nan
1499 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779.0 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2091 None 34 Human Functional pEC50 = 6.9 6.9 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulationAgonist activity at recombinant human beta2 adrenoceptor expressed in DU145 cells assessed as increase in cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
90666103 109390 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219033 109390 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cccc(O)c3)CC2)ccc1O 10.1039/C1MD00140J
24876564 61801 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773074 61801 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 668 20 5 7 7.5 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(CO)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
24791478 30601 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 420 8 1 7 2.7 COCCc1ncc(CN2CCC(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)cn1 nan
CHEMBL1393806 30601 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 420 8 1 7 2.7 COCCc1ncc(CN2CCC(C(=O)Nc3ccc(-n4cccn4)cc3)CC2)cn1 nan
76315638 85350 None 0 Human Functional pEC50 = 7.9 7.9 -23 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260986 85350 None 0 Human Functional pEC50 = 7.9 7.9 -23 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
6916441 99381 None 0 Human Functional pEC50 = 7.9 7.9 -158 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL282190 99381 None 0 Human Functional pEC50 = 7.9 7.9 -158 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 402 9 4 4 3.5 CC(Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
12582 950 None 27 Guinea pig Functional pEC50 = 7.9 7.9 1 7
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
2783 950 None 27 Guinea pig Functional pEC50 = 7.9 7.9 1 7
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
2783.0 950 None 27 Guinea pig Functional pEC50 = 7.9 7.9 1 7
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
CHEMBL49080 950 None 27 Guinea pig Functional pEC50 = 7.9 7.9 1 7
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
DB01407 950 None 27 Guinea pig Functional pEC50 = 7.9 7.9 1 7
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 276 3 3 3 3.0 CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)Cl)O 10.1021/jm801211c
9874175 58555 None 1 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
CHEMBL1683934 58555 None 1 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 640 16 5 7 7.0 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c3[nH]c(=O)ccc23)CC1 10.1039/C1MD00140J
90666123 109413 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
CHEMBL3219056 109413 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 752 16 6 10 6.1 CS(=O)(=O)Nc1cc([C@@H](O)CNCCc2ccc(OCCCN3CCC(OC(=O)Nc4ccccc4-c4ccc(O)c(Cl)c4)CC3)cc2)ccc1O 10.1039/C1MD00140J
54583100 61835 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773264 61835 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 731 21 5 8 7.4 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44554514 124054 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629356 124054 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 692 18 5 9 5.9 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)c5ccccc5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
5493324 98956 None 24 Human Functional pEC50 = 7.9 7.9 -416 3
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL279260 98956 None 24 Human Functional pEC50 = 7.9 7.9 -416 3
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
11785699 64861 None 0 Human Functional pEC50 = 7.9 7.9 -12 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182018 64861 None 0 Human Functional pEC50 = 7.9 7.9 -12 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 519 12 4 6 4.9 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC/C=C/c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44396798 169495 None 0 Human Functional pEC50 = 7.9 7.9 -27 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL442225 169495 None 0 Human Functional pEC50 = 7.9 7.9 -27 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 542 10 5 7 3.2 C[C@H](Cc1c[nH]c2c(S(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1016/j.bmcl.2004.09.054
1608445 24160 None 6 Human Functional pEC50 = 7.9 7.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 396 4 2 8 3.8 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCO)ncnc4c23)CO1 nan
CHEMBL1339094 24160 None 6 Human Functional pEC50 = 7.9 7.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 396 4 2 8 3.8 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCO)ncnc4c23)CO1 nan
45483846 199267 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL565685 199267 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 412 6 4 5 3.7 CC(C)(Cc1ccc(C(C)(C)C)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
44428083 92613 None 0 Guinea pig Functional pEC50 = 6.9 6.9 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 6.9 6.9 4 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
559926 97060 None 2 Guinea pig Functional pEC50 = 6.9 6.9 -27 2
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
CHEMBL266619 97060 None 2 Guinea pig Functional pEC50 = 6.9 6.9 -27 2
Agonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig tracheaAgonistic activity (beta2- adrenergic) for the percent maximal relaxation of isolated guinea pig trachea
ChEMBL 255 5 4 5 1.2 CC(C)(C)NCC(O)COc1ccc(O)c(O)c1 10.1021/jm00107a027
44428086 150167 None 0 Guinea pig Functional pEC50 = 5.9 5.9 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Guinea pig Functional pEC50 = 5.9 5.9 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
102335359 121612 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
CHEMBL3585932 121612 None 0 Rat Functional pEC50 = 5.9 5.9 - 1
Agonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to controlAgonist activity at beta2 adrenergic receptor in rat L6 cell lysate assessed as increase in intracellular 2-deoxyglucose uptake preincubated for 4 hrs followed by 2-deoxyglucose addition measured after 20 mins by fluorescence-based enzymatic assay relative to control
ChEMBL 433 5 7 9 -0.3 OC[C@H]1O[C@@H](Oc2ccc(C[C@@H]3NCCc4cc(O)c(O)cc43)cc2)[C@H](O)[C@@H](O)[C@@H]1O 10.1016/j.bmc.2017.10.011
9896817 102940 None 0 Human Functional pEC50 = 5.9 5.9 -44 3
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL305891 102940 None 0 Human Functional pEC50 = 5.9 5.9 -44 3
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)c2)cc1 10.1016/s0960-894x(00)00459-5
24180436 93270 None 0 Rat Functional pEC50 = 5.9 5.9 1 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 93270 None 0 Rat Functional pEC50 = 5.9 5.9 1 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
45483838 199388 None 0 Human Functional pEC50 = 6.9 6.9 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL566352 199388 None 0 Human Functional pEC50 = 6.9 6.9 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
659802 27162 None 9 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 7 2.4 CCCCCCN1C(=O)NC(=O)/C(=C\Nc2c(C)n(C)n(-c3ccccc3)c2=O)C1=O nan
CHEMBL1365995 27162 None 9 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 425 8 2 7 2.4 CCCCCCN1C(=O)NC(=O)/C(=C\Nc2c(C)n(C)n(-c3ccccc3)c2=O)C1=O nan
1267856 45959 None 7 Human Functional pEC50 = 5.9 5.9 31 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
CHEMBL1532219 45959 None 7 Human Functional pEC50 = 5.9 5.9 31 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 351 6 1 7 2.2 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccccc3)n2)cc1 nan
645398 50939 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 336 4 3 4 3.8 Cc1ccc(O)c(NC(=O)c2cccc(NC(=O)c3ccco3)c2)c1 nan
CHEMBL1577767 50939 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 336 4 3 4 3.8 Cc1ccc(O)c(NC(=O)c2cccc(NC(=O)c3ccco3)c2)c1 nan
24891819 55467 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
CHEMBL1406272 55467 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
CHEMBL1619809 55467 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 481 9 1 6 6.9 COc1ccc(CSc2ccc(-c3nc4ccccn4c3NCc3ccccc3)cc2OC)cc1 nan
53379897 63667 None 0 Rat Functional pEC50 = 6.9 6.9 -151 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800961 63667 None 0 Rat Functional pEC50 = 6.9 6.9 -151 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 337 6 4 4 3.5 C[C@H](Cc1ccc2ccccc2c1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
2231941 34215 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 11 1 9 3.4 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1cccc([N+](=O)[O-])c1 nan
CHEMBL1426242 34215 None 5 Human Functional pEC50 = 6.9 6.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 11 1 9 3.4 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1cccc([N+](=O)[O-])c1 nan
1599 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
3955 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
3955.0 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
7215 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
CHEMBL841 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
DB00836 2341 None 28 Human Functional pEC50 = 5.9 5.9 -1071 32
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.6019/CHEMBL5442687
1084214 45548 None 6 Human Functional pEC50 = 5.9 5.9 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
CHEMBL1528594 45548 None 6 Human Functional pEC50 = 5.9 5.9 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset2. (Class of assay: confirmatory)
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
70684522 76805 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76805 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
172446785 195127 None 0 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 389 11 2 3 4.8 CCc1ccccc1OC[C@@H](O)CNCCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2022.114961
CHEMBL5397120 195127 None 0 Human Functional pEC50 = 6.9 6.9 2 3
Agonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubationAgonist activity at human beta2-adrenergic receptor expressed in CHO-K1 cells co-expressing CRE-SPAP reporter gene assessed as CRE-SPAP production measured after 5 hrs incubation
ChEMBL 389 11 2 3 4.8 CCc1ccccc1OC[C@@H](O)CNCCC(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2022.114961
70684522 76805 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068577 76805 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 343 4 3 4 1.4 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(c1ccccc1)O2 10.1016/j.bmc.2011.11.054
1028 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
139148732 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
479 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
5816.0 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
CHEMBL679 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
DB00668 291 None 40 Human Functional pEC50 = 5.9 5.9 -7 19
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O nan
24794116 67111 None 1 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
CHEMBL1873201 67111 None 1 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 6 0 4 4.7 CSc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCC4)cc3)CC2)cc1 nan
54757772 66011 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP productionAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP production
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
CHEMBL1836647 66011 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP productionAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP production
ChEMBL 675 16 5 9 6.0 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Oc4nn(-c5c(O)cccc5F)c5c4CCCC5)CC3)ccc(O)c2[nH]1 10.1021/jm2007535
90666112 109400 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
CHEMBL3219044 109400 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 18 6 9 7.2 Cc1ccc(-c2ccc(O)c(Cl)c2)c(NC(=O)OC2CCN(CCCCCCCCCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)c1 10.1039/C1MD00140J
46221397 8705 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095778 8705 None 0 Human Functional pEC50 = 7.9 7.9 1 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 420 8 4 4 3.9 CCCc1cc2c(cc1CCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44609903 124057 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629359 124057 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc([C@](O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
10054373 58557 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
CHEMBL1683936 58557 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 603 17 5 7 6.6 O=C(Nc1ccccc1-c1ccccc1)OC1CCN(CCCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)CC1 10.1016/j.bmcl.2011.01.043
24180436 93270 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 93270 None 0 Rat Functional pEC50 = 7.9 7.9 1 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
46233013 203761 None 0 Human Functional pEC50 = 7.8 7.8 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
CHEMBL604125 203761 None 0 Human Functional pEC50 = 7.8 7.8 19 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 386 7 4 6 2.4 COc1cccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmcl.2009.12.087
3145649 39482 None 5 Human Functional pEC50 = 7.8 7.8 177 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
CHEMBL1472233 39482 None 5 Human Functional pEC50 = 7.8 7.8 177 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
3145570 47014 None 2 Human Functional pEC50 = 7.8 7.8 1 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
CHEMBL1541608 47014 None 2 Human Functional pEC50 = 7.8 7.8 1 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 397 4 0 5 3.5 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCOCC1 nan
127047221 140017 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
CHEMBL3799593 140017 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 319 8 4 6 1.8 COc1ccccc1OCCNC[C@@H](O)c1ccc(O)c(O)c1 10.1016/j.bmc.2016.04.028
10722793 113410 None 0 Human Functional pEC50 = 5.9 5.9 -114 3
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL331744 113410 None 0 Human Functional pEC50 = 5.9 5.9 -114 3
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 640 12 3 8 6.4 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(OC(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
2382050 36882 None 3 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 9 1 7 3.3 O=C(CCc1ccc(S(=O)(=O)N2CCOCC2)cc1)Nc1nc(COc2ccccc2)cs1 nan
CHEMBL1450612 36882 None 3 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 487 9 1 7 3.3 O=C(CCc1ccc(S(=O)(=O)N2CCOCC2)cc1)Nc1nc(COc2ccccc2)cs1 nan
24789191 39696 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 453 11 3 6 2.4 NC(=O)CC(NC(=O)c1ccccc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
CHEMBL1475105 39696 None 0 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 453 11 3 6 2.4 NC(=O)CC(NC(=O)c1ccccc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
44428083 92613 None 0 Rat Functional pEC50 = 4.9 4.9 -4 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Rat Functional pEC50 = 4.9 4.9 -4 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
2340194 34654 None 2 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 461 7 2 7 4.8 Cc1ccc(C(=O)OCC(=O)Nc2nc(-c3ccccc3)cs2)cc1NC(=O)c1ccco1 nan
CHEMBL1429919 34654 None 2 Human Functional pEC50 = 5.9 5.9 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 461 7 2 7 4.8 Cc1ccc(C(=O)OCC(=O)Nc2nc(-c3ccccc3)cs2)cc1NC(=O)c1ccco1 nan
145984324 165934 None 0 Human Functional pEC50 = 5.9 5.9 -25 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4248727 165934 None 0 Human Functional pEC50 = 5.9 5.9 -25 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 449 11 4 4 4.6 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=S)Nc2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
21977086 193075 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5200823 193075 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
CHEMBL5222486 193075 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 323 4 3 4 2.5 N#Cc1cc(C(CO)NC2CCCC2)cc(Br)c1N 10.1021/acs.jmedchem.1c02006
655617 30411 None 1 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 5 0 7 3.4 CC(=O)c1cccc(S(=O)(=O)N2CCCC(c3nc(-c4ccc(C)o4)no3)C2)c1 nan
CHEMBL1392252 30411 None 1 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 5 0 7 3.4 CC(=O)c1cccc(S(=O)(=O)N2CCCC(c3nc(-c4ccc(C)o4)no3)C2)c1 nan
168282645 192997 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5186002 192997 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222019 192997 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 386 6 3 3 4.6 CC(C)(Cc1ccccc1)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
11316919 3068 None 31 Human Functional pEC50 = 5.8 5.8 -2 8
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 451 4 0 4 5.3 Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F 10.6019/CHEMBL5442687
11693 3068 None 31 Human Functional pEC50 = 5.8 5.8 -2 8
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 451 4 0 4 5.3 Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F 10.6019/CHEMBL5442687
CHEMBL484929 3068 None 31 Human Functional pEC50 = 5.8 5.8 -2 8
GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2GPCR PRESTO-Tango dose-response in antagonist mode with target: ADRB2
ChEMBL 451 4 0 4 5.3 Clc1c(cccc1)n1nc2C(=O)N(CCOc2c1c1ccc(cc1)Cl)CC(C)(F)F 10.6019/CHEMBL5442687
123600 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600.0 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
123600.0 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
1575 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
9816 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
CHEMBL1002 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
DB13139 2314 None 0 Human Functional pEC50 = 6.8 6.8 1 3
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)[C@H](CNC(C)(C)C)O 10.1016/j.bmc.2011.11.054
4184788 25220 None 4 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 3 0 4 4.5 Cc1c(C(=O)N2CCc3ccccc3C2)oc2ccc(S(=O)(=O)N3CCCCCC3)cc12 nan
CHEMBL1348147 25220 None 4 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 452 3 0 4 4.5 Cc1c(C(=O)N2CCc3ccccc3C2)oc2ccc(S(=O)(=O)N3CCCCCC3)cc12 nan
1499 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
3779 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
3779.0 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
536 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
CHEMBL434 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
DB01064 2091 None 34 Human Functional pEC50 = 6.8 6.8 -102 38
Agonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assayAgonist activity at CLuc-tagged beta2 adrenergic receptor (unknown origin) expressed in HEK293 cells incubated for 10 mins by beta-arrestin 2 recruitment based firefly luciferase complementation assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/acs.jmedchem.3c02030
54583092 61816 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773198 61816 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 695 19 6 7 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(C[C@@H](C)NC[C@H](O)c3cc(O)cc(O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
1028 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816.0 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 291 None 40 Guinea pig Functional pEC50 = 7.8 7.8 -4 19
Effective dose for relaxation of guinea pig trachea.Effective dose for relaxation of guinea pig trachea.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
11625493 203168 None 1 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL600007 203168 None 1 Human Functional pEC50 = 7.8 7.8 12 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
1094286 50852 None 12 Human Functional pEC50 = 7.8 7.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
CHEMBL1577023 50852 None 12 Human Functional pEC50 = 7.8 7.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 5 1 5 4.2 Cc1ccc(OCC(=O)Nc2ccc(-c3nc4ncccc4o3)cc2)cc1 nan
319 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
321 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
444031 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
444031.0 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
784 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
CHEMBL1346 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
DB00496 1324 None 32 Human Functional pEC50 = 7.8 7.8 -2 18
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2011.05.097
90655865 111325 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 514 16 3 7 2.9 CN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
CHEMBL3265162 111325 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 514 16 3 7 2.9 CN(C)CCCN(CCNCCc1ccc(O)c2[nH]c(=O)sc12)C(=O)CCOCCc1ccccc1 10.1021/ml4005232
4183 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
6918554 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
6918554.0 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
7455 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
CHEMBL1095777 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
DB05039 2025 None 43 Human Functional pEC50 = 7.8 7.8 -1 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 392 6 4 4 3.1 CCc1cc2CC(Cc2cc1CC)NC[C@@H](c1ccc(c2c1ccc(=O)[nH]2)O)O 10.1016/j.bmcl.2011.10.049
24900874 70407 None 0 Human Functional pEC50 = 7.8 7.8 8 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
CHEMBL1945293 70407 None 0 Human Functional pEC50 = 7.8 7.8 8 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 417 11 5 7 1.9 COCCNCc1ccc(CCNC[C@H](O)c2ccc(O)c3[nH]c(=O)sc23)cc1 10.1016/j.bmcl.2011.10.049
44312924 164921 None 0 Human Functional pEC50 = 5.8 5.8 -39 3
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL421871 164921 None 0 Human Functional pEC50 = 5.8 5.8 -39 3
Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-2 adrenergic receptor (AR)
ChEMBL 421 6 3 6 4.2 COc1cc(-c2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
10651147 110746 None 0 Human Functional pEC50 = 5.8 5.8 -380 3
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32599 110746 None 0 Human Functional pEC50 = 5.8 5.8 -380 3
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 596 12 6 8 2.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
3986625 43199 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
CHEMBL1505690 43199 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
5307895 50142 None 5 Human Functional pEC50 = 5.8 5.8 9 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
CHEMBL1570251 50142 None 5 Human Functional pEC50 = 5.8 5.8 9 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 441 8 1 8 2.9 COc1ccc(OC)c(CCNC(=O)C2CCN(c3nnc(-n4cccc4)s3)CC2)c1 nan
168273723 192916 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5178340 192916 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221450 192916 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 6 3 3 2.6 CCCCNC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
1104203 44886 None 9 Human Functional pEC50 = 6.8 6.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
CHEMBL1522618 44886 None 9 Human Functional pEC50 = 6.8 6.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 350 4 1 7 3.6 O=C(Nc1ccc(-c2nc3ncccc3o2)cc1)c1ccc([N+](=O)[O-])o1 nan
1266768 34031 None 7 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
CHEMBL1424678 34031 None 7 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 365 6 1 7 2.5 CCOC(=O)c1ccc(NC(=O)Cn2nnc(-c3ccc(C)cc3)n2)cc1 nan
3301343 59762 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 4 2 9 2.3 CC1(C)Cc2c(c(N3CCOCC3)nc3sc4c(NCCN)ncnc4c23)CO1 nan
CHEMBL1724644 59762 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 414 4 2 9 2.3 CC1(C)Cc2c(c(N3CCOCC3)nc3sc4c(NCCN)ncnc4c23)CO1 nan
44441229 93802 None 0 Human Functional pEC50 = 6.8 6.8 -199 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247315 93802 None 0 Human Functional pEC50 = 6.8 6.8 -199 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2nc(C(=O)O)cs2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
57395241 70522 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946763 70522 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 448 11 4 6 3.4 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CNCCc4ccccn4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
57391792 70523 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1946764 70523 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 523 10 3 6 5.0 O=c1[nH]c2c(O)ccc(CCNCCc3ccc(CN4CC[C@@H](Oc5ccc(Cl)cc5)C4)cc3)c2s1 10.1016/j.bmcl.2011.10.049
90644144 112306 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 442 10 5 5 4.5 OCc1cc(C(O)CNCCc2ccc(NCc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290973 112306 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 442 10 5 5 4.5 OCc1cc(C(O)CNCCc2ccc(NCc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
11495581 77351 None 0 Human Functional pEC50 = 5.8 5.8 -50 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL208328 77351 None 0 Human Functional pEC50 = 5.8 5.8 -50 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 425 9 4 5 4.2 C[C@H](CNc1cccc(-c2ncccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
11546349 141420 None 0 Human Functional pEC50 = 5.8 5.8 -50 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
CHEMBL383511 141420 None 0 Human Functional pEC50 = 5.8 5.8 -50 3
Activity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-2 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 4 4 4.8 C[C@H](CNc1cccc(-c2ccc(C(=O)O)cc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0509445
90644143 112305 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 5 5 4.7 OCc1cc(C(O)CNCCc2ccc(NCc3ccc(Cl)c(Cl)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290972 112305 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 460 10 5 5 4.7 OCc1cc(C(O)CNCCc2ccc(NCc3ccc(Cl)c(Cl)c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644147 112309 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 488 12 4 5 5.0 OCc1cc(C(O)CNCCc2ccc(N3CCC(CCCc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290976 112309 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 488 12 4 5 5.0 OCc1cc(C(O)CNCCc2ccc(N3CCC(CCCc4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
145984042 165770 None 0 Human Functional pEC50 = 4.8 4.8 -3467 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4244929 165770 None 0 Human Functional pEC50 = 4.8 4.8 -3467 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 475 13 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Cc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
53380558 63669 None 2 Rat Functional pEC50 = 7.8 7.8 -4 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
CHEMBL1800963 63669 None 2 Rat Functional pEC50 = 7.8 7.8 -4 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 367 7 4 5 3.5 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)c2ccccc12 10.1016/j.bmc.2009.11.062
44392519 123859 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL362293 123859 None 0 Human Functional pEC50 = 7.8 7.8 -1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 493 11 4 6 4.4 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NCc2ccccc2)c1 10.1016/j.bmcl.2004.12.033
56663519 63666 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800960 63666 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
44392558 65276 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL182770 65276 None 0 Human Functional pEC50 = 6.8 6.8 -2 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
24817062 28786 None 5 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
CHEMBL1378531 28786 None 5 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 3 4.1 O=C(c1ccc(OC2CCN(Cc3ccc(F)cc3)CC2)cc1)N1CCCC1 nan
2307884 67398 None 3 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 347 3 0 2 4.7 O=C(COc1ccccc1F)N1c2ccccc2CCc2ccccc21 nan
CHEMBL1886907 67398 None 3 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 347 3 0 2 4.7 O=C(COc1ccccc1F)N1c2ccccc2CCc2ccccc21 nan
44428083 92613 None 0 Rat Functional pEC50 = 4.8 4.8 -4 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Rat Functional pEC50 = 4.8 4.8 -4 2
Vasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneVasodilating activity against phenylephrine-induced contraction in rat thoracic aorta in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
1292336 32283 None 6 Human Functional pEC50 = 6.8 6.8 9 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 8 1 6 5.1 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4ccco4)cc3)no2)cc1 nan
CHEMBL1410048 32283 None 6 Human Functional pEC50 = 6.8 6.8 9 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 8 1 6 5.1 CCCc1ccc(OCc2nc(-c3ccc(NC(=O)c4ccco4)cc3)no2)cc1 nan
1084214 45548 None 6 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
CHEMBL1528594 45548 None 6 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 432 8 1 6 2.7 CCOC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCC3)cc2)cc1 nan
16832456 51325 None 10 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 402 7 2 6 2.7 CC(=O)Nc1ccc(S(=O)(=O)NCCc2csc(-c3cccnc3)n2)cc1 nan
CHEMBL1581044 51325 None 10 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 402 7 2 6 2.7 CC(=O)Nc1ccc(S(=O)(=O)NCCc2csc(-c3cccnc3)n2)cc1 nan
168276741 192941 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5180409 192941 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
CHEMBL5221644 192941 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 330 4 3 3 3.1 Nc1c(F)cc(C(CO)NC2CCCCC2)cc1Br 10.1021/acs.jmedchem.1c02006
70686652 76804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
70686652 76804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
CHEMBL2068576 76804 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 283 3 4 5 -0.1 CC(C)(C)NC[C@H](O)c1ccc2c(c1)C[OH+][B-](O)(O)O2 10.1016/j.bmc.2011.11.054
6407382 45191 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
CHEMBL1525540 45191 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
2953239 31250 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
CHEMBL1401186 31250 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
2233849 33360 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
CHEMBL1419122 33360 None 5 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 10 1 7 4.1 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Cl)cc1 nan
24180436 93270 None 0 Guinea pig Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 93270 None 0 Guinea pig Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
90666119 109409 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219052 109409 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 728 19 6 9 6.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C[C@H]3C[C@@]3(COC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
54580128 61814 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773196 61814 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 723 20 6 7 7.2 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(CO)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44392457 166052 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL425161 166052 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
44428081 93187 None 0 Guinea pig Functional pEC50 = 6.8 6.8 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244321 93187 None 0 Guinea pig Functional pEC50 = 6.8 6.8 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 428 10 5 9 1.4 CC(Cc1ccc(OCc2nonc2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
45483831 199470 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 343 8 4 4 3.1 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL566992 199470 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 343 8 4 4 3.1 CCc1ccc(CC(C)(C)NCC(O)c2ccc(O)c(CO)c2)cc1 10.1016/j.bmcl.2009.10.013
443372 10236 None 19 Guinea pig Functional pEC50 = 5.8 5.8 -8 9
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1160723 10236 None 19 Guinea pig Functional pEC50 = 5.8 5.8 -8 9
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL2062275 10236 None 19 Guinea pig Functional pEC50 = 5.8 5.8 -8 9
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
1271047 44370 None 10 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 5 1 1 4.7 O=C(Nc1ccccc1)c1ccccc1CCc1ccccc1 nan
CHEMBL1518070 44370 None 10 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 301 5 1 1 4.7 O=C(Nc1ccccc1)c1ccccc1CCc1ccccc1 nan
664105 29788 None 5 Human Functional pEC50 = 5.8 5.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
CHEMBL1387056 29788 None 5 Human Functional pEC50 = 5.8 5.8 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 468 4 1 9 2.8 CC1(C)Cc2c(c(N3CCCC3)nc3sc4c(N5CCN(CCO)CC5)ncnc4c23)CO1 nan
54580133 61836 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773265 61836 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 654 19 5 7 7.7 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c(O)c3)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
6404528 44808 None 20 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nnc1Oc1ccccc1Cl nan
CHEMBL1521880 44808 None 20 Human Functional pEC50 = 6.8 6.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 307 3 0 4 4.5 N#Cc1cc(-c2ccccc2)nnc1Oc1ccccc1Cl nan
1231538 27526 None 29 Human Functional pEC50 = 5.8 5.8 1 3
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 523 6 1 6 6.0 O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1 nan
CHEMBL1368962 27526 None 29 Human Functional pEC50 = 5.8 5.8 1 3
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 523 6 1 6 6.0 O=C(Nc1ccc2nc(SCc3ccc(Cl)cc3)sc2c1)c1ccccc1C(=O)N1CCOCC1 nan
135799875 186526 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4876155 186526 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 276 3 4 4 1.7 CC(C)(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
24791840 59829 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
CHEMBL1727257 59829 None 2 Human Functional pEC50 = 5.8 5.8 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
25023953 187489 None 0 Golden hamster Functional pEC50 = 6.8 6.8 - 1
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
CHEMBL493489 187489 None 0 Golden hamster Functional pEC50 = 6.8 6.8 - 1
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 577 17 8 15 -1.5 O=CNc1cc(C(O)CNCCOCCOCCNc2ncnc3c2ncn3[C@@H]2O[C@H](CO)[C@@H](O)[C@H]2O)ccc1O 10.1021/jm800613s
1155 1629 None 38 Guinea pig Functional pEC50 = 7.8 7.8 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
3343 1629 None 38 Guinea pig Functional pEC50 = 7.8 7.8 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
557 1629 None 38 Guinea pig Functional pEC50 = 7.8 7.8 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
CHEMBL32800 1629 None 38 Guinea pig Functional pEC50 = 7.8 7.8 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
DB01288 1629 None 38 Guinea pig Functional pEC50 = 7.8 7.8 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
24180436 93270 None 0 Guinea pig Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 93270 None 0 Guinea pig Functional pEC50 = 7.8 7.8 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
46221603 8558 None 0 Human Functional pEC50 = 7.8 7.8 -7 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1094486 8558 None 0 Human Functional pEC50 = 7.8 7.8 -7 2
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 396 6 4 6 2.0 COc1cc2c(cc1OC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
44392577 122608 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL360133 122608 None 0 Human Functional pEC50 = 7.8 7.8 -2 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 455 10 4 6 3.2 CC#CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
11432806 66218 None 0 Human Functional pEC50 = 7.8 7.8 -134 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
11432806 66218 None 0 Human Functional pEC50 = 7.8 7.8 -134 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL184407 66218 None 0 Human Functional pEC50 = 7.8 7.8 -134 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.09.054
CHEMBL184407 66218 None 0 Human Functional pEC50 = 7.8 7.8 -134 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44396568 67307 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL188196 67307 None 0 Human Functional pEC50 = 6.8 6.8 -34 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
9873257 84979 None 14 Human Functional pEC50 = 5.8 5.8 -47 3
Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 84979 None 14 Human Functional pEC50 = 5.8 5.8 -47 3
Agonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-2 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
11758172 100988 None 0 Human Functional pEC50 = 5.8 5.8 -147 3
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
CHEMBL293994 100988 None 0 Human Functional pEC50 = 5.8 5.8 -147 3
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 592 11 3 7 5.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(F)c(F)c3)cs2)cc1 10.1021/jm000286i
44428086 150167 None 0 Rat Functional pEC50 = 4.8 4.8 -7 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Rat Functional pEC50 = 4.8 4.8 -7 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
2005835 22577 None 5 Human Functional pEC50 = 5.7 5.7 6 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 459 5 1 9 5.2 CSc1nc(SCCO)c2sc3nc(-c4ccco4)c4c(c3c2n1)CC(C)(C)OC4 nan
CHEMBL1326167 22577 None 5 Human Functional pEC50 = 5.7 5.7 6 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 459 5 1 9 5.2 CSc1nc(SCCO)c2sc3nc(-c4ccco4)c4c(c3c2n1)CC(C)(C)OC4 nan
24791840 59829 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
CHEMBL1727257 59829 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 406 6 0 3 4.9 CCc1ccc(CN2CCC(Oc3ccc(C(=O)N4CCCCC4)cc3)CC2)cc1 nan
12988999 192913 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5176025 192913 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221441 192913 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 354 3 3 3 3.5 CC(C)(C)NC(CO)c1cc(Br)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.1c02006
16735257 85765 None 0 Rat Functional pEC50 = 6.7 6.7 -812 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228992 85765 None 0 Rat Functional pEC50 = 6.7 6.7 -812 2
Agonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode arrayAgonist activity beta2-adrenergic receptor in rat ventricular myocytes assessed as cell contraction following electrical stimulation by optical edge tracking method using photodiode array
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
76319327 85360 None 0 Human Functional pEC50 = 7.7 7.7 -14 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL2261203 85360 None 0 Human Functional pEC50 = 7.7 7.7 -14 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 584 14 4 7 4.5 CCN(CC)C(=O)COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
1155 1629 None 38 Guinea pig Functional pEC50 = 7.7 7.7 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
3343 1629 None 38 Guinea pig Functional pEC50 = 7.7 7.7 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
557 1629 None 38 Guinea pig Functional pEC50 = 7.7 7.7 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
CHEMBL32800 1629 None 38 Guinea pig Functional pEC50 = 7.7 7.7 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
DB01288 1629 None 38 Guinea pig Functional pEC50 = 7.7 7.7 -3 11
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1021/jm0704595
9992825 84405 None 9 Guinea pig Functional pEC50 = 7.7 7.7 85 2
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
CHEMBL2218907 84405 None 9 Guinea pig Functional pEC50 = 7.7 7.7 85 2
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as relaxation of carbachol-induced tissue contraction
ChEMBL 261 2 3 4 1.1 CC(C)NC1CCn2c(=O)[nH]c3cccc(c32)C1O 10.1021/jm801211c
44396568 67307 None 0 Human Functional pEC50 = 7.7 7.7 -34 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 67307 None 0 Human Functional pEC50 = 7.7 7.7 -34 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
44392552 64547 None 0 Human Functional pEC50 = 7.7 7.7 -35 3
Effective concentration against human beta-2 adrenergic receptorEffective concentration against human beta-2 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181440 64547 None 0 Human Functional pEC50 = 7.7 7.7 -35 3
Effective concentration against human beta-2 adrenergic receptorEffective concentration against human beta-2 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
2977891 21810 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
CHEMBL1319376 21810 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 452 5 0 5 1.8 CN(CC(=O)N1CCN(c2ccccn2)CC1)S(=O)(=O)c1ccc(Br)cc1 nan
168278795 192962 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5183062 192962 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5221779 192962 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 304 3 3 3 2.6 CC(C)(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
10863093 50341 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL157210 50341 None 0 Human Functional pEC50 = 7.7 7.7 -3 3
Ability to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-2 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
57401200 70880 None 0 Guinea pig Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 510 11 4 8 2.7 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951065 70880 None 0 Guinea pig Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 510 11 4 8 2.7 COc1ccc(C2=NN(CCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
57401202 70884 None 0 Guinea pig Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 552 14 4 8 3.8 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
CHEMBL1951069 70884 None 0 Guinea pig Functional pEC50 = 7.7 7.7 - 1
Agonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contractionAgonist activity at beta2 adrenoceptor in guinea pig assessed as relaxation of histamine-induced tracheal ring contraction
ChEMBL 552 14 4 8 3.8 COc1ccc(C2=NN(CCCCCNCC(O)c3ccc(O)c(NC=O)c3)C(=O)C3CCCCC23)cc1OC 10.1016/j.bmcl.2012.01.013
145987938 167156 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
CHEMBL4289233 167156 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 4 5 2.1 COc1ccc(CCNC(CO)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.ejmech.2018.04.041
76329060 106492 None 0 Human Functional pEC50 = 7.7 7.7 199 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3126381 106492 None 0 Human Functional pEC50 = 7.7 7.7 199 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
CHEMBL3139685 106492 None 0 Human Functional pEC50 = 7.7 7.7 199 3
Agonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta2 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 493 17 4 7 3.5 CS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm401532g
90644153 112316 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290982 112316 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 470 11 5 6 5.3 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(Oc4ccccc4)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
1369799 44479 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
CHEMBL1519042 44479 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 401 5 1 5 5.2 CC(C)(C)c1ccc(OCC(=O)Nc2ccc(-c3nc4cccnc4o3)cc2)cc1 nan
135799865 186696 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
CHEMBL4878555 186696 None 0 Human Functional pEC50 = 4.7 4.7 - 1
Agonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assayAgonist activity at beta2 adrenoceptor in HEK293 cells co-expressing V2 receptor assessed as increase in cAMP accumulation measured after 30 mins by HTRF assay
ChEMBL 262 4 4 4 1.3 CC(C)NC(CO)c1ccc(O)c2[nH]c(=O)ccc12 10.1021/acs.jmedchem.0c01195
24819471 30286 None 0 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 9 0 6 3.9 CC(=O)c1ccc(OCc2cc(C(=O)N(C)CCOc3ccc(C)cc3)no2)cc1 nan
CHEMBL1391134 30286 None 0 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 408 9 0 6 3.9 CC(=O)c1ccc(OCc2cc(C(=O)N(C)CCOc3ccc(C)cc3)no2)cc1 nan
90666117 109407 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219050 109407 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 744 20 6 9 7.6 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
24817788 33493 None 1 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 7 3.2 Cc1ccc(OCc2cc(C(=O)NCc3cnn(-c4cccc(F)c4)c3)no2)cn1 nan
CHEMBL1420188 33493 None 1 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 407 7 1 7 3.2 Cc1ccc(OCc2cc(C(=O)NCc3cnn(-c4cccc(F)c4)c3)no2)cn1 nan
1073012 33730 None 22 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
CHEMBL1422244 33730 None 22 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 403 5 0 5 1.3 CCOC(=O)N1CCN(C(=O)CN(C)S(=O)(=O)c2ccc(Cl)cc2)CC1 nan
105 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
2083 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
2083.0 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
558 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
CHEMBL714 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
DB01001 3461 None 54 Human Functional pEC50 = 6.7 6.7 -13 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hrAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as intracellular cAMP accumulation after 1 hr
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.04.135
90644149 112311 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290978 112311 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 447 9 4 6 3.1 OCc1cc(C(O)CNCCc2ccc(N3CCN(c4ccccc4)CC3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644154 112319 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290985 112319 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3cccc4ccccc34)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644140 112329 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290994 112329 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 394 9 6 6 3.2 OCc1cc(C(O)CNCCc2ccc(Nc3ccc(O)cc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
1499 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
3779 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
3779.0 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
536 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
CHEMBL434 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
DB01064 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
16736091 85766 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
CHEMBL228996 85766 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2009.11.062
16736091 85766 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL228996 85766 None 0 Human Functional pEC50 = 8.7 8.7 251 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 317 7 4 5 2.4 COc1ccc(C[C@H](C)NC[C@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
1499 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
3779 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
3779.0 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
536 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
CHEMBL434 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
DB01064 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
1499 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
3779 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
3779.0 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
536 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
CHEMBL434 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
DB01064 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
1499 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
3779 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
3779.0 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
536 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
CHEMBL434 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
DB01064 2091 None 34 Human Functional pEC50 = 8.7 8.7 -102 38
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-2 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
2953239 31250 None 5 Human Functional pEC50 = 8.7 8.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
CHEMBL1401186 31250 None 5 Human Functional pEC50 = 8.7 8.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 5 0 5 1.4 Cc1ccc(S(=O)(=O)N(C)CC(=O)N2CCN(c3ccccn3)CC2)cc1 nan
68057795 125270 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645276 125270 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 804 17 6 10 6.0 COc1cc(NC(=O)CCCN(C)C(=O)CCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1CNC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548077 125314 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645319 125314 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 880 17 6 10 7.4 COc1ccc(CC(=O)Nc2cccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)c2)cc1CC(C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548088 125334 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
CHEMBL3645338 125334 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2cccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)c2)cc1 nan
59548072 125335 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
CHEMBL3645339 125335 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 836 16 6 9 6.6 CN(C(=O)CCN1CCC(OC(=O)Nc2ccccc2-c2ccccc2)CC1)c1ccc(CNC(=O)Cc2ccc(CNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 nan
59548116 125344 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645347 125344 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 894 18 6 10 7.1 COc1ccc(CC(=O)NCc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)cc1C[C@H](C)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
59548085 125346 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
CHEMBL3645349 125346 None 0 Human Functional pEC50 = 8.7 8.7 - 1
cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).cAMP Assay: cAMP assays were performed in a radioimmunoassay format using the Flashplate Adenylyl Cyclase Activation Assay System with [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences Inc., Boston, Mass.), according to the manufacturers instructions. For this assay, HEK-293 cell lines stably expressing cloned human β1 or β2 receptors were grown to near confluency in DMEM supplemented with 10% FBS and Geneticin (500 μg/mL); or CHO-K1 cell lines stably expressing cloned human β3 adrenergic receptors were grown to near confluency in Hams F-12 media supplemented with 10% FBS and Geneticin (250 μg/mL). Cells were rinsed with PBS and detached in dPBS (Dulbecco's Phosphate Buffered Saline, without CaCl2 and MgCl2) containing 2 mM EDTA or Trypsin-EDTA solution (0.05% trypsin/0.53 mM EDTA). After counting cells in Coulter cell counter, cells were pelleted by centrifugation at 1,000 rpm and re-suspended in stimulation buffer containing TBMX (PerkinElmer Kit) pre-warmed to room temperature to a concentration of 1.6×106 to 2.8×106 cells/mL. About 40,000 to 80,000 cells per well were used in this assay. Test compounds (10 mM in DMSO) were diluted into PBS containing 0.1% BSA in Beckman Biomek-2000 and tested at 11 different concentrations ranging from 100 μM to 1 pM. Reactions were incubated for 10 min at 37° C. and stopped by adding 100 μL of cold detection buffer containing [125I]-cAMP (NEN SMP004, PerkinElmer Life Sciences, Boston, Mass.).
ChEMBL 878 18 6 9 7.1 CC(Cc1cccc(CCNC(=O)Cc2ccc(N(C)C(=O)CCN3CCC(OC(=O)Nc4ccccc4-c4ccccc4)CC3)cc2)c1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 nan
319 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
321 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
444031 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
444031.0 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
784 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
CHEMBL1346 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
DB00496 1324 None 32 Human Functional pEC50 = 8.7 8.7 -2 18
Agonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assayAgonist activity at beta2-adrenoceptor in human bronchial smooth-muscle cell by cAMP assay
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2012.07.096
45269924 197904 None 0 Guinea pig Functional pEC50 = 8.7 8.7 - 1
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
CHEMBL552398 197904 None 0 Guinea pig Functional pEC50 = 8.7 8.7 - 1
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 283 6 5 6 -0.1 CC(C)(C)NC[C@@H](O)c1ccc(OB(O)O)c(CO)c1 10.1016/j.ejmech.2008.12.016
54580129 61815 None 0 Guinea pig Functional pEC50 = 8.7 8.7 3 2
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773197 61815 None 0 Guinea pig Functional pEC50 = 8.7 8.7 3 2
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as bronchorelaxation activity against histamine-induced contraction
ChEMBL 786 21 6 8 7.0 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCNC(=O)Cc2cccc(CC(C)(C)NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)c2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
44392534 65259 None 0 Human Functional pEC50 = 8.7 8.7 1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182689 65259 None 0 Human Functional pEC50 = 8.7 8.7 1 2
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-2 adrenergic receptor
ChEMBL 443 11 4 6 3.4 C=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
156014385 178455 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4636080 178455 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
CHEMBL4651252 178455 None 0 Human Functional pEC50 = 8.7 8.7 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 356 7 4 5 2.3 Cc1ccc(CCCNCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmc.2019.115178
156015552 178399 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4641339 178399 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
CHEMBL4650961 178399 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta2 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 328 6 4 5 1.6 O=C1COc2c(cc(O)cc2C(O)CNCCc2ccccc2)N1 10.1016/j.bmc.2019.115178
44419254 83176 None 0 Human Functional pEC50 = 8.6 8.6 4 2
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
CHEMBL218210 83176 None 0 Human Functional pEC50 = 8.6 8.6 4 2
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levelsAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP levels
ChEMBL 587 14 4 8 4.5 CC(C)(Cc1ccc(Oc2ccc(C(N)=O)cn2)cc1)NC[C@H](O)COc1cccc2[nH]c(=O)n(CCC3CCCC3)c12 10.1016/j.bmcl.2006.08.010
53239456 61838 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
CHEMBL1773267 61838 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assayAgonist activity at human beta2 adrenergic receptor expressed in CHO cells assessed as stimulation of intracellular cAMP production after 30 mins of washing by wash-off assay
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2010.10.132
53239456 61838 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
CHEMBL1773267 61838 None 0 Human Functional pEC50 = 8.6 8.6 1 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 705 19 5 7 7.8 CC(C)N(CC[C@H](c1ccccc1)c1cc(CCCCOc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)ccc1O)C(C)C 10.1016/j.bmcl.2015.10.008
46232768 202090 None 0 Human Functional pEC50 = 8.6 8.6 14 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL592879 202090 None 0 Human Functional pEC50 = 8.6 8.6 14 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
56658244 66429 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 66429 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 66429 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -1 4
Agonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contractionAgonist activity at adrenergic beta2 receptor in guinea pig trachea assessed as inhibition of electrically-stimulated contraction
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
10238776 66497 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -3 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1835853 66497 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -3 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
CHEMBL1852214 66497 None 0 Guinea pig Functional pEC50 = 8.6 8.6 -3 4
Agonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile responseAgonist activity at beta2 adrenergic receptor in guinea pig tracheal strip assessed as inhibition of electrically-induced bronchocontractile response
ChEMBL 473 17 6 6 3.6 NC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.08.043
56675509 64517 None 0 Human Functional pEC50 = 8.6 8.6 79 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814270 64517 None 0 Human Functional pEC50 = 8.6 8.6 79 3
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
56658244 66429 None 0 Human Functional pEC50 = 8.6 8.6 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 66429 None 0 Human Functional pEC50 = 8.6 8.6 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 66429 None 0 Human Functional pEC50 = 8.6 8.6 1 4
Agonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
56670092 64125 None 0 Human Functional pEC50 = 8.6 8.6 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807874 64125 None 0 Human Functional pEC50 = 8.6 8.6 112 3
Agonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 minsAgonist activity at human adrenergic beta2 receptor expressed in H292 cells assessed as stimulation of cAMP accumulation after 60 mins
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
1239 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
3410 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
3410.0 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
3465 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
DB00983 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assayAgonist activity at human beta-2 adrenergic receptor expressed in human H292 cells assessed as accumulation of intracellular cAMP after 1 hr by AlphaScreen assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/ml4005232
145987415 167344 None 0 Human Functional pEC50 = 8.6 8.6 1258 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3cccc(Cl)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4292648 167344 None 0 Human Functional pEC50 = 8.6 8.6 1258 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3cccc(Cl)c3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
155540608 173041 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
CHEMBL4516838 173041 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
1239 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410.0 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
90645345 112542 None 0 Human Functional pEC50 = 8.6 8.6 11 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 112542 None 0 Human Functional pEC50 = 8.6 8.6 11 3
Agonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assayAgonist activity at human beta2 adrenergic receptor in human BEAS-2B cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
57400229 70412 None 0 Human Functional pEC50 = 8.6 8.6 5 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
CHEMBL1945298 70412 None 0 Human Functional pEC50 = 8.6 8.6 5 4
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 497 12 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCOc3cccc(CNCCc4ccccc4F)c3)c2s1 10.1016/j.bmcl.2011.10.049
57401435 70424 None 0 Human Functional pEC50 = 8.6 8.6 31 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
CHEMBL1945503 70424 None 0 Human Functional pEC50 = 8.6 8.6 31 3
Agonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometryAgonist activity at human beta2 adrenoceptor expressed in H292 cells assessed as increase in cAMP accumulation after 60 mins by spectrophotometry
ChEMBL 458 11 5 6 2.8 O=c1ccc2c([C@@H](O)CNCCc3cccc(CNCCc4ccccn4)c3)ccc(O)c2[nH]1 10.1016/j.bmcl.2011.10.049
1239 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410.0 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1677 None 37 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassayAgonist activity at human beta2 receptor in BEAS-2B cells assessed as cAMP accumulation by radioimmunoassay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
42625898 185361 None 0 Human Functional pEC50 = 8.6 8.6 125 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL485847 185361 None 0 Human Functional pEC50 = 8.6 8.6 125 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46832801 14209 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084649 14209 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1198880 14209 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 431 16 4 6 3.6 Cc1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
46832803 14210 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
CHEMBL1084654 14210 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
CHEMBL1198881 14210 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 451 16 4 6 4.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccc(Cl)cc2)ccc1O 10.1021/jm100326d
46832505 14240 None 1 Human Functional pEC50 = 8.6 8.6 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1085395 14240 None 1 Human Functional pEC50 = 8.6 8.6 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
CHEMBL1199261 14240 None 1 Human Functional pEC50 = 8.6 8.6 12 3
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 417 16 4 6 3.3 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2ccccc2)ccc1O 10.1021/jm100326d
59119467 112317 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290983 112317 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 428 9 5 5 4.6 OCc1cc(C(O)CNCCc2ccc(Nc3ccc4ccccc4c3)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
90644139 112327 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290992 112327 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 424 10 5 6 4.2 CSc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
59119410 112328 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290993 112328 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 436 11 5 6 4.3 CC(C)Oc1ccc(Nc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2014.04.069
57391347 70250 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 6 6 3.2 Cc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
CHEMBL1940825 70250 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 436 11 6 6 3.2 Cc1ccc(C(O)CNc2ccc(CCNCC(O)c3ccc(O)c(CO)c3)cc2)cc1 10.1016/j.bmcl.2011.11.072
44434117 89783 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 561 13 5 8 4.1 CCn1c(C(=O)NCc2c(OC)cccc2OC)cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc21 10.1016/j.bmcl.2007.09.031
CHEMBL237709 89783 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levelsAgonist activity at human recombinant adrenergic beta-2 receptor expressed in CHO cells assessed as elevation in cAMP levels
ChEMBL 561 13 5 8 4.1 CCn1c(C(=O)NCc2c(OC)cccc2OC)cc2cc(C[C@@H](C)NC[C@H](O)c3ccc(O)c(CO)c3)ccc21 10.1016/j.bmcl.2007.09.031
10348864 58556 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
CHEMBL1683935 58556 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassayAgonist activity at human beta2-adrenoceptor expressed in HEK cells assessed as increase of cAMP level after 10 mins by radioimmunoassay
ChEMBL 616 18 5 7 6.7 O=CNc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccccc3)CC2)ccc1O 10.1016/j.bmcl.2011.01.043
3083544 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
3083544.0 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
CHEMBL1200811 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
CHEMBL1363 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
CHEMBL1951071 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
CHEMBL605993 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
DB00983 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
DB01274 26817 None 34 Human Functional pEC50 = 8.6 8.6 -2 6
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1021/acs.jmedchem.0c01195
16735272 85846 None 0 Human Functional pEC50 = 8.6 8.6 57 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL229614 85846 None 0 Human Functional pEC50 = 8.6 8.6 57 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 337 6 4 4 3.5 C[C@@H](Cc1cccc2ccccc12)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
45483815 200898 None 0 Human Functional pEC50 = 8.6 8.6 11 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1ccc(C(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL577289 200898 None 0 Human Functional pEC50 = 8.6 8.6 11 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1ccc(C(=O)O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
53380559 63662 None 0 Human Functional pEC50 = 8.6 8.6 4265 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
CHEMBL1800936 63662 None 0 Human Functional pEC50 = 8.6 8.6 4265 2
Agonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assayAgonist activity at human beta2 adrenergic receptor expressed in HEK 293 cells assessed as stimulation of cAMP accumulation by protein kinase binding assay
ChEMBL 317 7 5 5 2.4 CC[C@H](Cc1ccc(O)cc1)NC[C@H](O)c1cc(O)cc(O)c1 10.1016/j.bmc.2009.11.062
45375919 199467 None 0 Human Functional pEC50 = 8.5 8.5 87 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL566973 199467 None 0 Human Functional pEC50 = 8.5 8.5 87 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
164615990 185408 None 0 Human Functional pEC50 = 8.5 8.5 831 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassay
ChEMBL 427 9 5 6 1.6 CN(C)C(=O)CNc1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(O)c(CCO)c1)CC2 10.1021/acs.jmedchem.0c01195
CHEMBL4859326 185408 None 0 Human Functional pEC50 = 8.5 8.5 831 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassayAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in cAMP level incubated for 30 mins by immunoassay
ChEMBL 427 9 5 6 1.6 CN(C)C(=O)CNc1ccc2c(c1)C[C@@H](NC[C@H](O)c1ccc(O)c(CCO)c1)CC2 10.1021/acs.jmedchem.0c01195
45375919 199467 None 0 Human Functional pEC50 = 8.5 8.5 87 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL566973 199467 None 0 Human Functional pEC50 = 8.5 8.5 87 2
Agonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta2 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 7 5 6 2.1 CC(C)(Cc1cccc(C(=O)O)c1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44396531 66856 None 0 Human Functional pEC50 = 7.7 7.7 -38 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL186135 66856 None 0 Human Functional pEC50 = 7.7 7.7 -38 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
443372 10236 None 19 Golden hamster Functional pEC50 = 7.7 7.7 -2 9
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL1160723 10236 None 19 Golden hamster Functional pEC50 = 7.7 7.7 -2 9
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
CHEMBL2062275 10236 None 19 Golden hamster Functional pEC50 = 7.7 7.7 -2 9
Agonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPXAgonist activity at adrenergic beta2 receptor in Syrian hamster DDT1 MF2 cells assessed as stimulation of cAMP accumulation by radioimmunoassay in presence of 1 uM DPCPX
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm800613s
45483830 199451 None 0 Human Functional pEC50 = 7.7 7.7 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 329 7 4 4 2.8 Cc1ccccc1CC(C)(C)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL566777 199451 None 0 Human Functional pEC50 = 7.7 7.7 14 2
Agonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 2 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 329 7 4 4 2.8 Cc1ccccc1CC(C)(C)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
90666115 109404 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219048 109404 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 17 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
9933039 163140 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 163140 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
45271517 197298 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203998 197298 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549487 197298 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 499 10 4 4 4.8 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccc(Br)cc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45270690 197577 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203994 197577 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550037 197577 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44517694 197627 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL1203996 197627 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
CHEMBL550445 197627 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1cccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)c1 10.1016/j.bmc.2009.06.031
44517696 198227 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204007 198227 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL557705 198227 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44517692 199125 None 0 Human Functional pEC50 = 7.7 7.7 4 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203990 199125 None 0 Human Functional pEC50 = 7.7 7.7 4 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL564516 199125 None 0 Human Functional pEC50 = 7.7 7.7 4 3
Agonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta2 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 466 11 4 6 4.0 O=[N+]([O-])c1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
44331443 4450 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101674 4450 None 0 Human Functional pEC50 = 7.7 7.7 1 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 689 14 7 9 2.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(NC(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
3931 2248 None 39 Human Functional pEC50 = 7.7 7.7 -691 5
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
9829836 2248 None 39 Human Functional pEC50 = 7.7 7.7 -691 5
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
CHEMBL12998 2248 None 39 Human Functional pEC50 = 7.7 7.7 -691 5
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 584 17 6 7 4.5 CCCCCCNC(=O)Nc1ccc(cc1)S(=O)(=O)Nc1ccc(cc1)CCNC[C@@H](COc1ccc(cc1)O)O 10.1021/jm000544b
10697841 162964 None 0 Human Functional pEC50 = 7.7 7.7 4 2
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL417325 162964 None 0 Human Functional pEC50 = 7.7 7.7 4 2
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptorsIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 2 adrenergic receptors
ChEMBL 546 9 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(=O)N4CCC[C@H]4C(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
2297789 40725 None 4 Human Functional pEC50 = 7.7 7.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 469 11 2 6 4.8 CCCCN(CCCC)c1nc2ccccc2nc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 nan
CHEMBL1484690 40725 None 4 Human Functional pEC50 = 7.7 7.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 469 11 2 6 4.8 CCCCN(CCCC)c1nc2ccccc2nc1NS(=O)(=O)c1ccc(NC(C)=O)cc1 nan
1913590 19789 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 5 2 8 4.1 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCCO)ncnc4c23)CO1 nan
CHEMBL1301481 19789 None 5 Human Functional pEC50 = 7.7 7.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 5 2 8 4.1 CC1(C)Cc2c(c(-c3ccco3)nc3sc4c(NCCCO)ncnc4c23)CO1 nan
44610056 124058 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629360 124058 None 0 Human Functional pEC50 = 7.7 7.7 -1 2
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 704 14 5 9 5.5 O=c1ccc2c([C@@H](O)CNCCc3ccc(CCN4CCC(Cn5cnc([C@](O)(c6ccccc6)C6CCCCC6)n5)CC4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44331351 210600 None 0 Human Functional pEC50 = 4.7 4.7 -645 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL98088 210600 None 0 Human Functional pEC50 = 4.7 4.7 -645 3
Beta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptorBeta-2 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-2-adrenoceptor
ChEMBL 610 13 6 8 2.7 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(c3ccc(C(=O)N[C@@H](Cc4ccccc4)C(=O)O)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
44428086 150167 None 0 Rat Functional pEC50 = 4.7 4.7 -7 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Rat Functional pEC50 = 4.7 4.7 -7 2
Vasodilating activity against phenylephrine-induced contractions in rat thoracic aortaVasodilating activity against phenylephrine-induced contractions in rat thoracic aorta
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
2952777 194705 None 5 Human Functional pEC50 = 6.7 6.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
CHEMBL531401 194705 None 5 Human Functional pEC50 = 6.7 6.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 443 6 1 6 6.0 CC(Oc1ccc(Cl)cc1Cl)c1nc(-c2ccc(NC(=O)c3ccco3)cc2)no1 nan
666902 24992 None 5 Human Functional pEC50 = 6.7 6.7 213 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
CHEMBL1346316 24992 None 5 Human Functional pEC50 = 6.7 6.7 213 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 451 8 1 7 5.3 Clc1ccc(OCc2nnc(SCc3nc4ccccc4[nH]3)n2Cc2ccco2)cc1 nan
893042 51949 None 7 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 331 5 1 6 2.3 CCn1c(SCC(=O)N2CCCC2)nnc1-c1ccc(N)cc1 nan
CHEMBL1586182 51949 None 7 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 331 5 1 6 2.3 CCn1c(SCC(=O)N2CCCC2)nnc1-c1ccc(N)cc1 nan
90666116 109405 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219049 109405 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 730 19 6 9 7.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
59145957 124056 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
CHEMBL3629358 124056 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP productionAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as stumulation of intracellular cAMP production
ChEMBL 698 18 5 9 6.4 O=c1ccc2c([C@@H](O)CNCCCCCCCCCN3CCC(Cn4cnc(C(O)(c5ccccc5)C5CCCCC5)n4)CC3)ccc(O)c2[nH]1 10.1016/j.bmcl.2015.10.008
44396532 66777 None 0 Human Functional pEC50 = 7.7 7.7 -42 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185836 66777 None 0 Human Functional pEC50 = 7.7 7.7 -42 3
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-2 adrenergic receptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
9997789 186407 None 1 Human Functional pEC50 = 7.7 7.7 107 2
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
CHEMBL4874511 186407 None 1 Human Functional pEC50 = 7.7 7.7 107 2
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
CHEMBL5192245 186407 None 1 Human Functional pEC50 = 7.7 7.7 107 2
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 310 3 3 3 3.4 CC(C)(C)NC(CO)c1cc(Cl)c(N)c(C(F)(F)F)c1 10.1021/acs.jmedchem.0c01195
73057083 104330 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099658 104330 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 303 7 4 5 2.0 COc1ccc(CCNC[C@@H](O)c2cc(O)cc(O)c2)cc1 10.1016/j.bmc.2013.11.030
665098 19823 None 5 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 384 7 0 6 4.7 CCn1c(COc2ccc(Cl)cc2)nnc1SCc1ccc(C#N)cc1 nan
CHEMBL1301877 19823 None 5 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 384 7 0 6 4.7 CCn1c(COc2ccc(Cl)cc2)nnc1SCc1ccc(C#N)cc1 nan
6407382 45191 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
CHEMBL1525540 45191 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 527 4 1 6 5.8 Cc1cccc(Nc2nnc(-c3ccc(C(=O)N4C[C@H]5C[C@H](C4)c4cccc(=O)n4C5)cc3)c3ccccc23)c1 nan
1960 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260.0 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2857 None 46 Guinea pig Functional pEC50 = 6.7 6.7 -204 18
Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.Activity for Beta-2 adrenergic receptor was assessed from effect on relaxation of guinea pig trachea.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
16746244 48923 None 0 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1ccc(Br)cc1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
CHEMBL1559831 48923 None 0 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1ccc(Br)cc1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
2212788 28165 None 6 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
CHEMBL1373386 28165 None 6 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 490 10 1 7 4.2 C=CCn1c(CCNC(=O)c2cccs2)nnc1SCC(=O)c1ccc(Br)cc1 nan
3145649 39482 None 5 Human Functional pEC50 = 6.7 6.7 177 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
CHEMBL1472233 39482 None 5 Human Functional pEC50 = 6.7 6.7 177 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 395 4 0 4 4.7 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCCC1 nan
3986625 43199 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
CHEMBL1505690 43199 None 2 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 344 4 1 3 3.7 Cc1ccc(NC(=O)C(c2ccc(Cl)cc2)N2CCOCC2)cc1 nan
44396715 67472 None 0 Human Functional pEC50 = 7.7 7.7 -20 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL189081 67472 None 0 Human Functional pEC50 = 7.7 7.7 -20 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
90666110 109397 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219041 109397 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 718 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3cc(F)c(O)cc3F)CC2)ccc1O 10.1039/C1MD00140J
44428086 150167 None 0 Guinea pig Functional pEC50 = 6.7 6.7 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Guinea pig Functional pEC50 = 6.7 6.7 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
1165076 39962 None 2 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
CHEMBL1478198 39962 None 2 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 466 5 1 7 4.8 Cc1ccc(Cn2ccc(NC(=O)c3cc4nc(-c5ccco5)cc(C(F)(F)F)n4n3)n2)cc1 nan
44428085 93314 None 0 Guinea pig Functional pEC50 = 5.7 5.7 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
CHEMBL244906 93314 None 0 Guinea pig Functional pEC50 = 5.7 5.7 - 1
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 399 9 4 8 2.6 Cc1nonc1COc1ccc(CC(C)NCC(O)c2cc(O)cc(O)c2)cc1 10.1021/jm0704595
10221081 124167 None 1 Guinea pig Functional pEC50 = 5.7 5.7 -18 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 124167 None 1 Guinea pig Functional pEC50 = 5.7 5.7 -18 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
24789160 35367 None 0 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 501 12 3 6 2.9 NC(=O)CC(NC(=O)Cc1ccc(Cl)cc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
CHEMBL1437255 35367 None 0 Human Functional pEC50 = 5.7 5.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 501 12 3 6 2.9 NC(=O)CC(NC(=O)Cc1ccc(Cl)cc1)c1ccc(NCCCN2CCCC2=O)c([N+](=O)[O-])c1 nan
44428083 92613 None 0 Guinea pig Functional pEC50 = 4.7 4.7 4 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 4.7 4.7 4 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
3119289 47507 None 1 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 8 2 4 5.0 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3ccco3)cc2)c1 nan
CHEMBL1545591 47507 None 1 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 378 8 2 4 5.0 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3ccco3)cc2)c1 nan
24789183 32878 None 0 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1cccc(Br)c1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
CHEMBL1414874 32878 None 0 Human Functional pEC50 = 6.7 6.7 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 552 8 2 7 3.4 NC(=O)CC(NC(=O)c1cccc(Br)c1)c1ccc(N2CCN(c3ccccn3)CC2)c([N+](=O)[O-])c1 nan
2234461 43788 None 6 Human Functional pEC50 = 6.7 6.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
CHEMBL1510834 43788 None 6 Human Functional pEC50 = 6.7 6.7 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 432 7 1 6 2.7 COC(=O)c1ccc(NC(=O)COc2ccc(S(=O)(=O)N3CCCCC3)cc2)cc1 nan
16279412 59389 None 2 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 467 10 2 7 3.5 CCOc1ccccc1C(=O)NCC(=O)OCc1csc(CC(=O)Nc2ccc(C)cc2)n1 nan
CHEMBL1708092 59389 None 2 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 467 10 2 7 3.5 CCOc1ccccc1C(=O)NCC(=O)OCc1csc(CC(=O)Nc2ccc(C)cc2)n1 nan
59707188 109402 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219046 109402 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 734 18 6 9 7.0 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccc(F)cc3-c3ccc(O)c(Cl)c3)CC2)ccc1O 10.1039/C1MD00140J
90666121 109411 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
CHEMBL3219054 109411 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 742 18 6 9 7.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2C3CCC2CC(OC(=O)Nc2ccccc2-c2ccc(O)c(Cl)c2)C3)ccc1O 10.1039/C1MD00140J
11324939 94516 None 1 Human Functional pEC50 = 7.6 7.6 -6 2
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL25133 94516 None 1 Human Functional pEC50 = 7.6 7.6 -6 2
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 CC(Cc1c[nH]c2ccccc12)NCC(O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
659759 47285 None 9 Human Functional pEC50 = 7.6 7.6 14 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 47285 None 9 Human Functional pEC50 = 7.6 7.6 14 2
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
1854978 37724 None 5 Human Functional pEC50 = 7.6 7.6 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
CHEMBL1457704 37724 None 5 Human Functional pEC50 = 7.6 7.6 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset3. (Class of assay: confirmatory)
ChEMBL 422 5 1 7 5.5 CC(C)Cc1nc2sc3c(NCc4ccco4)ncnc3c2c2c1COC(C)(C)C2 nan
44428086 150167 None 0 Guinea pig Functional pEC50 = 6.6 6.6 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
CHEMBL395082 150167 None 0 Guinea pig Functional pEC50 = 6.6 6.6 7 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-oneAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of 1H-[1,2,4]oxadiazolo-[4,3-a]quinoxalin-1-one
ChEMBL 415 9 4 8 1.9 Cc1c(COc2ccc(CC(C)NCC(O)c3cc(O)cc(O)c3)cc2)no[n+]1[O-] 10.1021/jm0704595
10221081 124167 None 1 Guinea pig Functional pEC50 = 5.6 5.6 -18 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
CHEMBL363325 124167 None 1 Guinea pig Functional pEC50 = 5.6 5.6 -18 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 270 4 0 6 0.5 CCOc1no[n+]([O-])c1S(=O)(=O)c1ccccc1 10.1021/jm0704595
10028830 2246 None 31 Human Functional pEC50 = 4.6 4.6 -4897 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
3932 2246 None 31 Human Functional pEC50 = 4.6 4.6 -4897 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4238084 2246 None 31 Human Functional pEC50 = 4.6 4.6 -4897 3
Antagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta2 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 497 13 4 6 2.7 O[C@H](COc1cccc(c1)CNC(=O)C)CNCCc1ccc(cc1)NS(=O)(=O)c1ccccc1 10.1016/j.ejmech.2018.03.032
141286040 193111 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5203966 193111 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
CHEMBL5222714 193111 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysisAgonist activity at beta2 adrenoceptor (unknown origin) expressed in HEK293 cells assessed as cAMP accumulation incubated for 60 mins by microplate reader analysis
ChEMBL 290 4 3 3 2.2 CC(C)NC(CO)c1cc(F)c(N)c(Br)c1 10.1021/acs.jmedchem.1c02006
102139105 186437 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 392 10 5 7 2.5 COc1cc(CCC(O)CC(O)CCc2cc(O)c(O)c(OC)c2)ccc1O 10.1021/acs.jmedchem.0c01195
CHEMBL4874899 186437 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrsAgonist activity at beta2 adrenoceptor in human A431 cells measured for 24 hrs
ChEMBL 392 10 5 7 2.5 COc1cc(CCC(O)CC(O)CCc2cc(O)c(O)c(OC)c2)ccc1O 10.1021/acs.jmedchem.0c01195
1499 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779.0 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
90666118 109408 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
CHEMBL3219051 109408 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 702 18 6 9 6.5 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CC[C@@H](OC(=O)Nc3ccccc3-c3ccc(O)c(Cl)c3)C2)ccc1O 10.1039/C1MD00140J
1499 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3779.0 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
536 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
CHEMBL434 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
DB01064 2091 None 34 Human Functional pEC50 = 6.6 6.6 -102 38
Agonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation countingAgonist activity at recombinant human beta2 adrenoceptor expressed in HEK293T cells assessed as increase in IBMX-induced cAMP accumulation using [3H]-cAMP after 30 mins by liquid scintillation counting
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2011.11.054
3038500 9342 None 11 Human Functional pEC50 = 5.6 5.6 -575 6
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
CHEMBL111201 9342 None 11 Human Functional pEC50 = 5.6 5.6 -575 6
In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.In vitro functional efficacy in stimulating increase in cAMP in chinese hamster ovary (CHO) cells expressing the cloned human beta-2 receptor.
ChEMBL 624 11 3 7 6.6 O=S(=O)(Nc1ccc(CCNC[C@H](O)c2cccnc2)cc1)c1ccc(-c2nc(-c3ccc(C(F)(F)F)cc3)cs2)cc1 10.1021/jm000286i
44428083 92613 None 0 Guinea pig Functional pEC50 = 4.6 4.6 4 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL243266 92613 None 0 Guinea pig Functional pEC50 = 4.6 4.6 4 2
Agonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranololAgonist activity at adrenergic beta2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction in presence of propranolol
ChEMBL 444 10 5 9 0.7 CC(Cc1ccc(OCc2no[n+]([O-])c2C(N)=O)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
3145657 36692 None 9 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 381 4 0 4 4.3 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCC1 nan
CHEMBL1449091 36692 None 9 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 381 4 0 4 4.3 CC(Sc1nc(-c2ccccc2)cc(C(F)(F)F)n1)C(=O)N1CCCC1 nan
652434 54118 None 4 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 399 6 1 8 3.7 CCOc1ccc2nc(NC(=O)CSc3nc4cccnc4n3C)sc2c1 nan
CHEMBL1606638 54118 None 4 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 399 6 1 8 3.7 CCOc1ccc2nc(NC(=O)CSc3nc4cccnc4n3C)sc2c1 nan
44142358 21675 None 0 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 311 0 1 3 3.9 Nc1cccc(C#Cc2ccc3c(=O)c4ccccc4oc3c2)c1 nan
CHEMBL1318214 21675 None 0 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 311 0 1 3 3.9 Nc1cccc(C#Cc2ccc3c(=O)c4ccccc4oc3c2)c1 nan
5182299 24941 None 8 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
CHEMBL1345891 24941 None 8 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 457 5 1 4 4.5 O=C(Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1)c1c(F)cccc1F nan
20959170 28791 None 5 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 4 4.7 Cc1ccc(N(C)S(=O)(=O)c2cc(-c3cnc(C4CC4)o3)ccc2C)cc1 nan
CHEMBL1378598 28791 None 5 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 382 5 0 4 4.7 Cc1ccc(N(C)S(=O)(=O)c2cc(-c3cnc(C4CC4)o3)ccc2C)cc1 nan
9927453 96740 None 0 Human Functional pEC50 = 7.6 7.6 -18 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL26393 96740 None 0 Human Functional pEC50 = 7.6 7.6 -18 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
46221398 8706 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
CHEMBL1095779 8706 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assayAgonist activity at human beta2 adrenergic receptor assessed as increase in cAMP level by whole cell assay
ChEMBL 448 10 4 4 4.7 CCCCc1cc2c(cc1CCCC)CC(NC[C@H](O)c1ccc(O)c3[nH]c(=O)ccc13)C2 10.1021/jm100068m
9927453 96740 None 0 Human Functional pEC50 = 7.6 7.6 -18 3
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL26393 96740 None 0 Human Functional pEC50 = 7.6 7.6 -18 3
Agonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-2 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
90644142 112304 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
CHEMBL3290971 112304 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta2 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 365 7 4 4 2.5 OCc1cc(C(O)CNCCc2ccc(Br)cc2)ccc1O 10.1016/j.bmcl.2014.04.069
105 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
2083 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
2083.0 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
558 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
CHEMBL714 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
DB01001 3461 None 54 Human Functional pEC50 = 7.6 7.6 -13 3
Agonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta2-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.bmcl.2011.11.072
3366873 24348 None 6 Human Functional pEC50 = 7.6 7.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 10 3 6 4.2 COc1ccc(CNC(=O)CCCCCNc2nc(S)nc3ccccc23)cc1 nan
CHEMBL1340869 24348 None 6 Human Functional pEC50 = 7.6 7.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 410 10 3 6 4.2 COc1ccc(CNC(=O)CCCCCNc2nc(S)nc3ccccc23)cc1 nan
24180436 93270 None 0 Guinea pig Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
CHEMBL244687 93270 None 0 Guinea pig Functional pEC50 = 6.6 6.6 -1 2
Agonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contractionAgonist activity at adrenergic beta-2 receptor in guinea pig tracheal rings assessed as myorelaxing activity on carbachol-induced contraction
ChEMBL 527 10 4 10 2.6 CC(Cc1ccc(Oc2no[n+]([O-])c2S(=O)(=O)c2ccccc2)cc1)NCC(O)c1cc(O)cc(O)c1 10.1021/jm0704595
105 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
2083 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
2083.0 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
558 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
CHEMBL714 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
DB01001 3461 None 54 Human Functional pEC50 = 6.6 6.6 -13 3
Agonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technologyAgonist activity at human beta2 adrenoceptor expressed in CHO cells assessed as increase in intracellular cAMP level incubated for 1 hr by alphascreen technology
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1021/acs.jmedchem.0c01195
145989107 167225 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 13 4 5 3.7 O=c1ccc2c(C(CO)NCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4290441 167225 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 424 13 4 5 3.7 O=c1ccc2c(C(CO)NCCCCOCCCCc3ccccc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
11038599 47882 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL154906 47882 None 0 Human Functional pEC50 = 6.6 6.6 -15 3
Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.Concentration that causes 50% inhibition of human beta 2 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 516 11 5 6 3.7 C[C@H](CNc1cccc(CNC(=O)NS(=O)(=O)c2ccccc2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
9801145 93475 None 0 Human Functional pEC50 = 5.6 5.6 -316 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245874 93475 None 0 Human Functional pEC50 = 5.6 5.6 -316 3
Agonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-2 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 9 4 5 4.0 O=C(O)c1ccoc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1016/j.bmcl.2007.05.069
46832227 14202 None 2 Human Functional pEC50 = 5.6 5.6 5 2
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1083884 14202 None 2 Human Functional pEC50 = 5.6 5.6 5 2
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
CHEMBL1198851 14202 None 2 Human Functional pEC50 = 5.6 5.6 5 2
Agonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 327 13 5 6 1.1 OCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm100326d
42625743 12605 None 0 Human Functional pEC50 = 4.6 4.6 -12 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186943 12605 None 0 Human Functional pEC50 = 4.6 4.6 -12 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483407 12605 None 0 Human Functional pEC50 = 4.6 4.6 -12 3
Agonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta2 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCCOCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
2816345 29329 None 2 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 4 1 7 5.2 Cc1cc(C)c2c(N)c(-c3nnc(SCc4ccc(Cl)cc4)n3C)sc2n1 nan
CHEMBL1383213 29329 None 2 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 415 4 1 7 5.2 Cc1cc(C)c2c(N)c(-c3nnc(SCc4ccc(Cl)cc4)n3C)sc2n1 nan
4384568 163198 None 6 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
CHEMBL417709 163198 None 6 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 438 6 0 4 3.4 O=C1C2CCCCN2C(=O)N1CCCCN1CCN(c2cccc(C(F)(F)F)c2)CC1 nan
1481480 24276 None 12 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 484 8 0 7 4.9 CN(CCOc1ccc(-c2ccn(S(=O)(=O)c3cccc4ccccc34)n2)cc1)c1ccccn1 nan
CHEMBL1340208 24276 None 12 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 484 8 0 7 4.9 CN(CCOc1ccc(-c2ccn(S(=O)(=O)c3cccc4ccccc34)n2)cc1)c1ccccn1 nan
8441531 45462 None 4 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 394 8 2 4 5.4 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3cccs3)cc2)c1 nan
CHEMBL1527861 45462 None 4 Human Functional pEC50 = 6.6 6.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 394 8 2 4 5.4 CCCCOc1cccc(C(=O)Nc2ccc(NC(=O)c3cccs3)cc2)c1 nan
24794188 33728 None 1 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 3 5.4 O=C(c1ccc(OC2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1)N1CCCCC1 nan
CHEMBL1422222 33728 None 1 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 446 5 0 3 5.4 O=C(c1ccc(OC2CCN(Cc3ccc(C(F)(F)F)cc3)CC2)cc1)N1CCCCC1 nan
44396530 67109 None 0 Human Functional pEC50 = 7.6 7.6 -23 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL187317 67109 None 0 Human Functional pEC50 = 7.6 7.6 -23 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 591 14 4 8 4.8 CCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1007/s00044-009-9257-x
76333795 85349 None 0 Human Functional pEC50 = 7.6 7.6 -56 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
CHEMBL2260985 85349 None 0 Human Functional pEC50 = 7.6 7.6 -56 3
Agonist activity at Homo sapiens (human) beta2 adrenoreceptorAgonist activity at Homo sapiens (human) beta2 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
90666102 109389 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219032 109389 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 682 18 6 9 6.2 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)cc3)CC2)ccc1O 10.1039/C1MD00140J
59707195 109396 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
CHEMBL3219040 109396 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP productionAgonist activity at human beta-2 adrenoceptor expressed in CHO cells assessed as stimulation of intracellular cAMP production
ChEMBL 700 18 6 9 6.3 CS(=O)(=O)Nc1cc([C@@H](O)CNCCCCCCCCCN2CCC(OC(=O)Nc3ccccc3-c3ccc(O)c(F)c3)CC2)ccc1O 10.1039/C1MD00140J
1362375 22995 None 10 Human Functional pEC50 = 6.6 6.6 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
CHEMBL1329712 22995 None 10 Human Functional pEC50 = 6.6 6.6 - 1
PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory) PubChem BioAssay. Dose response for HTS for Beta-2AR agonists via FAP method from Powderset1. (Class of assay: confirmatory)
ChEMBL 388 6 2 5 4.8 CCc1ccc(OCC(=O)Nc2ccc(-c3nc4ccccc4o3)c(O)c2)cc1 nan
127046951 139989 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
CHEMBL3799427 139989 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositolAgonist activity at human beta2 receptor expressed in HEK293 cells cotransfected with Gqs5 protein assessed as [3H]IP3 accumulation after 120 mins by scintillation counting assay in presence of myo-[3H]-inositol
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1016/j.bmc.2016.04.028
659759 47285 None 9 Human Functional pEC50 = 6.6 6.6 14 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
CHEMBL1543973 47285 None 9 Human Functional pEC50 = 6.6 6.6 14 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 359 4 1 4 3.0 CC(=O)Nc1ccc(S(=O)(=O)N2CCCCC2c2cccnc2)cc1 nan
4508 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
4866774 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
509 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
838 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
838.0 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
CHEMBL1740 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
DB11124 3139 None 60 Human Functional pEC50 = 5.6 5.6 1 2
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 183 3 4 4 0.4 CNCC(c1ccc(c(c1)O)O)O nan
73056755 104333 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
CHEMBL3099661 104333 None 0 Human Functional pEC50 = 4.6 4.6 - 1
Agonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulationAgonist activity at human beta2 adrenergic receptor expressed in HEK293 cells assessed as stimulation of cAMP accumulation
ChEMBL 345 8 4 5 3.0 COc1ccc(C[C@H](NC[C@H](O)c2cc(O)cc(O)c2)C(C)C)cc1 10.1016/j.bmc.2013.11.030
2803618 59308 None 3 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 324 5 0 3 4.8 COc1ccc(C(C)=O)cc1COc1ccc(Cl)cc1Cl nan
CHEMBL1704973 59308 None 3 Human Functional pEC50 = 5.6 5.6 - 1
PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]PUBCHEM_BIOASSAY: Dose response for HTS for Beta-2AR agonists via FAP method from CP1. (Class of assay: confirmatory) [Related pubchem assays (depositor defined):AID485366, AID492947, AID504448]
ChEMBL 324 5 0 3 4.8 COc1ccc(C(C)=O)cc1COc1ccc(Cl)cc1Cl nan
105 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
2083.0 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
558 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
CHEMBL714 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
DB01001 3461 None 54 Guinea pig Functional pEC50 = 6.6 6.6 13 3
Agonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contractionAgonist activity at adrenergic beta2 receptor in Hartley guinea pig tracheal ring assessed as bronchorelaxation activity against carbachol-induced contraction
ChEMBL 239 4 4 4 1.3 OCc1cc(ccc1O)C(CNC(C)(C)C)O 10.1016/j.ejmech.2008.12.016
49837874 54970 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at beta2 adrenoceptor (unknown origin)Agonist activity at beta2 adrenoceptor (unknown origin)
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NC[C@H](O)c1ccc(O)c2c1OCC(=O)N2 10.1021/acs.jmedchem.0c01195
CHEMBL1615159 54970 None 0 Human Functional pEC50