Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Activity Chemical information
Sel. page Common
name
GPCRdb
ID
Reference
ligand
Vendors

Species

Assay
Type

Activity
Type
Activity
Relation
Activity
Value
p-value
(-log)
Fold
selectivity
Tested
GPCRs
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

3658 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709.0 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4107 None 38 Human Functional pAC50 = 9.5 9.5 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
11079 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436.0 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 2733 None 38 Human Functional pAC50 = 9.2 9.2 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
2142 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775.0 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3096 None 36 Human Functional pAC50 = 9.1 9.1 -1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
1960 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260.0 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 2857 None 46 Human Functional pAC50 = 8.9 8.9 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
11079 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3369 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
4436.0 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
5509 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL761 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB06711 2733 None 38 Human Functional pAC50 = 8.9 8.9 5 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1038/s41467-023-40064-9
3036780 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
3036780.0 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
46780481 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
9903970.0 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3187365 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL3544974 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
CHEMBL504548 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
DB06216 107587 None 16 Human Functional pAC50 = 8.9 8.9 -7 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 285 0 0 2 4.3 CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1 10.1038/s41467-023-40064-9
2803 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
2803.0 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 955 None 40 Human Functional pAC50 = 8.8 8.8 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
1960 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260.0 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 2857 None 46 Human Functional pAC50 = 8.8 8.8 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
129211 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
129211.0 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
2562 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
488 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
CHEMBL836 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
DB00706 3749 None 48 Human Functional pAC50 = 8.8 8.8 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1038/s41467-023-40064-9
124 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
2032 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
4636.0 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL762 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
DB00935 2981 None 32 Human Functional pAC50 = 8.7 8.7 -8 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1038/s41467-023-40064-9
16351 102785 None 36 Human Functional pAC50 = 8 8.0 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
16351.0 102785 None 36 Human Functional pAC50 = 8 8.0 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102785 None 36 Human Functional pAC50 = 8 8.0 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102785 None 36 Human Functional pAC50 = 8 8.0 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
9429 204590 None 44 Human Functional pAC50 = 6 6.0 -5 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
9429.0 204590 None 44 Human Functional pAC50 = 6 6.0 -5 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL609109 204590 None 44 Human Functional pAC50 = 6 6.0 -5 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
DB01622 204590 None 44 Human Functional pAC50 = 6 6.0 -5 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 6 0 6 3.2 CN1CCN(CCCN2c3ccccc3Sc3ccc(S(=O)(=O)N(C)C)cc32)CC1 10.1038/s41467-023-40064-9
3599 16886 None 60 Human Functional pAC50 = 5 5.0 1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 20 0 4 5.7 CCCCCCCCCCCCCCCCOP(=O)([O-])OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL125 16886 None 60 Human Functional pAC50 = 5 5.0 1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 20 0 4 5.7 CCCCCCCCCCCCCCCCOP(=O)([O-])OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
3062316 33583 None 70 Human Functional pAC50 = 5 5.0 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL1421 33583 None 70 Human Functional pAC50 = 5 5.0 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
CHEMBL5416410 33583 None 70 Human Functional pAC50 = 5 5.0 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 487 7 3 9 3.3 Cc1nc(Nc2ncc(C(=O)Nc3c(C)cccc3Cl)s2)cc(N2CCN(CCO)CC2)n1 10.1038/s41467-023-40064-9
54676537 152943 None 53 Human Functional pAC50 = 5 5.0 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 5 1 6 3.5 CC(=O)CC(c1ccc([N+](=O)[O-])cc1)c1c(O)c2ccccc2oc1=O 10.1038/s41467-023-40064-9
CHEMBL397420 152943 None 53 Human Functional pAC50 = 5 5.0 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 5 1 6 3.5 CC(=O)CC(c1ccc([N+](=O)[O-])cc1)c1c(O)c2ccccc2oc1=O 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 5.0 5.0 -5 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Functional pAC50 = 5.0 5.0 -5 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
3783 14010 None 16 Human Functional pAC50 = 6.0 6.0 -27 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 4 2.9 CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL1197051 14010 None 16 Human Functional pAC50 = 6.0 6.0 -27 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 4 2.9 CC(COc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
6989215 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
7391 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
92974 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
92974.0 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
971 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
CHEMBL2103827 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
DB06262 1485 None 54 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 213 3 5 5 -0.5 OC(=O)[C@H]([C@@H](c1ccc(c(c1)O)O)O)N 10.1038/s41467-023-40064-9
242 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795.0 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 None 70 Human Functional pAC50 = 6.0 6.0 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
2683 102943 None 17 Human Functional pAC50 = 5.0 5.0 -812 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL305906 102943 None 17 Human Functional pAC50 = 5.0 5.0 -812 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL334255 102943 None 17 Human Functional pAC50 = 5.0 5.0 -812 24
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
31101 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
31101.0 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 729 None 28 Human Functional pAC50 = 6.0 6.0 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
9417 133581 None 40 Human Functional pAC50 = 6.0 6.0 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133581 None 40 Human Functional pAC50 = 6.0 6.0 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133581 None 40 Human Functional pAC50 = 6.0 6.0 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
22530 56146 None 40 Human Functional pAC50 = 6.0 6.0 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1600878 56146 None 40 Human Functional pAC50 = 6.0 6.0 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL1625607 56146 None 40 Human Functional pAC50 = 6.0 6.0 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 2 0 2 3.7 CN1CCc2c(c3ccccc3n2Cc2ccccc2)C1 10.1038/s41467-023-40064-9
60860 208097 None 26 Human Functional pAC50 = 5.0 5.0 -21 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL1615777 208097 None 26 Human Functional pAC50 = 5.0 5.0 -21 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
CHEMBL818 208097 None 26 Human Functional pAC50 = 5.0 5.0 -21 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 2 3 1 1.3 N=C(N)NCc1cccc(I)c1 10.1038/s41467-023-40064-9
5354 155746 None 16 Human Functional pAC50 = 5.0 5.0 -102 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
CHEMBL404849 155746 None 16 Human Functional pAC50 = 5.0 5.0 -102 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 337 12 2 3 5.6 CCCCCCCCNC(C)C(O)c1ccc(SC(C)C)cc1 10.1038/s41467-023-40064-9
2441 98678 None 12 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 1 1 3 2.6 O=C1CN=C(c2ccccn2)c2cc(Br)ccc2N1 10.1038/s41467-023-40064-9
CHEMBL277062 98678 None 12 Human Functional pAC50 = 5.0 5.0 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 1 1 3 2.6 O=C1CN=C(c2ccccn2)c2cc(Br)ccc2N1 10.1038/s41467-023-40064-9
104850 3330 None 58 Human Functional pAC50 = 5.0 5.0 -1122 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
4150 3330 None 58 Human Functional pAC50 = 5.0 5.0 -1122 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
743 3330 None 58 Human Functional pAC50 = 5.0 5.0 -1122 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL111 3330 None 58 Human Functional pAC50 = 5.0 5.0 -1122 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
DB06155 3330 None 58 Human Functional pAC50 = 5.0 5.0 -1122 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 462 4 1 4 5.9 Clc1ccc(cc1)c1c(C)c(nn1c1ccc(cc1Cl)Cl)C(=O)NN1CCCCC1 10.1038/s41467-023-40064-9
1056 3371 None 67 Human Functional pAC50 = 5.0 5.0 -19 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
2405 3371 None 67 Human Functional pAC50 = 5.0 5.0 -19 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
77999 3371 None 67 Human Functional pAC50 = 5.0 5.0 -19 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
CHEMBL121 3371 None 67 Human Functional pAC50 = 5.0 5.0 -19 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
DB00412 3371 None 67 Human Functional pAC50 = 5.0 5.0 -19 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 6 2.5 O=C1NC(=O)C(S1)Cc1ccc(cc1)OCCN(c1ccccn1)C 10.1038/s41467-023-40064-9
4499 59795 None 61 Human Functional pAC50 = 5.0 5.0 -6 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
CHEMBL1726 59795 None 61 Human Functional pAC50 = 5.0 5.0 -6 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 6 1 7 3.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OCC(C)C)C1c1ccccc1[N+](=O)[O-] 10.1038/s41467-023-40064-9
103 4153 None 44 Human Functional pAC50 = 8.0 8.0 1 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2875 4153 None 44 Human Functional pAC50 = 8.0 8.0 1 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
5736 4153 None 44 Human Functional pAC50 = 8.0 8.0 1 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL285802 4153 None 44 Human Functional pAC50 = 8.0 8.0 1 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB09225 4153 None 44 Human Functional pAC50 = 8.0 8.0 1 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 331 4 0 3 4.9 CN(CCOC1=Cc2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
10184665 3991 None 42 Human Functional pAC50 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -645 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 485 16 4 6 4.6 OCc1cc(ccc1O)[C@H](CNCCCCCCOCCOCc1c(Cl)cccc1Cl)O 10.1038/s41467-023-40064-9
2267 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2267.0 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
271 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
7121 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL639 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00972 559 None 45 Human Functional pAC50 = 6.0 6.0 -45 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 3 0 4 4.3 CN1CCCC(CC1)n1nc(Cc2ccc(cc2)Cl)c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2274 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4917.0 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
7279 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL728 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00433 3173 None 38 Human Functional pAC50 = 6.0 6.0 -24 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 4 0 4 4.6 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
2601 3780 None 25 Human Functional pAC50 = 6.0 6.0 -354 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
443951 3780 None 25 Human Functional pAC50 = 6.0 6.0 -354 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
56 3780 None 25 Human Functional pAC50 = 6.0 6.0 -354 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL73151 3780 None 25 Human Functional pAC50 = 6.0 6.0 -354 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB13399 3780 None 25 Human Functional pAC50 = 6.0 6.0 -354 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 3 2 2 2.9 CCN(C(=O)N[C@@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
11626560 203394 None 56 Human Functional pAC50 = 6.0 6.0 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
CHEMBL601719 203394 None 56 Human Functional pAC50 = 6.0 6.0 -1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 449 5 2 6 5.0 C[C@@H](Oc1cc(-c2cnn(C3CCNCC3)c2)cnc1N)c1c(Cl)ccc(F)c1Cl 10.1038/s41467-023-40064-9
10071196 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
10071196.0 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
5142 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
8423 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
CHEMBL2111101 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
DB05316 3124 None 53 Human Functional pAC50 = 4.9 4.9 -776 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 8 1 3 4.7 CC(COc1ccc(cc1)CNC(=O)N(C1CCN(CC1)C)Cc1ccc(cc1)F)C 10.1038/s41467-023-40064-9
3675 7736 None 46 Human Functional pAC50 = 4.9 4.9 -91 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 136 3 2 2 0.7 NNCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1089 7736 None 46 Human Functional pAC50 = 4.9 4.9 -91 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 136 3 2 2 0.7 NNCCc1ccccc1 10.1038/s41467-023-40064-9
135409453 3773 None 26 Human Functional pAC50 = 5.9 5.9 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Functional pAC50 = 5.9 5.9 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Functional pAC50 = 5.9 5.9 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
2470 3653 None 40 Human Functional pAC50 = 4.9 4.9 -13803 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 None 40 Human Functional pAC50 = 4.9 4.9 -13803 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 None 40 Human Functional pAC50 = 4.9 4.9 -13803 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 None 40 Human Functional pAC50 = 4.9 4.9 -13803 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 None 40 Human Functional pAC50 = 4.9 4.9 -13803 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
180 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Functional pAC50 = 6.9 6.9 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
4822 45046 None 35 Human Functional pAC50 = 6.9 6.9 -16 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL152408 45046 None 35 Human Functional pAC50 = 6.9 6.9 -16 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 0 0 2 4.7 CN1CCC(=C2c3ccccc3Sc3ccccc32)CC1 10.1038/s41467-023-40064-9
16351 102785 None 36 Human Functional pAC50 = 5.9 5.9 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
16351.0 102785 None 36 Human Functional pAC50 = 5.9 5.9 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
CHEMBL304902 102785 None 36 Human Functional pAC50 = 5.9 5.9 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
DB13256 102785 None 36 Human Functional pAC50 = 5.9 5.9 -17 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 343 0 0 4 4.1 CN1CCN(C2=Nc3ccccc3Sc3ccc(Cl)cc32)CC1 10.1038/s41467-023-40064-9
37264 189531 None 18 Human Functional pAC50 = 5.9 5.9 8 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL513301 189531 None 18 Human Functional pAC50 = 5.9 5.9 8 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 435 6 2 10 1.3 COc1cc2c(N)nc(N3CCN(C(=O)OCC(C)(C)O)CC3)nc2c(OC)c1OC 10.1038/s41467-023-40064-9
643976 14524 None 29 Human Functional pAC50 = 4.9 4.9 -2 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 4.9 4.9 -2 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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
72093 35070 None 5 Human Functional pAC50 = 4.9 4.9 -10 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL1433361 35070 None 5 Human Functional pAC50 = 4.9 4.9 -10 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
CHEMBL2103773 35070 None 5 Human Functional pAC50 = 4.9 4.9 -10 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 483 16 1 4 6.3 CCCCCCCCOc1ccccc1C(=O)Nc1ccc(C(=O)OCC[N+](C)(CC)CC)cc1 10.1038/s41467-023-40064-9
65016 10211 None 50 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 505 11 3 7 2.4 CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1 10.1038/s41467-023-40064-9
CHEMBL116 10211 None 50 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 505 11 3 7 2.4 CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1 10.1038/s41467-023-40064-9
22323 15305 None 29 Human Functional pAC50 = 4.9 4.9 -3 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9571037 15305 None 29 Human Functional pAC50 = 4.9 4.9 -3 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1213553 15305 None 29 Human Functional pAC50 = 4.9 4.9 -3 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 2 5 2 2.9 CC(C)NC(=N)NC(=N)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
47319 26472 None 27 Human Functional pAC50 = 4.9 4.9 -4 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1360 26472 None 27 Human Functional pAC50 = 4.9 4.9 -4 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 929 24 0 12 8.1 COc1ccc(CC2c3cc(OC)c(OC)cc3CC[N+]2(C)CCC(=O)OCCCCCOC(=O)CC[N+]2(C)CCc3cc(OC)c(OC)cc3C2Cc2ccc(OC)c(OC)c2)cc1OC 10.1038/s41467-023-40064-9
3191 102913 None 65 Human Functional pAC50 = 4.9 4.9 -660 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
3191.0 102913 None 65 Human Functional pAC50 = 4.9 4.9 -660 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
CHEMBL305660 102913 None 65 Human Functional pAC50 = 4.9 4.9 -660 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
DB11742 102913 None 65 Human Functional pAC50 = 4.9 4.9 -660 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 469 9 0 3 7.2 CC(C)(C)c1ccc(C(=O)CCCN2CCC(OC(c3ccccc3)c3ccccc3)CC2)cc1 10.1038/s41467-023-40064-9
2372 106524 None 30 Human Functional pAC50 = 4.9 4.9 -144 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
CHEMBL314010 106524 None 30 Human Functional pAC50 = 4.9 4.9 -144 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 345 10 2 5 2.6 COc1ccc(CCNCC(O)COc2cccc(C)c2)cc1OC 10.1038/s41467-023-40064-9
216416 111644 None 40 Human Functional pAC50 = 4.9 4.9 -141 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL328190 111644 None 40 Human Functional pAC50 = 4.9 4.9 -141 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 413 6 1 3 5.7 Oc1ccc2c(c1)CC[C@H](c1ccccc1)[C@@H]2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
23480 124157 None 21 Human Functional pAC50 = 4.9 4.9 -15 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL363295 124157 None 21 Human Functional pAC50 = 4.9 4.9 -15 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 5 1 1 5.0 CC(CC(c1ccccc1)c1ccccc1)NC(C)(C)C 10.1038/s41467-023-40064-9
135412795 44765 None 17 Human Functional pAC50 = 4.9 4.9 -7 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 1 1 3 3.4 O=C1CN=C(c2ccccc2)c2c(sc3c2CCCC3)N1 10.1038/s41467-023-40064-9
CHEMBL1521495 44765 None 17 Human Functional pAC50 = 4.9 4.9 -7 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 1 1 3 3.4 O=C1CN=C(c2ccccc2)c2c(sc3c2CCCC3)N1 10.1038/s41467-023-40064-9
2805 161984 None 27 Human Functional pAC50 = 5.9 5.9 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL415087 161984 None 27 Human Functional pAC50 = 5.9 5.9 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 329 6 0 2 4.9 Clc1ccc(C(OCCN2CCCCC2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
3053 207592 None 64 Human Functional pAC50 = 5.9 5.9 1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 393 16 5 8 -2.7 O=C(O)CN(CCN(CC(=O)O)CC(=O)O)CCN(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL780 207592 None 64 Human Functional pAC50 = 5.9 5.9 1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 393 16 5 8 -2.7 O=C(O)CN(CCN(CC(=O)O)CC(=O)O)CCN(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
1024 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
5359318 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
5359318.0 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
556 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
65326 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
65326.0 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
9294 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
9294.0 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
CHEMBL1523964 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
CHEMBL211456 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
CHEMBL2146102 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
DB01364 1571 None 12 Human Functional pAC50 = 4.9 4.9 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 165 3 2 2 1.3 CN[C@H]([C@@H](c1ccccc1)O)C 10.1038/s41467-023-40064-9
119570 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
119570.0 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2233 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
953 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
CHEMBL301265 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
DB00413 3159 None 58 Human Functional pAC50 = 4.9 4.9 -10000 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 211 3 2 4 1.6 CCCN[C@H]1CCc2c(C1)sc(n2)N 10.1038/s41467-023-40064-9
2782 32008 None 48 Human Functional pAC50 = 4.9 4.9 -3801 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL1407943 32008 None 48 Human Functional pAC50 = 4.9 4.9 -3801 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
CHEMBL3216363 32008 None 48 Human Functional pAC50 = 4.9 4.9 -3801 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 3 4.3 Clc1ccc(Cn2c(CN3CCCC3)nc3ccccc32)cc1 10.1038/s41467-023-40064-9
4528 98179 None 50 Human Functional pAC50 = 4.9 4.9 -181 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
CHEMBL273575 98179 None 50 Human Functional pAC50 = 4.9 4.9 -181 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 238 1 1 2 2.8 CN1Cc2c(N)cccc2C(c2ccccc2)C1 10.1038/s41467-023-40064-9
5311017 120668 None 8 Human Functional pAC50 = 4.9 4.9 -13 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
5311017.0 120668 None 8 Human Functional pAC50 = 4.9 4.9 -13 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3545985 120668 None 8 Human Functional pAC50 = 4.9 4.9 -13 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00865 120668 None 8 Human Functional pAC50 = 4.9 4.9 -13 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 239 5 0 1 3.8 C[C@@H](Cc1ccccc1)N(C)Cc1ccccc1 10.1038/s41467-023-40064-9
26248 161633 None 72 Human Functional pAC50 = 4.9 4.9 -1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
CHEMBL41286 161633 None 72 Human Functional pAC50 = 4.9 4.9 -1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
16119814 56359 None 20 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1093 23 16 18 -3.3 CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@H]([C@H](O)CCN)NC(=O)[C@H]([C@H](O)[C@@H](O)c2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H]([C@@H](C)O)NC1=O 10.1038/s41467-023-40064-9
CHEMBL1630575 56359 None 20 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 1093 23 16 18 -3.3 CC[C@H](C)C[C@H](C)CCCCCCCCC(=O)N[C@H]1C[C@@H](O)[C@@H](NCCN)NC(=O)[C@@H]2[C@@H](O)CCN2C(=O)[C@H]([C@H](O)CCN)NC(=O)[C@H]([C@H](O)[C@@H](O)c2ccc(O)cc2)NC(=O)[C@@H]2C[C@@H](O)CN2C(=O)[C@H]([C@@H](C)O)NC1=O 10.1038/s41467-023-40064-9
443869 78170 None 28 Human Functional pAC50 = 5.9 5.9 1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2103761 78170 None 28 Human Functional pAC50 = 5.9 5.9 1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 7 1 8 3.8 COC(=O)C1=C(C)NC(C)=C(C(=O)O[C@H]2CCN(Cc3ccccc3)C2)[C@H]1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
68555 103167 None 14 Human Functional pAC50 = 6.9 6.9 -3 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.9 6.9 -3 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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
15942715 78222 None 18 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 5 1 5 4.0 CCCCOC(=O)C(=O)[C@H]1[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL2105087 78222 None 18 Human Functional pAC50 = 4.9 4.9 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 446 5 1 5 4.0 CCCCOC(=O)C(=O)[C@H]1[C@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@H]3[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
6918178 14450 None 36 Human Functional pAC50 = 4.9 4.9 1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 484 4 1 5 4.1 CCC(=O)O[C@]1(C(=O)CCl)[C@@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1200908 14450 None 36 Human Functional pAC50 = 4.9 4.9 1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 484 4 1 5 4.1 CCC(=O)O[C@]1(C(=O)CCl)[C@@H](C)C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@@]21C 10.1038/s41467-023-40064-9
667492 43919 None 36 Human Functional pAC50 = 4.9 4.9 1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 234 1 2 3 0.2 CN1C(=O)/C(=N\NC(N)=S)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1512080 43919 None 36 Human Functional pAC50 = 4.9 4.9 1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 234 1 2 3 0.2 CN1C(=O)/C(=N\NC(N)=S)c2ccccc21 10.1038/s41467-023-40064-9
3652 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
57 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
60809.0 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
CHEMBL21536 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
DB15357 4097 None 50 Human Functional pAC50 = 4.9 4.9 -2089 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 281 7 0 5 3.2 CCCCCCOc1nsnc1C1=CCCN(C1)C 10.1038/s41467-023-40064-9
213046 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
213046.0 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2385 None 44 Human Functional pAC50 = 6.9 6.9 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
3351 95055 None 40 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
CHEMBL254857 95055 None 40 Human Functional pAC50 = 4.9 4.9 -2 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 388 5 0 5 2.8 O=C(COc1ccc(Cl)cc1)N1CCN(Cc2ccc3c(c2)OCO3)CC1 10.1038/s41467-023-40064-9
6917906 67795 None 17 Human Functional pAC50 = 4.9 4.9 -6 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 887 35 10 12 1.7 CCCCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)CC[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](C)O[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1NC(C)=O)C(N)=O)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1908331 67795 None 17 Human Functional pAC50 = 4.9 4.9 -6 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 887 35 10 12 1.7 CCCCCCCCCCCCCCCCCC(=O)NCCCC[C@H](NC(=O)CC[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](C)O[C@H]1[C@H](O)[C@@H](CO)OC(O)[C@@H]1NC(C)=O)C(N)=O)C(=O)O 10.1038/s41467-023-40064-9
98941 46964 None 13 Human Functional pAC50 = 4.9 4.9 -66 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL154126 46964 None 13 Human Functional pAC50 = 4.9 4.9 -66 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 457 7 0 4 6.3 COc1ccc2c(c1)OC(C)(C)C(c1ccccc1)C2c1ccc(OCCN2CCCC2)cc1 10.1038/s41467-023-40064-9
CHEMBL4743867 216518 None 10 Human Functional pAC50 = 4.9 4.9 -4466 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL None None None OCCN1CCN(CCC=C2c3ccccc3Sc3ccc(C(F)(F)F)cc32)CC1 10.1038/s41467-023-40064-9
3474 38112 None 43 Human Functional pAC50 = 4.9 4.9 -4 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 6 3 6 3.1 O=C(OCC(O)CO)c1ccccc1Nc1ccnc2cc(Cl)ccc12 10.1038/s41467-023-40064-9
CHEMBL146095 38112 None 43 Human Functional pAC50 = 4.9 4.9 -4 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 6 3 6 3.1 O=C(OCC(O)CO)c1ccccc1Nc1ccnc2cc(Cl)ccc12 10.1038/s41467-023-40064-9
49843517 78325 None 41 Human Functional pAC50 = 4.9 4.9 -40 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
CHEMBL2107831 78325 None 41 Human Functional pAC50 = 4.9 4.9 -40 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 590 13 2 6 8.5 CCCCCCO[C@@H](C)c1cccc(-c2csc(NC(=O)c3cc(Cl)c(/C=C(\C)C(=O)O)c(Cl)c3)n2)c1OC 10.1038/s41467-023-40064-9
3103 41672 None 36 Human Functional pAC50 = 4.9 4.9 -138 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
3103.0 41672 None 36 Human Functional pAC50 = 4.9 4.9 -138 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1492 41672 None 36 Human Functional pAC50 = 4.9 4.9 -138 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB01146 41672 None 36 Human Functional pAC50 = 4.9 4.9 -138 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 0 2 3.9 CN1CCC(OC(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
16222096 80514 None 50 Human Functional pAC50 = 4.9 4.9 -50 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
CHEMBL2146883 80514 None 50 Human Functional pAC50 = 4.9 4.9 -50 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 4 3 4 3.8 O=C(c1ccc(F)c(F)c1Nc1ccc(I)cc1F)N1CC(O)([C@@H]2CCCCN2)C1 10.1038/s41467-023-40064-9
2580 78426 None 10 Human Functional pAC50 = 4.9 4.9 -660 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL2110775 78426 None 10 Human Functional pAC50 = 4.9 4.9 -660 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 446 6 1 4 4.1 NC(=O)C1(N2CCCCC2)CCN(CCCN2c3ccccc3CCc3ccccc32)CC1 10.1038/s41467-023-40064-9
448537 160344 None 54 Human Functional pAC50 = 4.9 4.9 -54 31
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160344 None 54 Human Functional pAC50 = 4.9 4.9 -54 31
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
16362 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16362.0 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
2172 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
90 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1423 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01100 3125 None 49 Human Functional pAC50 = 6.9 6.9 -14 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 7 1 3 5.9 Fc1ccc(cc1)C(c1ccc(cc1)F)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3634 84142 None 43 Human Functional pAC50 = 5.9 5.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL22077 84142 None 43 Human Functional pAC50 = 5.9 5.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 7 2 5 3.7 CCN(CC)CCNc1ccc(CO)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
3478 5428 None 61 Human Functional pAC50 = 4.9 4.9 -758 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 445 7 3 6 2.1 Cc1cnc(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc2)cn1 10.1038/s41467-023-40064-9
CHEMBL1073 5428 None 61 Human Functional pAC50 = 4.9 4.9 -758 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 445 7 3 6 2.1 Cc1cnc(C(=O)NCCc2ccc(S(=O)(=O)NC(=O)NC3CCCCC3)cc2)cn1 10.1038/s41467-023-40064-9
72287 61081 None 27 Human Functional pAC50 = 7.9 7.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
72287.0 61081 None 27 Human Functional pAC50 = 7.9 7.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1764 61081 None 27 Human Functional pAC50 = 7.9 7.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
DB01403 61081 None 27 Human Functional pAC50 = 7.9 7.9 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 328 5 0 4 4.5 COc1ccc2c(c1)N(C[C@H](C)CN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
19675 51685 None 37 Human Functional pAC50 = 6.9 6.9 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1584 51685 None 37 Human Functional pAC50 = 6.9 6.9 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 7 1 5 5.0 CC(=O)c1ccc2c(c1)N(CCCN1CCC(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2284 3182 None 26 Human Functional pAC50 = 6.9 6.9 -3 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
4926 3182 None 26 Human Functional pAC50 = 6.9 6.9 -3 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
7281 3182 None 26 Human Functional pAC50 = 6.9 6.9 -3 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL564 3182 None 26 Human Functional pAC50 = 6.9 6.9 -3 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00420 3182 None 26 Human Functional pAC50 = 6.9 6.9 -3 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 3 4.2 CN(CCCN1c2ccccc2Sc2c1cccc2)C 10.1038/s41467-023-40064-9
2398 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Functional pAC50 = 5.9 5.9 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
55483 207555 None 29 Human Functional pAC50 = 5.9 5.9 -8 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
CHEMBL77622 207555 None 29 Human Functional pAC50 = 5.9 5.9 -8 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 356 13 4 4 3.6 Oc1ccc(CCNCCCCCCNCCc2ccccc2)cc1O 10.1038/s41467-023-40064-9
2869 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
60 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
60857 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
60857.0 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
CHEMBL1185 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
DB00315 4152 None 54 Human Functional pAC50 = 4.9 4.9 -5011 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 287 5 2 3 1.9 CN(CCc1c[nH]c2c1cc(C[C@H]1COC(=O)N1)cc2)C 10.1038/s41467-023-40064-9
4762 14475 None 14 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 177 1 1 2 1.7 CC1NCCOC1c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201208 14475 None 14 Human Functional pAC50 = 4.9 4.9 1 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 177 1 1 2 1.7 CC1NCCOC1c1ccccc1 10.1038/s41467-023-40064-9
5556 205718 None 15 Human Functional pAC50 = 4.9 4.9 -33 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1038/s41467-023-40064-9
CHEMBL646 205718 None 15 Human Functional pAC50 = 4.9 4.9 -33 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 342 1 0 4 4.2 Cc1nnc2n1-c1ccc(Cl)cc1C(c1ccccc1Cl)=NC2 10.1038/s41467-023-40064-9
2218 15289 None 20 Human Functional pAC50 = 4.9 4.9 -5 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
CHEMBL1213033 15289 None 20 Human Functional pAC50 = 4.9 4.9 -5 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 8 0 2 4.4 CCN(CC)CCCN(c1ccccc1)C1Cc2ccccc2C1 10.1038/s41467-023-40064-9
2780 110592 None 24 Human Functional pAC50 = 4.9 4.9 -1479 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
2780.0 110592 None 24 Human Functional pAC50 = 4.9 4.9 -1479 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL325109 110592 None 24 Human Functional pAC50 = 4.9 4.9 -1479 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
DB13511 110592 None 24 Human Functional pAC50 = 4.9 4.9 -1479 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 373 5 2 4 3.3 COc1cc(N)c(Cl)cc1C(=O)NC1CCN(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
9417 133581 None 40 Human Functional pAC50 = 4.9 4.9 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL1524185 133581 None 40 Human Functional pAC50 = 4.9 4.9 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
CHEMBL370753 133581 None 40 Human Functional pAC50 = 4.9 4.9 -33 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 363 6 1 4 3.3 OCCN1CCN(CCCN2c3ccccc3C=Cc3ccccc32)CC1 10.1038/s41467-023-40064-9
5365247 138516 None 29 Human Functional pAC50 = 4.9 4.9 -100 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
CHEMBL37744 138516 None 29 Human Functional pAC50 = 4.9 4.9 -100 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 316 4 0 2 3.8 CN(C)C/C=C(/c1ccc(Br)cc1)c1cccnc1 10.1038/s41467-023-40064-9
2318 154946 None 18 Human Functional pAC50 = 4.9 4.9 -20 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL400599 154946 None 18 Human Functional pAC50 = 4.9 4.9 -20 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 351 7 1 3 4.1 CC(Cc1cccc(C(F)(F)F)c1)NCCOC(=O)c1ccccc1 10.1038/s41467-023-40064-9
2771 197264 None 50 Human Functional pAC50 = 4.9 4.9 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 197264 None 50 Human Functional pAC50 = 4.9 4.9 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 197264 None 50 Human Functional pAC50 = 4.9 4.9 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
3950 189617 None 67 Human Functional pAC50 = 4.9 4.9 -4 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 233 4 1 3 2.3 O=NN(CCCl)C(=O)NC1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL514 189617 None 67 Human Functional pAC50 = 4.9 4.9 -4 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 233 4 1 3 2.3 O=NN(CCCl)C(=O)NC1CCCCC1 10.1038/s41467-023-40064-9
37 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746.0 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 778 None 41 Human Functional pAC50 = 6.9 6.9 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
1599 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
3955.0 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7215 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL841 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00836 2341 None 28 Human Functional pAC50 = 4.9 4.9 -7585 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 476 7 1 3 5.1 Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
2723 154135 None 63 Human Functional pAC50 = 4.9 4.9 -7 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl 10.1038/s41467-023-40064-9
CHEMBL398440 154135 None 63 Human Functional pAC50 = 4.9 4.9 -7 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 156 0 1 1 2.7 Cc1cc(O)cc(C)c1Cl 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Functional pAC50 = 6.8 6.8 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
5351322 94844 None 30 Human Functional pAC50 = 5.8 5.8 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL25336 94844 None 30 Human Functional pAC50 = 5.8 5.8 1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 4 4 8 1.8 C(=N/NC1=NCCN1)\c1c2ccccc2c(/C=N/NC2=NCCN2)c2ccccc12 10.1038/s41467-023-40064-9
3117 210300 None 60 Human Functional pAC50 = 4.8 4.8 -20 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
CHEMBL964 210300 None 60 Human Functional pAC50 = 4.8 4.8 -20 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 4 0 4 3.6 CCN(CC)C(=S)SSC(=S)N(CC)CC 10.1038/s41467-023-40064-9
9818306 14424 None 13 Human Functional pAC50 = 4.8 4.8 -2 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 1 3 3.8 CC(=O)Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](O)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL1200430 14424 None 13 Human Functional pAC50 = 4.8 4.8 -2 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 1 3 3.8 CC(=O)Oc1ccc2c(c1)CC[C@@H]1[C@@H]2CC[C@]2(C)[C@@H](O)CC[C@@H]12 10.1038/s41467-023-40064-9
2398 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2801.0 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
701 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL415 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB01242 954 None 43 Human Functional pAC50 = 7.8 7.8 -72 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 4 0 2 4.5 CN(CCCN1c2ccccc2CCc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Functional pAC50 = 6.8 6.8 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
1530 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
3827.0 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
7206 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
CHEMBL534 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
DB00920 2182 None 36 Human Functional pAC50 = 4.8 4.8 -912 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 0 0 3 4.0 CN1CCC(=C2c3ccccc3CC(=O)c3c2ccs3)CC1 10.1038/s41467-023-40064-9
243 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
3052762 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
3052762.0 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
3502 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
CHEMBL117287 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
DB06480 3202 None 61 Human Functional pAC50 = 4.8 4.8 -1288 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 367 6 2 5 2.1 COCCCN1CCC(CC1)NC(=O)c1cc(Cl)c(c2c1OCC2)N 10.1038/s41467-023-40064-9
2351 4301 None 35 Human Functional pAC50 = 4.8 4.8 -3 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1008 4301 None 35 Human Functional pAC50 = 4.8 4.8 -3 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1257078 4301 None 35 Human Functional pAC50 = 4.8 4.8 -3 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 366 10 0 3 4.8 CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1 10.1038/s41467-023-40064-9
21772 78430 None 26 Human Functional pAC50 = 4.8 4.8 -1000 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
CHEMBL2110816 78430 None 26 Human Functional pAC50 = 4.8 4.8 -1000 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 293 4 0 1 4.5 CC(CC1c2ccccc2CCc2ccccc21)CN(C)C 10.1038/s41467-023-40064-9
4413 98126 None 43 Human Functional pAC50 = 4.8 4.8 -4 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
CHEMBL273264 98126 None 43 Human Functional pAC50 = 4.8 4.8 -4 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 347 4 5 4 2.6 N=C(N)Nc1ccc(C(=O)Oc2ccc3cc(C(=N)N)ccc3c2)cc1 10.1038/s41467-023-40064-9
60151560 167540 None 37 Human Functional pAC50 = 4.8 4.8 -1 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 439 11 1 5 5.3 CCO[C@@H](Cc1ccc(OCCn2c(C)ccc2-c2ccc(SC)cc2)cc1)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL4297530 167540 None 37 Human Functional pAC50 = 4.8 4.8 -1 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 439 11 1 5 5.3 CCO[C@@H](Cc1ccc(OCCn2c(C)ccc2-c2ccc(SC)cc2)cc1)C(=O)O 10.1038/s41467-023-40064-9
216239 23803 None 71 Human Functional pAC50 = 4.8 4.8 -8 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1200485 23803 None 71 Human Functional pAC50 = 4.8 4.8 -8 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
CHEMBL1336 23803 None 71 Human Functional pAC50 = 4.8 4.8 -8 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 464 5 3 4 5.6 CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3ccc(Cl)c(C(F)(F)F)c3)cc2)ccn1 10.1038/s41467-023-40064-9
1830 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
207 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
23897.0 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
CHEMBL460 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
DB01618 2590 None 33 Human Functional pAC50 = 4.8 4.8 -416 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 2.0 CCc1c(C)[nH]c2c1C(=O)C(CC2)CN1CCOCC1 10.1038/s41467-023-40064-9
196122 112651 None 39 Human Functional pAC50 = 4.8 4.8 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 478 13 1 6 4.5 CCOC1O[C@H]([C@@H](COCc2ccccc2)OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1O 10.1038/s41467-023-40064-9
CHEMBL3301681 112651 None 39 Human Functional pAC50 = 4.8 4.8 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 478 13 1 6 4.5 CCOC1O[C@H]([C@@H](COCc2ccccc2)OCc2ccccc2)[C@H](OCc2ccccc2)[C@H]1O 10.1038/s41467-023-40064-9
392622 56328 None 57 Human Functional pAC50 = 4.8 4.8 -8 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Functional pAC50 = 4.8 4.8 -8 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
1570 57315 None 64 Human Functional pAC50 = 5.8 5.8 2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
CHEMBL1650619 57315 None 64 Human Functional pAC50 = 5.8 5.8 2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 127 0 1 3 1.5 On1ccccc1=S 10.1038/s41467-023-40064-9
1548955 88615 None 14 Human Functional pAC50 = 4.8 4.8 -43 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2800 88615 None 14 Human Functional pAC50 = 4.8 4.8 -43 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL2355051 88615 None 14 Human Functional pAC50 = 4.8 4.8 -43 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 405 9 0 2 6.6 CCN(CC)CCOc1ccc(C(=C(Cl)c2ccccc2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
1155 1629 None 38 Human Functional pAC50 = 5.8 5.8 -363 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.8 5.8 -363 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.8 5.8 -363 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.8 5.8 -363 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.8 5.8 -363 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
9270 14435 None 44 Human Functional pAC50 = 4.8 4.8 -5 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 384 2 0 4 4.4 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=C[C@@H](OC(C)=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1200624 14435 None 44 Human Functional pAC50 = 4.8 4.8 -5 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 384 2 0 4 4.4 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=C[C@@H](OC(C)=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Functional pAC50 = 6.8 6.8 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Functional pAC50 = 6.8 6.8 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Functional pAC50 = 6.8 6.8 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Functional pAC50 = 6.8 6.8 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
60663 175773 None 30 Human Functional pAC50 = 5.8 5.8 -8 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1421212 175773 None 30 Human Functional pAC50 = 5.8 5.8 -8 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1534525 175773 None 30 Human Functional pAC50 = 5.8 5.8 -8 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL45816 175773 None 30 Human Functional pAC50 = 5.8 5.8 -8 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
5994 4643 None 51 Human Functional pAC50 = 4.8 4.8 -5 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL103 4643 None 51 Human Functional pAC50 = 4.8 4.8 -5 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 1 0 2 4.7 CC(=O)[C@H]1CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@]4(C)[C@H]3CC[C@]12C 10.1038/s41467-023-40064-9
4034 55838 None 37 Human Functional pAC50 = 4.8 4.8 -12 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
4034.0 55838 None 37 Human Functional pAC50 = 4.8 4.8 -12 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1623 55838 None 37 Human Functional pAC50 = 4.8 4.8 -12 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
DB00737 55838 None 37 Human Functional pAC50 = 4.8 4.8 -12 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 0 2 5.6 Cc1cccc(CN2CCN(C(c3ccccc3)c3ccc(Cl)cc3)CC2)c1 10.1038/s41467-023-40064-9
441383 20340 None 41 Human Functional pAC50 = 4.8 4.8 -165 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1306 20340 None 41 Human Functional pAC50 = 4.8 4.8 -165 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 531 8 0 8 4.5 CC(C)N1CCN(c2ccc(OC[C@H]3CO[C@](Cn4cncn4)(c4ccc(Cl)cc4Cl)O3)cc2)CC1 10.1038/s41467-023-40064-9
2470 3653 None 40 Human Functional pAC50 = 5.8 5.8 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 None 40 Human Functional pAC50 = 5.8 5.8 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 None 40 Human Functional pAC50 = 5.8 5.8 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 None 40 Human Functional pAC50 = 5.8 5.8 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 None 40 Human Functional pAC50 = 5.8 5.8 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5440 28732 None 28 Human Functional pAC50 = 5.8 5.8 -1995 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28732 None 28 Human Functional pAC50 = 5.8 5.8 -1995 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28732 None 28 Human Functional pAC50 = 5.8 5.8 -1995 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28732 None 28 Human Functional pAC50 = 5.8 5.8 -1995 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
3926 209699 None 30 Human Functional pAC50 = 5.8 5.8 -2 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL92870 209699 None 30 Human Functional pAC50 = 5.8 5.8 -2 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 491 9 1 3 5.8 Cc1cccc(C)c1NC(=O)CN1CCN(CCCC(c2ccc(F)cc2)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
31703 194829 None 40 Human Functional pAC50 = 4.8 4.8 -25 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL359744 194829 None 40 Human Functional pAC50 = 4.8 4.8 -25 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL53463 194829 None 40 Human Functional pAC50 = 4.8 4.8 -25 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
24826799 10802 None 64 Human Functional pAC50 = 4.8 4.8 -50 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
CHEMBL1171837 10802 None 64 Human Functional pAC50 = 4.8 4.8 -50 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 532 4 1 6 4.5 Cc1ccc(C(=O)Nc2ccc(CN3CCN(C)CC3)c(C(F)(F)F)c2)cc1C#Cc1cnc2cccnn12 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 4.8 4.8 -5 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Functional pAC50 = 4.8 4.8 -5 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
5584 205669 None 29 Human Functional pAC50 = 6.8 6.8 -9 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
5584.0 205669 None 29 Human Functional pAC50 = 6.8 6.8 -9 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL644 205669 None 29 Human Functional pAC50 = 6.8 6.8 -9 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB00726 205669 None 29 Human Functional pAC50 = 6.8 6.8 -9 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 294 4 0 2 4.1 CC(CN(C)C)CN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
4735 197545 None 57 Human Functional pAC50 = 4.8 4.8 -199 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL361506 197545 None 57 Human Functional pAC50 = 4.8 4.8 -199 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL55 197545 None 57 Human Functional pAC50 = 4.8 4.8 -199 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 10 4 4 2.9 N=C(N)c1ccc(OCCCCCOc2ccc(C(=N)N)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL508338 189074 None 0 Human Functional pAC50 = 4.8 4.8 -181 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL None None None None 10.1038/s41467-023-40064-9
1712 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
4078 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
4078.0 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
7227 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
CHEMBL1088 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
DB00933 2492 None 34 Human Functional pAC50 = 7.8 7.8 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 4 0 4 4.9 CN1CCCCC1CCN1c2ccccc2Sc2c1cc(cc2)S(=O)C 10.1038/s41467-023-40064-9
2865 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854.0 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 None 47 Human Functional pAC50 = 7.8 7.8 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
10531 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
10531.0 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
121 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
888 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL1732 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00320 1420 None 13 Human Functional pAC50 = 5.8 5.8 -301 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 583 4 3 6 2.1 CN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
2286 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
4927.0 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7282 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL643 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01069 3183 None 36 Human Functional pAC50 = 5.8 5.8 -37 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 3 0 3 4.2 CN(C(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
56959 31564 None 60 Human Functional pAC50 = 5.8 5.8 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1404 31564 None 60 Human Functional pAC50 = 5.8 5.8 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
CHEMBL1526084 31564 None 60 Human Functional pAC50 = 5.8 5.8 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 9 2 6 2.3 COc1ccccc1OCC(O)CN1CCN(CC(=O)Nc2c(C)cccc2C)CC1 10.1038/s41467-023-40064-9
213 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
2717 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
5533.0 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL621 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
DB00656 3853 None 34 Human Functional pAC50 = 5.8 5.8 -5 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 371 5 0 6 2.4 Clc1cccc(c1)N1CCN(CC1)CCCn1nc2n(c1=O)cccc2 10.1038/s41467-023-40064-9
6231 29778 None 23 Human Functional pAC50 = 4.8 4.8 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 0 1 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=C(CCC(=O)C4)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1387 29778 None 23 Human Functional pAC50 = 4.8 4.8 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 0 1 2 3.6 C#C[C@]1(O)CC[C@H]2[C@@H]3CCC4=C(CCC(=O)C4)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
2247 505 None 55 Human Functional pAC50 = 4.8 4.8 -26 42
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Functional pAC50 = 4.8 4.8 -26 42
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Functional pAC50 = 4.8 4.8 -26 42
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Functional pAC50 = 4.8 4.8 -26 42
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Functional pAC50 = 4.8 4.8 -26 42
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
10180 98923 None 36 Human Functional pAC50 = 4.8 4.8 -33 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
CHEMBL279014 98923 None 36 Human Functional pAC50 = 4.8 4.8 -33 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 6 1 4 4.5 CCN(CC)CCNc1ccc(C)c2sc3ccccc3c(=O)c12 10.1038/s41467-023-40064-9
9324 9240 None 40 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 0 4 4.8 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL110691 9240 None 40 Human Functional pAC50 = 4.8 4.8 -3 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 0 4 4.8 CC(=O)O[C@]1(C(C)=O)CC[C@H]2[C@@H]3C=C(Cl)C4=CC(=O)CC[C@]4(C)[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
1662 188812 None 53 Human Functional pAC50 = 4.8 4.8 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 162 4 3 3 -0.3 CC(O)(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
CHEMBL50444 188812 None 53 Human Functional pAC50 = 4.8 4.8 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 162 4 3 3 -0.3 CC(O)(CC(=O)O)CC(=O)O 10.1038/s41467-023-40064-9
25151352 140693 None 56 Human Functional pAC50 = 5.8 5.8 -4 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
CHEMBL3813873 140693 None 56 Human Functional pAC50 = 5.8 5.8 -4 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 417 5 2 4 5.2 FC(F)(F)c1ccc(CNc2ccc(Cc3c[nH]c4ncc(Cl)cc34)cn2)cn1 10.1038/s41467-023-40064-9
4046 2483 None 21 Human Functional pAC50 = 4.8 4.8 -35 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
4252 2483 None 21 Human Functional pAC50 = 4.8 4.8 -35 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
CHEMBL416956 2483 None 21 Human Functional pAC50 = 4.8 4.8 -35 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
DB00358 2483 None 21 Human Functional pAC50 = 4.8 4.8 -35 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 378 2 2 3 4.4 OC(c1cc(nc2c1cccc2C(F)(F)F)C(F)(F)F)C1CCCCN1 10.1038/s41467-023-40064-9
54454 5260 None 48 Human Functional pAC50 = 4.7 4.7 -7 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
CHEMBL1064 5260 None 48 Human Functional pAC50 = 4.7 4.7 -7 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 418 6 1 5 4.6 CCC(C)(C)C(=O)O[C@H]1C[C@@H](C)C=C2C=C[C@H](C)[C@H](CC[C@@H]3C[C@@H](O)CC(=O)O3)[C@H]21 10.1038/s41467-023-40064-9
9822750 78440 None 44 Human Functional pAC50 = 4.7 4.7 -4 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL2111097 78440 None 44 Human Functional pAC50 = 4.7 4.7 -4 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)[C@@H]1c1ccccc1Cl 10.1038/s41467-023-40064-9
119369 2606 None 50 Human Functional pAC50 = 4.7 4.7 -602 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
2197 2606 None 50 Human Functional pAC50 = 4.7 4.7 -602 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
4004 2606 None 50 Human Functional pAC50 = 4.7 4.7 -602 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL420762 2606 None 50 Human Functional pAC50 = 4.7 4.7 -602 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 4 1 3 5.3 O=C(N1CCCC(c2c1cccc2)N(C)C)c1ccc(cc1)NC(=O)c1ccccc1C 10.1038/s41467-023-40064-9
2005 78259 None 59 Human Functional pAC50 = 4.7 4.7 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 173 6 2 2 0.8 CC(=O)NCCCCCC(=O)O 10.1038/s41467-023-40064-9
CHEMBL2105922 78259 None 59 Human Functional pAC50 = 4.7 4.7 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 173 6 2 2 0.8 CC(=O)NCCCCCC(=O)O 10.1038/s41467-023-40064-9
2162 41527 None 58 Human Functional pAC50 = 5.7 5.7 -5 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
CHEMBL1491 41527 None 58 Human Functional pAC50 = 5.7 5.7 -5 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 408 8 2 7 2.3 CCOC(=O)C1=C(COCCN)NC(C)=C(C(=O)OC)C1c1ccccc1Cl 10.1038/s41467-023-40064-9
12555 17968 None 39 Human Functional pAC50 = 4.7 4.7 -38 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
CHEMBL12610 17968 None 39 Human Functional pAC50 = 4.7 4.7 -38 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 7 0 4 3.4 CN(C)CCCOc1nn(Cc2ccccc2)c2ccccc12 10.1038/s41467-023-40064-9
10133 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
145714624 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
4361 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
608 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL240597 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
DB06777 910 None 49 Human Functional pAC50 = 4.7 4.7 -6 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 4 3 3 4.5 O[C@@H]1CC[C@]2([C@@H](C1)C[C@H]([C@@H]1[C@@H]2CC[C@]2([C@H]1CC[C@@H]2[C@@H](CCC(=O)O)C)C)O)C 10.1038/s41467-023-40064-9
657202 12534 None 3 Human Functional pAC50 = 4.7 4.7 -524 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
CHEMBL1186610 12534 None 3 Human Functional pAC50 = 4.7 4.7 -524 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 282 6 0 2 3.5 CCCC(CCC)C(=O)O[C@H]1C[C@H]2CC[C@@H](C1)[N+]2(C)C 10.1038/s41467-023-40064-9
9911830 19155 None 57 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 454 6 2 7 5.6 COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL1289494 19155 None 57 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 454 6 2 7 5.6 COc1cc2nccc(Oc3ccc(NC(=O)Nc4cc(C)on4)c(Cl)c3)c2cc1OC 10.1038/s41467-023-40064-9
5281718 34259 None 55 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 6 8 0.4 OC[C@H]1O[C@@H](Oc2cc(O)cc(/C=C/c3ccc(O)cc3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL142652 34259 None 55 Human Functional pAC50 = 4.7 4.7 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 5 6 8 0.4 OC[C@H]1O[C@@H](Oc2cc(O)cc(/C=C/c3ccc(O)cc3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
4041 99565 None 9 Human Functional pAC50 = 4.7 4.7 -19 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 270 1 0 2 3.6 CN1CCN=C(c2ccccc2)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
CHEMBL28333 99565 None 9 Human Functional pAC50 = 4.7 4.7 -19 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 270 1 0 2 3.6 CN1CCN=C(c2ccccc2)c2cc(Cl)ccc21 10.1038/s41467-023-40064-9
2695 3841 None 53 Human Functional pAC50 = 5.7 5.7 -2 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
5504 3841 None 53 Human Functional pAC50 = 5.7 5.7 -2 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
7310 3841 None 53 Human Functional pAC50 = 5.7 5.7 -2 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL770 3841 None 53 Human Functional pAC50 = 5.7 5.7 -2 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00797 3841 None 53 Human Functional pAC50 = 5.7 5.7 -2 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 160 2 1 2 1.2 c1ccc(cc1)CC1=NCCN1 10.1038/s41467-023-40064-9
45138674 16653 None 45 Human Functional pAC50 = 5.7 5.7 1 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
CHEMBL1241951 16653 None 45 Human Functional pAC50 = 5.7 5.7 1 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 572 6 1 7 5.7 COc1cccc(N2CCN(C3=Nc4c(F)cccc4[C@H](CC(=O)O)N3c3cc(C(F)(F)F)ccc3OC)CC2)c1 10.1038/s41467-023-40064-9
8569 22651 None 59 Human Functional pAC50 = 4.7 4.7 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 244 3 2 4 2.3 COc1ccc(C(=O)c2ccccc2O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1326877 22651 None 59 Human Functional pAC50 = 4.7 4.7 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 244 3 2 4 2.3 COc1ccc(C(=O)c2ccccc2O)c(O)c1 10.1038/s41467-023-40064-9
24821094 67115 None 58 Human Functional pAC50 = 4.7 4.7 -6 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
CHEMBL1873475 67115 None 58 Human Functional pAC50 = 4.7 4.7 -6 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
3658 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
517 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
5709.0 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
CHEMBL312448 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
DB06694 4107 None 38 Human Functional pAC50 = 8.6 8.6 1 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 244 2 1 2 3.1 Cc1cc(cc(c1CC1=NCCN1)C)C(C)(C)C 10.1038/s41467-023-40064-9
1028 291 None 40 Human Functional pAC50 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
2146 3100 None 45 Human Functional pAC50 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.6 8.6 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
4151 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125.0 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
150 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
1764 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
8226.0 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
CHEMBL1201356 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
DB00353 2509 None 14 Human Functional pAC50 = 7.7 7.7 -194 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 339 4 3 3 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CO 10.1038/s41467-023-40064-9
135398737 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
135398737.0 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
38 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
722 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL42 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
DB00363 958 None 57 Human Functional pAC50 = 7.7 7.7 -17 43
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 0 1 4 3.7 CN1CCN(CC1)C1=Nc2cc(Cl)ccc2Nc2c1cccc2 10.1038/s41467-023-40064-9
31729 208242 None 9 Human Functional pAC50 = 5.7 5.7 -131 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL83063 208242 None 9 Human Functional pAC50 = 5.7 5.7 -131 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 6 4 4 2.4 CC(NCCc1ccc(O)cc1)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
202 1508 None 46 Human Functional pAC50 = 4.7 4.7 -3 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
60835 1508 None 46 Human Functional pAC50 = 4.7 4.7 -3 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
972 1508 None 46 Human Functional pAC50 = 4.7 4.7 -3 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL1175 1508 None 46 Human Functional pAC50 = 4.7 4.7 -3 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
DB00476 1508 None 46 Human Functional pAC50 = 4.7 4.7 -3 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 297 6 1 3 4.6 CNCC[C@@H](c1cccs1)Oc1cccc2c1cccc2 10.1038/s41467-023-40064-9
448537 160344 None 54 Human Functional pAC50 = 4.7 4.7 -54 31
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL411 160344 None 54 Human Functional pAC50 = 4.7 4.7 -54 31
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 268 4 2 2 4.8 CC/C(=C(/CC)c1ccc(O)cc1)c1ccc(O)cc1 10.1038/s41467-023-40064-9
3035016 12598 None 44 Human Functional pAC50 = 4.7 4.7 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 3 5 10 0.6 CC(=O)[C@]1(N)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](O)[C@H](O)CO2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
CHEMBL1186894 12598 None 44 Human Functional pAC50 = 4.7 4.7 -1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 3 5 10 0.6 CC(=O)[C@]1(N)Cc2c(O)c3c(c(O)c2[C@@H](O[C@H]2C[C@H](O)[C@H](O)CO2)C1)C(=O)c1ccccc1C3=O 10.1038/s41467-023-40064-9
89683805 154523 None 55 Human Functional pAC50 = 4.7 4.7 -6760 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 473 6 3 8 4.3 CC(C)(O)CNc1nc(Nc2ccnc(C(F)(F)F)c2)nc(-c2cccc(C(F)(F)F)n2)n1 10.1038/s41467-023-40064-9
CHEMBL3989908 154523 None 55 Human Functional pAC50 = 4.7 4.7 -6760 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 473 6 3 8 4.3 CC(C)(O)CNc1nc(Nc2ccnc(C(F)(F)F)c2)nc(-c2cccc(C(F)(F)F)n2)n1 10.1038/s41467-023-40064-9
44439 165782 None 16 Human Functional pAC50 = 4.7 4.7 -63 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 377 9 3 5 2.8 COc1ccc(CCC(C)NCC(O)c2ccc(O)c([S+](C)[O-])c2)cc1 10.1038/s41467-023-40064-9
CHEMBL424518 165782 None 16 Human Functional pAC50 = 4.7 4.7 -63 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 377 9 3 5 2.8 COc1ccc(CCC(C)NCC(O)c2ccc(O)c([S+](C)[O-])c2)cc1 10.1038/s41467-023-40064-9
444795 140086 None 62 Human Functional pAC50 = 4.7 4.7 -57 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 10.1038/s41467-023-40064-9
CHEMBL38 140086 None 62 Human Functional pAC50 = 4.7 4.7 -57 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 5 1 1 5.6 CC1=C(/C=C/C(C)=C/C=C/C(C)=C/C(=O)O)C(C)(C)CCC1 10.1038/s41467-023-40064-9
5489013 57421 None 24 Human Functional pAC50 = 6.7 6.7 -21 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 8 2 4 3.0 COc1cccc(C(=O)CCN[C@@H](C)[C@H](O)c2ccccc2)c1 10.1038/s41467-023-40064-9
CHEMBL1651913 57421 None 24 Human Functional pAC50 = 6.7 6.7 -21 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 8 2 4 3.0 COc1cccc(C(=O)CCN[C@@H](C)[C@H](O)c2ccccc2)c1 10.1038/s41467-023-40064-9
1923 104780 None 79 Human Functional pAC50 = 4.7 4.7 -3 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 1 2 1.9 Oc1cccc2cccnc12 10.1038/s41467-023-40064-9
CHEMBL310555 104780 None 79 Human Functional pAC50 = 4.7 4.7 -3 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 1 2 1.9 Oc1cccc2cccnc12 10.1038/s41467-023-40064-9
1753 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
483 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
6082 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
6082.0 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
CHEMBL524 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
DB00723 2504 None 16 Human Functional pAC50 = 7.7 7.7 2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1038/s41467-023-40064-9
2726 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
2726.0 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
621 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
83 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
CHEMBL71 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
DB00477 919 None 48 Human Functional pAC50 = 6.7 6.7 -29 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 4 0 3 4.9 CN(CCCN1c2ccccc2Sc2c1cc(Cl)cc2)C 10.1038/s41467-023-40064-9
135409453 3773 None 26 Human Functional pAC50 = 5.7 5.7 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
226 3773 None 26 Human Functional pAC50 = 5.7 5.7 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
CHEMBL76370 3773 None 26 Human Functional pAC50 = 5.7 5.7 -363 35
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 7 3 3 2.6 CCCCCN=C(N/N=C/c1c[nH]c2c1cc(OC)cc2)N 10.1038/s41467-023-40064-9
214 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
2740 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
5566.0 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
66064 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL422 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
DB00831 3860 None 43 Human Functional pAC50 = 5.7 5.7 -22 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 407 4 0 4 4.9 CN1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)C(F)(F)F 10.1038/s41467-023-40064-9
26248 161633 None 72 Human Functional pAC50 = 4.7 4.7 -1 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
CHEMBL41286 161633 None 72 Human Functional pAC50 = 4.7 4.7 -1 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 368 3 1 7 2.0 CC(=O)Oc1cccc2c1C(=O)c1c(OC(C)=O)cc(C(=O)O)cc1C2=O 10.1038/s41467-023-40064-9
11289 14443 None 47 Human Functional pAC50 = 4.7 4.7 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 380 6 0 3 5.9 COc1ccc(C(Cl)=C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1200761 14443 None 47 Human Functional pAC50 = 4.7 4.7 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 380 6 0 3 5.9 COc1ccc(C(Cl)=C(c2ccc(OC)cc2)c2ccc(OC)cc2)cc1 10.1038/s41467-023-40064-9
2880 98061 None 34 Human Functional pAC50 = 4.7 4.7 -13 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL27289 98061 None 34 Human Functional pAC50 = 4.7 4.7 -13 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 5 0 3 4.6 C=C(c1ccccc1OCc1cccc(Cl)c1)n1ccnc1 10.1038/s41467-023-40064-9
3356 205826 None 57 Human Functional pAC50 = 4.7 4.7 -33 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 414 7 2 4 3.4 O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1200822 205826 None 57 Human Functional pAC50 = 4.7 4.7 -33 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 414 7 2 4 3.4 O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL652 205826 None 57 Human Functional pAC50 = 4.7 4.7 -33 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 414 7 2 4 3.4 O=C(NCC1CCCCN1)c1cc(OCC(F)(F)F)ccc1OCC(F)(F)F 10.1038/s41467-023-40064-9
54684141 210459 None 52 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 270 2 2 3 3.0 C/C(O)=C(\C#N)C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL973 210459 None 52 Human Functional pAC50 = 4.7 4.7 1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 270 2 2 3 3.0 C/C(O)=C(\C#N)C(=O)Nc1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
1499 2091 None 34 Human Functional pAC50 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 5.7 5.7 -44668 38
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1038/s41467-023-40064-9
16564 207453 None 20 Human Functional pAC50 = 4.7 4.7 -144 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
CHEMBL76725 207453 None 20 Human Functional pAC50 = 4.7 4.7 -144 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 207 2 3 3 0.3 N=C(N)NCC1COc2ccccc2O1 10.1038/s41467-023-40064-9
2028 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
359 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
4634 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
4634.0 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
CHEMBL1231 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
DB01062 2979 None 52 Human Functional pAC50 = 4.7 4.7 -10715 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 357 7 1 4 3.3 CCN(CC#CCOC(=O)C(c1ccccc1)(C1CCCCC1)O)CC 10.1038/s41467-023-40064-9
34040 28093 None 52 Human Functional pAC50 = 4.7 4.7 -7244 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
34040.0 28093 None 52 Human Functional pAC50 = 4.7 4.7 -7244 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
CHEMBL1372950 28093 None 52 Human Functional pAC50 = 4.7 4.7 -7244 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
DB00699 28093 None 52 Human Functional pAC50 = 4.7 4.7 -7244 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 483 4 0 6 3.9 CO[C@]12C[C@@H](COC(=O)c3cncc(Br)c3)CN(C)[C@@H]1Cc1cn(C)c3cccc2c13 10.1038/s41467-023-40064-9
3081361 93987 None 66 Human Functional pAC50 = 4.7 4.7 -35 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
CHEMBL24828 93987 None 66 Human Functional pAC50 = 4.7 4.7 -35 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 474 5 1 5 4.4 COc1cc2/c(=N/c3ccc(Br)cc3F)nc[nH]c2cc1OCC1CCN(C)CC1 10.1038/s41467-023-40064-9
5344 173577 None 67 Human Functional pAC50 = 4.7 4.7 -3981 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1038/s41467-023-40064-9
CHEMBL453 173577 None 67 Human Functional pAC50 = 4.7 4.7 -3981 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 267 3 2 5 1.7 Cc1noc(NS(=O)(=O)c2ccc(N)cc2)c1C 10.1038/s41467-023-40064-9
3157 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
3157.0 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1470 None 44 Human Functional pAC50 = 7.7 7.7 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
2142 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775.0 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3096 None 36 Human Functional pAC50 = 6.7 6.7 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
1890 2759 None 31 Human Functional pAC50 = 5.7 5.7 -4 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
4449 2759 None 31 Human Functional pAC50 = 5.7 5.7 -4 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
7247 2759 None 31 Human Functional pAC50 = 5.7 5.7 -4 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
CHEMBL623 2759 None 31 Human Functional pAC50 = 5.7 5.7 -4 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
DB01149 2759 None 31 Human Functional pAC50 = 5.7 5.7 -4 28
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 469 10 0 7 3.6 CCc1nn(c(=O)n1CCOc1ccccc1)CCCN1CCN(CC1)c1cccc(c1)Cl 10.1038/s41467-023-40064-9
10453870 73688 None 45 Human Functional pAC50 = 4.7 4.7 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 4 4 6 2.1 OC[C@H]1O[C@@H](c2ccc(F)c(Cc3cc4ccccc4s3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL2018096 73688 None 45 Human Functional pAC50 = 4.7 4.7 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 4 4 6 2.1 OC[C@H]1O[C@@H](c2ccc(F)c(Cc3cc4ccccc4s3)c2)[C@H](O)[C@@H](O)[C@@H]1O 10.1038/s41467-023-40064-9
9419 35931 None 28 Human Functional pAC50 = 4.7 4.7 -72 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
9419.0 35931 None 28 Human Functional pAC50 = 4.7 4.7 -72 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1442422 35931 None 28 Human Functional pAC50 = 4.7 4.7 -72 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
DB13225 35931 None 28 Human Functional pAC50 = 4.7 4.7 -72 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 295 3 0 3 3.0 CN(C)CCN1C(=O)c2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
4601 209205 None 27 Human Functional pAC50 = 4.6 4.6 -1148 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
4601.0 209205 None 27 Human Functional pAC50 = 4.6 4.6 -1148 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201023 209205 None 27 Human Functional pAC50 = 4.6 4.6 -1148 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL900 209205 None 27 Human Functional pAC50 = 4.6 4.6 -1148 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
DB01173 209205 None 27 Human Functional pAC50 = 4.6 4.6 -1148 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 269 6 0 2 3.7 Cc1ccccc1C(OCCN(C)C)c1ccccc1 10.1038/s41467-023-40064-9
8609 14449 None 44 Human Functional pAC50 = 4.6 4.6 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 229 2 2 4 2.2 Nc1ccc(C(=O)Oc2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL1200868 14449 None 44 Human Functional pAC50 = 4.6 4.6 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 229 2 2 4 2.2 Nc1ccc(C(=O)Oc2ccccc2)c(O)c1 10.1038/s41467-023-40064-9
5205 78216 None 42 Human Functional pAC50 = 6.6 6.6 -2 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
CHEMBL2104895 78216 None 42 Human Functional pAC50 = 6.6 6.6 -2 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 0 0 1 3.8 CN1CCC2=C(C1)c1ccccc1Cc1ccccc12 10.1038/s41467-023-40064-9
1209 1658 None 52 Human Functional pAC50 = 4.6 4.6 -91 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
203 1658 None 52 Human Functional pAC50 = 4.6 4.6 -91 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
3386 1658 None 52 Human Functional pAC50 = 4.6 4.6 -91 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL41 1658 None 52 Human Functional pAC50 = 4.6 4.6 -91 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
DB00472 1658 None 52 Human Functional pAC50 = 4.6 4.6 -91 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 6 1 2 4.4 CNCCC(c1ccccc1)Oc1ccc(cc1)C(F)(F)F 10.1038/s41467-023-40064-9
2202 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
4850.0 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
49 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
CHEMBL1371770 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
DB12478 3132 None 63 Human Functional pAC50 = 4.6 4.6 -389 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 3 0 6 1.5 c1cnc(nc1)N1CCN(CC1)Cc1ccc2c(c1)OCO2 10.1038/s41467-023-40064-9
39941 118370 None 43 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 3 1 3 4.3 CC(C(=O)O)c1ccc2oc(-c3ccc(Cl)cc3)nc2c1 10.1038/s41467-023-40064-9
CHEMBL340978 118370 None 43 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 301 3 1 3 4.3 CC(C(=O)O)c1ccc2oc(-c3ccc(Cl)cc3)nc2c1 10.1038/s41467-023-40064-9
5280453 208429 None 49 Human Functional pAC50 = 4.6 4.6 -5 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL846 208429 None 49 Human Functional pAC50 = 4.6 4.6 -5 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 416 6 3 3 5.7 C=C1/C(=C\C=C2/CCC[C@]3(C)[C@@H]([C@H](C)CCCC(C)(C)O)CC[C@@H]23)C[C@@H](O)C[C@@H]1O 10.1038/s41467-023-40064-9
2749 32651 None 61 Human Functional pAC50 = 4.6 4.6 1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 207 1 1 3 2.4 Cc1cc(C2CCCCC2)n(O)c(=O)c1 10.1038/s41467-023-40064-9
CHEMBL1413 32651 None 61 Human Functional pAC50 = 4.6 4.6 1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 207 1 1 3 2.4 Cc1cc(C2CCCCC2)n(O)c(=O)c1 10.1038/s41467-023-40064-9
9846332 52074 None 27 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 444 2 3 5 2.4 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C(Cl)=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO 10.1038/s41467-023-40064-9
CHEMBL1587228 52074 None 27 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 444 2 3 5 2.4 C[C@@H]1C[C@H]2[C@@H]3C[C@H](F)C4=CC(=O)C(Cl)=C[C@]4(C)[C@@]3(F)[C@@H](O)C[C@]2(C)[C@@]1(O)C(=O)CO 10.1038/s41467-023-40064-9
3157 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
3157.0 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
7170 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
954 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
CHEMBL707 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
DB00590 1470 None 44 Human Functional pAC50 = 6.6 6.6 -38 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 451 4 2 8 1.5 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1COc2c(O1)cccc2 10.1038/s41467-023-40064-9
27901 78236 None 18 Human Functional pAC50 = 4.6 4.6 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL2105458 78236 None 18 Human Functional pAC50 = 4.6 4.6 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 286 4 0 3 3.8 CN1CCC(N(Cc2cccs2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
2993 114756 None 14 Human Functional pAC50 = 4.6 4.6 -177 13
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL121663 114756 None 14 Human Functional pAC50 = 4.6 4.6 -177 13
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL333826 114756 None 14 Human Functional pAC50 = 4.6 4.6 -177 13
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
1343 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519.0 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1889 None 43 Human Functional pAC50 = 7.6 7.6 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
2169 44861 None 29 Human Functional pAC50 = 6.6 6.6 -4 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 44861 None 29 Human Functional pAC50 = 6.6 6.6 -4 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
9853053 120583 None 54 Human Functional pAC50 = 5.6 5.6 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL354541 120583 None 54 Human Functional pAC50 = 5.6 5.6 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 693 10 2 3 8.4 O=C(NC1CCN(CCCCC2(C(=O)NCC(F)(F)F)c3ccccc3-c3ccccc32)CC1)c1ccccc1-c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
93154 5438 None 24 Human Functional pAC50 = 5.6 5.6 -316 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL107360 5438 None 24 Human Functional pAC50 = 5.6 5.6 -316 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 1 0 2 4.0 c1ccc2c(c1)CCc1ccccc1N2C1CN2CCC1CC2 10.1038/s41467-023-40064-9
3735 208689 None 52 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 571 4 2 2 3.7 CCC(Cc1c(I)cc(I)c(N)c1I)C(=O)O 10.1038/s41467-023-40064-9
CHEMBL867 208689 None 52 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 571 4 2 2 3.7 CCC(Cc1c(I)cc(I)c(N)c1I)C(=O)O 10.1038/s41467-023-40064-9
65863 14471 None 40 Human Functional pAC50 = 4.6 4.6 -14 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1201196 14471 None 40 Human Functional pAC50 = 4.6 4.6 -14 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 436 6 0 4 7.0 Clc1ccc(C(Cn2ccnc2)OCc2csc3c(Cl)cccc23)c(Cl)c1 10.1038/s41467-023-40064-9
7547 5506 None 61 Human Functional pAC50 = 5.6 5.6 -3 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 2 2 1 5.3 O=C(Nc1ccc(Cl)cc1)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1076347 5506 None 61 Human Functional pAC50 = 5.6 5.6 -3 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 2 2 1 5.3 O=C(Nc1ccc(Cl)cc1)Nc1ccc(Cl)c(Cl)c1 10.1038/s41467-023-40064-9
65646 121365 None 16 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 6 2 9 0.8 Cc1oc(=O)oc1COC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
CHEMBL3580454 121365 None 16 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 461 6 2 9 0.8 Cc1oc(=O)oc1COC(=O)[C@@H]1N2C(=O)[C@@H](NC(=O)[C@H](N)c3ccccc3)[C@H]2SC1(C)C 10.1038/s41467-023-40064-9
71743 78296 None 47 Human Functional pAC50 = 4.6 4.6 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 3 0 4 3.6 O=C(Oc1ccc2c(c1)CCCN2C(=O)C(Cl)Cl)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2107014 78296 None 47 Human Functional pAC50 = 4.6 4.6 -1 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 353 3 0 4 3.6 O=C(Oc1ccc2c(c1)CCCN2C(=O)C(Cl)Cl)c1ccco1 10.1038/s41467-023-40064-9
5440 28732 None 28 Human Functional pAC50 = 4.6 4.6 -1995 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5440.0 28732 None 28 Human Functional pAC50 = 4.6 4.6 -1995 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1378 28732 None 28 Human Functional pAC50 = 4.6 4.6 -1995 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB00372 28732 None 28 Human Functional pAC50 = 4.6 4.6 -1995 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 399 6 0 5 5.0 CCSc1ccc2c(c1)N(CCCN1CCN(C)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
2705 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
360 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
443879.0 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
CHEMBL1382 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
DB01036 3842 None 44 Human Functional pAC50 = 4.6 4.6 -1288 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 7 1 2 5.3 Cc1ccc(c(c1)[C@@H](c1ccccc1)CCN(C(C)C)C(C)C)O 10.1038/s41467-023-40064-9
104870 98934 None 37 Human Functional pAC50 = 5.6 5.6 -8 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
5374 98934 None 37 Human Functional pAC50 = 5.6 5.6 -8 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
CHEMBL279085 98934 None 37 Human Functional pAC50 = 5.6 5.6 -8 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 209 2 1 4 1.3 C=CCN1CCc2nc(N)sc2CC1 10.1038/s41467-023-40064-9
21722 17999 None 26 Human Functional pAC50 = 4.6 4.6 -16 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
CHEMBL126224 17999 None 26 Human Functional pAC50 = 4.6 4.6 -16 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 284 4 0 2 4.3 CN(C)CCCn1c2c(c3ccccc31)CCCCCC2 10.1038/s41467-023-40064-9
5282219 35878 None 48 Human Functional pAC50 = 4.6 4.6 -4 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 450 12 1 5 5.7 CC(C)=CCOc1ccc(/C=C/C(=O)c2ccc(OCC=C(C)C)cc2OCC(=O)O)cc1 10.1038/s41467-023-40064-9
CHEMBL1441961 35878 None 48 Human Functional pAC50 = 4.6 4.6 -4 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 450 12 1 5 5.7 CC(C)=CCOc1ccc(/C=C/C(=O)c2ccc(OCC=C(C)C)cc2OCC(=O)O)cc1 10.1038/s41467-023-40064-9
16678941 78182 None 61 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 452 5 2 5 4.7 Cc1ccc(NC(=O)C2(c3ccc4c(c3)OC(F)(F)O4)CC2)nc1-c1cccc(C(=O)O)c1 10.1038/s41467-023-40064-9
CHEMBL2103870 78182 None 61 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 452 5 2 5 4.7 Cc1ccc(NC(=O)C2(c3ccc4c(c3)OC(F)(F)O4)CC2)nc1-c1cccc(C(=O)O)c1 10.1038/s41467-023-40064-9
71927 78434 None 13 Human Functional pAC50 = 4.6 4.6 -2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL2106667 78434 None 13 Human Functional pAC50 = 4.6 4.6 -2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL2110922 78434 None 13 Human Functional pAC50 = 4.6 4.6 -2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 202 2 1 3 0.9 COc1cc(N)cn[n+]1-c1ccccc1 10.1038/s41467-023-40064-9
1549120 198942 None 55 Human Functional pAC50 = 4.6 4.6 -16 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL56337 198942 None 55 Human Functional pAC50 = 4.6 4.6 -16 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 319 4 1 4 2.9 CC(/C=C1\SC(=S)N(CC(=O)O)C1=O)=C\c1ccccc1 10.1038/s41467-023-40064-9
24821094 67115 None 58 Human Functional pAC50 = 4.6 4.6 -6 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
CHEMBL1873475 67115 None 58 Human Functional pAC50 = 4.6 4.6 -6 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 440 5 1 7 4.2 C=CC(=O)N1CCC[C@@H](n2nc(-c3ccc(Oc4ccccc4)cc3)c3c(N)ncnc32)C1 10.1038/s41467-023-40064-9
446156 39838 None 23 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 459 11 3 5 4.9 COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL1477 39838 None 23 Human Functional pAC50 = 4.6 4.6 -1 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 459 11 3 5 4.9 COCc1c(C(C)C)nc(C(C)C)c(/C=C/[C@@H](O)C[C@@H](O)CC(=O)O)c1-c1ccc(F)cc1 10.1038/s41467-023-40064-9
1027 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3241 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
3241.0 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
7176 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL1106 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB00751 1576 None 51 Human Functional pAC50 = 5.6 5.6 -676 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 0 2 1 2.7 N=C1NCC2N1c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
37464 19228 None 19 Human Functional pAC50 = 5.6 5.6 -707 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
37464.0 19228 None 19 Human Functional pAC50 = 5.6 5.6 -707 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
CHEMBL1290 19228 None 19 Human Functional pAC50 = 5.6 5.6 -707 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
DB01359 19228 None 19 Human Functional pAC50 = 5.6 5.6 -707 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 6 2 3 3.5 CC(C)(C)NC[C@H](O)COc1ccccc1C1CCCC1 10.1038/s41467-023-40064-9
37907 35407 None 55 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 4 0 4 3.7 CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)n1ccnc1 10.1038/s41467-023-40064-9
CHEMBL1437764 35407 None 55 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 4 0 4 3.7 CC(C)(C)C(=O)C(Oc1ccc(Cl)cc1)n1ccnc1 10.1038/s41467-023-40064-9
3336 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5248 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1405922 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5248 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL254832 95054 None 22 Human Functional pAC50 = 4.6 4.6 -5248 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 315 7 1 1 5.6 CC(NCCC(c1ccccc1)c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
6989 101006 None 67 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL29411 101006 None 67 Human Functional pAC50 = 4.6 4.6 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 150 1 1 1 2.8 Cc1ccc(C(C)C)c(O)c1 10.1038/s41467-023-40064-9
60663 175773 None 30 Human Functional pAC50 = 4.6 4.6 -8 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1421212 175773 None 30 Human Functional pAC50 = 4.6 4.6 -8 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL1534525 175773 None 30 Human Functional pAC50 = 4.6 4.6 -8 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
CHEMBL45816 175773 None 30 Human Functional pAC50 = 4.6 4.6 -8 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 495 11 1 5 5.3 COCC(=O)O[C@]1(CCN(C)CCCc2nc3ccccc3[nH]2)CCc2cc(F)ccc2[C@@H]1C(C)C 10.1038/s41467-023-40064-9
3606 205946 None 40 Human Functional pAC50 = 4.6 4.6 -3 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
CHEMBL6615 205946 None 40 Human Functional pAC50 = 4.6 4.6 -3 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 270 5 2 2 4.8 CCC(c1ccc(O)cc1)C(CC)c1ccc(O)cc1 10.1038/s41467-023-40064-9
65948 18563 None 62 Human Functional pAC50 = 4.6 4.6 -12 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 582 9 2 9 4.7 CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1 10.1038/s41467-023-40064-9
CHEMBL1275868 18563 None 62 Human Functional pAC50 = 4.6 4.6 -12 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 582 9 2 9 4.7 CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1 10.1038/s41467-023-40064-9
54679224 59923 None 67 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 2 3 1.1 Oc1cc(O)c(Cl)cn1 10.1038/s41467-023-40064-9
CHEMBL1730601 59923 None 67 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 145 0 2 3 1.1 Oc1cc(O)c(Cl)cn1 10.1038/s41467-023-40064-9
180 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
200 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2160.0 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL629 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00321 401 None 38 Human Functional pAC50 = 7.6 7.6 -63 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 3 0 1 4.2 CN(CCC=C1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Functional pAC50 = 7.6 7.6 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
2337 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
50 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
5002.0 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL716 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
DB01224 3256 None 51 Human Functional pAC50 = 6.6 6.6 -4 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 5 1 6 2.9 OCCOCCN1CCN(CC1)C1=Nc2ccccc2Sc2c1cccc2 10.1038/s41467-023-40064-9
135 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Functional pAC50 = 5.6 5.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
2333 142422 None 66 Human Functional pAC50 = 5.6 5.6 -2 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
CHEMBL388590 142422 None 66 Human Functional pAC50 = 5.6 5.6 -2 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 422 3 1 3 5.5 CCc1oc2ccccc2c1C(=O)c1cc(Br)c(O)c(Br)c1 10.1038/s41467-023-40064-9
135 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
1796 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
4184.0 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL6437 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
DB06148 2532 None 33 Human Functional pAC50 = 6.6 6.6 -72 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 264 0 0 2 3.1 CN1CCN2C(C1)c1ccccc1Cc1c2cccc1 10.1038/s41467-023-40064-9
135400189 44589 None 42 Human Functional pAC50 = 4.6 4.6 -26 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 488 8 1 8 2.1 CCCc1nc(C)c2c(=O)nc(-c3cc(S(=O)(=O)N4CCN(CC)CC4)ccc3OCC)[nH]n12 10.1038/s41467-023-40064-9
CHEMBL1520 44589 None 42 Human Functional pAC50 = 4.6 4.6 -26 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 488 8 1 8 2.1 CCCc1nc(C)c2c(=O)nc(-c3cc(S(=O)(=O)N4CCN(CC)CC4)ccc3OCC)[nH]n12 10.1038/s41467-023-40064-9
1155 1629 None 38 Human Functional pAC50 = 4.6 4.6 -363 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 4.6 4.6 -363 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 4.6 4.6 -363 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 4.6 4.6 -363 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 4.6 4.6 -363 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 6 5 5 2.1 CC(Cc1ccc(cc1)O)NCC(c1cc(O)cc(c1)O)O 10.1038/s41467-023-40064-9
65981 18461 None 59 Human Functional pAC50 = 4.6 4.6 -2 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 452 10 2 4 5.2 CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL1272 18461 None 59 Human Functional pAC50 = 4.6 4.6 -2 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 452 10 2 4 5.2 CCOc1cc(CC(=O)N[C@@H](CC(C)C)c2ccccc2N2CCCCC2)ccc1C(=O)O 10.1038/s41467-023-40064-9
6010 30706 None 19 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 302 0 1 2 4.3 C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@@]2(C)[C@H]1CC[C@]2(C)O 10.1038/s41467-023-40064-9
CHEMBL1395 30706 None 19 Human Functional pAC50 = 4.6 4.6 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 302 0 1 2 4.3 C[C@]12CCC(=O)C=C1CC[C@@H]1[C@@H]2CC[C@@]2(C)[C@H]1CC[C@]2(C)O 10.1038/s41467-023-40064-9
5328940 100270 None 65 Human Functional pAC50 = 5.6 5.6 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
CHEMBL288441 100270 None 65 Human Functional pAC50 = 5.6 5.6 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 529 9 1 8 5.2 COc1cc(Nc2c(C#N)cnc3cc(OCCCN4CCN(C)CC4)c(OC)cc23)c(Cl)cc1Cl 10.1038/s41467-023-40064-9
1960 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
439260.0 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
505 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
CHEMBL1437 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
DB00368 2857 None 46 Human Functional pAC50 = 6.6 6.6 -2 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
2448 99377 None 50 Human Functional pAC50 = 6.6 6.6 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
2448.0 99377 None 50 Human Functional pAC50 = 6.6 6.6 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL28218 99377 None 50 Human Functional pAC50 = 6.6 6.6 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
DB12401 99377 None 50 Human Functional pAC50 = 6.6 6.6 -12 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 419 6 1 3 4.5 O=C(CCCN1CCC(O)(c2ccc(Br)cc2)CC1)c1ccc(F)cc1 10.1038/s41467-023-40064-9
3151 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
3151.0 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
945 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
965 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL219916 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB01184 1462 None 65 Human Functional pAC50 = 5.6 5.6 -223 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 425 5 2 5 3.4 Clc1ccc2c(c1)[nH]c(=O)n2C1CCN(CC1)CCCn1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
6256 9673 None 53 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 2 3 6 -0.8 O=c1[nH]c(=O)n([C@H]2C[C@H](O)[C@@H](CO)O2)cc1C(F)(F)F 10.1038/s41467-023-40064-9
CHEMBL1129 9673 None 53 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 2 3 6 -0.8 O=c1[nH]c(=O)n([C@H]2C[C@H](O)[C@@H](CO)O2)cc1C(F)(F)F 10.1038/s41467-023-40064-9
4006 59126 None 56 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 288 4 0 6 3.1 CC(C)OC(=O)C(C(=O)OC(C)C)=C1SC=CS1 10.1038/s41467-023-40064-9
CHEMBL1697754 59126 None 56 Human Functional pAC50 = 4.6 4.6 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 288 4 0 6 3.1 CC(C)OC(=O)C(C(=O)OC(C)C)=C1SC=CS1 10.1038/s41467-023-40064-9
14052 172681 None 32 Human Functional pAC50 = 4.6 4.6 -5495 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 204 9 4 4 -0.3 CC[C@@H](CO)NCCN[C@@H](CC)CO 10.1038/s41467-023-40064-9
CHEMBL44884 172681 None 32 Human Functional pAC50 = 4.6 4.6 -5495 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 204 9 4 4 -0.3 CC[C@@H](CO)NCCN[C@@H](CC)CO 10.1038/s41467-023-40064-9
1046 205109 None 68 Human Functional pAC50 = 4.6 4.6 -1412 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
CHEMBL614 205109 None 68 Human Functional pAC50 = 4.6 4.6 -1412 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 123 1 1 3 -0.4 NC(=O)c1cnccn1 10.1038/s41467-023-40064-9
43082 60303 None 26 Human Functional pAC50 = 4.6 4.6 -72 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1742452 60303 None 26 Human Functional pAC50 = 4.6 4.6 -72 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 357 6 0 2 5.5 CC(OCCN1CCCCCC1)(c1ccccc1)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
219024 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
219024.0 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
2362 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
5596 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
CHEMBL317052 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
DB06213 3300 None 47 Human Functional pAC50 = 4.6 4.6 -6456 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 390 4 5 12 -2.4 OC[C@H]1O[C@H]([C@@H]([C@@H]1O)O)n1cnc2c1nc(nc2N)n1ncc(c1)C(=O)NC 10.1038/s41467-023-40064-9
2520 206466 None 47 Human Functional pAC50 = 4.6 4.6 -50 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL1280 206466 None 47 Human Functional pAC50 = 4.6 4.6 -50 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
CHEMBL6966 206466 None 47 Human Functional pAC50 = 4.6 4.6 -50 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 454 13 0 6 5.1 COc1ccc(CCN(C)CCCC(C#N)(c2ccc(OC)c(OC)c2)C(C)C)cc1OC 10.1038/s41467-023-40064-9
11154555 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
11154555.0 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
5037 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
7671 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL2028019 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL3085826 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB06016 800 None 50 Human Functional pAC50 = 5.5 5.5 -1148 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 5 1 3 4.3 O=C(N(C)C)N[C@@H]1CC[C@H](CC1)CCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
2406 100458 None 56 Human Functional pAC50 = 5.5 5.5 -16 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
CHEMBL290106 100458 None 56 Human Functional pAC50 = 5.5 5.5 -16 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 2 2 3 5.9 Oc1c(Cl)cc(Cl)cc1Sc1cc(Cl)cc(Cl)c1O 10.1038/s41467-023-40064-9
3627 44143 None 12 Human Functional pAC50 = 5.5 5.5 -39 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1515447 44143 None 12 Human Functional pAC50 = 5.5 5.5 -39 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 314 3 0 2 4.1 CN1CCCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
2247 505 None 55 Human Functional pAC50 = 7.5 7.5 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Functional pAC50 = 7.5 7.5 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Functional pAC50 = 7.5 7.5 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Functional pAC50 = 7.5 7.5 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Functional pAC50 = 7.5 7.5 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2749 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
5574.0 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
7237 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
CHEMBL829 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
DB01246 344 None 32 Human Functional pAC50 = 7.5 7.5 -1 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 298 4 0 3 4.5 CN(CC(CN1c2ccccc2Sc2c1cccc2)C)C 10.1038/s41467-023-40064-9
2142 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
4920903 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
502 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
5775.0 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL597 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
DB00692 3096 None 36 Human Functional pAC50 = 6.5 6.5 -1 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 4 2 4 2.8 Cc1ccc(cc1)N(c1cccc(c1)O)CC1=NCCN1 10.1038/s41467-023-40064-9
6337614 13001 None 38 Human Functional pAC50 = 4.5 4.5 -26 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL1189679 13001 None 38 Human Functional pAC50 = 4.5 4.5 -26 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 296 1 0 2 2.7 O=C1c2cccc3c2[C@H](CCC3)CN1[C@@H]1CN2CCC1CC2 10.1038/s41467-023-40064-9
242 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
34 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
60795.0 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
CHEMBL1112 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
DB01238 470 None 70 Human Functional pAC50 = 6.5 6.5 -120 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1038/s41467-023-40064-9
9051 14447 None 46 Human Functional pAC50 = 4.5 4.5 -5 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 0 2 4.5 CC(=O)[C@H]1CC[C@H]2[C@@H]3C=CC4=CC(=O)CC[C@@]4(C)[C@@H]3CC[C@]12C 10.1038/s41467-023-40064-9
CHEMBL1200853 14447 None 46 Human Functional pAC50 = 4.5 4.5 -5 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 0 2 4.5 CC(=O)[C@H]1CC[C@H]2[C@@H]3C=CC4=CC(=O)CC[C@@]4(C)[C@@H]3CC[C@]12C 10.1038/s41467-023-40064-9
4121 50850 None 43 Human Functional pAC50 = 4.5 4.5 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 2 2 5 0.6 CN1C(CCl)Nc2cc(Cl)c(S(N)(=O)=O)cc2S1(=O)=O 10.1038/s41467-023-40064-9
CHEMBL1577 50850 None 43 Human Functional pAC50 = 4.5 4.5 -1 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 359 2 2 5 0.6 CN1C(CCl)Nc2cc(Cl)c(S(N)(=O)=O)cc2S1(=O)=O 10.1038/s41467-023-40064-9
24765256 173401 None 21 Human Functional pAC50 = 4.5 4.5 -2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 757 6 3 9 3.9 CC[C@@H]1C[C@]1(NC(=O)[C@@H]1C[C@@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)OCC(C)(C)CCCCc1cccc3c1CN(C3)C(=O)O2)C(=O)NS(=O)(=O)C1CC1 10.1038/s41467-023-40064-9
CHEMBL4525964 173401 None 21 Human Functional pAC50 = 4.5 4.5 -2 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 757 6 3 9 3.9 CC[C@@H]1C[C@]1(NC(=O)[C@@H]1C[C@@H]2CN1C(=O)[C@H](C(C)(C)C)NC(=O)OCC(C)(C)CCCCc1cccc3c1CN(C3)C(=O)O2)C(=O)NS(=O)(=O)C1CC1 10.1038/s41467-023-40064-9
15387 45836 None 41 Human Functional pAC50 = 6.5 6.5 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1531134 45836 None 41 Human Functional pAC50 = 6.5 6.5 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 5 0 2 3.5 CC1CCN(CCCC(=O)c2ccc(F)cc2)CC1 10.1038/s41467-023-40064-9
5748845 78260 None 10 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 9 4 13 -3.2 CO/N=C(\C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccc(N)n3CCO)CS[C@H]12)c1csc(N)n1 10.1038/s41467-023-40064-9
CHEMBL2105940 78260 None 10 Human Functional pAC50 = 4.5 4.5 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 522 9 4 13 -3.2 CO/N=C(\C(=O)N[C@@H]1C(=O)N2C(C(=O)[O-])=C(C[n+]3ccc(N)n3CCO)CS[C@H]12)c1csc(N)n1 10.1038/s41467-023-40064-9
68818 78297 None 21 Human Functional pAC50 = 8.5 8.5 3 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 217 1 2 3 2.2 c1ccc2c(SC3=NCCN3)c[nH]c2c1 10.1038/s41467-023-40064-9
CHEMBL2107015 78297 None 21 Human Functional pAC50 = 8.5 8.5 3 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 217 1 2 3 2.2 c1ccc2c(SC3=NCCN3)c[nH]c2c1 10.1038/s41467-023-40064-9
3294 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360.0 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 None 61 Human Functional pAC50 = 8.5 8.5 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
115368 3056 None 34 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
2112 3056 None 34 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
7556 3056 None 34 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1472975 3056 None 34 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
DB08922 3056 None 34 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 6 0 6 3.4 O=C1N(CCCCN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1CCCC2 10.1038/s41467-023-40064-9
4151 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
493 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
5312125.0 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL24778 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
DB06207 3607 None 59 Human Functional pAC50 = 8.5 8.5 1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1038/s41467-023-40064-9
6077 150786 None 16 Human Functional pAC50 = 8.5 8.5 3 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL39560 150786 None 16 Human Functional pAC50 = 8.5 8.5 3 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 326 5 0 4 4.4 CC(=O)c1ccc2c(c1)N(CCCN(C)C)c1ccccc1S2 10.1038/s41467-023-40064-9
2107 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
4747.0 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
9216 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL251940 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB01608 3055 None 44 Human Functional pAC50 = 8.5 8.5 2 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 365 4 1 5 4.0 N#Cc1ccc2c(c1)N(CCCN1CCC(CC1)O)c1c(S2)cccc1 10.1038/s41467-023-40064-9
62867 3129 None 27 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
7557 3129 None 27 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL398880 3129 None 27 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01621 3129 None 27 Human Functional pAC50 = 8.5 8.5 -1 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 475 8 1 6 4.0 OCCC1CCN(CC1)CCCN1c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2407 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
59227.0 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
941 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
CHEMBL1303 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
DB05271 3372 None 50 Human Functional pAC50 = 8.5 8.5 1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 315 6 1 3 4.3 CCCN([C@H]1CCc2c(C1)cccc2O)CCc1cccs1 10.1038/s41467-023-40064-9
5568 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
5568.0 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
66069 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL1201102 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
CHEMBL570 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
DB00508 199956 None 21 Human Functional pAC50 = 8.5 8.5 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 352 4 0 3 5.3 CN(C)CCCN1c2ccccc2Sc2ccc(C(F)(F)F)cc21 10.1038/s41467-023-40064-9
11976 920 None 44 Human Functional pAC50 = 8.5 8.5 -1 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467 920 None 44 Human Functional pAC50 = 8.5 8.5 -1 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
667467.0 920 None 44 Human Functional pAC50 = 8.5 8.5 -1 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
CHEMBL908 920 None 44 Human Functional pAC50 = 8.5 8.5 -1 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
DB01239 920 None 44 Human Functional pAC50 = 8.5 8.5 -1 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 315 3 0 2 5.2 CN(C)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)Cl 10.1038/s41467-023-40064-9
2585 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
2585.0 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
522 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
551 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
CHEMBL723 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
DB01136 803 None 59 Human Functional pAC50 = 6.5 6.5 -50 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 406 10 3 5 3.7 COc1ccccc1OCCNCC(COc1cccc2c1c1ccccc1[nH]2)O 10.1038/s41467-023-40064-9
1524 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
197 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822.0 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
88 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL51 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB12465 2181 None 61 Human Functional pAC50 = 6.5 6.5 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2583 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999.0 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 3776 None 69 Human Functional pAC50 = 5.5 5.5 -3019 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
3601 14509 None 4 Human Functional pAC50 = 5.5 5.5 -45 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1201349 14509 None 4 Human Functional pAC50 = 5.5 5.5 -45 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 502 9 0 0 8.2 C[N+](C)(CCCCCC[N+](C)(C)C1c2ccccc2-c2ccccc21)C1c2ccccc2-c2ccccc21 10.1038/s41467-023-40064-9
212 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
2639 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
941651.0 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
CHEMBL1201 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
DB01623 3806 None 35 Human Functional pAC50 = 6.5 6.5 -28 22
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 443 5 0 5 3.5 CN1CCN(CC1)CC/C=C\1/c2ccccc2Sc2c1cc(cc2)S(=O)(=O)N(C)C 10.1038/s41467-023-40064-9
1043 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
149 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
8223 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
8223.0 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
CHEMBL442 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
DB00696 1582 None 6 Human Functional pAC50 = 5.5 5.5 -15488 22
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 581 4 3 6 2.0 O=C([C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)N[C@]1(C)O[C@@]2(N(C1=O)[C@@H](Cc1ccccc1)C(=O)N1[C@H]2CCC1)O 10.1038/s41467-023-40064-9
118422671 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
1887 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
189562.0 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
71301.0 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
7246 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
9844194.0 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL2365658 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL3526436 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
CHEMBL434394 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
DB04861 2757 None 41 Human Functional pAC50 = 5.5 5.5 -1023 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 405 6 3 5 2.4 OC(C1CCc2c(O1)ccc(c2)F)CNCC(C1CCc2c(O1)ccc(c2)F)O 10.1038/s41467-023-40064-9
4452 2762 None 13 Human Functional pAC50 = 5.5 5.5 -10232 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
983 2762 None 13 Human Functional pAC50 = 5.5 5.5 -10232 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
CHEMBL20734 2762 None 13 Human Functional pAC50 = 5.5 5.5 -10232 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 6 2 4 3.8 COc1cc(NC)c(cc1C(=O)NC1CCN(C1C)Cc1ccccc1)Cl 10.1038/s41467-023-40064-9
1720 2957 None 23 Human Functional pAC50 = 5.5 5.5 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1038/s41467-023-40064-9
4086 2957 None 23 Human Functional pAC50 = 5.5 5.5 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1038/s41467-023-40064-9
7250 2957 None 23 Human Functional pAC50 = 5.5 5.5 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL776 2957 None 23 Human Functional pAC50 = 5.5 5.5 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1038/s41467-023-40064-9
DB00816 2957 None 23 Human Functional pAC50 = 5.5 5.5 - 1
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 211 4 4 4 1.1 OC(c1cc(O)cc(c1)O)CNC(C)C 10.1038/s41467-023-40064-9
2389 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
5073.0 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
96 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
CHEMBL85 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
DB00734 3331 None 72 Human Functional pAC50 = 7.5 7.5 -13 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1038/s41467-023-40064-9
228 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
33 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
6005.0 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
CHEMBL53 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
DB00714 445 None 20 Human Functional pAC50 = 6.5 6.5 -75 20
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 267 0 2 3 2.9 CN1CCc2c3[C@H]1Cc1ccc(c(c1c3ccc2)O)O 10.1038/s41467-023-40064-9
2169 44861 None 29 Human Functional pAC50 = 6.5 6.5 -4 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
CHEMBL152231 44861 None 29 Human Functional pAC50 = 6.5 6.5 -4 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 380 9 3 6 1.4 COc1ccccc1OCCNCC(O)c1ccc(C)c(S(N)(=O)=O)c1 10.1038/s41467-023-40064-9
3584 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401.0 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 3777 None 45 Human Functional pAC50 = 6.5 6.5 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5482 14425 None 55 Human Functional pAC50 = 5.5 5.5 -3 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1200438 14425 None 55 Human Functional pAC50 = 5.5 5.5 -3 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 386 6 0 4 5.9 Clc1ccc(C(Cn2ccnc2)OCc2ccsc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
2993 114756 None 14 Human Functional pAC50 = 5.5 5.5 -177 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL121663 114756 None 14 Human Functional pAC50 = 5.5 5.5 -177 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL333826 114756 None 14 Human Functional pAC50 = 5.5 5.5 -177 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 456 11 2 2 6.2 Cc1cc(N)c2ccccc2[n+]1CCCCCCCCCC[n+]1c(C)cc(N)c2ccccc21 10.1038/s41467-023-40064-9
681 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
681.0 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
940 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
947 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL59 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00988 1465 None 47 Human Functional pAC50 = 6.5 6.5 -162 15
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 153 2 3 3 0.6 NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
2105 3054 None 28 Human Functional pAC50 = 6.5 6.5 -158 25
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
47811 3054 None 28 Human Functional pAC50 = 6.5 6.5 -158 25
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
48 3054 None 28 Human Functional pAC50 = 6.5 6.5 -158 25
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
CHEMBL531 3054 None 28 Human Functional pAC50 = 6.5 6.5 -158 25
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
DB01186 3054 None 28 Human Functional pAC50 = 6.5 6.5 -158 25
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 314 4 1 2 4.3 CCCN1C[C@H](CSC)C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3 10.1038/s41467-023-40064-9
2220 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
27400.0 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
93 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL294951 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB06153 3134 None 58 Human Functional pAC50 = 5.5 5.5 -269 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 0 0 2 4.4 CN1CCC(=C2c3ccsc3CCc3c2cccc3)CC1 10.1038/s41467-023-40064-9
1086 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
3290.0 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
7181 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
CHEMBL1206 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
DB00392 1590 None 21 Human Functional pAC50 = 5.5 5.5 -91 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 5 0 3 5.0 CCN(C(CN1c2ccccc2Sc2c1cccc2)C)CC 10.1038/s41467-023-40064-9
2200 20210 None 38 Human Functional pAC50 = 6.5 6.5 1 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2200.0 20210 None 38 Human Functional pAC50 = 6.5 6.5 1 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1256819 20210 None 38 Human Functional pAC50 = 6.5 6.5 1 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1305 20210 None 38 Human Functional pAC50 = 6.5 6.5 1 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
DB08799 20210 None 38 Human Functional pAC50 = 6.5 6.5 1 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 265 5 1 3 2.7 c1ccc(CN(CC2=NCCN2)c2ccccc2)cc1 10.1038/s41467-023-40064-9
2136 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
4768.0 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
7268 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL753 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
DB00925 3095 None 24 Human Functional pAC50 = 6.5 6.5 1 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 303 8 0 2 4.2 ClCCN(C(COc1ccccc1)C)Cc1ccccc1 10.1038/s41467-023-40064-9
68712 100392 None 40 Human Functional pAC50 = 5.5 5.5 -4 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
CHEMBL289480 100392 None 40 Human Functional pAC50 = 5.5 5.5 -4 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 180 3 1 3 1.2 C1COC(NC(C2CC2)C2CC2)=N1 10.1038/s41467-023-40064-9
65700 78289 None 22 Human Functional pAC50 = 5.5 5.5 -10 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL2106919 78289 None 22 Human Functional pAC50 = 5.5 5.5 -10 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 238 1 1 2 3.3 CNC1Cc2ccccc2N(C)c2ccccc21 10.1038/s41467-023-40064-9
4066 207084 None 54 Human Functional pAC50 = 6.5 6.5 -21 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
4066.0 207084 None 54 Human Functional pAC50 = 6.5 6.5 -21 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
CHEMBL73451 207084 None 54 Human Functional pAC50 = 6.5 6.5 -21 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
DB01071 207084 None 54 Human Functional pAC50 = 6.5 6.5 -21 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 322 2 0 3 4.6 c1ccc2c(c1)Sc1ccccc1N2CC1CN2CCC1CC2 10.1038/s41467-023-40064-9
3108 209745 None 64 Human Functional pAC50 = 5.5 5.5 -1 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 504 12 4 12 -0.0 OCCN(CCO)c1nc(N2CCCCC2)c2nc(N(CCO)CCO)nc(N3CCCCC3)c2n1 10.1038/s41467-023-40064-9
CHEMBL932 209745 None 64 Human Functional pAC50 = 5.5 5.5 -1 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 504 12 4 12 -0.0 OCCN(CCO)c1nc(N2CCCCC2)c2nc(N(CCO)CCO)nc(N3CCCCC3)c2n1 10.1038/s41467-023-40064-9
47936 193531 None 56 Human Functional pAC50 = 5.5 5.5 -74 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
CHEMBL52606 193531 None 56 Human Functional pAC50 = 5.5 5.5 -74 6
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 410 2 3 7 1.5 C=C[C@@]1(C)CC(=O)[C@@]2(O)[C@](C)(O1)[C@@H](OC(C)=O)[C@@H](O)[C@H]1C(C)(C)CC[C@H](O)[C@@]12C 10.1038/s41467-023-40064-9
3158 56283 None 21 Human Functional pAC50 = 6.4 6.4 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
3158.0 56283 None 21 Human Functional pAC50 = 6.4 6.4 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1628227 56283 None 21 Human Functional pAC50 = 6.4 6.4 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
DB01142 56283 None 21 Human Functional pAC50 = 6.4 6.4 -125 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 3 0 2 4.0 CN(C)CCC=C1c2ccccc2COc2ccccc21 10.1038/s41467-023-40064-9
1971 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
2404 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
4543.0 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL445 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
DB00540 2866 None 32 Human Functional pAC50 = 7.4 7.4 -89 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 263 3 1 1 3.8 CNCCC=C1c2ccccc2CCc2c1cccc2 10.1038/s41467-023-40064-9
3584 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
5401.0 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
7302 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
CHEMBL611 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
DB01162 3777 None 45 Human Functional pAC50 = 6.4 6.4 -69 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 4 2 7 0.9 COc1cc2nc([nH]c(=N)c2cc1OC)N1CCN(CC1)C(=O)C1CCCO1 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Functional pAC50 = 5.4 5.4 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
441074 19421 None 48 Human Functional pAC50 = 5.4 5.4 -1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
CHEMBL1294 19421 None 48 Human Functional pAC50 = 5.4 5.4 -1 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 4 1 4 3.2 C=C[C@H]1CN2CC[C@H]1C[C@@H]2[C@@H](O)c1ccnc2ccc(OC)cc12 10.1038/s41467-023-40064-9
115 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
2092 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
2092.0 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
7109 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
CHEMBL709 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
DB00346 343 None 50 Human Functional pAC50 = 7.4 7.4 14 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 389 8 3 7 2.0 COc1cc2nc([nH]c(=N)c2cc1OC)N(CCCN=C(C1CCCO1)O)C 10.1038/s41467-023-40064-9
4260 52574 None 20 Human Functional pAC50 = 5.4 5.4 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
4260.0 52574 None 20 Human Functional pAC50 = 5.4 5.4 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
CHEMBL159226 52574 None 20 Human Functional pAC50 = 5.4 5.4 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
DB09205 52574 None 20 Human Functional pAC50 = 5.4 5.4 -3 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 279 6 0 4 3.0 CC(=O)Oc1cc(C(C)C)c(OCCN(C)C)cc1C 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Functional pAC50 = 7.4 7.4 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
5022 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6918248.0 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
8182 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL231068 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
DB04908 1651 None 58 Human Functional pAC50 = 6.4 6.4 -8 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 390 4 1 4 3.2 O=c1[nH]c2c(n1CCN1CCN(CC1)c1cccc(c1)C(F)(F)F)cccc2 10.1038/s41467-023-40064-9
6075 150196 None 34 Human Functional pAC50 = 6.4 6.4 -14 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL395110 150196 None 34 Human Functional pAC50 = 6.4 6.4 -14 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 2 0 3 4.6 CN1CCCC(CN2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
5591 157623 None 57 Human Functional pAC50 = 5.4 5.4 -4 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
CHEMBL408 157623 None 57 Human Functional pAC50 = 5.4 5.4 -4 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 441 5 2 6 4.4 Cc1c(C)c2c(c(C)c1O)CCC(C)(COc1ccc(CC3SC(=O)NC3=O)cc1)O2 10.1038/s41467-023-40064-9
2181 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
4830 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
4830.0 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
92 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
CHEMBL440294 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
DB09286 3128 None 36 Human Functional pAC50 = 6.4 6.4 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 7 1 4 2.6 O=C(c1ccc(cc1)F)CCCN1CCC(CC1)(N1CCCCC1)C(=O)N 10.1038/s41467-023-40064-9
2146 3100 None 45 Human Functional pAC50 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.4 8.4 -20 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1038/s41467-023-40064-9
17676 7074 None 25 Human Functional pAC50 = 8.4 8.4 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
17676.0 7074 None 25 Human Functional pAC50 = 8.4 8.4 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
5281082 7074 None 25 Human Functional pAC50 = 8.4 8.4 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
CHEMBL1085 7074 None 25 Human Functional pAC50 = 8.4 8.4 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
DB01063 7074 None 25 Human Functional pAC50 = 8.4 8.4 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 411 7 1 6 3.5 CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2 10.1038/s41467-023-40064-9
1427 2013 None 42 Human Functional pAC50 = 6.4 6.4 -112 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
357 2013 None 42 Human Functional pAC50 = 6.4 6.4 -112 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
3696 2013 None 42 Human Functional pAC50 = 6.4 6.4 -112 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
CHEMBL11 2013 None 42 Human Functional pAC50 = 6.4 6.4 -112 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
DB00458 2013 None 42 Human Functional pAC50 = 6.4 6.4 -112 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 280 4 0 2 3.9 CN(CCCN1c2ccccc2CCc2c1cccc2)C 10.1038/s41467-023-40064-9
1385580 29284 None 49 Human Functional pAC50 = 5.4 5.4 -478 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615 29284 None 49 Human Functional pAC50 = 5.4 5.4 -478 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
4615.0 29284 None 49 Human Functional pAC50 = 5.4 5.4 -478 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL13828 29284 None 49 Human Functional pAC50 = 5.4 5.4 -478 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
DB12877 29284 None 49 Human Functional pAC50 = 5.4 5.4 -478 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 7 1 4 4.1 O=c1[nH]c2ccccc2n1CCCN1CCN(C(c2ccccc2)c2ccccc2)CC1 10.1038/s41467-023-40064-9
3952 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5353646.0 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5443 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
5702063.0 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL1331786 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
CHEMBL420 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
DB00629 1888 None 32 Human Functional pAC50 = 7.4 7.4 -4 21
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 230 2 2 2 1.6 NC(=N/N=C\c1c(Cl)cccc1Cl)N 10.1038/s41467-023-40064-9
4209 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893.0 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 3163 None 48 Human Functional pAC50 = 7.4 7.4 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5329102 194838 None 50 Human Functional pAC50 = 6.4 6.4 -3 37
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
CHEMBL535 194838 None 50 Human Functional pAC50 = 6.4 6.4 -3 37
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 398 7 3 3 3.3 CCN(CC)CCNC(=O)c1c(C)[nH]c(/C=C2\C(=O)Nc3ccc(F)cc32)c1C 10.1038/s41467-023-40064-9
5803 162321 None 58 Human Functional pAC50 = 5.4 5.4 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
CHEMBL41632 162321 None 58 Human Functional pAC50 = 5.4 5.4 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 622 4 2 3 4.6 O=C(O)Cc1cc(I)c(Oc2ccc(O)c(I)c2)c(I)c1 10.1038/s41467-023-40064-9
71897 78277 None 10 Human Functional pAC50 = 6.4 6.4 -141 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
CHEMBL2106537 78277 None 10 Human Functional pAC50 = 6.4 6.4 -141 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 304 4 1 3 2.7 Cc1cc(CCN2CCN(c3cccc(Cl)c3)CC2)n[nH]1 10.1038/s41467-023-40064-9
44591583 184642 None 65 Human Functional pAC50 = 5.4 5.4 3 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 2 1 4 1.6 N#Cc1ccc(Oc2ccc3c(c2)COB3O)cc1 10.1038/s41467-023-40064-9
CHEMBL484785 184642 None 65 Human Functional pAC50 = 5.4 5.4 3 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 251 2 1 4 1.6 N#Cc1ccc(Oc2ccc3c(c2)COB3O)cc1 10.1038/s41467-023-40064-9
5453 206077 None 58 Human Functional pAC50 = 7.4 7.4 1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
CHEMBL671 206077 None 58 Human Functional pAC50 = 7.4 7.4 1 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 189 3 0 1 0.2 S=P(N1CC1)(N1CC1)N1CC1 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Functional pAC50 = 6.4 6.4 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3947 208853 None 39 Human Functional pAC50 = 5.4 5.4 -6 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL87708 208853 None 39 Human Functional pAC50 = 5.4 5.4 -6 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 418 7 0 3 5.8 CN(CCCN1c2ccccc2CCc2ccccc21)CC(=O)c1ccc(Cl)cc1 10.1038/s41467-023-40064-9
3152 188518 None 61 Human Functional pAC50 = 5.4 5.4 -9 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
CHEMBL502 188518 None 61 Human Functional pAC50 = 5.4 5.4 -9 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 379 6 0 4 4.4 COc1cc2c(cc1OC)C(=O)C(CC1CCN(Cc3ccccc3)CC1)C2 10.1038/s41467-023-40064-9
55645 84404 None 3 Human Functional pAC50 = 6.4 6.4 -1258 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
55645.0 84404 None 3 Human Functional pAC50 = 6.4 6.4 -1258 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
CHEMBL2218861 84404 None 3 Human Functional pAC50 = 6.4 6.4 -1258 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 395 7 2 4 2.1 CCCN1CC(NS(=O)(=O)N(CC)CC)CC2Cc3c(O)cccc3CC21 10.1038/s41467-023-40064-9
3689 102826 None 36 Human Functional pAC50 = 6.4 6.4 -64 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1372983 102826 None 36 Human Functional pAC50 = 6.4 6.4 -64 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
CHEMBL305187 102826 None 36 Human Functional pAC50 = 6.4 6.4 -64 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 5 2 3 3.8 CC(C(O)c1ccc(O)cc1)N1CCC(Cc2ccccc2)CC1 10.1038/s41467-023-40064-9
2324 77126 None 16 Human Functional pAC50 = 5.4 5.4 -2 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
CHEMBL2074972 77126 None 16 Human Functional pAC50 = 5.4 5.4 -2 11
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 505 7 1 8 4.2 COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1 10.1038/s41467-023-40064-9
4418 34231 None 58 Human Functional pAC50 = 6.3 6.3 -4 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
4418.0 34231 None 58 Human Functional pAC50 = 6.3 6.3 -4 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
CHEMBL142635 34231 None 58 Human Functional pAC50 = 6.3 6.3 -4 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
DB12092 34231 None 58 Human Functional pAC50 = 6.3 6.3 -4 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1038/s41467-023-40064-9
100 3805 None 44 Human Functional pAC50 = 6.3 6.3 -8 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2637 3805 None 44 Human Functional pAC50 = 6.3 6.3 -8 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
5452 3805 None 44 Human Functional pAC50 = 6.3 6.3 -8 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
CHEMBL479 3805 None 44 Human Functional pAC50 = 6.3 6.3 -8 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
DB00679 3805 None 44 Human Functional pAC50 = 6.3 6.3 -8 38
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 370 4 0 4 5.9 CSc1ccc2c(c1)N(CCC1CCCCN1C)c1c(S2)cccc1 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Functional pAC50 = 5.3 5.3 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Functional pAC50 = 5.3 5.3 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Functional pAC50 = 5.3 5.3 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Functional pAC50 = 5.3 5.3 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
2895 206050 None 27 Human Functional pAC50 = 6.3 6.3 -16 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
2895.0 206050 None 27 Human Functional pAC50 = 6.3 6.3 -16 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL669 206050 None 27 Human Functional pAC50 = 6.3 6.3 -16 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
DB00924 206050 None 27 Human Functional pAC50 = 6.3 6.3 -16 15
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 275 3 0 1 4.6 CN(C)CCC=C1c2ccccc2C=Cc2ccccc21 10.1038/s41467-023-40064-9
54682461 84720 None 41 Human Functional pAC50 = 5.3 5.3 1 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
CHEMBL222559 84720 None 41 Human Functional pAC50 = 5.3 5.3 1 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 602 11 2 6 7.3 CCC[C@@]1(CCc2ccccc2)CC(O)=C([C@H](CC)c2cccc(NS(=O)(=O)c3ccc(C(F)(F)F)cn3)c2)C(=O)O1 10.1038/s41467-023-40064-9
82153 43915 None 34 Human Functional pAC50 = 7.3 7.3 11 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
CHEMBL1512 43915 None 34 Human Functional pAC50 = 7.3 7.3 11 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 434 2 2 6 2.3 CC1(C)O[C@@H]2C[C@H]3[C@@H]4C[C@H](F)C5=CC(=O)C=C[C@]5(C)[C@H]4[C@@H](O)C[C@]3(C)[C@]2(C(=O)CO)O1 10.1038/s41467-023-40064-9
4011 82440 None 34 Human Functional pAC50 = 6.3 6.3 -8 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
CHEMBL21731 82440 None 34 Human Functional pAC50 = 6.3 6.3 -8 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 277 4 1 1 4.2 CNCCCC12CCC(c3ccccc31)c1ccccc12 10.1038/s41467-023-40064-9
2710 84342 None 29 Human Functional pAC50 = 5.3 5.3 -10 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
2710.0 84342 None 29 Human Functional pAC50 = 5.3 5.3 -10 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL1889091 84342 None 29 Human Functional pAC50 = 5.3 5.3 -10 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
CHEMBL22150 84342 None 29 Human Functional pAC50 = 5.3 5.3 -10 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
DB08936 84342 None 29 Human Functional pAC50 = 5.3 5.3 -10 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 300 3 0 2 3.7 CN1CCN(C(c2ccccc2)c2ccc(Cl)cc2)CC1 10.1038/s41467-023-40064-9
54758501 139154 None 52 Human Functional pAC50 = 5.3 5.3 -1621 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
CHEMBL3786343 139154 None 52 Human Functional pAC50 = 5.3 5.3 -1621 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 486 7 2 8 5.1 C=CC(=O)Nc1cccc(Oc2nc(Nc3ccc(N4CCN(C)CC4)cc3)nc3ccsc23)c1 10.1038/s41467-023-40064-9
6719 32676 None 23 Human Functional pAC50 = 5.3 5.3 -6 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 4 0 3 4.1 O=C1c2ccccc2C(=O)C1C(=O)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1413199 32676 None 23 Human Functional pAC50 = 5.3 5.3 -6 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 340 4 0 3 4.1 O=C1c2ccccc2C(=O)C1C(=O)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
4195 14477 None 34 Human Functional pAC50 = 5.3 5.3 2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
4195.0 14477 None 34 Human Functional pAC50 = 5.3 5.3 2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
CHEMBL1201212 14477 None 34 Human Functional pAC50 = 5.3 5.3 2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
DB00211 14477 None 34 Human Functional pAC50 = 5.3 5.3 2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
36811 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
36811.0 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
535 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
937 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
CHEMBL926 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
DB00841 1454 None 27 Human Functional pAC50 = 8.3 8.3 -1 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 301 7 4 4 3.0 CC(CCc1ccc(cc1)O)NCCc1ccc(c(c1)O)O 10.1038/s41467-023-40064-9
3083544 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
3083544.0 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1200811 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1363 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL1951071 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
CHEMBL605993 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
DB00983 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
DB01274 26817 None 34 Human Functional pAC50 = 7.3 7.3 -407 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 344 9 4 5 2.2 COc1ccc(C[C@@H](C)NC[C@H](O)c2ccc(O)c(NC=O)c2)cc1 10.1038/s41467-023-40064-9
643976 14524 None 29 Human Functional pAC50 = 5.3 5.3 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 5.3 5.3 -2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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
133 2496 None 39 Human Functional pAC50 = 7.3 7.3 -131 27
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
1723 2496 None 39 Human Functional pAC50 = 7.3 7.3 -131 27
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
28693 2496 None 39 Human Functional pAC50 = 7.3 7.3 -131 27
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
CHEMBL19215 2496 None 39 Human Functional pAC50 = 7.3 7.3 -131 27
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
DB13520 2496 None 39 Human Functional pAC50 = 7.3 7.3 -131 27
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 403 4 1 4 4.1 O=C(OCc1ccccc1)NC[C@H]1CN(C)[C@H]2[C@H](C1)c1cccc3c1c(C2)cn3C 10.1038/s41467-023-40064-9
3033538 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
3033538.0 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
7155 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
781 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
CHEMBL1201216 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
DB00298 1319 None 27 Human Functional pAC50 = 6.3 6.3 -63 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 325 4 0 5 2.3 Cc1ccccc1N1CCN(CC1)CCc1nnc2n1CCCC2 10.1038/s41467-023-40064-9
2771 197264 None 50 Human Functional pAC50 = 5.3 5.3 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1200781 197264 None 50 Human Functional pAC50 = 5.3 5.3 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL549 197264 None 50 Human Functional pAC50 = 5.3 5.3 -46 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCCC1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
191 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
201 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
2170.0 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
CHEMBL1113 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
DB00543 403 None 60 Human Functional pAC50 = 5.3 5.3 -67 36
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 313 0 1 4 3.4 Clc1ccc2c(c1)C(=Nc1c(O2)cccc1)N1CCNCC1 10.1038/s41467-023-40064-9
107641 61163 None 56 Human Functional pAC50 = 5.3 5.3 -2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 4 1 2 3.4 CCC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
CHEMBL1765292 61163 None 56 Human Functional pAC50 = 5.3 5.3 -2 2
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 4 1 2 3.4 CCC(C(=O)O)c1ccc(N2Cc3ccccc3C2=O)cc1 10.1038/s41467-023-40064-9
2540 4402 None 68 Human Functional pAC50 = 5.3 5.3 -1047 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1014 4402 None 68 Human Functional pAC50 = 5.3 5.3 -1047 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 610 10 1 11 6.3 CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1 10.1038/s41467-023-40064-9
11504295 2923 None 40 Human Functional pAC50 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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 = 7.3 7.3 -416 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
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
1547484 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1547484.0 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
654 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
9072 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL43064 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00568 940 None 51 Human Functional pAC50 = 5.3 5.3 -50 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 368 6 0 2 5.1 c1ccc(cc1)/C=C/CN1CCN(CC1)C(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
5639 98949 None 48 Human Functional pAC50 = 6.2 6.2 7 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
CHEMBL279229 98949 None 48 Human Functional pAC50 = 6.2 6.2 7 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 387 7 1 8 0.7 COc1ccccc1N1CCN(CCCNc2cc(=O)n(C)c(=O)n2C)CC1 10.1038/s41467-023-40064-9
2995 206863 None 31 Human Functional pAC50 = 6.2 6.2 -213 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
2995.0 206863 None 31 Human Functional pAC50 = 6.2 6.2 -213 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1696 206863 None 31 Human Functional pAC50 = 6.2 6.2 -213 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL72 206863 None 31 Human Functional pAC50 = 6.2 6.2 -213 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
DB01151 206863 None 31 Human Functional pAC50 = 6.2 6.2 -213 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 266 4 1 2 3.5 CNCCCN1c2ccccc2CCc2ccccc21 10.1038/s41467-023-40064-9
114948 60317 None 11 Human Functional pAC50 = 5.2 5.2 -457 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
114948.0 60317 None 11 Human Functional pAC50 = 5.2 5.2 -457 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL1743263 60317 None 11 Human Functional pAC50 = 5.2 5.2 -457 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
DB11274 60317 None 11 Human Functional pAC50 = 5.2 5.2 -457 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 577 5 3 6 2.5 CC(C)C[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
146570 43468 None 43 Human Functional pAC50 = 5.2 5.2 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
CHEMBL1508 43468 None 43 Human Functional pAC50 = 5.2 5.2 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 5 0 3 3.8 CN(C)CCC[C@@]1(c2ccc(F)cc2)OCc2cc(C#N)ccc21 10.1038/s41467-023-40064-9
4167 14506 None 28 Human Functional pAC50 = 6.2 6.2 -109 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
4167.0 14506 None 28 Human Functional pAC50 = 6.2 6.2 -109 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
CHEMBL1201342 14506 None 28 Human Functional pAC50 = 6.2 6.2 -109 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
DB00340 14506 None 28 Human Functional pAC50 = 6.2 6.2 -109 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 2 0 2 5.0 CN1CCCC(CC2c3ccccc3Sc3ccccc32)C1 10.1038/s41467-023-40064-9
2855 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
3322 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5717 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
5717.0 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
CHEMBL603 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
DB00549 4132 None 63 Human Functional pAC50 = 5.2 5.2 -2951 12
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1038/s41467-023-40064-9
2335 11852 None 18 Human Functional pAC50 = 5.2 5.2 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
8478 11852 None 18 Human Functional pAC50 = 5.2 5.2 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL1182210 11852 None 18 Human Functional pAC50 = 5.2 5.2 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
CHEMBL221753 11852 None 18 Human Functional pAC50 = 5.2 5.2 -38 34
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 11 0 2 6.1 CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1 10.1038/s41467-023-40064-9
5832 14466 None 37 Human Functional pAC50 = 5.2 5.2 -7 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 1 0 3 4.1 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
CHEMBL1201146 14466 None 37 Human Functional pAC50 = 5.2 5.2 -7 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 340 1 0 3 4.1 C#C[C@]1(OC(C)=O)CC[C@H]2[C@@H]3CCC4=CC(=O)CC[C@@H]4[C@H]3CC[C@@]21C 10.1038/s41467-023-40064-9
208898 66220 None 50 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
208898.0 66220 None 50 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
CHEMBL184412 66220 None 50 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
DB04855 66220 None 50 Human Functional pAC50 = 5.2 5.2 -9 11
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 556 18 1 6 7.0 CCCCc1oc2ccc(NS(C)(=O)=O)cc2c1C(=O)c1ccc(OCCCN(CCCC)CCCC)cc1 10.1038/s41467-023-40064-9
37 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
460 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
54746.0 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
CHEMBL1201087 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
DB00248 778 None 41 Human Functional pAC50 = 6.2 6.2 -141 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 451 8 2 4 3.2 C=CCN1C[C@@H](C[C@H]2[C@H]1Cc1c[nH]c3c1c2ccc3)C(=O)N(C(=O)NCC)CCCN(C)C 10.1038/s41467-023-40064-9
5419 18067 None 45 Human Functional pAC50 = 8.2 8.2 10 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
5419.0 18067 None 45 Human Functional pAC50 = 8.2 8.2 10 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL1200413 18067 None 45 Human Functional pAC50 = 8.2 8.2 10 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL1266 18067 None 45 Human Functional pAC50 = 8.2 8.2 10 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
DB06764 18067 None 45 Human Functional pAC50 = 8.2 8.2 10 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 200 1 1 2 2.1 c1ccc2c(c1)CCCC2C1=NCCN1 10.1038/s41467-023-40064-9
1028 291 None 40 Human Functional pAC50 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
1028 291 None 40 Human Functional pAC50 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 8.2 8.2 1 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1038/s41467-023-40064-9
1524 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
197 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
3822.0 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
88 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
CHEMBL51 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
DB12465 2181 None 61 Human Functional pAC50 = 7.2 7.2 -23 18
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 5 1 5 2.4 Fc1ccc(cc1)C(=O)C1CCN(CC1)CCn1c(=O)[nH]c2c(c1=O)cccc2 10.1038/s41467-023-40064-9
2713 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5353524 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5360566 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
88536661 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
9552079 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL1330113 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
CHEMBL790 207729 None 57 Human Functional pAC50 = 6.2 6.2 -1 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 504 9 10 4 4.2 N=C(NCCCCCCNC(=N)NC(=N)Nc1ccc(Cl)cc1)NC(=N)Nc1ccc(Cl)cc1 10.1038/s41467-023-40064-9
5324346 208040 None 37 Human Functional pAC50 = 5.2 5.2 2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL1409 208040 None 37 Human Functional pAC50 = 5.2 5.2 2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
CHEMBL814 208040 None 37 Human Functional pAC50 = 5.2 5.2 2 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 318 9 1 4 3.2 COCCCC/C(=N\OCCN)c1ccc(C(F)(F)F)cc1 10.1038/s41467-023-40064-9
1353 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
3559.0 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
86 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
CHEMBL54 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
DB00502 1911 None 63 Human Functional pAC50 = 7.2 7.2 -23 39
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 375 6 1 3 4.4 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)(O)c1ccc(cc1)Cl 10.1038/s41467-023-40064-9
102 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
3659 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
8969.0 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
CHEMBL15245 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
DB01392 4127 None 36 Human Functional pAC50 = 5.2 5.2 -380 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 354 1 2 4 2.6 COC(=O)[C@H]1[C@@H](O)CC[C@@H]2[C@@H]1C[C@@H]1N(C2)CCc2c1[nH]c1c2cccc1 10.1038/s41467-023-40064-9
392622 56328 None 57 Human Functional pAC50 = 5.2 5.2 -8 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
CHEMBL163 56328 None 57 Human Functional pAC50 = 5.2 5.2 -8 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 720 17 4 9 5.9 CC(C)c1nc(CN(C)C(=O)N[C@H](C(=O)N[C@@H](Cc2ccccc2)C[C@H](O)[C@H](Cc2ccccc2)NC(=O)OCc2cncs2)C(C)C)cs1 10.1038/s41467-023-40064-9
3354 41798 None 37 Human Functional pAC50 = 5.2 5.2 -7 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
3354.0 41798 None 37 Human Functional pAC50 = 5.2 5.2 -7 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
CHEMBL1493 41798 None 37 Human Functional pAC50 = 5.2 5.2 -7 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
DB01148 41798 None 37 Human Functional pAC50 = 5.2 5.2 -7 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 391 5 0 5 4.4 Cc1c(-c2ccccc2)oc2c(C(=O)OCCN3CCCCC3)cccc2c1=O 10.1038/s41467-023-40064-9
447715 199383 None 50 Human Functional pAC50 = 5.2 5.2 -7 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
CHEMBL566315 199383 None 50 Human Functional pAC50 = 5.2 5.2 -7 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 420 5 3 3 5.1 CC[C@@H]1[C@@H]2C[C@H](O)CC[C@]2(C)[C@H]2CC[C@@]3(C)[C@@H](CC[C@@H]3[C@H](C)CCC(=O)O)[C@@H]2[C@@H]1O 10.1038/s41467-023-40064-9
25382 9159 None 27 Human Functional pAC50 = 6.2 6.2 -16 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL110094 9159 None 27 Human Functional pAC50 = 6.2 6.2 -16 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 291 3 0 1 4.7 CN(C)CCC=C1c2ccccc2C(C)(C)c2ccccc21 10.1038/s41467-023-40064-9
2435 3590 None 59 Human Functional pAC50 = 6.2 6.2 -25 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
60149 3590 None 59 Human Functional pAC50 = 6.2 6.2 -25 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
98 3590 None 59 Human Functional pAC50 = 6.2 6.2 -25 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
CHEMBL12713 3590 None 59 Human Functional pAC50 = 6.2 6.2 -25 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
DB06144 3590 None 59 Human Functional pAC50 = 6.2 6.2 -25 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 440 5 1 3 4.6 Clc1ccc2c(c1)c(cn2c1ccc(cc1)F)C1CCN(CC1)CCN1CCNC1=O 10.1038/s41467-023-40064-9
2683 102943 None 17 Human Functional pAC50 = 5.2 5.2 -812 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL305906 102943 None 17 Human Functional pAC50 = 5.2 5.2 -812 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
CHEMBL334255 102943 None 17 Human Functional pAC50 = 5.2 5.2 -812 24
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 304 15 0 0 6.5 CCCCCCCCCCCCCCCC[n+]1ccccc1 10.1038/s41467-023-40064-9
2435 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
2435.0 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
395 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
520 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
5386 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
CHEMBL844 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
DB00484 722 None 63 Human Functional pAC50 = 6.2 6.2 -213 10
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 10.1038/s41467-023-40064-9
25295 13625 None 28 Human Functional pAC50 = 5.2 5.2 -4 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL1194287 13625 None 28 Human Functional pAC50 = 5.2 5.2 -4 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 289 6 0 3 3.3 CN(C)CCN(Cc1ccc(Cl)cc1)c1ccccn1 10.1038/s41467-023-40064-9
10607 204704 None 64 Human Functional pAC50 = 5.2 5.2 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 414 4 1 8 2.4 COc1cc([C@@H]2c3cc4c(cc3[C@H](O)[C@H]3COC(=O)[C@H]23)OCO4)cc(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL61 204704 None 64 Human Functional pAC50 = 5.2 5.2 - 1
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 414 4 1 8 2.4 COc1cc([C@@H]2c3cc4c(cc3[C@H](O)[C@H]3COC(=O)[C@H]23)OCO4)cc(OC)c1OC 10.1038/s41467-023-40064-9
73417116 154521 None 0 Human Functional pAC50 = 5.2 5.2 -11 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL3989843 154521 None 0 Human Functional pAC50 = 5.2 5.2 -11 5
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 266 2 2 2 3.0 N[C@@H]1C[C@H]1c1ccccc1.N[C@H]1C[C@@H]1c1ccccc1 10.1038/s41467-023-40064-9
5314 206566 None 14 Human Functional pAC50 = 6.2 6.2 25 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 290 9 0 4 0.3 C[N+](C)(C)CCOC(=O)CCC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
CHEMBL703 206566 None 14 Human Functional pAC50 = 6.2 6.2 25 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 290 9 0 4 0.3 C[N+](C)(C)CCOC(=O)CCC(=O)OCC[N+](C)(C)C 10.1038/s41467-023-40064-9
20628 96601 None 25 Human Functional pAC50 = 5.2 5.2 -17 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
CHEMBL26291 96601 None 25 Human Functional pAC50 = 5.2 5.2 -17 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 324 6 1 5 3.7 CN(C)CCCNc1c2ccccc2nc2cccc([N+](=O)[O-])c12 10.1038/s41467-023-40064-9
2865 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
59 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
60854.0 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL708 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
DB00246 4143 None 47 Human Functional pAC50 = 6.2 6.2 -23 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 412 4 1 5 3.8 O=C1Nc2c(C1)cc(c(c2)Cl)CCN1CCN(CC1)c1nsc2c1cccc2 10.1038/s41467-023-40064-9
5353853 17993 None 30 Human Functional pAC50 = 5.2 5.2 -39 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
9556529 17993 None 30 Human Functional pAC50 = 5.2 5.2 -39 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
CHEMBL1262 17993 None 30 Human Functional pAC50 = 5.2 5.2 -39 20
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 427 6 0 4 6.1 Clc1ccc(CO/N=C(\Cn2ccnc2)c2ccc(Cl)cc2Cl)c(Cl)c1 10.1038/s41467-023-40064-9
2402 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
5095.0 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
7295 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
CHEMBL589 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
DB00268 3370 None 38 Human Functional pAC50 = 5.2 5.2 -354 17
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 260 7 1 2 3.5 CCCN(CCC)CCc1cccc2c1CC(=N2)O 10.1038/s41467-023-40064-9
1593 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
30668.0 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
9868 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
CHEMBL17860 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
DB04948 2340 None 41 Human Functional pAC50 = 8.2 8.2 -3 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 258 3 1 3 2.8 CC(C1=NCCN1)Oc1c(Cl)cccc1Cl 10.1038/s41467-023-40064-9
4567 9950 None 29 Human Functional pAC50 = 7.2 7.2 2 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 7.2 7.2 2 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 299 7 3 3 3.4 CC(CCc1ccccc1)NC(C)C(O)c1ccc(O)cc1 10.1038/s41467-023-40064-9
16363 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
16363.0 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
312 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
9215 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
CHEMBL297302 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
DB12867 596 None 33 Human Functional pAC50 = 7.2 7.2 -13 21
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 381 6 1 4 3.8 Fc1ccc(cc1)C(=O)CCCN1CCC(CC1)n1c(=O)[nH]c2c1cccc2 10.1038/s41467-023-40064-9
168871 89164 None 10 Human Functional pAC50 = 6.2 6.2 -53 13
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
CHEMBL2365712 89164 None 10 Human Functional pAC50 = 6.2 6.2 -53 13
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 563 4 3 6 2.1 CC(C)[C@H]1C(=O)N2CCC[C@H]2[C@]2(O)O[C@](NC(=O)[C@@H]3C[C@@H]4c5cccc6[nH]cc(c56)C[C@H]4N(C)C3)(C(C)C)C(=O)N12 10.1038/s41467-023-40064-9
3598 187927 None 45 Human Functional pAC50 = 6.2 6.2 1 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
CHEMBL496 187927 None 45 Human Functional pAC50 = 6.2 6.2 1 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 2 2 2 6.6 Oc1c(Cl)cc(Cl)c(Cl)c1Cc1c(O)c(Cl)cc(Cl)c1Cl 10.1038/s41467-023-40064-9
2247 505 None 55 Human Functional pAC50 = 6.2 6.2 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
249 505 None 55 Human Functional pAC50 = 6.2 6.2 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
2603 505 None 55 Human Functional pAC50 = 6.2 6.2 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
CHEMBL296419 505 None 55 Human Functional pAC50 = 6.2 6.2 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
DB00637 505 None 55 Human Functional pAC50 = 6.2 6.2 -26 42
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 458 8 1 5 5.4 COc1ccc(cc1)CCN1CCC(CC1)Nc1nc2c(n1Cc1ccc(cc1)F)cccc2 10.1038/s41467-023-40064-9
40466858 16162 None 49 Human Functional pAC50 = 6.2 6.2 -20 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
5284514 16162 None 49 Human Functional pAC50 = 6.2 6.2 -20 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
5284514.0 16162 None 49 Human Functional pAC50 = 6.2 6.2 -20 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
CHEMBL1224 16162 None 49 Human Functional pAC50 = 6.2 6.2 -20 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
DB09488 16162 None 49 Human Functional pAC50 = 6.2 6.2 -20 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 6 1 3 4.0 Cc1ccc(/C(=C\CN2CCCC2)c2cccc(/C=C/C(=O)O)n2)cc1 10.1038/s41467-023-40064-9
5077 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
7552 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
9913767 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
9913767.0 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
CHEMBL238804 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
DB11362 3578 None 61 Human Functional pAC50 = 5.1 5.1 -275 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 496 12 1 7 3.9 O=C(NS(=O)(=O)C)COCCCCN(c1cnc(c(n1)c1ccccc1)c1ccccc1)C(C)C 10.1038/s41467-023-40064-9
1613 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
205 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
3964.0 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
CHEMBL831 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
DB00408 2348 None 42 Human Functional pAC50 = 7.1 7.1 -10 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 327 0 0 4 3.8 CN1CCN(CC1)C1=Nc2ccccc2Oc2c1cc(Cl)cc2 10.1038/s41467-023-40064-9
4195 14477 None 34 Human Functional pAC50 = 5.1 5.1 2 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
4195.0 14477 None 34 Human Functional pAC50 = 5.1 5.1 2 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
CHEMBL1201212 14477 None 34 Human Functional pAC50 = 5.1 5.1 2 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
DB00211 14477 None 34 Human Functional pAC50 = 5.1 5.1 2 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 254 6 3 5 -0.2 COc1ccc(OC)c(C(O)CNC(=O)CN)c1 10.1038/s41467-023-40064-9
12488 1657 None 39 Human Functional pAC50 = 6.1 6.1 -19 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
941361 1657 None 39 Human Functional pAC50 = 6.1 6.1 -19 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
CHEMBL30008 1657 None 39 Human Functional pAC50 = 6.1 6.1 -19 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
DB04841 1657 None 39 Human Functional pAC50 = 6.1 6.1 -19 28
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 404 6 0 2 5.4 C1CN(CCN1C/C=C/C2=CC=CC=C2)C(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F 10.1038/s41467-023-40064-9
1909 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
2559 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
4474 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL1484 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
CHEMBL3302409 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
DB00622 2822 None 46 Human Functional pAC50 = 6.1 6.1 -1 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 479 9 1 8 3.7 COC(=O)C1=C(C)NC(=C(C1c1cccc(c1)[N+](=O)[O-])C(=O)OCCN(Cc1ccccc1)C)C 10.1038/s41467-023-40064-9
82146 4532 None 68 Human Functional pAC50 = 6.1 6.1 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
CHEMBL1023 4532 None 68 Human Functional pAC50 = 6.1 6.1 1 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
213046 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
213046.0 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
4168 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
7461 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
CHEMBL1237021 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
DB08815 2385 None 44 Human Functional pAC50 = 7.1 7.1 -6 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 492 5 0 6 4.3 O=C1N(C[C@@H]2CCCC[C@H]2CN2CCN(CC2)c2nsc3c2cccc3)C(=O)[C@@H]2[C@H]1[C@H]1CC[C@@H]2C1 10.1038/s41467-023-40064-9
137 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
2119 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
563 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
66368 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
CHEMBL266195 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
DB00866 370 None 37 Human Functional pAC50 = 5.1 5.1 -3467 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 249 8 2 3 2.2 C=CCc1ccccc1OCC(CNC(C)C)O 10.1038/s41467-023-40064-9
68617 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1709 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
CHEMBL809 207985 None 33 Human Functional pAC50 = 5.1 5.1 -14 30
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 305 2 1 1 5.2 CN[C@H]1CC[C@@H](c2ccc(Cl)c(Cl)c2)c2ccccc21 10.1038/s41467-023-40064-9
11823027 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
11823027.0 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
4411 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
4411.0 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
CHEMBL3246778 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
CHEMBL521606 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
DB01203 192725 None 29 Human Functional pAC50 = 5.1 5.1 -436 3
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 309 5 4 5 0.6 CC(C)(C)NCC(O)COc1cccc2c1CC(O)C(O)C2 10.1038/s41467-023-40064-9
1690 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
4058 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
4058.0 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
5750 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
7221 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL607 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
DB00454 3058 None 10 Human Functional pAC50 = 5.1 5.1 -2 4
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 247 3 0 3 2.2 CCOC(=O)C1(CCN(CC1)C)c1ccccc1 10.1038/s41467-023-40064-9
2291 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
2561 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
4932.0 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL631 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
DB01182 3184 None 43 Human Functional pAC50 = 5.1 5.1 -147 13
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 341 11 2 4 3.2 CCCNCC(COc1ccccc1C(=O)CCc1ccccc1)O 10.1038/s41467-023-40064-9
1588 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
28864 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
28864.0 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
43 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
CHEMBL157138 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
DB00589 2325 None 21 Human Functional pAC50 = 7.1 7.1 -467 23
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 338 3 2 2 2.8 CCN(C(=O)N[C@@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c[nH]3)CC 10.1038/s41467-023-40064-9
82146 4532 None 68 Human Functional pAC50 = 5.1 5.1 1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
CHEMBL1023 4532 None 68 Human Functional pAC50 = 5.1 5.1 1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 348 3 1 1 6.1 C=C(c1ccc(C(=O)O)cc1)c1cc2c(cc1C)C(C)(C)CCC2(C)C 10.1038/s41467-023-40064-9
2803 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
2803.0 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
516 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
704 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
CHEMBL134 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
DB00575 955 None 40 Human Functional pAC50 = 8.1 8.1 -3 14
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl 10.1038/s41467-023-40064-9
2470 3653 None 40 Human Functional pAC50 = 7.1 7.1 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
3300 3653 None 40 Human Functional pAC50 = 7.1 7.1 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
5265 3653 None 40 Human Functional pAC50 = 7.1 7.1 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
99 3653 None 40 Human Functional pAC50 = 7.1 7.1 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL267930 3653 None 40 Human Functional pAC50 = 7.1 7.1 -13803 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 6 1 4 3.2 Fc1ccc(cc1)C(=O)CCCN1CCC2(CC1)C(=O)NCN2c1ccccc1 10.1038/s41467-023-40064-9
154257 178724 None 43 Human Functional pAC50 = 5.1 5.1 -13 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
CHEMBL46740 178724 None 43 Human Functional pAC50 = 5.1 5.1 -13 19
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 470 7 2 5 6.3 Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12 10.1038/s41467-023-40064-9
6324616 168927 None 18 Human Functional pAC50 = 5.1 5.1 1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 697 2 6 12 4.8 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(cc(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
CHEMBL437765 168927 None 18 Human Functional pAC50 = 5.1 5.1 1 3
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 697 2 6 12 4.8 CO[C@H]1/C=C/O[C@@]2(C)Oc3c(C)c(O)c4c(O)c(cc(O)c4c3C2=O)NC(=O)/C(C)=C\C=C\[C@H](C)[C@H](O)[C@@H](C)[C@@H](O)[C@@H](C)[C@H](OC(C)=O)[C@@H]1C 10.1038/s41467-023-40064-9
3949 100668 None 35 Human Functional pAC50 = 5.1 5.1 -8 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
CHEMBL29188 100668 None 35 Human Functional pAC50 = 5.1 5.1 -8 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 468 8 0 5 4.9 COc1ccc(CN2CCN(C(c3ccc(F)cc3)c3ccc(F)cc3)CC2)c(OC)c1OC 10.1038/s41467-023-40064-9
444029 167860 None 7 Human Functional pAC50 = 5.1 5.1 -1 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 509 6 2 9 2.0 C=C[C@@]1(C)CC(=O)[C@]2(O)[C@@]3(C)[C@@H](O)CCC(C)(C)[C@@H]3[C@H](OC(=O)CCN(C)C)[C@H](OC(C)=O)[C@@]2(C)O1 10.1038/s41467-023-40064-9
CHEMBL4303178 167860 None 7 Human Functional pAC50 = 5.1 5.1 -1 2
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 509 6 2 9 2.0 C=C[C@@]1(C)CC(=O)[C@]2(O)[C@@]3(C)[C@@H](O)CCC(C)(C)[C@@H]3[C@H](OC(=O)CCN(C)C)[C@H](OC(C)=O)[C@@]2(C)O1 10.1038/s41467-023-40064-9
4631 197216 None 23 Human Functional pAC50 = 5.1 5.1 -1071 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C 10.1038/s41467-023-40064-9
4631.0 197216 None 23 Human Functional pAC50 = 5.1 5.1 -1071 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C 10.1038/s41467-023-40064-9
CHEMBL546 197216 None 23 Human Functional pAC50 = 5.1 5.1 -1071 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C 10.1038/s41467-023-40064-9
DB01580 197216 None 23 Human Functional pAC50 = 5.1 5.1 -1071 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 265 9 2 4 2.0 C=CCOc1ccccc1OCC(O)CNC(C)C 10.1038/s41467-023-40064-9
71398 106495 None 32 Human Functional pAC50 = 5.1 5.1 -1174 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
CHEMBL313972 106495 None 32 Human Functional pAC50 = 5.1 5.1 -1174 14
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 302 5 4 4 3.6 C[C@@H](Cc1ccc(O)c(O)c1)[C@H](C)Cc1ccc(O)c(O)c1 10.1038/s41467-023-40064-9
31101 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
31101.0 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
35 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
403 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
CHEMBL493 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
DB01200 729 None 28 Human Functional pAC50 = 6.1 6.1 -199 29
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 653 5 3 6 3.2 CC(C[C@H]1C(=O)N2CCC[C@H]2[C@]2(N1C(=O)[C@@](O2)(NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)c([nH]3)Br)C(C)C)O)C 10.1038/s41467-023-40064-9
11057 176253 None 16 Human Functional pAC50 = 6.1 6.1 -1 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
3468 176253 None 16 Human Functional pAC50 = 6.1 6.1 -1 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL459265 176253 None 16 Human Functional pAC50 = 6.1 6.1 -1 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
CHEMBL64894 176253 None 16 Human Functional pAC50 = 6.1 6.1 -1 25
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 372 4 0 2 4.5 CN(C)c1ccc(C(=C2C=CC(=[N+](C)C)C=C2)c2ccc(N(C)C)cc2)cc1 10.1038/s41467-023-40064-9
636403 188375 None 19 Human Functional pAC50 = 5.1 5.1 -3 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
CHEMBL499915 188375 None 19 Human Functional pAC50 = 5.1 5.1 -3 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 570 5 2 5 6.8 CC1(C)[C@@H](OC(=O)CCC(=O)O)CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@@](C)(C(=O)O)CC[C@]5(C)CC[C@@]4(C)[C@]3(C)CC[C@@H]12 10.1038/s41467-023-40064-9
124087 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
124087.0 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
7157 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
814 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
CHEMBL1172 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
DB00967 1389 None 72 Human Functional pAC50 = 5.1 5.1 -112 27
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 310 0 1 2 4.0 Clc1ccc2c(c1)CCc1c(C2=C2CCNCC2)nccc1 10.1038/s41467-023-40064-9
41684 31229 None 62 Human Functional pAC50 = 5.1 5.1 -19 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
CHEMBL1401 31229 None 62 Human Functional pAC50 = 5.1 5.1 -19 32
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 1 7 2.2 CC(=O)Oc1ccccc1C(=O)Nc1ncc([N+](=O)[O-])s1 10.1038/s41467-023-40064-9
5284550 41735 None 12 Human Functional pAC50 = 6.1 6.1 -87 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
5284550.0 41735 None 12 Human Functional pAC50 = 6.1 6.1 -87 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL108947 41735 None 12 Human Functional pAC50 = 6.1 6.1 -87 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
CHEMBL1492500 41735 None 12 Human Functional pAC50 = 6.1 6.1 -87 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
DB09167 41735 None 12 Human Functional pAC50 = 6.1 6.1 -87 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 295 3 0 2 4.7 CN(C)CC/C=C1\c2ccccc2CSc2ccccc21 10.1038/s41467-023-40064-9
21855 84280 None 37 Human Functional pAC50 = 5.1 5.1 -112 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
21855.0 84280 None 37 Human Functional pAC50 = 5.1 5.1 -112 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
CHEMBL22108 84280 None 37 Human Functional pAC50 = 5.1 5.1 -112 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
DB08801 84280 None 37 Human Functional pAC50 = 5.1 5.1 -112 9
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 292 5 0 2 4.1 CC(C1=C(CCN(C)C)Cc2ccccc21)c1ccccn1 10.1038/s41467-023-40064-9
134 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
1775 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
9681.0 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
CHEMBL1065 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
DB00247 2514 None 19 Human Functional pAC50 = 6.1 6.1 -457 18
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 353 4 2 4 1.9 CC[C@H](NC(=O)[C@H]1CN(C)[C@H]2C(=C1)c1cccc3c1c(C2)cn3C)CO 10.1038/s41467-023-40064-9
2391 209912 None 61 Human Functional pAC50 = 5.1 5.1 -9 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 361 5 0 5 4.1 CC(=O)Oc1ccc(C(c2ccc(OC(C)=O)cc2)c2ccccn2)cc1 10.1038/s41467-023-40064-9
CHEMBL942 209912 None 61 Human Functional pAC50 = 5.1 5.1 -9 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 361 5 0 5 4.1 CC(=O)Oc1ccc(C(c2ccc(OC(C)=O)cc2)c2ccccn2)cc1 10.1038/s41467-023-40064-9
151537 162759 None 30 Human Functional pAC50 = 5.1 5.1 -1 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
41867 162759 None 30 Human Functional pAC50 = 5.1 5.1 -1 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
CHEMBL417 162759 None 30 Human Functional pAC50 = 5.1 5.1 -1 4
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 543 5 6 12 0.0 COc1cccc2c1C(=O)c1c(O)c3c(c(O)c1C2=O)C[C@@](O)(C(=O)CO)C[C@@H]3O[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 10.1038/s41467-023-40064-9
3294 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
71360.0 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
87 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
CHEMBL14376 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
DB04946 2006 None 61 Human Functional pAC50 = 8.0 8.0 -3 23
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 426 8 0 6 4.8 COc1cc(ccc1OCCCN1CCC(CC1)c1noc2c1ccc(c2)F)C(=O)C 10.1038/s41467-023-40064-9
1343 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
3519.0 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
522 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
CHEMBL862 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
DB01018 1889 None 43 Human Functional pAC50 = 8.0 8.0 -9 12
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 245 2 2 1 1.3 O=C(Cc1c(Cl)cccc1Cl)N=C(N)N 10.1038/s41467-023-40064-9
2683 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
5487.0 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
7308 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
CHEMBL1079 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
DB00697 3834 None 40 Human Functional pAC50 = 8.0 8.0 -10 6
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 10.1038/s41467-023-40064-9
4209 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
4893.0 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
503 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
5385 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
CHEMBL2 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
DB00457 3163 None 48 Human Functional pAC50 = 8 8.0 -24 17
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1038/s41467-023-40064-9
12574 2605 None 60 Human Functional pAC50 = 7.1 7.1 -1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810 2605 None 60 Human Functional pAC50 = 7.1 7.1 -1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
4810.0 2605 None 60 Human Functional pAC50 = 7.1 7.1 -1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
CHEMBL19236 2605 None 60 Human Functional pAC50 = 7.1 7.1 -1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
DB09242 2605 None 60 Human Functional pAC50 = 7.1 7.1 -1 8
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 241 2 2 6 0.8 CC1=NC(=C(C(=N1)Cl)NC2=NCCN2)OC 10.1038/s41467-023-40064-9
2419 3463 None 53 Human Functional pAC50 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
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 = 6.0 6.0 -2511 19
Agonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate readerAgonist activity at human ADRA1A in an in vitro cell-based assay (NIBR assay) measured by fluorescent imaging plate reader
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1038/s41467-023-40064-9
25102847 78250 None 62 Human Functional pAC50 = 5.0 5.0 -7 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
CHEMBL2105717 78250 None 62 Human Functional pAC50 = 5.0 5.0 -7 10
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 501 8 2 6 5.5 COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC 10.1038/s41467-023-40064-9
3397 207946 None 70 Human Functional pAC50 = 5.0 5.0 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
CHEMBL806 207946 None 70 Human Functional pAC50 = 5.0 5.0 -1 7
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 276 3 1 3 3.2 CC(C)C(=O)Nc1ccc([N+](=O)[O-])c(C(F)(F)F)c1 10.1038/s41467-023-40064-9
135398745 2914 None 65 Human Functional pAC50 = 6.0 6.0 -14 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
135398745.0 2914 None 65 Human Functional pAC50 = 6.0 6.0 -14 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
47 2914 None 65 Human Functional pAC50 = 6.0 6.0 -14 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
CHEMBL715 2914 None 65 Human Functional pAC50 = 6.0 6.0 -14 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
DB00334 2914 None 65 Human Functional pAC50 = 6.0 6.0 -14 33
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 312 1 1 5 1.7 CN1CCN(CC1)C1=c2cc(sc2=Nc2c(N1)cccc2)C 10.1038/s41467-023-40064-9
277 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
2913.0 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
765 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
CHEMBL516 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
DB00434 1301 None 39 Human Functional pAC50 = 6.0 6.0 -954 29
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 287 0 0 1 4.7 CN1CCC(=C2c3ccccc3C=Cc3c2cccc3)CC1 10.1038/s41467-023-40064-9
610479 15507 None 60 Human Functional pAC50 = 5.0 5.0 1 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
CHEMBL121626 15507 None 60 Human Functional pAC50 = 5.0 5.0 1 5
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 261 3 2 2 4.1 Cc1c(Cl)cccc1Nc1ccccc1C(=O)O 10.1038/s41467-023-40064-9
3280 48463 None 17 Human Functional pAC50 = 5.0 5.0 -5 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
CHEMBL1555736 48463 None 17 Human Functional pAC50 = 5.0 5.0 -5 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 395 10 0 5 5.4 CCOc1ccc(Cc2nccc3cc(OCC)c(OCC)cc23)cc1OCC 10.1038/s41467-023-40064-9
3166 169523 None 18 Human Functional pAC50 = 5.0 5.0 -1230 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
CHEMBL442444 169523 None 18 Human Functional pAC50 = 5.0 5.0 -1230 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 317 8 0 3 4.2 CCN(CC)CCOC(=O)C(c1ccccc1)C1CCCCC1 10.1038/s41467-023-40064-9
2583 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
592 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
65999.0 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
CHEMBL1017 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
DB00966 3776 None 69 Human Functional pAC50 = 5.0 5.0 -3019 16
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 514 7 1 5 7.3 CCCc1nc2c(n1Cc1ccc(cc1)c1ccccc1C(=O)O)cc(cc2C)c1nc2c(n1C)cccc2 10.1038/s41467-023-40064-9
1201549 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
1201549.0 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
333 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
7601 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL1201203 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL438151 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
DB00245 597 None 17 Human Functional pAC50 = 6.0 6.0 -138 26
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 307 4 0 2 4.4 CN1[C@@H]2CC[C@H]1C[C@H](C2)OC(c1ccccc1)c1ccccc1 10.1038/s41467-023-40064-9
2600 3779 None 53 Human Functional pAC50 = 5.0 5.0 -151 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
2608 3779 None 53 Human Functional pAC50 = 5.0 5.0 -151 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
5405 3779 None 53 Human Functional pAC50 = 5.0 5.0 -151 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
CHEMBL17157 3779 None 53 Human Functional pAC50 = 5.0 5.0 -151 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
DB00342 3779 None 53 Human Functional pAC50 = 5.0 5.0 -151 32
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 471 8 2 3 6.4 OC(c1ccc(cc1)C(C)(C)C)CCCN1CCC(CC1)C(c1ccccc1)(c1ccccc1)O 10.1038/s41467-023-40064-9
1400 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3658.0 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
7199 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
91513 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
CHEMBL896 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
DB00557 1957 None 46 Human Functional pAC50 = 5.0 5.0 -15 16
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 374 8 1 4 3.1 OCCOCCN1CCN(CC1)C(c1ccc(cc1)Cl)c1ccccc1 10.1038/s41467-023-40064-9
3678 94845 None 37 Human Functional pAC50 = 6.0 6.0 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
3678.0 94845 None 37 Human Functional pAC50 = 6.0 6.0 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
CHEMBL253371 94845 None 37 Human Functional pAC50 = 6.0 6.0 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
DB01616 94845 None 37 Human Functional pAC50 = 6.0 6.0 -33 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 281 9 0 1 4.6 CCN(CCCc1ccccc1)CCCc1ccccc1 10.1038/s41467-023-40064-9
7019 168079 None 72 Human Functional pAC50 = 5.0 5.0 -2 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL1308088 168079 None 72 Human Functional pAC50 = 5.0 5.0 -2 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
CHEMBL43184 168079 None 72 Human Functional pAC50 = 5.0 5.0 -2 8
Antagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopyAntagonist activity at human ADRA1A in an in vitro cell-based assay measured by fluorescence spectroscopy
ChEMBL 194 0 1 2 3.0 Nc1c2ccccc2nc2ccccc12 10.1038/s41467-023-40064-9
150311 9814 None 69 Human Functional pAC50 = 5 5.0 -2 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
CHEMBL1138 9814 None 69 Human Functional pAC50 = 5 5.0 -2 7
Agonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopyAgonist activity at human ADRA1A in an in vitro cell-based assay (CRO assay) measured by fluorescence spectroscopy
ChEMBL 409 6 2 3 4.9 O=C1[C@H](CC[C@H](O)c2ccc(F)cc2)[C@@H](c2ccc(O)cc2)N1c1ccc(F)cc1 10.1038/s41467-023-40064-9
10934575 206944 None 0 Human Functional pEC50 = 10.0 10.0 3 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72441 206944 None 0 Human Functional pEC50 = 10.0 10.0 3 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 4 2 4 2.1 CSc1ccc(C)cc1NCC1=NCCN1 10.1021/jm000542r
44362146 165029 None 0 Human Functional pEC50 = 9.6 9.6 50 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL422477 165029 None 0 Human Functional pEC50 = 9.6 9.6 50 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1ccc(-c2ccsc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44574074 189578 None 0 Human Functional pEC50 = 9.4 9.4 977 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513691 189578 None 0 Human Functional pEC50 = 9.4 9.4 977 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 2 0 4 2.7 c1ccc([C@@H]2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
11109088 206638 None 0 Human Functional pEC50 = 9.4 9.4 1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70751 206638 None 0 Human Functional pEC50 = 9.4 9.4 1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 255 4 2 4 2.5 CSc1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
22493318 44771 None 0 Human Functional pEC50 = 9.3 9.3 13 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL152155 44771 None 0 Human Functional pEC50 = 9.3 9.3 13 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 241 4 2 4 2.4 c1coc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44362194 34391 None 0 Human Functional pEC50 = 9.3 9.3 10 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142784 34391 None 0 Human Functional pEC50 = 9.3 9.3 10 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1ccc(-c2ccoc2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493352 48288 None 0 Human Functional pEC50 = 9.2 9.2 2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155326 48288 None 0 Human Functional pEC50 = 9.2 9.2 2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ncco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
22493236 60416 None 0 Human Functional pEC50 = 9.1 9.1 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL17491 60416 None 0 Human Functional pEC50 = 9.1 9.1 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 242 4 3 5 0.9 c1ccc(-c2nc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44271661 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL414185 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44271661 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL414185 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
Effective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determinedEffective concentration showing agonistic activity towards Human alpha-1A adrenergic receptor, expressed in rat 1 fibroblast cells was determined
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493280 48289 None 0 Human Functional pEC50 = 9.1 9.1 1 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL155327 48289 None 0 Human Functional pEC50 = 9.1 9.1 1 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2ccno2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44271661 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL414185 161890 None 0 Human Functional pEC50 = 9.1 9.1 -1 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 233 4 2 5 0.9 COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44369431 45369 None 0 Human Functional pEC50 = 9.1 9.1 57 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL152693 45369 None 0 Human Functional pEC50 = 9.1 9.1 57 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccsc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44362208 35442 None 0 Human Functional pEC50 = 9 9.0 3 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143801 35442 None 0 Human Functional pEC50 = 9 9.0 3 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 258 4 1 4 2.8 c1csc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493258 98717 None 0 Human Functional pEC50 = 9 9.0 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL277375 98717 None 0 Human Functional pEC50 = 9 9.0 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cc[nH]n2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44574078 178866 None 0 Human Functional pEC50 = 9 9.0 120 3
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468711 178866 None 0 Human Functional pEC50 = 9 9.0 120 3
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1cncc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44219718 188954 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL506744 188954 None 0 Human Functional pEC50 = 9 9.0 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(-c2cncnc2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44362286 98940 None 0 Human Functional pEC50 = 8.9 8.9 7 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL279136 98940 None 0 Human Functional pEC50 = 8.9 8.9 7 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 1 4 2.3 c1coc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362195 121153 None 0 Human Functional pEC50 = 8.9 8.9 2 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL357129 121153 None 0 Human Functional pEC50 = 8.9 8.9 2 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 241 4 2 3 2.1 c1c[nH]c(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493263 98137 None 0 Human Functional pEC50 = 8.9 8.9 50 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL273316 98137 None 0 Human Functional pEC50 = 8.9 8.9 50 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 5 2 6 1.4 CCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493365 98517 None 0 Human Functional pEC50 = 8.9 8.9 15 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
CHEMBL275844 98517 None 0 Human Functional pEC50 = 8.9 8.9 15 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 241 4 3 4 1.5 c1ccc(-c2cn[nH]c2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(03)00050-7
44329788 210561 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97859 210561 None 0 Human Functional pEC50 = 8.9 8.9 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 2.1 CCC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
11098175 206628 None 0 Human Functional pEC50 = 8.8 8.8 2 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL70691 206628 None 0 Human Functional pEC50 = 8.8 8.8 2 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 251 5 2 5 1.8 COc1ccc(SC)c(NCC2=NCCN2)c1 10.1021/jm000542r
10221005 206780 None 0 Human Functional pEC50 = 8.7 8.7 72 3
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71479 206780 None 0 Human Functional pEC50 = 8.7 8.7 72 3
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 4 2 5 0.8 Cc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44362185 121093 None 0 Human Functional pEC50 = 8.7 8.7 19 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL356605 121093 None 0 Human Functional pEC50 = 8.7 8.7 19 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1cncc(-c2ccccc2OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493343 63992 None 0 Human Functional pEC50 = 8.7 8.7 19 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18069 63992 None 0 Human Functional pEC50 = 8.7 8.7 19 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 2 6 0.9 Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44343410 11559 None 1 Human Functional pEC50 = 8 8.0 -1 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL118055 11559 None 1 Human Functional pEC50 = 8 8.0 -1 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 219 4 2 3 2.7 CSc1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9837963 62991 None 0 Human Functional pEC50 = 8 8.0 8 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17851 62991 None 0 Human Functional pEC50 = 8 8.0 8 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329796 210838 None 0 Human Functional pEC50 = 8 8.0 1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99559 210838 None 0 Human Functional pEC50 = 8 8.0 1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 7 2 5 2.1 CCCCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493289 49702 None 0 Human Functional pEC50 = 8 8.0 4 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL156661 49702 None 0 Human Functional pEC50 = 8 8.0 4 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1cnc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
11034737 206986 None 0 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72724 206986 None 0 Human Functional pEC50 = 8.0 8.0 -1 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 289 4 2 4 2.8 CSc1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44362145 34492 None 0 Human Functional pEC50 = 7 7.0 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142864 34492 None 0 Human Functional pEC50 = 7 7.0 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2ncc[nH]2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
22493401 210708 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98769 210708 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 288 7 2 4 2.0 CCCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493225 62532 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17819 62532 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 270 4 2 6 1.2 Cc1nc(-c2ccccc2NCC2=NCCN2)n(C)n1 10.1016/s0960-894x(03)00050-7
44574878 178652 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL466916 178652 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
22493372 120302 None 0 Human Functional pEC50 = 7.0 7.0 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL352225 120302 None 0 Human Functional pEC50 = 7.0 7.0 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
11059195 102227 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL302698 102227 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 321 4 2 5 1.5 CS(=O)(=O)c1ccc(C(F)(F)F)cc1NCC1=NCCN1 10.1021/jm000542r
44574987 178782 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467915 178782 None 0 Human Functional pEC50 = 8.0 8.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 3 0 3 2.8 FC(F)Oc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
76632 100104 None 24 Human Functional pEC50 = 5.0 5.0 -5 2
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
CHEMBL287047 100104 None 24 Human Functional pEC50 = 5.0 5.0 -5 2
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 181 4 1 3 1.2 COc1ccc(OC)c(CCN)c1 10.1021/jm00144a012
44449657 96119 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260009 96119 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 2 1 3 3.5 Cc1oncc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571891 170119 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL444252 170119 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 280 3 1 4 2.8 Cc1noc(Cc2cccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
2435 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
2435.0 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
395 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
520 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
5386 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
CHEMBL844 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
DB00484 722 None 63 Bovine Functional pEC50 = 6.0 6.0 -26 10
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 291 1 2 5 1.8 Brc1c(ccc2c1nccn2)NC1=NCCN1 nan
44449690 96214 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
CHEMBL260575 96214 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1ccc(-c2cccc3c2CCC3c2ncc[nH]2)nc1 10.1016/j.bmcl.2008.03.070
1960 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260.0 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2857 None 46 Rat Functional pEC50 = 5.9 5.9 -93 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
44574105 178913 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL469127 178913 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 1 4 1.3 CNS(=O)(=O)CCc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44574045 189395 None 0 Human Functional pEC50 = 7.9 7.9 60 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
CHEMBL512062 189395 None 0 Human Functional pEC50 = 7.9 7.9 60 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 260 2 0 2 3.9 c1ccc(-c2ccccc2[C@@H]2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.166
2765 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
515 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
CHEMBL13852 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
DB09202 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(02)00753-9
22493274 11042 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117581 11042 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 4 2 4 2.1 c1ccc(N2CCCCC2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
10015132 163964 None 0 Human Functional pEC50 = 7.9 7.9 29 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
CHEMBL420683 163964 None 0 Human Functional pEC50 = 7.9 7.9 29 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(02)00753-9
9817256 206696 None 0 Human Functional pEC50 = 7.9 7.9 251 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL71001 206696 None 0 Human Functional pEC50 = 7.9 7.9 251 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
2765 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
515 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
CHEMBL13852 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
DB09202 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00764-8
10038958 118789 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL341747 118789 None 0 Human Functional pEC50 = 7.9 7.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cnsc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
10015132 163964 None 0 Human Functional pEC50 = 7.9 7.9 29 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL420683 163964 None 0 Human Functional pEC50 = 7.9 7.9 29 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 253 4 1 4 2.1 c1ccc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
22493265 62154 None 0 Human Functional pEC50 = 7.9 7.9 19 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17776 62154 None 0 Human Functional pEC50 = 7.9 7.9 19 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 6 2 6 1.8 CCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
2765 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
515 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
CHEMBL13852 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
DB09202 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00569-8
44329790 112609 None 0 Human Functional pEC50 = 7.9 7.9 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329928 112609 None 0 Human Functional pEC50 = 7.9 7.9 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 247 5 2 5 1.3 CCOC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493224 210804 None 2 Human Functional pEC50 = 7.9 7.9 6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL99362 210804 None 2 Human Functional pEC50 = 7.9 7.9 6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 5 3 4 0.9 CCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
2765 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
515 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
CHEMBL13852 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
DB09202 943 None 16 Human Functional pEC50 = 7.9 7.9 4 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 216 4 1 3 1.9 C1CN=C(N1)COc1ccccc1C1CC1 10.1016/s0960-894x(01)00822-8
12924821 102952 None 4 Human Functional pEC50 = 6.9 6.9 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
CHEMBL30596 102952 None 4 Human Functional pEC50 = 6.9 6.9 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 207 2 1 3 1.5 COc1ccc(OC)c2c1CCC(N)C2 10.1021/jm00144a012
44593577 178569 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 178569 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
44343251 10523 None 1 Human Functional pEC50 = 6.9 6.9 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL116843 10523 None 1 Human Functional pEC50 = 6.9 6.9 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 251 4 2 4 1.4 CS(=O)(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
44362510 118997 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL342324 118997 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 267 4 1 4 2.4 Cc1cccc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
22493257 210105 None 2 Human Functional pEC50 = 6.9 6.9 2 2
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95245 210105 None 2 Human Functional pEC50 = 6.9 6.9 2 2
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 272 4 2 4 1.3 O=C(c1ccccc1NCC1=NCCN1)N1CCCC1 10.1016/s0960-894x(01)00569-8
44362289 121762 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
CHEMBL358802 121762 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1cnc(-c2ccccc2OCC2=NCCN2)nc1 10.1016/s0960-894x(01)00764-8
44449306 95659 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257801 95659 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 305 5 2 3 2.6 CCCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449730 156199 None 0 Human Functional pEC50 = 7.9 7.9 22 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL406316 156199 None 0 Human Functional pEC50 = 7.9 7.9 22 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2cn[nH]c2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
9817256 206696 None 0 Human Functional pEC50 = 7.9 7.9 251 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
CHEMBL71001 206696 None 0 Human Functional pEC50 = 7.9 7.9 251 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 283 5 2 6 0.5 COc1ccc(S(C)(=O)=O)c(NCC2=NCCN2)c1 10.1021/jm000542r
44449278 95705 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95705 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44574877 178646 None 0 Human Functional pEC50 = 6.8 6.8 23 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466869 178646 None 0 Human Functional pEC50 = 6.8 6.8 23 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.7 COc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44574135 189287 None 1 Human Functional pEC50 = 7.8 7.8 18 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL511211 189287 None 1 Human Functional pEC50 = 7.8 7.8 18 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2ccn[nH]2)c1 10.1016/j.bmcl.2009.03.166
22493269 46840 None 0 Human Functional pEC50 = 7.8 7.8 6 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154023 46840 None 0 Human Functional pEC50 = 7.8 7.8 6 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1ncoc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44343257 10503 None 0 Human Functional pEC50 = 7.8 7.8 13 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL116700 10503 None 0 Human Functional pEC50 = 7.8 7.8 13 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 250 4 1 2 3.7 c1ccc(-c2ccccc2OCc2c[nH]cn2)cc1 10.1016/s0960-894x(02)00753-9
10199052 210413 None 0 Human Functional pEC50 = 7.8 7.8 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL97044 210413 None 0 Human Functional pEC50 = 7.8 7.8 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 258 5 3 4 1.0 O=C(NC1CC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
619552 102753 None 2 Rat Functional pEC50 = 5.8 5.8 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL304747 102753 None 2 Rat Functional pEC50 = 5.8 5.8 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 250 2 0 3 2.5 Cn1nc(Cc2ccccc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
45280075 122429 None 0 Human Functional pEC50 = 5.8 5.8 -91 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3600395 122429 None 0 Human Functional pEC50 = 5.8 5.8 -91 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 430 10 4 6 2.5 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C4CC4)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44343235 10199 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL115977 10199 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 4 1 4 2.6 c1ccc(-c2ccno2)c(OCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44362013 35392 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
CHEMBL143766 35392 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1cc(-c2ccccc2OCC2=NCCN2)sn1 10.1016/s0960-894x(01)00764-8
481 2892 None 6 Human Functional pEC50 = 6.8 6.8 8 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
9838763 2892 None 6 Human Functional pEC50 = 6.8 6.8 8 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
CHEMBL72958 2892 None 6 Human Functional pEC50 = 6.8 6.8 8 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1021/jm000542r
10199335 207205 None 0 Human Functional pEC50 = 7.8 7.8 120 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74467 207205 None 0 Human Functional pEC50 = 7.8 7.8 120 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44574834 172724 None 1 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
CHEMBL449279 172724 None 1 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.3 c1ccc2c(c1)CC(c1ncc[nH]1)C2 10.1016/j.bmcl.2009.03.162
2146 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041.0 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3100 None 45 Rat Functional pEC50 = 5.8 5.8 -186 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44449247 95467 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256984 95467 None 0 Human Functional pEC50 = 6.8 6.8 1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 2 1 2 2.8 COc1c(C)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571843 179427 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473425 179427 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 2.7 COCCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571937 189659 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL514333 189659 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 282 3 1 3 2.9 Fc1ccn(Cc2cccc3c2CCC3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
9794803 11010 None 0 Human Functional pEC50 = 7.8 7.8 4 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL117381 11010 None 0 Human Functional pEC50 = 7.8 7.8 4 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449692 157077 None 0 Human Functional pEC50 = 6.8 6.8 8 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL407308 157077 None 0 Human Functional pEC50 = 6.8 6.8 8 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 1 3 3.1 c1cc(-c2ncco2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
44281493 100050 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
CHEMBL286702 100050 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@H]1NCCCC21 10.1021/jm00144a012
44574106 178531 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466012 178531 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 3 1 3 3.3 CNC(=O)c1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574107 188868 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL505414 188868 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1ccc(C2Cc3nccn3C2)c(-c2cncnc2)c1 10.1016/j.bmcl.2009.03.166
44574935 172725 None 0 Human Functional pEC50 = 7.7 7.7 19 3
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL449284 172725 None 0 Human Functional pEC50 = 7.7 7.7 19 3
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
9794803 11010 None 0 Human Functional pEC50 = 7.7 7.7 4 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL117381 11010 None 0 Human Functional pEC50 = 7.7 7.7 4 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnco2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9859855 60417 None 0 Human Functional pEC50 = 7.7 7.7 12 2
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17492 60417 None 0 Human Functional pEC50 = 7.7 7.7 12 2
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 254 4 2 4 2.1 Cn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
124 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
2032 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
4636 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
4636.0 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
CHEMBL762 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
DB00935 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00569-8
22493320 4205 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100198 4205 None 0 Human Functional pEC50 = 7.7 7.7 3 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 246 4 2 4 0.8 CN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329481 4233 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL100383 4233 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 289 7 2 5 2.4 CCC(CC)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10378649 108649 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL320419 108649 None 0 Human Functional pEC50 = 7.7 7.7 15 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 7 3 4 1.6 CCCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
124 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
2032 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
4636 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
4636.0 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
CHEMBL762 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
DB00935 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1016/s0960-894x(01)00822-8
11811395 207159 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74071 207159 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 281 5 2 5 1.3 CC(C)S(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44571844 172658 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL448510 172658 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 295 4 2 2 3.1 FC(F)(F)CNCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493367 66206 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18436 66206 None 0 Human Functional pEC50 = 6.7 6.7 1 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 298 7 2 6 2.2 CCCCn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44574075 172679 None 0 Human Functional pEC50 = 8.7 8.7 72 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448802 172679 None 0 Human Functional pEC50 = 8.7 8.7 72 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
44369351 119666 None 0 Human Functional pEC50 = 8.7 8.7 2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL346380 119666 None 0 Human Functional pEC50 = 8.7 8.7 2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 4 2.8 c1csc(-c2ccccc2NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
11140347 206991 None 1 Human Functional pEC50 = 8.6 8.6 -1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL72768 206991 None 1 Human Functional pEC50 = 8.6 8.6 -1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1ccc(F)cc1NCC1=NCCN1 10.1021/jm000542r
44362196 34497 None 0 Human Functional pEC50 = 8.6 8.6 7 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142871 34497 None 0 Human Functional pEC50 = 8.6 8.6 7 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2nccs2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362288 35638 None 0 Human Functional pEC50 = 8.6 8.6 251 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL143973 35638 None 0 Human Functional pEC50 = 8.6 8.6 251 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 254 4 1 5 1.5 c1ccc(-c2cnccn2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
9881853 98527 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275902 98527 None 0 Human Functional pEC50 = 8.6 8.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 5 2 4 2.6 CCn1cccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10198532 210155 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95523 210155 None 0 Human Functional pEC50 = 8.6 8.6 1 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 232 4 3 4 0.5 CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44369434 45395 None 0 Human Functional pEC50 = 8.6 8.6 17 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
CHEMBL152725 45395 None 0 Human Functional pEC50 = 8.6 8.6 17 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 255 4 2 4 2.7 Cc1ccc(-c2ccccc2NCC2=NCCN2)o1 10.1016/s0960-894x(01)00822-8
9947861 206620 None 0 Human Functional pEC50 = 8.6 8.6 21 3
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70634 206620 None 0 Human Functional pEC50 = 8.6 8.6 21 3
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1ccc(Cl)cc1NCC1=NCCN1 10.1021/jm000542r
124 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
2032 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
4636.0 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
CHEMBL762 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
DB00935 2981 None 32 Human Functional pEC50 = 7.7 7.7 -8 24
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm000542r
10422033 121039 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL356195 121039 None 0 Human Functional pEC50 = 7.7 7.7 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 246 5 2 5 1.5 CO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281250 114870 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
CHEMBL33405 114870 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 247 2 1 3 2.5 COc1ccc(OC)c2c1CC[C@@H]1NCCCC21 10.1021/jm00144a012
44449691 96215 None 0 Human Functional pEC50 = 5.7 5.7 2 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL260576 96215 None 0 Human Functional pEC50 = 5.7 5.7 2 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 1 2 3.6 c1cncc(-c2cccc3c2CCC3c2ncc[nH]2)c1 10.1016/j.bmcl.2008.03.070
4038180 204 None 12 Human Functional pEC50 = 7.7 7.7 -1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 204 None 12 Human Functional pEC50 = 7.7 7.7 -1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 204 None 12 Human Functional pEC50 = 7.7 7.7 -1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
44449278 95705 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95705 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
1960 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
439260.0 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
505 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
CHEMBL1437 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
DB00368 2857 None 46 Human Functional pEC50 = 5.7 5.7 -2 18
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm960354u
10135864 122584 None 0 Human Functional pEC50 = 6.7 6.7 -10 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601200 122584 None 0 Human Functional pEC50 = 6.7 6.7 -10 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 404 9 4 6 1.9 Cc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44574937 178766 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467688 178766 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
44449276 95704 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257976 95704 None 0 Human Functional pEC50 = 5.7 5.7 1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 241 2 2 2 1.8 CNC(=O)c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
11090351 163486 None 0 Human Functional pEC50 = 7.6 7.6 20 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL419448 163486 None 0 Human Functional pEC50 = 7.6 7.6 20 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
44449278 95705 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257977 95705 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 CS(=O)(=O)Nc1cccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44593577 178569 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 178569 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
10221004 206689 None 0 Human Functional pEC50 = 6.6 6.6 20 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70973 206689 None 0 Human Functional pEC50 = 6.6 6.6 20 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 267 5 2 5 0.9 CCS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
22493356 47025 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL154170 47025 None 0 Human Functional pEC50 = 7.6 7.6 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 266 4 2 4 2.5 Cc1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10804826 23623 None 1 Human Functional pEC50 = 4.6 4.6 1 2
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23623 None 1 Human Functional pEC50 = 4.6 4.6 1 2
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
216249 1305 None 38 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
3469 1305 None 38 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
CHEMBL257978 1305 None 38 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 317 5 2 5 1.4 Clc1ccc(c(c1NS(=O)(=O)C)C)OCC1=NCCN1 10.1016/j.bmcl.2008.03.070
10423384 34605 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
CHEMBL142958 34605 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 272 4 1 4 3.1 Cc1ccc(-c2ccccc2OCC2=NCCN2)s1 10.1016/s0960-894x(01)00764-8
10084685 119500 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
CHEMBL344957 119500 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 273 4 1 5 2.5 Cc1csc(-c2ccccc2OCC2=NCCN2)n1 10.1016/s0960-894x(01)00764-8
10221066 163257 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL417999 163257 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44271931 98446 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL275386 98446 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 283 6 2 5 2.4 CCCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
10180440 122585 None 0 Human Functional pEC50 = 6.6 6.6 -6 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601201 122585 None 0 Human Functional pEC50 = 6.6 6.6 -6 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 4 7 1.6 COc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
2683 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
5487 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
5487.0 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
7308 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
CHEMBL1079 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
DB00697 3834 None 40 Bovine Functional pEC50 = 6.6 6.6 1 6
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 253 1 2 6 1.7 Clc1ccc2c(c1NC1=NCCN1)nsn2 nan
44574138 178610 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466635 178610 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(C2Cc3nccn3C2)c(-n2cccn2)c1 10.1016/j.bmcl.2009.03.166
44593557 184024 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL481322 184024 None 12 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44574874 178498 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL465599 178498 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
122184771 122586 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601202 122586 None 0 Human Functional pEC50 = 6.6 6.6 -3 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 434 11 4 7 2.0 CCOc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
44449723 156225 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL406348 156225 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 1 3 2.9 Cn1nccc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
124 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636.0 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2981 None 32 Rat Functional pEC50 = 6.5 6.5 -52 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2146 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
485 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
6041.0 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
CHEMBL1215 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
DB00388 3100 None 45 Human Functional pEC50 = 5.5 5.5 -20 14
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O 10.1021/jm960354u
44574134 178609 None 0 Human Functional pEC50 = 8.5 8.5 91 3
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL466634 178609 None 0 Human Functional pEC50 = 8.5 8.5 91 3
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(-c2ncco2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574077 178865 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL468710 178865 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 0 4 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2nccs2)c1 10.1016/j.bmcl.2009.03.166
44574136 189149 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL509350 189149 None 0 Human Functional pEC50 = 8.5 8.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 1 3 2.8 Fc1ccc(-c2ccn[nH]2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44449725 96243 None 0 Human Functional pEC50 = 8.5 8.5 208 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL260720 96243 None 0 Human Functional pEC50 = 8.5 8.5 208 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 2 2 3.2 Cc1n[nH]cc1-c1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44269124 28826 None 0 Human Functional pEC50 = 8.5 8.5 23 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
CHEMBL13789 28826 None 0 Human Functional pEC50 = 8.5 8.5 23 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(02)00753-9
44269124 28826 None 0 Human Functional pEC50 = 8.5 8.5 23 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL13789 28826 None 0 Human Functional pEC50 = 8.5 8.5 23 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 252 4 1 3 2.7 c1ccc(-c2ccccc2OCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
10060965 35243 None 0 Human Functional pEC50 = 8.5 8.5 39 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL143562 35243 None 0 Human Functional pEC50 = 8.5 8.5 39 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 4 2.6 Cc1ccoc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816515 62998 None 0 Human Functional pEC50 = 8.5 8.5 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17856 62998 None 0 Human Functional pEC50 = 8.5 8.5 5 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
44329797 108162 None 0 Human Functional pEC50 = 8.5 8.5 67 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL319553 108162 None 0 Human Functional pEC50 = 8.5 8.5 67 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 261 5 2 5 1.7 CC(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
10244367 50057 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL156950 50057 None 0 Human Functional pEC50 = 8.5 8.5 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N\OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11000184 13057 None 0 Human Functional pEC50 = 8.5 8.5 4 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1190038 13057 None 0 Human Functional pEC50 = 8.5 8.5 4 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540035 13057 None 0 Human Functional pEC50 = 8.5 8.5 4 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 235 5 2 4 2.2 CCSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
44343247 110698 None 0 Human Functional pEC50 = 8.4 8.4 15 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL325745 110698 None 0 Human Functional pEC50 = 8.4 8.4 15 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 258 6 3 3 2.2 CCCNC(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
15959112 205990 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL66433 205990 None 0 Rat Functional pEC50 = 5.5 5.5 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 280 2 1 5 2.7 Oc1nnc(Cc2ccc3c(c2)OCO3)c2ccccc12 10.1016/j.bmcl.2006.02.003
11264016 99700 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
CHEMBL284307 99700 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 193 2 1 3 1.1 COc1ccc(OC)c2c1CC(N)C2 10.1021/jm00144a012
44281507 99981 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
CHEMBL286226 99981 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@@H](N)C1 10.1021/jm00144a012
44280965 100037 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
CHEMBL286609 100037 None 0 Human Functional pEC50 = 4.5 4.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 233 2 1 3 2.4 COc1ccc(OC)c2c1C1CCC2[C@H](N)C1 10.1021/jm00144a012
10804826 23623 None 1 Rat Functional pEC50 = 4.5 4.5 -1 2
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL133451 23623 None 1 Rat Functional pEC50 = 4.5 4.5 -1 2
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@@H]2C1=NCCN1 10.1021/jm960354u
44593557 184024 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
CHEMBL481322 184024 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2009.03.166
44593557 184024 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481322 184024 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 262 3 1 2 3.3 COCc1c(Cl)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9816986 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL421011 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
9816986 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL421011 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00764-8
9816986 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL421011 164234 None 0 Human Functional pEC50 = 7.5 7.5 21 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 2 4 1.6 CCN(CC)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44593577 178569 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466296 178569 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.7 c1ccc(C2CCc3nc[nH]c3C2)cc1 10.1016/j.bmcl.2009.03.162
481 2892 None 6 Human Functional pEC50 = 6.5 6.5 8 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
9838763 2892 None 6 Human Functional pEC50 = 6.5 6.5 8 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
CHEMBL72958 2892 None 6 Human Functional pEC50 = 6.5 6.5 8 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 248 4 3 4 0.2 NC[C@@H](c1cc(ccc1F)NS(=O)(=O)C)O 10.1016/s0960-894x(01)00764-8
22493344 98715 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL277361 98715 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 323 5 2 5 2.5 FC(F)(F)Cn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44449277 155273 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402388 155273 None 0 Human Functional pEC50 = 7.5 7.5 -1 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 1 2 2.5 COc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449305 155700 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL404566 155700 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 4 2 3 2.2 CCS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44571889 184135 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
CHEMBL482148 184135 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 264 3 1 3 2.7 c1cc(Cn2cccn2)c2c(c1)[C@H](c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
44449337 155206 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL402003 155206 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1ccn[nH]1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
22493272 44769 None 0 Human Functional pEC50 = 6.5 6.5 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
CHEMBL152154 44769 None 0 Human Functional pEC50 = 6.5 6.5 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1nc(-c2ccccc2NCC2=NCCN2)co1 10.1016/s0960-894x(01)00822-8
44574133 188483 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL501404 188483 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 269 2 0 4 3.0 Fc1ccc(C2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
122184835 122607 None 0 Human Functional pEC50 = 7.5 7.5 3 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601310 122607 None 0 Human Functional pEC50 = 7.5 7.5 3 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 420 10 5 7 1.1 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(CO)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44449249 95251 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255938 95251 None 0 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 291 3 2 3 2.2 Cc1ccc2c(c1NS(C)(=O)=O)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10420352 168843 None 6 Human Functional pEC50 = 5.5 5.5 -83 2
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL43711 168843 None 6 Human Functional pEC50 = 5.5 5.5 -83 2
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
44280982 99818 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
CHEMBL285082 99818 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 205 2 1 3 1.3 COc1ccc(OC)c2c1CC1C2[C@@H]1N 10.1021/jm00144a012
124 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
2032 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
4636.0 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
CHEMBL762 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
DB00935 2981 None 32 Human Functional pEC50 = 6.5 6.5 -8 24
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 260 2 2 3 2.9 Cc1cc(c(c(c1CC1=NCCN1)C)O)C(C)(C)C 10.1021/jm960354u
44574936 178735 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL467495 178735 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 218 1 0 2 2.9 Clc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44369646 120227 None 0 Human Functional pEC50 = 7.4 7.4 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
CHEMBL351543 120227 None 0 Human Functional pEC50 = 7.4 7.4 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 271 4 2 4 3.1 Cc1ccc(-c2ccccc2NCC2=NCCN2)s1 10.1016/s0960-894x(01)00822-8
44571841 179426 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473424 179426 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 228 3 1 2 2.6 COCc1cccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44574988 189338 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511576 189338 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 227 2 1 3 1.3 NC(=O)c1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
521 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
5311068 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
5311068.0 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
835 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
CHEMBL778 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
DB00633 1404 None 49 Bovine Functional pEC50 = 6.4 6.4 -501 5
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 200 2 1 1 3.2 Cc1cccc(c1C)[C@@H](c1c[nH]cn1)C nan
22493349 119751 None 0 Human Functional pEC50 = 7.4 7.4 2 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
CHEMBL347268 119751 None 0 Human Functional pEC50 = 7.4 7.4 2 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 256 4 2 5 2.1 Cc1cc(-c2ccccc2NCC2=NCCN2)on1 10.1016/s0960-894x(01)00822-8
17804479 95713 None 18 Human Functional pEC50 = 6.4 6.4 -1 4
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258007 95713 None 18 Human Functional pEC50 = 6.4 6.4 -1 4
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 1 1 2.9 c1ccc2c(c1)CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
10083742 34615 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
CHEMBL142967 34615 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 256 4 1 5 1.5 Cn1nccc1-c1ccccc1OCC1=NCCN1 10.1016/s0960-894x(01)00764-8
44329739 112387 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL329272 112387 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 287 5 2 5 2.2 O=C(OC1CCCC1)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
104452 205559 None 47 Rat Functional pEC50 = 5.4 5.4 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
CHEMBL63976 205559 None 47 Rat Functional pEC50 = 5.4 5.4 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 270 2 1 3 3.6 Oc1nnc(Cc2ccc(Cl)cc2)c2ccccc12 10.1016/j.bmcl.2006.02.003
22493381 98135 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
CHEMBL273312 98135 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1cc(-c2ccccc2NCC2=NCCN2)cn1 10.1016/s0960-894x(03)00050-7
22493231 210124 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
CHEMBL95333 210124 None 0 Human Functional pEC50 = 6.4 6.4 -5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 286 4 2 4 1.7 O=C(c1ccccc1NCC1=NCCN1)N1CCCCC1 10.1016/s0960-894x(01)00569-8
44574104 189598 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL513871 189598 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 353 4 1 4 3.3 CS(=O)(=O)Nc1cccc(-c2ccccc2[C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
9838376 168403 None 0 Human Functional pEC50 = 8.4 8.4 15 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
CHEMBL434074 168403 None 0 Human Functional pEC50 = 8.4 8.4 15 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 272 4 2 5 2.5 Cc1nc(-c2ccccc2NCC2=NCCN2)cs1 10.1016/s0960-894x(01)00822-8
11108001 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117248 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL540542 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Agonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1A adrenoceptors assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1021/jm000542r
9816460 119957 None 0 Human Functional pEC50 = 8.3 8.3 39 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL349082 119957 None 0 Human Functional pEC50 = 8.3 8.3 39 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 253 4 2 5 1.6 c1ccc(-c2cnccn2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
1028 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
139148732 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
479 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
5816.0 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
CHEMBL679 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
DB00668 291 None 40 Human Functional pEC50 = 6.4 6.4 1 19
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00118a019
11058166 207163 None 0 Human Functional pEC50 = 7.4 7.4 10 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
CHEMBL74114 207163 None 0 Human Functional pEC50 = 7.4 7.4 10 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cccc(F)c1NCC1=NCCN1 10.1021/jm000542r
44574986 189319 None 0 Human Functional pEC50 = 7.4 7.4 7 3
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511411 189319 None 0 Human Functional pEC50 = 7.4 7.4 7 3
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 202 1 0 2 2.4 Fc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
22493415 49987 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL156893 49987 None 0 Human Functional pEC50 = 7.4 7.4 -1 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 268 4 3 6 1.1 Nc1nccc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
44449686 96137 None 0 Human Functional pEC50 = 6.4 6.4 7 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL260116 96137 None 0 Human Functional pEC50 = 6.4 6.4 7 2
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 267 2 1 3 3.6 c1cc(-c2nccs2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
25066019 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL256982 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
25066019 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL256982 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
25066019 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL256982 95465 None 0 Human Functional pEC50 = 7.4 7.4 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 325 3 2 3 2.9 CS(=O)(=O)Nc1c(Cl)ccc2c1CCCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
11079593 206573 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70326 206573 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 271 4 2 5 0.6 CS(=O)(=O)c1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
15959119 77084 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL207277 77084 None 0 Rat Functional pEC50 = 5.4 5.4 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 310 4 0 3 3.8 C=CCn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
44369647 47221 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
CHEMBL154346 47221 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 242 4 2 5 1.8 c1ccc(-c2cnoc2)c(NCC2=NCCN2)c1 10.1016/s0960-894x(01)00822-8
44449248 95250 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL255937 95250 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 248 2 1 2 3.2 COc1c(Cl)ccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95744 None 1 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL258178 95744 None 1 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449338 95744 None 1 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
CHEMBL258178 95744 None 1 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 1 1 2.5 c1ccc2c(c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2009.03.162
44593580 178647 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 178647 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
11747739 13240 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1191324 13240 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL542402 13240 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 237 4 2 4 0.8 C[S+]([O-])c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574103 172691 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448908 172691 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 0 4 2.4 c1ccc(-n2cccn2)c([C@@H]2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
44574137 189199 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL510023 189199 None 0 Human Functional pEC50 = 8.3 8.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 268 2 0 4 2.5 Fc1ccc(-n2cccn2)c(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.166
11108001 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117248 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL540542 10876 None 0 Human Functional pEC50 = 8.3 8.3 -2 5
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 221 4 2 4 1.8 CSc1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44362149 33940 None 0 Human Functional pEC50 = 8.3 8.3 2 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL142387 33940 None 0 Human Functional pEC50 = 8.3 8.3 2 3
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 259 4 1 5 2.2 c1ccc(-c2ccns2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
44362150 119454 None 0 Human Functional pEC50 = 8.3 8.3 15 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
CHEMBL344551 119454 None 0 Human Functional pEC50 = 8.3 8.3 15 2
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 242 4 2 4 1.5 c1ccc(-c2cc[nH]n2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(01)00764-8
10859076 13687 None 0 Human Functional pEC50 = 8.3 8.3 5 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL1194763 13687 None 0 Human Functional pEC50 = 8.3 8.3 5 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL553276 13687 None 0 Human Functional pEC50 = 8.3 8.3 5 4
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 249 5 2 4 2.6 CC(C)Sc1ccccc1NCC1=NCCN1 10.1021/jm000542r
6604803 116582 None 0 Rat Functional pEC50 = 8.3 8.3 1 3
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116582 None 0 Rat Functional pEC50 = 8.3 8.3 1 3
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
6604803 116582 None 0 Human Functional pEC50 = 8.3 8.3 -1 3
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
CHEMBL336161 116582 None 0 Human Functional pEC50 = 8.3 8.3 -1 3
In vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostateIn vitro agonist potency towards Alpha-1A adrenergic receptor in canine prostate
ChEMBL 309 3 3 5 1.2 CS(=O)(=O)Nc1c(O)ccc2c1CCC[C@H]2C1=NCCN1 10.1021/jm960354u
4038180 204 None 12 Rat Functional pEC50 = 8.2 8.2 1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
480 204 None 12 Rat Functional pEC50 = 8.2 8.2 1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
CHEMBL109783 204 None 12 Rat Functional pEC50 = 8.2 8.2 1 6
In vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferensIn vitro agonist potency towards Alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 309 3 3 5 1.2 Oc1ccc2c(c1NS(=O)(=O)C)CCCC2C1=NCCN1 10.1021/jm960354u
9816461 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL117094 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL544290 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44343245 110678 None 1 Human Functional pEC50 = 7.3 7.3 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL325648 110678 None 1 Human Functional pEC50 = 7.3 7.3 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 256 4 2 3 3.0 c1ccc(N2CCCCC2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
44343275 110837 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL326067 110837 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 240 4 2 4 2.7 c1ccc(-c2cnco2)c(NCc2c[nH]cn2)c1 10.1016/s0960-894x(02)00753-9
22493233 169390 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
CHEMBL441412 169390 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 268 4 2 4 2.4 Cc1ccc(-c2ccccc2NCC2=NCCN2)n1C 10.1016/s0960-894x(03)00050-7
9903313 172781 None 0 Human Functional pEC50 = 7.3 7.3 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL450018 172781 None 0 Human Functional pEC50 = 7.3 7.3 5 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 2 4 1.2 CCN(C)C(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493379 210585 None 0 Human Functional pEC50 = 7.3 7.3 2 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98016 210585 None 0 Human Functional pEC50 = 7.3 7.3 2 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 5 3 4 1.2 CC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493411 168133 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL432192 168133 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.6 CCC(C)NC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329701 210137 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95398 210137 None 0 Human Functional pEC50 = 6.3 6.3 -6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 6 2 5 1.9 CC(C)COC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44574044 178536 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL466046 178536 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1[C@@H]1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44219719 178783 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL467916 178783 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 209 1 0 3 2.1 N#Cc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
10399043 120226 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL351542 120226 None 0 Human Functional pEC50 = 7.3 7.3 -2 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 232 5 2 5 1.1 CO/N=C/c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
10916464 206611 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70563 206611 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 287 4 2 5 1.2 CS(=O)(=O)c1cc(Cl)ccc1NCC1=NCCN1 10.1021/jm000542r
44574875 188750 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL503269 188750 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 232 1 1 1 3.3 Clc1cccc(C2CCc3nc[nH]c3C2)c1 10.1016/j.bmcl.2009.03.162
44449245 95466 None 0 Human Functional pEC50 = 7.3 7.3 6 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
CHEMBL256983 95466 None 0 Human Functional pEC50 = 7.3 7.3 6 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 250 2 2 2 2.9 c1cc(-c2ccn[nH]2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.03.070
22493347 119676 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL346465 119676 None 0 Human Functional pEC50 = 7.3 7.3 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CCO/N=C(\C)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44281057 99729 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
CHEMBL284486 99729 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 221 2 1 3 1.9 COc1ccc(OC)c2c1CCCC(N)C2 10.1021/jm00144a012
9816461 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL117094 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL544290 10723 None 4 Human Functional pEC50 = 7.3 7.3 60 2
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1AAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1A
ChEMBL 253 4 2 5 0.5 CS(=O)(=O)c1ccccc1NCC1=NCCN1 10.1021/jm000542r
44574938 189022 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
CHEMBL507755 189022 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1cccc(C2Cc3nccn3C2)c1 10.1016/j.bmcl.2009.03.162
44571888 184023 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL481321 184023 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1cc(F)cc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343244 9954 None 0 Human Functional pEC50 = 8.2 8.2 5 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114669 9954 None 0 Human Functional pEC50 = 8.2 8.2 5 2
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 241 3 3 4 2.0 Oc1ccc2cccc(NCC3=NCCN3)c2c1 10.1016/s0960-894x(02)00753-9
44343236 111427 None 0 Human Functional pEC50 = 8.2 8.2 15 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
CHEMBL327005 111427 None 0 Human Functional pEC50 = 8.2 8.2 15 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 243 4 1 5 1.7 c1ccc(-c2ccno2)c(OCC2=NCCN2)c1 10.1016/s0960-894x(02)00753-9
9903932 59529 None 0 Human Functional pEC50 = 8.2 8.2 501 2
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17151 59529 None 0 Human Functional pEC50 = 8.2 8.2 501 2
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 284 5 2 6 1.9 CC(C)n1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44271932 65232 None 0 Human Functional pEC50 = 8.2 8.2 6 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL18256 65232 None 0 Human Functional pEC50 = 8.2 8.2 6 3
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 255 4 2 5 1.5 Cn1ccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
22493392 47169 None 0 Human Functional pEC50 = 8.2 8.2 3 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
CHEMBL154298 47169 None 0 Human Functional pEC50 = 8.2 8.2 3 3
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 252 4 2 4 2.2 c1ccc(-c2ccccc2NCC2=NCCN2)nc1 10.1016/s0960-894x(01)00822-8
9838192 111375 None 18 Rabbit Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
CHEMBL326702 111375 None 18 Rabbit Functional pEC50 = 7.2 7.2 -2 3
Agonist activity at rabbit urethra adrenergic alpha1A receptorAgonist activity at rabbit urethra adrenergic alpha1A receptor
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmc.2008.02.091
122184772 122587 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601203 122587 None 0 Human Functional pEC50 = 7.2 7.2 -1 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 424 9 4 6 2.3 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(Cl)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44574132 178694 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
CHEMBL467259 178694 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 280 2 0 4 2.8 Fc1cccc(-c2cncnc2)c1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.166
44571842 179378 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL473043 179378 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 242 4 1 2 3.0 CCOCc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44571887 188523 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL502078 188523 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1c(F)ccc2c1CC[C@H]2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
44343243 9847 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
CHEMBL114054 9847 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 239 3 3 3 2.9 Oc1ccc2cccc(NCc3c[nH]cn3)c2c1 10.1016/s0960-894x(02)00753-9
44343173 11025 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
CHEMBL117482 11025 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 272 6 2 3 2.5 CCN(CC)C(=O)c1ccccc1NCc1c[nH]cn1 10.1016/s0960-894x(02)00753-9
9838294 59693 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17221 59693 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 269 5 2 5 2.0 CCn1nccc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
11079 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
3369 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
4436 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
4436.0 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
5509 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
CHEMBL761 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
DB06711 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00569-8
11079 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
3369 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
4436 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
4436.0 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
5509 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
CHEMBL761 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
DB06711 2733 None 38 Human Functional pEC50 = 7.2 7.2 5 7
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 210 2 1 2 2.4 C1CN=C(N1)Cc1cccc2c1cccc2 10.1016/s0960-894x(01)00822-8
25154770 183758 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL480272 183758 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 246 3 1 2 2.8 COCc1ccc(F)c2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
22493325 119826 None 0 Human Functional pEC50 = 6.2 6.2 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
CHEMBL347920 119826 None 0 Human Functional pEC50 = 6.2 6.2 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1noc(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(01)00822-8
22493287 120157 None 0 Human Functional pEC50 = 6.2 6.2 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL350906 120157 None 0 Human Functional pEC50 = 6.2 6.2 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 320 4 2 4 3.2 FC(F)(F)c1cccnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
11097789 103053 None 1 Human Functional pEC50 = 8.1 8.1 -1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL306792 103053 None 1 Human Functional pEC50 = 8.1 8.1 -1 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1cc(F)ccc1NCC1=NCCN1 10.1021/jm000542r
11140345 206629 None 0 Human Functional pEC50 = 8.1 8.1 2 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
CHEMBL70692 206629 None 0 Human Functional pEC50 = 8.1 8.1 2 5
Agonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptorAgonist potency at Alpha-1 adrenergic receptor assayed in rat-1 fibroblasts expressing human Alpha-1 adrenergic receptor
ChEMBL 239 4 2 4 2.0 CSc1c(F)cccc1NCC1=NCCN1 10.1021/jm000542r
9795167 107550 None 0 Human Functional pEC50 = 8.1 8.1 6 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
CHEMBL318544 107550 None 0 Human Functional pEC50 = 8.1 8.1 6 3
Activation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblastsActivation of human alpha-1A adrenergic receptor expressed in rat-1 fibroblasts
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(02)00753-9
44352155 116872 None 0 Human Functional pEC50 = 8.1 8.1 7 5
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
CHEMBL337862 116872 None 0 Human Functional pEC50 = 8.1 8.1 7 5
Activation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathwayActivation of recombinant human adrenergic,alpha-1A receptor expressed in rat-1 fibroblasts determined via calcium mobilization through Gq coupled PLC pathway
ChEMBL 251 4 2 3 2.8 c1ccc(-c2ccccc2NCC2=NCCN2)cc1 10.1016/s0960-894x(01)00764-8
9795167 107550 None 0 Human Functional pEC50 = 8.1 8.1 6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL318544 107550 None 0 Human Functional pEC50 = 8.1 8.1 6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 260 6 3 4 1.2 CCCNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44329703 210621 None 0 Human Functional pEC50 = 8.1 8.1 7 2
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL98243 210621 None 0 Human Functional pEC50 = 8.1 8.1 7 2
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 275 4 2 5 2.1 CC(C)(C)OC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
44449304 95658 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257800 95658 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 277 3 2 3 1.9 CS(=O)(=O)Nc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
12764879 178528 None 0 Human Functional pEC50 = 7.2 7.2 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 178528 None 0 Human Functional pEC50 = 7.2 7.2 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
172745 100177 None 2 Human Functional pEC50 = 4.2 4.2 -234 2
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
CHEMBL287587 100177 None 2 Human Functional pEC50 = 4.2 4.2 -234 2
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 187 2 4 4 0.2 NCC(O)c1ccc(O)c(O)c1F 10.1021/jm00118a019
1753 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
483 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
6082 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
6082.0 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
CHEMBL524 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
DB00723 2504 None 16 Human Functional pEC50 = 6.1 6.1 2 4
Alpha-1 adrenergic receptor agonist activity in rabbit ear arteryAlpha-1 adrenergic receptor agonist activity in rabbit ear artery
ChEMBL 211 4 2 4 1.1 COc1ccc(c(c1)C(C(N)C)O)OC 10.1021/jm00144a012
12764880 178651 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL466914 178651 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 198 1 0 2 2.6 c1ccc(C2CCc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
22493359 121753 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
CHEMBL358685 121753 None 0 Human Functional pEC50 = 6.1 6.1 -1 2
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 257 4 2 6 1.5 Cc1nc(-c2ccccc2NCC2=NCCN2)no1 10.1016/s0960-894x(01)00822-8
12764879 178528 None 0 Human Functional pEC50 = 7.1 7.1 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 178528 None 0 Human Functional pEC50 = 7.1 7.1 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44593580 178647 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
CHEMBL466876 178647 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 242 3 1 2 2.8 COCc1ccccc1C1CCc2nc[nH]c2C1 10.1016/j.bmcl.2009.03.162
44449303 95657 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
CHEMBL257799 95657 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.03.070
44449303 95657 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL257799 95657 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 284 2 2 2 3.5 Clc1ccc2c(c1-c1cn[nH]c1)CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
9840212 62141 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
CHEMBL17764 62141 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 324 5 2 6 1.9 FC(F)(F)Cn1ncnc1-c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(03)00050-7
44329133 210160 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
CHEMBL95565 210160 None 0 Human Functional pEC50 = 7.1 7.1 -6 3
Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.Agonist potency against cloned human alpha 1A adrenoceptor expressed in rat-1 fibroblasts.
ChEMBL 274 6 3 4 1.5 CC(C)CNC(=O)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00569-8
22493408 61219 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
CHEMBL17657 61219 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cellsAgonism of human alpha-1A adrenergic receptor expressed in rat 1 fibroblast cells
ChEMBL 256 4 3 5 1.2 Cc1n[nH]c(-c2ccccc2NCC2=NCCN2)n1 10.1016/s0960-894x(03)00050-7
541604 165434 None 7 Human Functional pEC50 = 6.1 6.1 - 1
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
CHEMBL42359 165434 None 7 Human Functional pEC50 = 6.1 6.1 - 1
Agonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortexAgonistic potency at alpha-1 adrenergic receptor for the amine-induced increase of phosphatidylinositol breakdown in synaptoneurosomes from guinea pig cerebral cortex
ChEMBL 201 3 4 4 0.5 CNCC(O)c1cc(O)c(O)cc1F 10.1021/jm00118a019
44574079 189418 None 0 Human Functional pEC50 = 7.1 7.1 8 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL512289 189418 None 0 Human Functional pEC50 = 7.1 7.1 8 2
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 261 2 0 3 3.3 c1ccc([C@@H]2Cc3nccn3C2)c(-c2ccncc2)c1 10.1016/j.bmcl.2009.03.166
11522042 206137 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 284 2 0 3 3.2 Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
CHEMBL67457 206137 None 0 Rat Functional pEC50 = 6.1 6.1 - 1
Vasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contractionVasorelaxation of noradrenaline-stimulated Wistar rat vas deferens contraction
ChEMBL 284 2 0 3 3.2 Cn1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O 10.1016/j.bmcl.2006.02.003
45381933 122605 None 0 Human Functional pEC50 = 6.1 6.1 -12 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
CHEMBL3601308 122605 None 0 Human Functional pEC50 = 6.1 6.1 -12 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 458 9 4 6 2.7 CS(=O)(=O)Nc1cccc([C@@H](O)CNCCOc2ccc3c(C(F)(F)F)n[nH]c3c2)c1 10.1021/acs.jmedchem.5b00638
44574989 189339 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 3 0 3 2.4 COCc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
CHEMBL511577 189339 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 228 3 0 3 2.4 COCc1ccccc1C1Cc2nccn2C1 10.1016/j.bmcl.2009.03.162
12764879 178528 None 0 Human Functional pEC50 = 7.1 7.1 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL465963 178528 None 0 Human Functional pEC50 = 7.1 7.1 100 2
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 184 1 0 2 2.2 c1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
44571840 188320 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 276 3 1 3 2.0 CS(=O)(=O)Cc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
CHEMBL499180 188320 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 276 3 1 3 2.0 CS(=O)(=O)Cc1cccc2c1CCC2c1ncc[nH]1 10.1016/j.bmcl.2008.10.066
45381852 122588 None 0 Human Functional pEC50 = 6.1 6.1 -60 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
CHEMBL3601204 122588 None 0 Human Functional pEC50 = 6.1 6.1 -60 2
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 418 10 4 6 2.2 CCc1n[nH]c2cc(OCCNC[C@H](O)c3cccc(NS(C)(=O)=O)c3)ccc12 10.1021/acs.jmedchem.5b00638
22493254 169191 None 0 Human Functional pEC50 = 7.1 7.1 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N/OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
CHEMBL439822 169191 None 0 Human Functional pEC50 = 7.1 7.1 - 1
In vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assayIn vitro activation of human alpha-1A receptor expressed in rat-1 fibroblasts via calcium mobilization through the Gq coupled PLC pathway as functional assay
ChEMBL 260 6 2 5 1.9 CC/C(=N/OC)c1ccccc1NCC1=NCCN1 10.1016/s0960-894x(01)00822-8
44571845 189243 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 289 3 1 2 2.9 FC1(F)CN(Cc2cccc3c2CCC3c2ncc[nH]2)C1 10.1016/j.bmcl.2008.10.066
CHEMBL510613 189243 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 289 3 1 2 2.9 FC1(F)CN(Cc2cccc3c2CCC3c2ncc[nH]2)C1 10.1016/j.bmcl.2008.10.066
2803 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
2803.0 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
516 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
704 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
CHEMBL134 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
DB00575 955 None 40 Bovine Functional pEC50 = 7.1 7.1 -6 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 229 1 2 3 2.4 Clc1cccc(c1NC1=NCCN1)Cl nan
2146 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
485 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
6041 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
6041.0 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
CHEMBL1215 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
DB00388 3100 None 45 Bovine Functional pEC50 = 8.1 8.1 1 14
Agonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assayAgonist activity at bovine recombinant alpha-1A receptor expressed in HEK293 cells coexpressing Gag-pol assessed as increase in intracellular calcium measured after 60 mins by fluo-4 dye based FLIPR assay
ChEMBL 167 3 3 3 0.6 CNC[C@@H](c1cccc(c1)O)O nan
44574080 189054 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
CHEMBL508084 189054 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 264 2 0 4 2.6 Cn1cc(-c2ccccc2[C@@H]2Cc3nccn3C2)cn1 10.1016/j.bmcl.2009.03.166
9838192 111375 None 18 Human Functional pEC50 = 8.1 8.1 2 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2008.03.070
CHEMBL326702 111375 None 18 Human Functional pEC50 = 8.1 8.1 2 3
Agonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha-1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 265 5 2 3 1.8 CCS(=O)(=O)Nc1cccc(Cc2c[nH]cn2)c1 10.1016/j.bmcl.2008.03.070
44571938 180179 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
CHEMBL474796 180179 None 0 Human Functional pEC50 = 8.1 8.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 300 3 1 3 3.0 Fc1ccn(Cc2c(F)ccc3c2CC[C@H]3c2ncc[nH]2)n1 10.1016/j.bmcl.2008.10.066
1960 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
439260 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
439260.0 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
505 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
CHEMBL1437 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
DB00368 2857 None 46 Human Functional pEC50 = 8.0 8.0 -2 18
Agonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assayAgonist activity at human alpha1A-adrenergic receptor expressed in HEK293 cells assessed as calcium flux by fluorescence assay
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/acs.jmedchem.5b00638
44571890 192085 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 265 3 1 4 2.1 c1cc(Cn2ccnn2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
CHEMBL520117 192085 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assayAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells by calcium mobilization-based fluorescence assay
ChEMBL 265 3 1 4 2.1 c1cc(Cn2ccnn2)c2c(c1)C(c1ncc[nH]1)CC2 10.1016/j.bmcl.2008.10.066
44574076 172564 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
CHEMBL448147 172564 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 251 2 0 4 2.9 c1ccc([C@H]2Cc3nccn3C2)c(-c2ncco2)c1 10.1016/j.bmcl.2009.03.166
44574985 188514 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
CHEMBL501920 188514 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPRAgonist activity at human cloned adrenergic alpha1A receptor expressed in CHO cells assessed as calcium mobilization by FLIPR
ChEMBL 214 2 0 3 2.2 COc1ccc(C2Cc3nccn3C2)cc1 10.1016/j.bmcl.2009.03.162
123562321 140598 None 0 Human Functional pIC50 = 9.5 9.5 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1ccc(F)cc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810110 140598 None 0 Human Functional pIC50 = 9.5 9.5 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1ccc(F)cc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
129211 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
129211.0 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
2562 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
488 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
CHEMBL836 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
DB00706 3749 None 48 Human Functional pIC50 = 9.5 9.5 -1 14
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1016/j.ejmech.2020.112616
499 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
5685 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
CHEMBL25554 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levelsAntagonist activity against human recombinant alpha1 receptor expressed in CHOK1 cells assessed as reduction in epinephrine-induced increase in intracellular Ca2+ levels
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.ejmech.2014.12.045
499 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
5685 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
CHEMBL25554 4077 None 13 Human Functional pIC50 = 9 9.0 - 1
Antagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ releaseAntagonist activity at human recombinant alpha1A adrenoceptor assessed as inhibition of epinephrine-induced intracellular Ca2+ release
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm401895u
123854385 140603 None 0 Human Functional pIC50 = 8.9 8.9 72 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 527 13 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810145 140603 None 0 Human Functional pIC50 = 8.9 8.9 72 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 527 13 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
4151 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
493 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
5312125 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
5312125.0 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
CHEMBL24778 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
DB06207 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.6b01217
4151 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
493 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
5312125 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
5312125.0 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
CHEMBL24778 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
DB06207 3607 None 59 Human Functional pIC50 = 8.7 8.7 1 11
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 OCCCN1CCc2c1c(cc(c2)C[C@H](NCCOc1ccccc1OCC(F)(F)F)C)C(=O)N 10.1021/acs.jmedchem.5b02023
9913616 140470 None 8 Human Functional pIC50 = 8.7 8.7 8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 13 3 6 3.7 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808572 140470 None 8 Human Functional pIC50 = 8.7 8.7 8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 13 3 6 3.7 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
10160408 140527 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 13 3 6 3.1 CCOc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809248 140527 None 0 Human Functional pIC50 = 8.7 8.7 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 13 3 6 3.1 CCOc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
86344174 140555 None 0 Human Functional pIC50 = 8.7 8.7 251 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809490 140555 None 0 Human Functional pIC50 = 8.7 8.7 251 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
2389 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
5073 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
5073.0 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
96 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
CHEMBL85 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
DB00734 3331 None 72 Human Functional pIC50 = 8 8.0 -13 29
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.bmcl.2018.01.038
2389 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
5073 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
5073.0 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
96 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
CHEMBL85 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
DB00734 3331 None 72 Human Functional pIC50 = 8.0 8.0 -13 29
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 410 4 0 6 3.6 Fc1ccc2c(c1)onc2C1CCN(CC1)CCc1c(C)nc2n(c1=O)CCCC2 10.1016/j.ejmech.2017.12.099
145946682 167673 None 0 Human Functional pIC50 = 6.0 6.0 -10 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4225239 167673 None 0 Human Functional pIC50 = 6.0 6.0 -10 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4300633 167673 None 0 Human Functional pIC50 = 6.0 6.0 -10 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 444 7 0 3 5.6 Fc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
145964299 164227 None 0 Human Functional pIC50 = 8.0 8.0 -1 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4210030 164227 None 0 Human Functional pIC50 = 8.0 8.0 -1 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 426 8 1 6 3.8 CNC(=O)c1cc(OCCCCN2CCC(c3noc4cc(F)ccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
76071739 142884 None 0 Human Functional pIC50 = 7.9 7.9 -25 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3892879 142884 None 0 Human Functional pIC50 = 7.9 7.9 -25 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
145946986 167705 None 0 Human Functional pIC50 = 5.9 5.9 -4 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4227241 167705 None 0 Human Functional pIC50 = 5.9 5.9 -4 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4300995 167705 None 0 Human Functional pIC50 = 5.9 5.9 -4 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 460 7 0 3 6.2 Clc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
145990794 166896 None 0 Human Functional pIC50 = 6.9 6.9 -19 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4284346 166896 None 0 Human Functional pIC50 = 6.9 6.9 -19 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 437 6 0 5 3.8 O=C1[C@H]2[C@@H]3CC[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
131978695 150950 None 0 Human Functional pIC50 = 6.9 6.9 5 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 440 5 1 4 5.4 COc1ccc2[nH]c3c(c2c1)CC1c2cc(OCc4ccccc4)c(OC)cc2CCN1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3957222 150950 None 0 Human Functional pIC50 = 6.9 6.9 5 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 440 5 1 4 5.4 COc1ccc2[nH]c3c(c2c1)CC1c2cc(OCc4ccccc4)c(OC)cc2CCN1C3 10.1021/acs.jmedchem.6b01217
134138882 147816 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3932187 147816 None 0 Human Functional pIC50 = 6.9 6.9 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
44575544 174102 None 0 Human Functional pIC50 = 7.9 7.9 -3 4
Inhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
CHEMBL454246 174102 None 0 Human Functional pIC50 = 7.9 7.9 -3 4
Inhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetryInhibition of adrenergic receptor 1a expressed in HEK293 cells assessed as inhibition of calcium influx after 10 mins by Fluo-4-AM based fluorimetry
ChEMBL 794 5 5 13 3.0 CC(C)CC(=O)O[C@H]1/C=C/C=C/C(=O)O[C@H]2[C@@H](C)C[C@@H]3[C@]2(O)[C@H](O)[C@@]2(CO)O[C@H]2[C@H]2[C@H]4OC5(c6ccccc6)O[C@@H]([C@@H](C)[C@@]23O5)[C@@]4(O)[C@](C)(O)C[C@H]2CC[C@H]1[C@H]2C 10.1021/np3000359
127044893 140495 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 411 11 3 5 2.4 Cc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808878 140495 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 411 11 3 5 2.4 Cc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134157118 154291 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 332 0 0 4 3.6 Cn1c2c(c3ccccc31)CC1c3cc4c(cc3CCN1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3985901 154291 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 332 0 0 4 3.6 Cn1c2c(c3ccccc31)CC1c3cc4c(cc3CCN1C2)OCO4 10.1021/acs.jmedchem.6b01217
123141715 140622 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 459 12 3 6 3.4 COc1cc(Cl)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810401 140622 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 459 12 3 6 3.4 COc1cc(Cl)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
44347716 16315 None 0 Rat Functional pIC50 = 4.8 4.8 4 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 590 27 4 8 6.3 COc1cccc(CNCCCCCCNCCSSCCNCCCCCCNCc2ccccc2OC)c1 10.1021/jm000995w
CHEMBL122621 16315 None 0 Rat Functional pIC50 = 4.8 4.8 4 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 590 27 4 8 6.3 COc1cccc(CNCCCCCCNCCSSCCNCCCCCCNCc2ccccc2OC)c1 10.1021/jm000995w
145966333 164155 None 0 Human Functional pIC50 = 6.8 6.8 -134 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4209188 164155 None 0 Human Functional pIC50 = 6.8 6.8 -134 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 424 8 1 6 3.6 CNC(=O)c1cc(OCCCCN2CCN(c3cccc4sccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
123986550 140485 None 0 Human Functional pIC50 = 7.8 7.8 223 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 521 14 3 6 4.2 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3808717 140485 None 0 Human Functional pIC50 = 7.8 7.8 223 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 521 14 3 6 4.2 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
134142282 145778 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3916182 145778 None 0 Human Functional pIC50 = 7.8 7.8 2 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
242 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
34 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
60795 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
60795.0 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
CHEMBL1112 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
DB01238 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.ejmech.2017.12.099
242 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
34 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
60795.0 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
CHEMBL1112 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
DB01238 470 None 70 Human Functional pIC50 = 6.8 6.8 -120 33
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 447 7 1 4 4.9 O=C1CCc2c(N1)cc(cc2)OCCCCN1CCN(CC1)c1cccc(c1Cl)Cl 10.1016/j.bmcl.2018.01.038
145983928 166507 None 0 Human Functional pIC50 = 6.8 6.8 -48 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4277101 166507 None 0 Human Functional pIC50 = 6.8 6.8 -48 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 435 6 0 5 3.6 O=C1[C@H]2[C@@H]3C=C[C@@H](C3)[C@H]2C(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
10820251 96675 None 0 Rat Functional pIC50 = 5.7 5.7 -1 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203233 96675 None 0 Rat Functional pIC50 = 5.7 5.7 -1 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL263434 96675 None 0 Rat Functional pIC50 = 5.7 5.7 -1 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCNCCSSCCNCCCCCCNCc3ccccc3C(=O)N(C)CCCCCCN(C)c3nc(N)c4cc(OC)c(OC)cc4n3)nc(N)c2cc1OC 10.1021/jm000995w
10606263 141638 None 0 Rat Functional pIC50 = 5.7 5.7 20 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccc(CNCCCCCCNCCSSCCNCCCCCCNCc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL384790 141638 None 0 Rat Functional pIC50 = 5.7 5.7 20 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccc(CNCCCCCCNCCSSCCNCCCCCCNCc5ccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)cc5)cc4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
123472560 140581 None 0 Human Functional pIC50 = 8.7 8.7 616 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809840 140581 None 0 Human Functional pIC50 = 8.7 8.7 616 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
129211 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
129211.0 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
2562 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
488 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
CHEMBL836 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
DB00706 3749 None 48 Human Functional pIC50 = 8.7 8.7 -1 14
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/acs.jmedchem.6b01217
123415538 140464 None 0 Human Functional pIC50 = 8.6 8.6 8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 491 11 3 5 3.6 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
CHEMBL3808511 140464 None 0 Human Functional pIC50 = 8.6 8.6 8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 491 11 3 5 3.6 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
123667086 140486 None 0 Human Functional pIC50 = 8.6 8.6 -8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 573 13 3 6 3.8 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Br)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808726 140486 None 0 Human Functional pIC50 = 8.6 8.6 -8 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 573 13 3 6 3.8 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Br)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
127044912 140515 None 0 Human Functional pIC50 = 8.6 8.6 -26 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 501 14 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
CHEMBL3809093 140515 None 0 Human Functional pIC50 = 8.6 8.6 -26 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 501 14 3 6 4.3 CC(Cc1cc(C(N)=O)c2c(ccn2CCCO)c1)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
117839022 140618 None 0 Human Functional pIC50 = 8.6 8.6 407 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810346 140618 None 0 Human Functional pIC50 = 8.6 8.6 407 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
124018870 140498 None 0 Human Functional pIC50 = 8.5 8.5 -7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1ccc(F)cc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808896 140498 None 0 Human Functional pIC50 = 8.5 8.5 -7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1ccc(F)cc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123368349 140520 None 0 Human Functional pIC50 = 8.5 8.5 95 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 505 12 3 6 2.9 COc1cc(Br)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809175 140520 None 0 Human Functional pIC50 = 8.5 8.5 95 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 505 12 3 6 2.9 COc1cc(Br)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123387804 140508 None 0 Human Functional pIC50 = 7.7 7.7 -52 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 423 12 3 5 3.3 CCc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3808999 140508 None 0 Human Functional pIC50 = 7.7 7.7 -52 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 423 12 3 5 3.3 CCc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
156767236 183063 None 0 Human Functional pIC50 = 7.7 7.7 9 2
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 449 11 1 5 4.7 COc1ccccc1N1CCN(CCCCn2cc(CCCC(=O)O)c3ccccc32)CC1 10.1016/j.ejmech.2020.112616
CHEMBL4792905 183063 None 0 Human Functional pIC50 = 7.7 7.7 9 2
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 449 11 1 5 4.7 COc1ccccc1N1CCN(CCCCn2cc(CCCC(=O)O)c3ccccc32)CC1 10.1016/j.ejmech.2020.112616
134157566 154115 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1cccc2[nH]c3c(c12)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3984249 154115 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1cccc2[nH]c3c(c12)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
134137522 143185 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3895460 143185 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
123204312 140559 None 0 Human Functional pIC50 = 7.7 7.7 74 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 11 3 5 2.7 Cc1cccc(C)c1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809532 140559 None 0 Human Functional pIC50 = 7.7 7.7 74 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 11 3 5 2.7 Cc1cccc(C)c1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134150827 152256 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 392 5 1 4 4.6 CCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3968227 152256 None 0 Human Functional pIC50 = 6.7 6.7 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 392 5 1 4 4.6 CCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
134155537 151074 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 406 6 1 4 5.0 CCCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3958316 151074 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 406 6 1 4 5.0 CCCCOc1cc2c(cc1OC)CCN1Cc3[nH]c4ccc(OC)cc4c3CC21 10.1021/acs.jmedchem.6b01217
123322716 140610 None 0 Human Functional pIC50 = 7.6 7.6 17 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 5 2.7 CCc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3810198 140610 None 0 Human Functional pIC50 = 7.6 7.6 17 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 5 2.7 CCc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134149598 148565 None 0 Human Functional pIC50 = 6.6 6.6 33 2
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3938121 148565 None 0 Human Functional pIC50 = 6.6 6.6 33 2
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 336 0 1 3 3.7 Fc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
123801568 140576 None 0 Human Functional pIC50 = 7.6 7.6 100 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 11 3 7 1.9 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b02023
CHEMBL3809781 140576 None 0 Human Functional pIC50 = 7.6 7.6 100 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 11 3 7 1.9 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc2c(c1)OCO2 10.1021/acs.jmedchem.5b02023
134150128 152189 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 424 3 1 4 5.1 c1ccc(COc2ccc3[nH]c4c(c3c2)CC2c3cc5c(cc3CCN2C4)OCO5)cc1 10.1021/acs.jmedchem.6b01217
CHEMBL3967696 152189 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 424 3 1 4 5.1 c1ccc(COc2ccc3[nH]c4c(c3c2)CC2c3cc5c(cc3CCN2C4)OCO5)cc1 10.1021/acs.jmedchem.6b01217
9891967 107581 None 21 Human Functional pIC50 = 8.5 8.5 4 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3187195 107581 None 21 Human Functional pIC50 = 8.5 8.5 4 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 495 13 3 6 3.1 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123644751 140590 None 0 Human Functional pIC50 = 8.5 8.5 125 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3810005 140590 None 0 Human Functional pIC50 = 8.5 8.5 125 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123475619 140578 None 0 Human Functional pIC50 = 8.4 8.4 43 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 12 3 6 3.5 COc1cc(Br)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809794 140578 None 0 Human Functional pIC50 = 8.4 8.4 43 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 12 3 6 3.5 COc1cc(Br)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
76071859 150441 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3953156 150441 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2[nH]c3c(c2c1)C[C@@H]1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
156767234 182702 None 0 Human Functional pIC50 = 7.5 7.5 10 2
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 467 11 1 4 5.7 O=C(O)CCCc1cn(CCCCCN2CCN(c3ccccc3Cl)CC2)c2ccccc12 10.1016/j.ejmech.2020.112616
CHEMBL4788144 182702 None 0 Human Functional pIC50 = 7.5 7.5 10 2
Antagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assayAntagonist activity at human alpha1A receptor transfected in HEK293 cells co-transfected with Galpha16 assessed as reduction in intracellular calcium release incubated for 40 mins by Fluo-4AM dye based fluorescence assay
ChEMBL 467 11 1 4 5.7 O=C(O)CCCc1cn(CCCCCN2CCN(c3ccccc3Cl)CC2)c2ccccc12 10.1016/j.ejmech.2020.112616
123393714 140561 None 0 Human Functional pIC50 = 6.5 6.5 3 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1ccc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1C 10.1021/acs.jmedchem.5b02023
CHEMBL3809543 140561 None 0 Human Functional pIC50 = 6.5 6.5 3 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1ccc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1C 10.1021/acs.jmedchem.5b02023
145993493 167453 None 0 Human Functional pIC50 = 6.4 6.4 -47 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
CHEMBL4294617 167453 None 0 Human Functional pIC50 = 6.4 6.4 -47 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 439 6 0 5 4.5 O=C1CC2(CCCC2)CC(=O)N1CCCCN1CCN(c2cccc3sccc23)CC1 10.1016/j.ejmech.2017.12.099
145993117 167017 None 0 Human Functional pIC50 = 6.4 6.4 -309 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
CHEMBL4286717 167017 None 0 Human Functional pIC50 = 6.4 6.4 -309 6
Antagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assayAntagonist activity at adrenergic alpha1A receptor (unknown origin) after 10 mins by calcium 5 dye based FLIPR assay
ChEMBL 427 7 0 5 4.4 CCC1(C)CC(=O)N(CCCCN2CCN(c3cccc4sccc34)CC2)C(=O)C1 10.1016/j.ejmech.2017.12.099
123311113 140608 None 0 Human Functional pIC50 = 7.4 7.4 91 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 523 14 3 6 3.6 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3810187 140608 None 0 Human Functional pIC50 = 7.4 7.4 91 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 523 14 3 6 3.6 CCc1ccc(OCC(F)(F)F)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c1 10.1021/acs.jmedchem.5b02023
10582125 81865 None 0 Rat Functional pIC50 = 5.4 5.4 14 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4cccc(CNCCCCCCNCCSSCCNCCCCCCNCc5cccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)c5)c4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL216443 81865 None 0 Rat Functional pIC50 = 5.4 5.4 14 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4cccc(CNCCCCCCNCCSSCCNCCCCCCNCc5cccc(C(=O)N6CCN(c7nc(N)c8cc(OC)c(OC)cc8n7)CC6)c5)c4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
123688273 140568 None 0 Human Functional pIC50 = 8.4 8.4 36 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 513 13 3 6 3.2 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3809630 140568 None 0 Human Functional pIC50 = 8.4 8.4 36 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 513 13 3 6 3.2 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
127044911 140535 None 0 Human Functional pIC50 = 8.4 8.4 -10 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 6 2.7 COc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809319 140535 None 0 Human Functional pIC50 = 8.4 8.4 -10 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 425 12 3 6 2.7 COc1ccccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
123183757 140564 None 0 Human Functional pIC50 = 8.3 8.3 10 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1cc(F)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3809600 140564 None 0 Human Functional pIC50 = 8.3 8.3 10 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 445 12 3 6 2.3 COc1cc(F)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
127044894 140454 None 0 Human Functional pIC50 = 8.3 8.3 3 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 427 12 3 6 2.1 COc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808408 140454 None 0 Human Functional pIC50 = 8.3 8.3 3 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 427 12 3 6 2.1 COc1ccccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
134147190 149886 None 0 Human Functional pIC50 = 6.4 6.4 3 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 334 0 2 4 3.3 Oc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3948551 149886 None 0 Human Functional pIC50 = 6.4 6.4 3 3
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 334 0 2 4 3.3 Oc1ccc2[nH]c3c(c2c1)CC1c2cc4c(cc2CCN1C3)OCO4 10.1021/acs.jmedchem.6b01217
10034370 157084 None 0 Rat Functional pIC50 = 7.3 7.3 38 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203232 157084 None 0 Rat Functional pIC50 = 7.3 7.3 38 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL407315 157084 None 0 Rat Functional pIC50 = 7.3 7.3 38 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3cccc(CNCCCCCCNCCSSCCNCCCCCCNCc4cccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)c4)c3)nc(N)c2cc1OC 10.1021/jm000995w
127043026 140534 None 0 Human Functional pIC50 = 6.3 6.3 8 2
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809314 140534 None 0 Human Functional pIC50 = 6.3 6.3 8 2
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 507 13 3 6 4.0 Cc1ccc(OCC(F)(F)F)c(OCCN[C@@H](C)Cc2cc(C(N)=O)c3c(ccn3CCCO)c2)c1 10.1021/acs.jmedchem.5b02023
16638286 149688 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3946997 149688 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 323 0 0 5 2.8 c1c2c(cc3c1OCO3)CN1CCc3cc4c(cc3C1C2)OCO4 10.1021/acs.jmedchem.6b01217
10034371 166075 None 0 Rat Functional pIC50 = 5.3 5.3 -2 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL1203235 166075 None 0 Rat Functional pIC50 = 5.3 5.3 -2 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL425267 166075 None 0 Rat Functional pIC50 = 5.3 5.3 -2 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1277 47 6 20 10.9 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CNCCCCCCNCCSSCCNCCCCCCNCc4ccc(C(=O)N(C)CCCCCCN(C)c5nc(N)c6cc(OC)c(OC)cc6n5)cc4)cc3)nc(N)c2cc1OC 10.1021/jm000995w
10630100 96654 None 0 Rat Functional pIC50 = 5.3 5.3 1 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccccc4CNCCCCCCNCCSSCCNCCCCCCNCc4ccccc4C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
CHEMBL263289 96654 None 0 Rat Functional pIC50 = 5.3 5.3 1 2
Antagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from ratAntagonist affinity [non competitive (irreversible)] at alpha-1A-adrenoceptors on isolated prostatic Vas deferens from rat
ChEMBL 1161 33 6 20 7.3 COc1cc2nc(N3CCN(C(=O)c4ccccc4CNCCCCCCNCCSSCCNCCCCCCNCc4ccccc4C(=O)N4CCN(c5nc(N)c6cc(OC)c(OC)cc6n5)CC4)CC3)nc(N)c2cc1OC 10.1021/jm000995w
145947950 167835 None 0 Human Functional pIC50 = 6.3 6.3 1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4224703 167835 None 0 Human Functional pIC50 = 6.3 6.3 1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
CHEMBL4302771 167835 None 0 Human Functional pIC50 = 6.3 6.3 1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 440 7 0 3 5.8 Cc1cccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)c1 10.1016/j.bmcl.2018.03.070
21171 187082 None 25 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL490533 187082 None 25 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 339 2 0 5 3.1 COc1ccc2c(c1OC)CN1CCc3cc4c(cc3[C@@H]1C2)OCO4 10.1021/acs.jmedchem.6b01217
142565322 197388 None 0 Human Functional pIC50 = 5.3 5.3 -426 5
Adrenoceptor reporter cell assay (ADRA1A)Adrenoceptor reporter cell assay (ADRA1A)
ChEMBL 391 6 2 6 2.4 CNc1cc[n+](CCNC(=O)c2ccn3c(-c4c(C)noc4C)cnc3c2)cc1 10.6019/CHEMBL5463728
CHEMBL5395039 197388 None 0 Human Functional pIC50 = 5.3 5.3 -426 5
Adrenoceptor reporter cell assay (ADRA1A)Adrenoceptor reporter cell assay (ADRA1A)
ChEMBL 391 6 2 6 2.4 CNc1cc[n+](CCNC(=O)c2ccn3c(-c4c(C)noc4C)cnc3c2)cc1 10.6019/CHEMBL5463728
CHEMBL5410211 197388 None 0 Human Functional pIC50 = 5.3 5.3 -426 5
Adrenoceptor reporter cell assay (ADRA1A)Adrenoceptor reporter cell assay (ADRA1A)
ChEMBL 391 6 2 6 2.4 CNc1cc[n+](CCNC(=O)c2ccn3c(-c4c(C)noc4C)cnc3c2)cc1 10.6019/CHEMBL5463728
CHEMBL5498852 197388 None 0 Human Functional pIC50 = 5.3 5.3 -426 5
Adrenoceptor reporter cell assay (ADRA1A)Adrenoceptor reporter cell assay (ADRA1A)
ChEMBL 391 6 2 6 2.4 CNc1cc[n+](CCNC(=O)c2ccn3c(-c4c(C)noc4C)cnc3c2)cc1 10.6019/CHEMBL5463728
21823379 144814 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 304 1 1 2 3.8 COc1ccc2c(c1)CCN1Cc3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3908813 144814 None 1 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 304 1 1 2 3.8 COc1ccc2c(c1)CCN1Cc3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
4418 34231 None 58 Human Functional pIC50 = 6.3 6.3 -4 18
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
4418.0 34231 None 58 Human Functional pIC50 = 6.3 6.3 -4 18
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
CHEMBL142635 34231 None 58 Human Functional pIC50 = 6.3 6.3 -4 18
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
DB12092 34231 None 58 Human Functional pIC50 = 6.3 6.3 -4 18
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 392 7 1 5 3.4 COc1ccccc1N1CCN(CC(O)COc2cccc3ccccc23)CC1 10.1016/j.bmcl.2018.03.070
145947047 167735 None 0 Human Functional pIC50 = 6.3 6.3 -1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4227513 167735 None 0 Human Functional pIC50 = 6.3 6.3 -1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4301557 167735 None 0 Human Functional pIC50 = 6.3 6.3 -1 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 425 7 0 2 6.6 c1ccc(C2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
123576734 140511 None 0 Human Functional pIC50 = 7.2 7.2 15 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 455 13 3 6 2.7 CCc1ccc(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(OC)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809032 140511 None 0 Human Functional pIC50 = 7.2 7.2 15 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 455 13 3 6 2.7 CCc1ccc(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(OC)c1 10.1021/acs.jmedchem.5b02023
76071738 148417 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2[C@@H]1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3937032 148417 None 0 Human Functional pIC50 = 7.2 7.2 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 0 1 3 3.6 c1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2[C@@H]1C3)OCO4 10.1021/acs.jmedchem.6b01217
145946630 167672 None 0 Human Functional pIC50 = 7.2 7.2 12 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4224794 167672 None 0 Human Functional pIC50 = 7.2 7.2 12 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
CHEMBL4300618 167672 None 0 Human Functional pIC50 = 7.2 7.2 12 3
Antagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assayAntagonist activity at alpha 1A adrenergic receptor (unknown origin) by luciferase reporter gene assay
ChEMBL 456 8 0 4 5.5 COc1ccc(N2CCN(CCc3ccc(COc4ccc5c(c4)CCCC5)cc3)CC2)cc1 10.1016/j.bmcl.2018.03.070
123752717 140557 None 0 Human Functional pIC50 = 7.2 7.2 26 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1cc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(C)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809500 140557 None 0 Human Functional pIC50 = 7.2 7.2 26 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 439 11 3 5 3.1 Cc1cc(C)c(OCCNC(C)Cc2cc3c(c(C(N)=O)c2)N(CCCO)CC3)c(C)c1 10.1021/acs.jmedchem.5b02023
134145079 150310 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
CHEMBL3952204 150310 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 348 1 1 4 3.6 COc1ccc2c3c([nH]c2c1)CN1CCc2cc4c(cc2C1C3)OCO4 10.1021/acs.jmedchem.6b01217
127044906 140505 None 0 Human Functional pIC50 = 7.2 7.2 7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
CHEMBL3808981 140505 None 0 Human Functional pIC50 = 7.2 7.2 7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 529 13 3 6 3.7 C[C@@H](Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1cc(Cl)ccc1OCC(F)(F)F 10.1021/acs.jmedchem.5b02023
123183788 140613 None 0 Human Functional pIC50 = 8.1 8.1 7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 12 3 6 2.4 COc1cc(C)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3810220 140613 None 0 Human Functional pIC50 = 8.1 8.1 7 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 441 12 3 6 2.4 COc1cc(C)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
123378354 140474 None 0 Human Functional pIC50 = 7.2 7.2 6 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 11 3 5 3.0 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
CHEMBL3808595 140474 None 0 Human Functional pIC50 = 7.2 7.2 6 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 493 11 3 5 3.0 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccc(F)cc1Br 10.1021/acs.jmedchem.5b02023
145963961 164498 None 0 Human Functional pIC50 = 7.2 7.2 -32 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
CHEMBL4213342 164498 None 0 Human Functional pIC50 = 7.2 7.2 -32 6
Antagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assayAntagonistic activity at alpha-1A adrenergic receptor (unknown origin) after 10 mins by FLIPR assay
ChEMBL 425 8 1 7 3.0 CNC(=O)c1cc(OCCCCN2CCN(c3nsc4ccccc34)CC2)ccn1 10.1016/j.bmcl.2018.01.038
134157568 154549 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3984336 154549 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
CHEMBL3990197 154549 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 352 4 0 4 3.1 COc1cc2cc[n+]3c(c2cc1OC)Cc1ccc(OC)c(OC)c1C3 10.1021/acs.jmedchem.6b01217
127044916 140569 None 0 Human Functional pIC50 = 8.1 8.1 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1cc(F)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
CHEMBL3809676 140569 None 0 Human Functional pIC50 = 8.1 8.1 1 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 443 12 3 6 2.9 COc1cc(F)ccc1OCCNC(C)Cc1cc(C(N)=O)c2c(ccn2CCCO)c1 10.1021/acs.jmedchem.5b02023
123437117 140456 None 0 Human Functional pIC50 = 8.1 8.1 23 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 461 12 3 6 2.8 COc1cc(Cl)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
CHEMBL3808417 140456 None 0 Human Functional pIC50 = 8.1 8.1 23 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 461 12 3 6 2.8 COc1cc(Cl)ccc1OCCNC(C)Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2 10.1021/acs.jmedchem.5b02023
127045050 140480 None 0 Human Functional pIC50 = 8.1 8.1 -5 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 14 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
CHEMBL3808632 140480 None 0 Human Functional pIC50 = 8.1 8.1 -5 3
Antagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 minsAntagonist activity at human alpha-1A adrenergic receptor transfected in HEK293 cells assessed as reduction in agonist-induced calcium mobilization after 10 mins
ChEMBL 503 14 3 6 3.7 CC(Cc1cc2c(c(C(N)=O)c1)N(CCCO)CC2)NCCOc1ccccc1OCc1ccccc1 10.1021/acs.jmedchem.5b02023
118167692 164304 None 12 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at alpha1A adrenergic receptor (unknown origin)Antagonist activity at alpha1A adrenergic receptor (unknown origin)
ChEMBL 521 7 1 7 3.0 Cn1cnc(-c2cnc(O[C@H]3CCN(C(=O)Cc4ccc(OC(F)(F)F)cc4)C[C@H]3F)c(C(N)=O)c2)c1 10.1021/acs.jmedchem.8b00633
CHEMBL4210892 164304 None 12 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at alpha1A adrenergic receptor (unknown origin)Antagonist activity at alpha1A adrenergic receptor (unknown origin)
ChEMBL 521 7 1 7 3.0 Cn1cnc(-c2cnc(O[C@H]3CCN(C(=O)Cc4ccc(OC(F)(F)F)cc4)C[C@H]3F)c(C(N)=O)c2)c1 10.1021/acs.jmedchem.8b00633
134134752 144297 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 1 1 2 4.4 COc1ccc2c(c1)CCN1C(C)c3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
CHEMBL3904395 144297 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assayAntagonist activity at human full-length N-terminal SNAP-tagged alpha1A adrenoceptor expressed in HEK293 cells assessed as inhibition of agonist-induced calcium mobilization preincubated for 10 mins followed by agonist addition by fluo-4 AM dye-based assay
ChEMBL 318 1 1 2 4.4 COc1ccc2c(c1)CCN1C(C)c3[nH]c4ccccc4c3CC21 10.1021/acs.jmedchem.6b01217
10813278 106996 None 0 Rabbit Functional pKd = 10.7 10.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 6 3.5 Cc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(-n2cccc2)c1 10.1021/jm970166j
CHEMBL314880 106996 None 0 Rabbit Functional pKd = 10.7 10.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 446 8 1 6 3.5 Cc1ccc(N2CCN(CCCNc3ncccc3C(=O)N(C)C)CC2)c(-n2cccc2)c1 10.1021/jm970166j
10697270 106234 None 0 Rabbit Functional pKd = 10 10.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 519 9 2 8 3.2 CNC(=O)c1cnc2c(c(C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL313775 106234 None 0 Rabbit Functional pKd = 10 10.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 519 9 2 8 3.2 CNC(=O)c1cnc2c(c(C)nn2C)c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
10552132 112851 None 0 Rabbit Functional pKd = 10 10.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 465 9 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL330579 112851 None 0 Rabbit Functional pKd = 10 10.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 465 9 1 6 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
13305910 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
13305910 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL1182155 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL215421 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3741808 11840 None 0 Rat Functional pKd = 10.0 10.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
10506159 111463 None 0 Rabbit Functional pKd = 9.9 9.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 8 1 9 3.4 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccc(F)cc4-c4ncco4)CC3)c12 10.1021/jm970166j
CHEMBL327231 111463 None 0 Rabbit Functional pKd = 9.9 9.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 8 1 9 3.4 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccc(F)cc4-c4ncco4)CC3)c12 10.1021/jm970166j
10693231 205219 None 0 Human Functional pKd = 9.8 9.8 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62033 205219 None 0 Human Functional pKd = 9.8 9.8 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
129211 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
129211.0 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
2562 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
488 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
CHEMBL836 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
DB00706 3749 None 48 Rabbit Functional pKd = 9.8 9.8 - 14
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970166j
10526964 209423 None 0 Rabbit Functional pKd = 9.8 9.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
CHEMBL91278 209423 None 0 Rabbit Functional pKd = 9.8 9.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 437 10 1 6 3.2 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2OCC2CC2)CC1 10.1021/jm970166j
10764021 209449 None 0 Rabbit Functional pKd = 9.7 9.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 9 1 5 3.4 CCCc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91400 209449 None 0 Rabbit Functional pKd = 9.7 9.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 9 1 5 3.4 CCCc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
24897950 56368 None 0 Rat Functional pKd = 9.6 9.6 - 0
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
CHEMBL1630940 56368 None 0 Rat Functional pKd = 9.6 9.6 - 0
Antagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Wistar rat vas deferens assessed as noradrenaline induced contractions after 30 mins
ChEMBL 462 11 2 6 2.9 COc1ccc(C[C@@H](C)NCCOc2ccccc2OCC(F)(F)F)cc1S(N)(=O)=O 10.1016/j.ejmech.2010.09.042
71462043 84602 None 0 Rat Functional pKd = 9.6 9.6 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153555 84602 None 0 Rat Functional pKd = 9.6 9.6 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220895 84602 None 0 Rat Functional pKd = 9.6 9.6 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
129211 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211.0 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
129211.0 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
2562 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
488 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
CHEMBL836 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
DB00706 3749 None 48 Human Functional pKd = 9.5 9.5 -1 14
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
499 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
5685 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic activity at ADRA1A in isolated rat prostatic vas deferensAntagonistic activity at ADRA1A in isolated rat prostatic vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1016/j.bmcl.2005.09.027
499 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
5685 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.5 9.5 - 1
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
10526831 111452 None 0 Rabbit Functional pKd = 9.5 9.5 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 434 8 1 7 3.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ncco2)CC1 10.1021/jm970166j
CHEMBL327168 111452 None 0 Rabbit Functional pKd = 9.5 9.5 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 434 8 1 7 3.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ncco2)CC1 10.1021/jm970166j
13305910 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182155 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL215421 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL3741808 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
13305910 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL1182155 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL215421 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
CHEMBL3741808 11840 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 345 8 1 6 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2ccccc2O1 10.1016/j.ejmech.2012.09.049
129211 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211.0 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
2562 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
488 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
CHEMBL836 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
DB00706 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm970364a
129211 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
129211.0 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
2562 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
488 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
CHEMBL836 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
DB00706 3749 None 48 Rat Functional pKd = 9.5 9.5 - 14
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 408 11 2 6 2.3 CCOc1ccccc1OCCN[C@@H](Cc1ccc(c(c1)S(=O)(=O)N)OC)C 10.1021/jm000541z
44289437 169966 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
CHEMBL44403 169966 None 0 Rat Functional pKd = 9.5 9.5 - 0
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
10789770 100939 None 0 Human Functional pKd = 9.5 9.5 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL293695 100939 None 0 Human Functional pKd = 9.5 9.5 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
10645210 208937 None 0 Rabbit Functional pKd = 9.4 9.4 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 8 1 5 3.5 CC(C)c1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88211 208937 None 0 Rabbit Functional pKd = 9.4 9.4 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 409 8 1 5 3.5 CC(C)c1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
499 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
5685 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
499 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
5685 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.4 9.4 - 1
Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )Antagonistic activity against (-)-noradrenaline-induced contraction of rat prostatic vas deferens (Alpha-1A adrenergic receptor )
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm021078o
44289437 169966 None 0 Rat Functional pKd = 9.4 9.4 - 0
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
CHEMBL44403 169966 None 0 Rat Functional pKd = 9.4 9.4 - 0
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 431 9 1 5 4.7 COc1cccc(OC)c1OCCNCC1CC(c2ccccc2)c2ccccc2C1=O 10.1021/jm011066n
10787790 106046 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 9 1 6 2.8 CCOc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL313157 106046 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 9 1 6 2.8 CCOc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10744240 107090 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 508 9 2 7 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C(N)=O)cccc23)CC1 10.1021/jm970166j
CHEMBL315496 107090 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 508 9 2 7 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C(N)=O)cccc23)CC1 10.1021/jm970166j
10763212 168299 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 394 9 1 6 3.3 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C2CC2)CC1 10.1021/jm970166j
CHEMBL433348 168299 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 394 9 1 6 3.3 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)C2CC2)CC1 10.1021/jm970166j
9893282 208927 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 533 9 1 8 3.5 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
CHEMBL88160 208927 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 533 9 1 8 3.5 Cc1nn(C)c2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
44323795 209066 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2cc(C)ccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL89030 209066 None 0 Rabbit Functional pKd = 9.3 9.3 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 410 8 1 5 3.3 COc1ccccc1N1CCN(CCCNc2cc(C)ccc2C(=O)N(C)C)CC1 10.1021/jm970166j
499 4077 None 13 Rat Functional pKd = 9.3 9.3 - 1
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
5685 4077 None 13 Rat Functional pKd = 9.3 9.3 - 1
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.3 9.3 - 1
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm011066n
9824384 118851 None 0 Rat Functional pKd = 9.2 9.2 - 0
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
CHEMBL342062 118851 None 0 Rat Functional pKd = 9.2 9.2 - 0
Antagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochlorideAntagonist activity at alpha1A adrenergic receptor in Wistar rat prostatic rat vas deferens assessed as inhibition of noradrenaline-induced contraction preincubated for 30 mins followed by noradrenaline addition measured after 45 mins in presence of cocaine hydrochloride
ChEMBL 437 4 1 8 3.1 COc1cc2nc(N3CCN(C(=O)c4ccco4)[C@@H]4CCCC[C@@H]43)nc(N)c2cc1OC 10.1016/j.bmc.2018.05.023
10478121 170905 None 0 Human Functional pKd = 9.2 9.2 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL445325 170905 None 0 Human Functional pKd = 9.2 9.2 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
10743446 107127 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2nc(C)n3C)CC1 10.1021/jm970166j
CHEMBL315785 107127 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2nc(C)n3C)CC1 10.1021/jm970166j
10549680 112447 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 1 6 3.1 CSc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL329601 112447 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 1 6 3.1 CSc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10647512 209483 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 456 8 2 6 1.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3ccn[n+]2-3)CC1 10.1021/jm970166j
CHEMBL91547 209483 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 456 8 2 6 1.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3ccn[n+]2-3)CC1 10.1021/jm970166j
10621397 209550 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 407 8 1 5 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm970166j
CHEMBL91951 209550 None 0 Rabbit Functional pKd = 9.2 9.2 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 407 8 1 5 3.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C2CC2)CC1 10.1021/jm970166j
499 4077 None 13 Rat Functional pKd = 9.2 9.2 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
5685 4077 None 13 Rat Functional pKd = 9.2 9.2 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
CHEMBL25554 4077 None 13 Rat Functional pKd = 9.2 9.2 - 1
Activity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostateActivity at adrenergic alpha 1A receptor assessed as antagonsim of noradrenaline-induced contraction of Sprague-Dawley rat prostate
ChEMBL 345 8 1 6 2.5 COc1cccc(c1OCCNCC1COc2c(O1)cccc2)OC 10.1021/jm060358r
10574245 111585 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 422 8 1 7 2.3 COc1ccccc1N1CCN(CCCNc2ncc(C#N)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL327872 111585 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 422 8 1 7 2.3 COc1ccccc1N1CCN(CCCNc2ncc(C#N)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
10577066 112475 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 2 6 2.3 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3c(Cl)cn[n+]2-3)CC1 10.1021/jm970166j
CHEMBL329773 112475 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 2 6 2.3 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)c[nH]c3c(Cl)cn[n+]2-3)CC1 10.1021/jm970166j
10530686 209361 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 549 9 1 6 5.2 CN(C)C(=O)c1cnc2c(Cl)cccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL90878 209361 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 549 9 1 6 5.2 CN(C)C(=O)c1cnc2c(Cl)cccc2c1NCCCN1CCN(c2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
11795906 209524 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 8 1 6 2.7 COc1cc(C)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL91785 209524 None 0 Rabbit Functional pKd = 9.1 9.1 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 411 8 1 6 2.7 COc1cc(C)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
14423371 97507 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL27013 97507 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1021/jm9810654
71462043 84602 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153555 84602 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220895 84602 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 379 8 1 6 3.2 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(Cl)c2O1 10.1016/j.ejmech.2012.09.049
14423371 97507 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
CHEMBL27013 97507 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from ratAntagonistic affinity against Alpha-1A adrenergic receptor was determined in isolated prostatic vas deferens tissue from rat
ChEMBL 441 11 1 8 3.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccco3)nc(N)c2cc1OC 10.1016/s0960-894x(98)00217-0
10456471 100587 None 0 Human Functional pKd = 9.0 9.0 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL291303 100587 None 0 Human Functional pKd = 9.0 9.0 - 0
In vitro antagonistic activity against alpha-1A receptor in dog prostate.In vitro antagonistic activity against alpha-1A receptor in dog prostate.
ChEMBL 451 6 1 7 2.4 COc1cc2[nH]c(=O)n(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
10572854 112629 None 0 Rabbit Functional pKd = 9 9.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL330060 112629 None 0 Rabbit Functional pKd = 9 9.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 396 8 1 5 3.0 COc1ccccc1N1CCN(CCCNc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10786203 209727 None 0 Rabbit Functional pKd = 9 9.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 8 2 6 2.1 CNC(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC)CC1 10.1021/jm970166j
CHEMBL93054 209727 None 0 Rabbit Functional pKd = 9 9.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 383 8 2 6 2.1 CNC(=O)c1cccnc1NCCCN1CCN(c2ccccc2OC)CC1 10.1021/jm970166j
11430491 63021 None 0 Rat Functional pKd = 9 9.0 - 0
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
CHEMBL178673 63021 None 0 Rat Functional pKd = 9 9.0 - 0
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 435 5 1 9 2.4 COc1cc2nc(N3CCN(C(=O)CC4CCSS4)CC3)nc(N)c2cc1OC 10.1021/jm049153d
10527469 156356 None 2 Human Functional pKd = 9 9.0 - 0
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 156356 None 2 Human Functional pKd = 9 9.0 - 0
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostateIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in dog prostate
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
4209 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
4893 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
4893.0 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
503 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
5385 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
CHEMBL2 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
DB00457 3163 None 48 Rat Functional pKd = 9.0 9.0 -1 17
Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)Blocking activity was assessed by antagonism of (-)-noradrenaline induced contraction of rat prostatic vas deferens (alpha1A adrenoceptor)
ChEMBL 383 4 1 8 1.8 COc1cc2nc(nc(c2cc1OC)N)N1CCN(CC1)C(=O)c1ccco1 10.1021/jm049153d
10478121 170905 None 0 Rat Functional pKd = 9.0 9.0 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
CHEMBL445325 170905 None 0 Rat Functional pKd = 9.0 9.0 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 435 6 0 7 3.1 COc1cc2ncn(CCN3C[C@@H]4CCc5c(OC)cccc5[C@@H]4C3)c(=O)c2cc1OC 10.1021/jm000541z
16121006 11845 None 0 Rat Functional pKd = 9.0 9.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL1182182 11845 None 0 Rat Functional pKd = 9.0 9.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
CHEMBL217469 11845 None 0 Rat Functional pKd = 9.0 9.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 365 7 1 5 3.7 COc1ccc2ccccc2c1OCCNC[C@H]1COc2ccccc2O1 10.1021/jm060358r
11742834 165865 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
CHEMBL42472 165865 None 0 Rat Functional pKd = 9.0 9.0 - 0
Antagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostate Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
10527469 156356 None 2 Rat Functional pKd = 8.9 8.9 - 0
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
CHEMBL40650 156356 None 2 Rat Functional pKd = 8.9 8.9 - 0
In vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferensIn vitro antagonism against Alpha-1A adrenergic receptor using phenylephrine (PE) challenge in rat vas deferens
ChEMBL 448 4 1 7 3.0 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(sc5cccnc54)c3=O)C[C@@H]21 10.1021/jm970364a
10834793 84613 None 0 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153557 84613 None 0 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2220925 84613 None 0 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostate assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 363 8 1 6 2.7 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(F)c2O1 10.1016/j.ejmech.2012.09.049
132266 1278 None 10 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
486 1278 None 10 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
CHEMBL423294 1278 None 10 Rat Functional pKd = 8.9 8.9 - 0
Antagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deferenceAntagonist activity at rat alpha1A adrenoceptor assessed as inhibition if norepinephrine-induced contraction of vas deference
ChEMBL 437 4 1 8 3.1 COc1cc2nc(nc(c2cc1OC)N)N1CCN([C@@H]2[C@H]1CCCC2)C(=O)c1ccco1 10.1021/jm8016046
10505222 209123 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 1 7 3.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C#N)cccc23)CC1 10.1021/jm970166j
CHEMBL89397 209123 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 490 8 1 7 3.6 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c(C#N)cccc23)CC1 10.1021/jm970166j
10575254 209341 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 443 8 1 5 4.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1021/jm970166j
CHEMBL90746 209341 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 443 8 1 5 4.1 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2-c2ccccc2)CC1 10.1021/jm970166j
10814587 209350 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 480 8 1 7 3.4 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3nc(C)ccc23)CC1 10.1021/jm970166j
CHEMBL90810 209350 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 480 8 1 7 3.4 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3nc(C)ccc23)CC1 10.1021/jm970166j
10646065 209360 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
CHEMBL90874 209360 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 425 8 2 6 3.2 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)NC(C)(C)C)CC1 10.1021/jm970166j
10624682 209496 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2c(C)nn3C)CC1 10.1021/jm970166j
CHEMBL91605 209496 None 0 Rabbit Functional pKd = 8.9 8.9 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 483 8 1 8 2.8 COc1cc(F)ccc1N1CCN(CCCNc2c(C(=O)N(C)C)cnc3c2c(C)nn3C)CC1 10.1021/jm970166j
10789770 100939 None 0 Rat Functional pKd = 8.9 8.9 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL293695 100939 None 0 Rat Functional pKd = 8.9 8.9 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 451 6 1 7 2.4 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4c(OC)c(OC)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
11742834 165865 None 0 Rat Functional pKd = 8.9 8.9 - 0
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
CHEMBL42472 165865 None 0 Rat Functional pKd = 8.9 8.9 - 0
Antagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptorAntagonistic affinity tested against isolated Rat Prostatic Vas Deferens Alpha-1A adrenergic receptor
ChEMBL 419 9 1 5 4.7 COc1cccc(OC)c1OCCNC[C@@H]1C[C@H](c2ccccc2)c2ccccc2O1 10.1021/jm011066n
10693231 205219 None 0 Rat Functional pKd = 8.8 8.8 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
CHEMBL62033 205219 None 0 Rat Functional pKd = 8.8 8.8 - 0
In vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferensIn vitro antagonistic activity towards alpha-1A adrenergic receptor in rat vas deferens
ChEMBL 416 4 1 6 2.2 COc1cccc2c1CC[C@H]1CN(CCn3c(=O)[nH]c4cc(C#N)ccc4c3=O)C[C@@H]21 10.1021/jm000541z
9865577 112372 None 2 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL329160 112372 None 2 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 1 6 2.4 COc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10621790 163911 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 415 8 1 6 2.6 COc1cc(F)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL420620 163911 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 415 8 1 6 2.6 COc1cc(F)ccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10839699 209209 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 9 1 8 3.8 Cc1noc2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
CHEMBL90022 209209 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 520 9 1 8 3.8 Cc1noc2ncc(C(=O)N(C)C)c(NCCCN3CCN(c4ccccc4OCC(F)(F)F)CC3)c12 10.1021/jm970166j
10552164 209358 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
CHEMBL90869 209358 None 0 Rabbit Functional pKd = 8.8 8.8 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 466 9 1 6 3.4 CN(C)C(=O)c1cccnc1N1CCC(NCCOc2ccccc2OCC(F)(F)F)CC1 10.1021/jm970166j
10549596 84639 None 1 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2153553 84639 None 1 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
CHEMBL2221147 84639 None 1 Rat Functional pKd = 8.8 8.8 - 0
Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 minsAntagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat prostatic vas deferens assessed as inhibition of noradrenaline-induced contractions after 30 mins
ChEMBL 375 9 1 7 2.5 COc1cccc(OC)c1OCCNC[C@H]1COc2cccc(OC)c2O1 10.1016/j.ejmech.2012.09.049
10501886 111464 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1ccccc1N1CCN(CCCNc2ncc(O)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL327232 111464 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 2 7 2.1 COc1ccccc1N1CCN(CCCNc2ncc(O)cc2C(=O)N(C)C)CC1 10.1021/jm970166j
10693071 208932 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 0 5 3.7 COc1ccccc1N1CCN(CCCSc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88181 208932 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 413 8 0 5 3.7 COc1ccccc1N1CCN(CCCSc2ccccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10833725 208969 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
CHEMBL88435 208969 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 381 7 1 5 2.7 Cc1ccccc1N1CCN(CCCNc2ncccc2C(=O)N(C)C)CC1 10.1021/jm970166j
10500734 209037 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 392 7 1 6 2.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C#N)CC1 10.1021/jm970166j
CHEMBL88856 209037 None 0 Rabbit Functional pKd = 8.7 8.7 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 392 7 1 6 2.3 CN(C)C(=O)c1cccnc1NCCCN1CCN(c2ccccc2C#N)CC1 10.1021/jm970166j
44324012 209707 None 0 Rabbit Functional pKd = 8 8.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
CHEMBL92901 209707 None 0 Rabbit Functional pKd = 8 8.0 - 0
Antagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assayAntagonistic activity against alpha 1A/1L receptor was assessed in a rabbit bladder neck functional assay
ChEMBL 397 8 2 6 2.4 COc1ccccc1N1CCN(CCCNc2nc(C)cc(C)c2C(N)=O)CC1 10.1021/jm970166j
11994673 12320 None 0 Rat Functional pKd = 8.0 8.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL1185036 12320 None 0 Rat Functional pKd = 8.0 8.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
CHEMBL385371 12320 None 0 Rat Functional pKd = 8.0 8.0 - 0
Activity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferensActivity at adrenergic alpha 1A receptor assessed as antagonism of noradrenaline-induced contraction of Sprague-Dawley rat vas deferens
ChEMBL 419 7 1 5 4.5 COc1ccc2ccccc2c1OCCNC[C@H]1COc2cc3c(cc2O1)CCCC3 10.1021/jm060358r
10745791 36519 None 0 Rat Functional pKd = 8.0 8.0 - 0
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 579 19 3 9 4.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCN)nc(N)c2cc1OC 10.1021/jm9810654
CHEMBL144776 36519 None 0 Rat Functional pKd = 8.0 8.0 - 0
Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.Antagonism of the norepinephrine induced contraction of rat isolated prostatic vas deferens.
ChEMBL 579 19 3 9 4.6 COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccccc3CNCCCCCCN)nc(N)c2cc1OC 10.1021/jm9810654
10394346 16970 None 0 Rat Functional pKd = 8.0 8.0 - 0
Functional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferensFunctional Alpha-1A adrenergic receptor antagonistic activity of noradrenaline induced contractions in prostatic portion of rat vas deferens
ChEMBL 638 11 2 10 3.0 Cc1c(-c2ccccc2)oc2c(C(=O)NCCCN3CCN(c4ccccc4OCc4no[n+]([O-])c4C(N)=O)CC3)cccc2c1=O 10.1021/jm030825u
CHEMBL125365 16970 None 0 Rat