Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
9849126 12167 0 None 3 4 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL1185969 12167 0 None 3 4 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL443435 12167 0 None 3 4 Guinea pig 10.4 pEC50 = 10.4 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
1499 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
3779 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
536 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
CHEMBL434 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
DB01064 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm701324c
1499 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
3779 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
536 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
CHEMBL434 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
DB01064 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2008.08.009
1499 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
3779 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
536 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
CHEMBL434 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
DB01064 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm800222k
1499 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
3779 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
536 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
CHEMBL434 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
DB01064 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm8000345
1499 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
3779 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
536 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
CHEMBL434 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
DB01064 1970 36 None -74 36 Human 10.1 pEC50 = 10.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmcl.2004.11.001
11268355 95724 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL26183 95724 0 None 1 3 Human 9.9 pEC50 = 9.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
1239 1566 42 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3410 1566 42 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
3465 1566 42 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
CHEMBL1256786 1566 42 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
DB00983 1566 42 None 1 5 Guinea pig 9.5 pEC50 = 9.5 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1021/jm801016j
24936881 17165 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1257913 17165 0 None 1 3 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 476 8 3 8 4.1 Oc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
12065 600 13 None -6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
45483813 600 13 None -6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
CHEMBL579394 600 13 None -6 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 370 6 4 5 2.7 Cc1ccccc1CC(C)(C)NCC(c1c2c(c(cc1)O)NC(=O)CO2)O 10.1016/j.bmcl.2009.10.013
9891927 183333 4 None -5 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL446840 183333 4 None -5 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483200 183333 4 None -5 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483201 183333 4 None -5 4 Guinea pig 9.1 pEC50 = 9.1 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
45483810 190747 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL567863 190747 0 None -3 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 356 6 4 5 2.4 CC(C)(Cc1ccccc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
123686 9375 38 None 74 3 Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 N#Cc1ccccc1OCC(O)CNCCNC(=O)Nc1ccccc1 10.1021/jm400348g
CHEMBL11268 9375 38 None 74 3 Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 N#Cc1ccccc1OCC(O)CNCCNC(=O)Nc1ccccc1 10.1021/jm400348g
CHEMBL3392321 9375 38 None 74 3 Human 9.1 pEC50 = 9.1 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 354 9 4 5 1.7 N#Cc1ccccc1OCC(O)CNCCNC(=O)Nc1ccccc1 10.1021/jm400348g
1499 1970 36 None -74 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
3779 1970 36 None -74 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
536 1970 36 None -74 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
CHEMBL434 1970 36 None -74 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
DB01064 1970 36 None -74 36 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm9000709
13345218 190824 0 None -8 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL568272 190824 0 None -8 2 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 372 6 5 6 2.1 CC(C)(Cc1ccc(O)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
44392175 131024 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
CHEMBL369346 131024 0 None 1 2 Human 9.1 pEC50 = 9.1 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 480 12 5 7 3.2 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc([N+](=O)[O-])c1 10.1016/j.bmcl.2004.11.001
1499 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
3779 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
536 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
CHEMBL434 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
DB01064 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.Activity against human beta 1 adrenergic receptor (AR), expressed in CHO cells.
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0101500
1499 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
3779 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
536 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
CHEMBL434 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
DB01064 1970 36 None -74 36 Human 9.0 pEC50 = 9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1021/jm0509445
44392230 65056 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
CHEMBL183283 65056 0 None 1 2 Human 8.9 pEC50 = 8.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 479 12 6 6 3.0 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)Nc1cccc(C(=O)O)c1 10.1016/j.bmcl.2004.11.001
24822304 97190 0 None 6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL272234 97190 0 None 6 2 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 412 9 3 5 4.1 O=C(O)c1ccc(Oc2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
90645347 111797 0 None -7 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298987 111797 0 None -7 3 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 12 6 7 5.6 CC(C)(N)COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.095
45101519 192125 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL577917 192125 0 None -1 2 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
24936492 17197 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
CHEMBL1258026 17197 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 482 8 3 9 4.1 Oc1ccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5cccs5)c34)CC2)cc1 10.1016/j.bmcl.2010.08.039
9927453 96014 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL26393 96014 0 None -1 3 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
42625513 12286 0 None -3 4 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL1186722 12286 0 None -3 4 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
CHEMBL475389 12286 0 None -3 4 Guinea pig 8.7 pEC50 = 8.7 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm801016j
90645346 111779 0 None -2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298762 111779 0 None -2 3 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 578 13 6 7 4.7 O=C(NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1)c1ccccc1 10.1016/j.bmcl.2014.04.095
42625517 12446 0 None -19 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187654 12446 0 None -19 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL514032 12446 0 None -19 4 Guinea pig 8.0 pEC50 = 8 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
11180293 111792 0 None -22 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298897 111792 0 None -22 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 543 12 6 8 3.1 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCNCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
56668796 66056 0 None -31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1835860 66056 0 None -31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
CHEMBL1852632 66056 0 None -31 3 Human 8.0 pEC50 = 8 Functional
Agonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 598 20 7 7 4.3 O=C(CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)NC1CCCC1 10.1016/j.bmc.2011.08.043
45273268 189236 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1204004 189236 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL556274 189236 0 None 194 2 Human 8.0 pEC50 = 8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 362 10 3 4 4.0 O[C@@H](CNCCc1ccc(Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
10217757 111554 0 None -31 4 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
CHEMBL3290998 111554 0 None -31 4 Human 8.0 pEC50 = 8 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 497 12 5 6 5.2 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c(NC=O)c3)cc2)cc1-c1ccccc1 10.1016/j.bmcl.2014.04.069
155774 3863 25 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
2848 3863 25 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
538 3863 25 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
CHEMBL75753 3863 25 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
DB13781 3863 25 None 64 3 Human 8.0 pEC50 = 8.0 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 339 8 4 6 -0.2 OC(COc1ccc(cc1)O)CNCCNC(=O)N1CCOCC1 10.1021/jm400348g
10863093 49865 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL157210 49865 0 None -19 3 Human 7.0 pEC50 = 7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 439 10 4 6 2.1 C[C@H](CNc1ccc(CC(=O)NS(C)(=O)=O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
16049450 63552 0 None -125 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807827 63552 0 None -125 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
16049234 63553 0 None -177 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807828 63553 0 None -177 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3ccccc3Cl)c2s1 10.1016/j.bmcl.2011.05.097
16049448 63554 0 None -56 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807829 63554 0 None -56 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 515 13 5 7 4.2 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCSCCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
16049374 63558 0 None -89 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807869 63558 0 None -89 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 481 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCSCCNCCc3cccc(Cl)c3)c2s1 10.1016/j.bmcl.2011.05.097
1499 1970 36 None -74 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
3779 1970 36 None -74 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
536 1970 36 None -74 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
CHEMBL434 1970 36 None -74 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
DB01064 1970 36 None -74 36 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.03.044
9888047 92725 0 None -398 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245673 92725 0 None -398 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1cccc(-c2occc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441231 147267 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393470 147267 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1cccc(-c2csc(C(=O)O)n2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441235 150204 0 None -251 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL395834 150204 0 None -251 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1ccc(-c2sccc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
45271523 188738 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204000 188738 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550096 188738 0 None -10 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 435 10 4 4 4.4 Cc1ccc(NC(=S)Nc2ccc(CCNC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmc.2009.06.031
45272417 189050 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL2448074 189050 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL552368 189050 0 None -1 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 455 10 4 4 4.7 O[C@@H](CNCCc1ccc(NC(=S)Nc2cccc(Cl)c2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
42625823 12404 0 None -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187371 12404 0 None -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL500782 12404 0 None -501 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 576 19 5 7 4.7 O=S(=O)(NC1CCCCC1)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
46832804 6743 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
CHEMBL1084655 6743 0 None -50 3 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 496 17 5 8 1.9 NS(=O)(=O)c1ccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1 10.1021/jm100326d
10553603 99009 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL284612 99009 0 None 1 3 Human 7.0 pEC50 = 7 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 506 10 6 8 1.5 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(NC(=O)CC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
1499 1970 36 None -74 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 1970 36 None -74 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 1970 36 None -74 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 1970 36 None -74 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 1970 36 None -74 36 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
42625517 12446 0 None -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1187654 12446 0 None -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL514032 12446 0 None -1995 4 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 536 19 5 7 3.8 CC(C)NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625588 179570 0 None -630 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL475237 179570 0 None -630 3 Human 6.0 pEC50 = 6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 508 18 5 7 2.9 NS(=O)(=O)Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
10121328 4206 0 None -100 3 Human 6.0 pEC50 = 6 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
CHEMBL101606 4206 0 None -100 3 Human 6.0 pEC50 = 6 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
ChEMBL 593 11 5 10 1.4 CS(=O)(=O)Nc1cc([C@@H](O)CNCC2CCN(S(=O)(=O)c3ccc(-n4cc(C(=O)O)cn4)cc3)CC2)ccc1O 10.1016/s0960-894x(02)00608-x
11575154 76639 0 None -100000 2 Human 5.0 pEC50 = 5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
CHEMBL207943 76639 0 None -100000 2 Human 5.0 pEC50 = 5 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 411 9 4 5 3.8 O=C(O)c1ccncc1-c1cccc(NCCNC[C@H](O)c2cccc(Cl)c2)c1 10.1021/jm0509445
44237766 57727 0 None -10000 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682221 57727 0 None -10000 2 Rat 5.0 pEC50 = 5 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 550 10 6 6 5.5 O=C(Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)Nc1cccc(Oc2ccccc2)c1 10.1016/j.bmcl.2010.12.096
155517986 169382 0 None -478630 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4445289 169382 0 None -478630 2 Human 5.0 pEC50 = 5 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 366 7 4 4 3.3 CC(C)(CCc1ccccc1)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
44313150 103078 0 None -6 3 Human 5.0 pEC50 = 5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL308868 103078 0 None -6 3 Human 5.0 pEC50 = 5 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2cccc(-c3cccc(CC4NCCc5cc(O)c(O)cc54)c3)c2)cc1 10.1016/s0960-894x(00)00459-5
1960 2699 57 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
439260 2699 57 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
505 2699 57 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL1437 2699 57 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00368 2699 57 None -79 13 Guinea pig 5.0 pEC50 = 5 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 169 2 4 4 0.1 NC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
10301101 102263 0 None -1659 2 Human 4.0 pEC50 = 4 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL306423 102263 0 None -1659 2 Human 4.0 pEC50 = 4 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 509 9 3 6 3.5 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3cccc4[nH]c5ccccc5c34)CC2)cc1 10.1016/s0960-894x(03)00387-1
145984792 164917 0 None -12882 3 Human 4.0 pEC50 = 4 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4246134 164917 0 None -12882 3 Human 4.0 pEC50 = 4 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 461 12 4 5 3.1 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)c3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
45483848 190743 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 394 7 3 3 5.3 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
CHEMBL567843 190743 0 None - 1 Human 6.0 pEC50 = 6 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 394 7 3 3 5.3 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(Cl)c(N)c(Cl)c2)cc1 10.1016/j.bmcl.2009.10.013
11567751 194355 0 None -29 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 374 6 4 5 2.5 CC(C)(Cc1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600401 194355 0 None -29 2 Human 7.0 pEC50 = 7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 374 6 4 5 2.5 CC(C)(Cc1ccc(F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
10145482 3940 0 None -34 2 Human 6.0 pEC50 = 6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100057 3940 0 None -34 2 Human 6.0 pEC50 = 6 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 604 12 5 7 3.4 O=C(NCc1cc(F)ccc1F)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
10281165 4181 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
CHEMBL101485 4181 0 None -16 2 Human 6.0 pEC50 = 6.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 560 11 5 7 3.3 O=C(Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1)NC1CCCCC1 10.1016/s0960-894x(02)00607-8
11539348 194383 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600616 194383 0 None -9 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 434 6 4 5 3.1 CC(C)(Cc1ccc(Br)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
44309649 197870 0 None -186 2 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL71348 197870 0 None -186 2 Human 5.0 pEC50 = 5.0 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 436 9 3 7 1.6 COc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(03)00387-1
10280301 109025 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL322973 109025 0 None -2 2 Human 7.0 pEC50 = 7.0 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 536 12 5 6 3.9 O=C(NCc1ccc(F)cc1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
10231394 166994 0 None -190 2 Human 5.0 pEC50 = 5.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL430662 166994 0 None -190 2 Human 5.0 pEC50 = 5.0 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 562 15 5 7 3.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
24823782 97370 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
CHEMBL273097 97370 0 None 3 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 396 8 3 4 4.0 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)nc1 10.1021/jm701324c
45484646 190897 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL568667 190897 0 None -1 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 456 10 6 7 2.0 CC(C)(Cc1ccc(NC(=O)CCCN)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
24894323 175619 0 None -52 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459645 175619 0 None -52 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 468 12 4 5 5.2 CCCOc1cc(-c2ccc(NCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
155536813 171379 0 None -263 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
CHEMBL4473790 171379 0 None -263 2 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 368 8 4 5 2.5 COc1ccccc1CCCNCC(O)c1ccc(O)c2[nH]c(=O)ccc12 10.1016/j.bmc.2018.10.043
45270680 188648 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203993 188648 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL549421 188648 0 None 5 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 421 10 4 4 4.1 O[C@@H](CNCCc1ccc(NC(=S)Nc2ccccc2)cc1)COc1ccccc1 10.1016/j.bmc.2009.06.031
45269853 190173 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL563872 190173 0 None -4 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
52943968 17442 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
CHEMBL1258824 17442 0 None 1 3 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cyclic AMP formation by HTRF assay
ChEMBL 518 9 4 8 3.8 NC(=O)Nc1cccc(OCC(O)CNC2CCN(c3ncnc4scc(-c5ccccc5)c34)CC2)c1 10.1016/j.bmcl.2010.08.039
16222840 189338 0 None -316 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
CHEMBL557253 189338 0 None -316 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 566 11 4 7 4.7 C[C@H](NCCc1ccc(-c2ccc(C(=O)NS(C)(=O)=O)c(OC3CCCCC3)c2)cc1)[C@H](O)c1ccc(O)cc1 10.1016/j.bmcl.2009.06.083
24895559 172269 0 None -338 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452034 172269 0 None -338 2 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 483 12 3 5 5.4 CC(C)COc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44377726 56320 0 None -389 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
CHEMBL164378 56320 0 None -389 2 Human 5.9 pEC50 = 5.9 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 550 10 5 10 1.6 CS(=O)(=O)Nc1cc(O[C@@H](O)CNC2CCN(c3ccc(CC4SC(=O)NC4=O)cc3)CC2)ccc1O 10.1016/s0960-894x(01)00063-4
1499 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
3779 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
536 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
CHEMBL434 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
DB01064 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2009.06.031
1499 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
3779 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
536 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
CHEMBL434 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
DB01064 1970 36 None -74 36 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.ejmech.2009.01.022
16223251 175620 0 None -204 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459646 175620 0 None -204 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 449 11 4 6 3.9 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895787 184029 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488431 184029 0 None -1 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
44309272 197462 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL68766 197462 0 None -2 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 611 14 6 8 2.9 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1 10.1016/s0960-894x(03)00387-1
44392181 65527 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183744 65527 0 None -10 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccccc1NC(=O)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44441230 93130 0 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247518 93130 0 None -7 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2csc(C(=O)O)n2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
2687 848 12 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
532 848 12 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
5387 848 12 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
CHEMBL420746 848 12 None 162 2 Human 7.9 pEC50 = 7.9 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 279 5 4 4 1.0 OC(COc1cccc2c1[nH]c(=O)[nH]2)CNC(C)(C)C 10.1021/jm400348g
44441226 93011 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL246908 93011 0 None 1 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2nc(C(=O)O)co2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
1239 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3410 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
3465 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
CHEMBL1256786 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
DB00983 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.095
90645345 111763 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298692 111763 0 None -11 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 574 12 6 8 4.7 CC(C)(C)OC(=O)NCCOc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1 10.1016/j.bmcl.2014.04.095
56943485 111787 0 None -12 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
CHEMBL3298831 111787 0 None -12 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 544 12 5 8 3.6 O=c1ccc2c([C@@H](O)CNCCc3ccc(Nc4ccc(OCCN5CCOCC5)cc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmcl.2014.04.095
46832798 13921 0 None -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1084648 13921 0 None -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
CHEMBL1198879 13921 0 None -31 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 485 16 4 6 4.6 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cc(Cl)ccc2Cl)ccc1O 10.1021/jm100326d
46832509 13930 0 None -50 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085399 13930 0 None -50 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198908 13930 0 None -50 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 510 18 5 8 2.7 CS(=O)(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
46832232 13933 0 None -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1085837 13933 0 None -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
CHEMBL1198923 13933 0 None -100 3 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 467 16 4 6 4.5 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc3ccccc23)ccc1O 10.1021/jm100326d
1239 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3410 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
3465 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
CHEMBL1256786 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
DB00983 1566 42 None -109 5 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assayAgonist activity at human recombinant beta1 receptor assessed as cAMP accumulation by radioimmunoassay and cell based assay
ChEMBL 344 9 4 5 2.2 O=CNc1cc(ccc1O)C(CNC(Cc1ccc(cc1)OC)C)O 10.1016/j.bmcl.2014.04.069
24895557 172268 0 None -575 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL452033 172268 0 None -575 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 469 12 3 5 5.2 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44392490 64702 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182708 64702 0 None -1 3 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 507 10 4 6 4.0 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
44268327 97621 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
CHEMBL274807 97621 0 None -1 3 Human 5.9 pEC50 = 5.9 Functional
Compound was tested for agonist activity against cloned human beta-1 adrenergic receptorCompound was tested for agonist activity against cloned human beta-1 adrenergic receptor
ChEMBL 448 11 4 6 3.0 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C1CCCCC1 10.1016/s0960-894x(98)00169-3
10575455 99290 0 None -60 3 Human 5.9 pEC50 = 5.9 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL286574 99290 0 None -60 3 Human 5.9 pEC50 = 5.9 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 448 8 5 7 1.2 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(C(N)=O)cc3)CC2)ccc1O 10.1021/jm000544b
145982668 165102 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4250215 165102 0 None -15 3 Human 6.9 pEC50 = 6.9 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 418 11 3 4 4.1 CCc1ccccc1OC[C@@H](O)CNCCc1ccc(NC(=O)c2ccccc2)cc1 10.1016/j.ejmech.2018.03.032
2419 3262 73 None -2238 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
5152 3262 73 None -2238 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
559 3262 73 None -2238 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
CHEMBL1263 3262 73 None -2238 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
DB00938 3262 73 None -2238 6 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1016/j.bmc.2018.10.043
53357711 63957 0 None -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814279 63957 0 None -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814280 63957 0 None -125 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 531 19 7 7 3.3 O=C(O)CNC(=O)Nc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
56675511 65863 0 None -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814273 65863 0 None -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
CHEMBL1851850 65863 0 None -100 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 527 18 5 7 3.2 O=C1CNC(=O)N1Cc1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1016/j.bmc.2011.05.064
42625587 12425 0 None -125 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL1187520 12425 0 None -125 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
CHEMBL506518 12425 0 None -125 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 562 18 4 7 4.3 O=S(=O)(c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1)N1CCCCC1 10.1021/jm801016j
9845280 76751 0 None -7 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
CHEMBL208352 76751 0 None -7 3 Human 5.9 pEC50 = 5.9 Functional
Activity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP productionActivity at human beta-1 adrenergic receptor expressed in CHO cells by stimulation of cAMP production
ChEMBL 424 9 3 5 4.5 COC(=O)c1cccc(-c2cccc(NCCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1021/jm0509445
23661589 92764 0 None -19952 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL245873 92764 0 None -19952 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 430 9 4 5 4.9 C[C@H](CNc1cccc(-c2sccc2C(=O)O)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
42625741 12325 0 None -158 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186940 12325 0 None -158 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL483202 12325 0 None -158 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCCCOCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625898 183703 0 None -501 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL485847 183703 0 None -501 3 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 591 17 7 9 1.5 NS(=O)(=O)O.NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
145983711 164572 0 None -2691 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4237802 164572 0 None -2691 3 Human 4.9 pEC50 = 4.9 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 476 12 5 5 3.5 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NC(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
24895265 184028 0 None -70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
CHEMBL488430 184028 0 None -70 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 409 8 3 3 5.0 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm8000345
44392552 63985 0 None -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
CHEMBL181440 63985 0 None -23 3 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2ccccc2)c1 10.1016/j.bmcl.2004.12.033
155564340 174589 0 None -263 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
CHEMBL4576089 174589 0 None -263 2 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 493 11 5 5 4.9 CC(CC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)CC(C)(C)C 10.1016/j.bmc.2018.10.043
44574826 177756 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467301 177756 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1cn(Cc2ccccc2)cn1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45270697 188780 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1203995 188780 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL550444 188780 0 None -20 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 451 11 4 5 4.1 COc1ccccc1NC(=S)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44580039 184284 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
CHEMBL490222 184284 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc1C(=O)O)c1ccccc1 10.1016/j.bmcl.2008.08.009
45271036 188838 0 None -2951 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL550871 188838 0 None -2951 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 526 11 4 7 3.8 CC(C)Oc1cc(-c2ccc(CCN[C@@H](C)[C@H](O)c3cccc(O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
24895363 172758 0 None -3162 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453322 172758 0 None -3162 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 447 11 3 4 5.3 CC(C)COc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895261 183999 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL488223 183999 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
42639967 12240 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186557 12240 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL469610 12240 0 None -128 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 497 11 3 7 3.1 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44591506 178478 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473495 178478 0 None -676 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 435 10 4 6 3.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
11152564 99327 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
CHEMBL286818 99327 0 None -4 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 358 7 3 3 4.1 COc1cccc2c(C[C@H](C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1016/s0960-894x(03)00073-8
44574651 177675 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 11 4 5 3.3 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466704 177675 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 444 11 4 5 3.3 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.bmc.2009.03.044
213051 91922 2 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL24350 91922 2 None -4 2 Human 7.9 pEC50 = 7.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 402 9 4 4 3.5 C[C@@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
5581 100964 8 None -5 6 Human 7.9 pEC50 = 7.9 Functional
Compound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptorCompound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptor
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
CHEMBL299175 100964 8 None -5 6 Human 7.9 pEC50 = 7.9 Functional
Compound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptorCompound was evaluated for its inhibitory activity against human Beta-1 adrenergic receptor
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1016/s0960-894x(00)00459-5
9804536 164885 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
CHEMBL4245391 164885 0 None -7 3 Human 7.8 pEC50 = 7.8 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 465 11 4 5 3.5 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1)c1ccccc1 10.1016/j.ejmech.2018.03.032
44574825 177754 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nc2ccccc2n1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467298 177754 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 534 13 3 6 4.8 O=C(Cc1nc2ccccc2n1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
45273276 189291 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204005 189291 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL556689 189291 0 None -2 3 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 429 10 4 5 3.6 N#C/N=C(\Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
44579966 187623 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
CHEMBL521611 187623 0 None -15 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 429 9 3 4 4.8 O=C(O)c1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)ccc1F 10.1016/j.bmcl.2008.08.009
24949572 176187 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
CHEMBL463182 176187 0 None -34 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 438 7 3 5 4.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)c1 10.1021/jm800222k
44565931 12173 0 None -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL1186040 12173 0 None -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
CHEMBL446806 12173 0 None -4677 4 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 552 11 4 8 3.6 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)cc1OC1CCCCC1 10.1021/jm9000709
11381882 98617 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
CHEMBL282039 98617 0 None 2 2 Human 6.9 pEC50 = 6.9 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 328 6 3 2 4.1 C[C@@H](Cc1c[nH]c2ccccc12)NC[C@@H](O)c1cccc(Cl)c1 10.1016/s0960-894x(03)00073-8
155515718 169136 0 None -2884 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
CHEMBL4441752 169136 0 None -2884 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1ccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)cc1 10.1016/j.bmc.2018.10.043
24894317 172867 0 None -22 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL453575 172867 0 None -22 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 11 3 4 5.6 CC(C)Cc1cc(-c2ccc(OCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44392228 64321 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
CHEMBL182127 64321 0 None -7 2 Human 7.8 pEC50 = 7.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 441 11 5 5 3.1 O=C(Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1)NC1CCCCC1 10.1016/j.bmcl.2004.11.001
1028 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
139148732 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
479 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
5816 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
CHEMBL679 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
DB00668 278 64 None -3 16 Guinea pig 7.8 pEC50 = 7.8 Functional
Effective dose required to stimulate contractions in isolated guinea pig atrium.Effective dose required to stimulate contractions in isolated guinea pig atrium.
ChEMBL 183 3 4 4 0.4 CNC[C@@H](c1ccc(c(c1)O)O)O 10.1021/jm00019a001
155524038 170065 0 None -120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4454489 170065 0 None -120 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 414 8 4 4 4.2 O=c1ccc2c(C(O)CNCCCc3ccc(-c4ccccc4)cc3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
155550544 173476 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 388 7 4 4 3.6 O=c1ccc2c(C(O)CNCCCc3ccc4ccccc4c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4550290 173476 0 None -1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 388 7 4 4 3.6 O=c1ccc2c(C(O)CNCCCc3ccc4ccccc4c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
44126933 189771 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL561291 189771 0 None 1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 470 11 4 5 4.3 O=C(Cc1ccc2ccccc2c1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
45268516 189849 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
CHEMBL561743 189849 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassayAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as stimulation of cAMP level after 1 hr by enzyme immunoassay
ChEMBL 605 13 5 9 2.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1016/j.bmcl.2009.06.083
16222940 183927 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL487682 183927 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3ccc(N)nc3)cc2)ccc1C(=O)O 10.1021/jm8000345
24895259 186465 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL512147 186465 0 None -588 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 528 12 5 7 3.8 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44591507 178505 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL473702 178505 0 None -2290 4 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 433 10 4 5 4.1 CC(C)Cc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)O 10.1021/jm9000709
9842600 185450 0 None -38 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
CHEMBL498305 185450 0 None -38 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 375 7 3 4 3.0 O=C(O)COc1ccc2c(c1)C[C@@H](NC[C@H](O)c1cccc(Cl)c1)CC2 10.1021/jm800222k
44377535 54927 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL161949 54927 0 None -117 2 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 508 8 4 9 2.8 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)Oc4cccc5nc(O)ccc45)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
56673609 63562 0 None -112 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
CHEMBL1807873 63562 0 None -112 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 499 13 5 7 3.5 O=c1[nH]c2c(O)ccc([C@@H](O)CNCCCOCCNCCc3cccc(Cl)c3Cl)c2s1 10.1016/j.bmcl.2011.05.097
56672116 65820 0 None -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814276 65820 0 None -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851624 65820 0 None -630 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 570 19 5 8 2.4 NC(=O)CN1C(=O)CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
44441227 147262 0 None -10 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL393469 147262 0 None -10 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1cccc(-c2nc(C(=O)O)co2)c1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
145981079 165870 0 None -39 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccc(Cl)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
CHEMBL4282047 165870 0 None -39 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 358 6 4 4 2.8 O=c1ccc2c(C(CO)NCCc3ccc(Cl)cc3)ccc(O)c2[nH]1 10.1016/j.ejmech.2018.04.041
24949889 185489 0 None -35 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
CHEMBL498531 185489 0 None -35 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 451 7 3 4 5.4 O=C(O)c1cccc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CCC3)c1 10.1021/jm800222k
42639311 12252 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1186600 12252 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL472089 12252 0 None -56 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 524 14 3 6 4.5 CCCCCOc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
44392558 64714 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL182770 64714 0 None -2 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 471 11 4 6 4.1 CC(C)=CCNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44237669 57723 0 None -7943 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
CHEMBL1682217 57723 0 None -7943 2 Rat 5.8 pEC50 = 5.8 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 540 9 6 5 4.7 O=C(NCc1c(Cl)cccc1Cl)Nc1cccc(CCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmcl.2010.12.096
9933039 162234 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 162234 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
9933039 162234 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL417613 162234 0 None -6 3 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
44309523 101495 0 None -52 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
CHEMBL302803 101495 0 None -52 3 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cellsAgonistic activity against cloned human beta1-AR (beta-1-adrenergic receptor) in CHO cells
ChEMBL 420 10 3 6 2.3 CCCCOc1ccc(S(=O)(=O)N2CC(NC[C@H](O)c3ccc(O)cc3)C2)cc1 10.1016/s0960-894x(03)00387-1
10601234 111291 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
CHEMBL32888 111291 0 None -23 3 Human 5.8 pEC50 = 5.8 Functional
Increased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptorIncreased cAMP levels of Chinese hamster ovary (CHO) cells expressing human beta 1 Adrenergic receptor
ChEMBL 493 11 5 8 1.7 CS(=O)(=O)Nc1cc([C@@H](O)CNC2CCN(c3ccc(COCC(=O)O)cc3)CC2)ccc1O 10.1021/jm000544b
10140889 5824 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL108061 5824 0 None -4 2 Human 6.8 pEC50 = 6.8 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 484 12 4 6 3.3 CCN(CC)C(=O)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44574978 186459 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
CHEMBL512099 186459 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 524 12 2 6 4.0 O=C(Cc1nccn1Cc1ccccc1)N1CCCc2cc(CCNC[C@H](O)COc3ccccc3)ccc21 10.1016/j.bmc.2009.03.044
24823464 96944 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL270964 96944 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm701324c
24823464 96944 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL270964 96944 0 None -588 3 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 418 10 4 4 4.7 CC(C)Nc1cc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm9000709
44392457 165145 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
CHEMBL425161 165145 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cells expressing human beta-1 adrenergic receptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1016/j.bmcl.2004.12.033
44127677 189014 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL552089 189014 0 None -2 2 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 471 11 4 6 3.7 O=C(Cc1ccc2ccccc2n1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
567 691 6 None -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
9841972 691 6 None -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
CHEMBL284782 691 6 None -676 7 Human 5.8 pEC50 = 5.8 Functional
Agonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-ARAgonistic activity against human Beta-1 adrenergic receptor by measuring cAMP accumulation in CHO cells expressing beta3-AR
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1016/s0960-894x(03)00073-8
11703823 194750 0 None -131 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL603274 194750 0 None -131 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 390 6 4 5 3.0 CC(C)(Cc1ccc(Cl)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
24950234 175162 0 None -223 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
CHEMBL458923 175162 0 None -223 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 10 4 5 5.8 CCCNc1cc(Oc2ccc3c(c2)C[C@@H](NC[C@H](O)c2cccc(Cl)c2)CC3)cc(C(=O)O)c1 10.1021/jm800222k
131487 4748 7 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
CHEMBL10494 4748 7 None - 1 Guinea pig 6.8 pEC50 = 6.8 Functional
Agonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atriaAgonistic activity (beta-1 adrenergic receptor) for the percent maximal increase in contraction rate of isolated guinea pig atria
ChEMBL 273 5 4 5 1.4 CC(C)(C)NCC(O)COc1cc(O)c(O)cc1F 10.1021/jm00107a027
24822648 96933 0 None -28 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
CHEMBL270889 96933 0 None -28 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(C(=O)O)ccc1-c1ccc(CCNC[C@H](O)c2cccc(Cl)c2)cc1 10.1021/jm701324c
45484558 190439 0 None -4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL565770 190439 0 None -4 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 498 11 8 7 1.6 CC(C)(Cc1ccc(NC(=O)CCCNC(=N)N)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
44574687 177679 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 406 11 3 6 2.2 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466713 177679 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 406 11 3 6 2.2 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccnc2)cc1 10.1016/j.bmc.2009.03.044
44219629 177726 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467083 177726 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 484 13 3 6 3.7 O=C(Cc1nccn1Cc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44126931 188964 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
CHEMBL551831 188964 0 None -1 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 496 12 4 5 4.7 O=C(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)C(c1ccccc1)c1ccccc1 10.1016/j.ejmech.2009.01.022
24895664 175857 0 None -251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL459863 175857 0 None -251 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 467 12 3 4 5.8 CCCOc1cc(-c2ccc(CCCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm8000345
44396568 66736 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL188196 66736 0 None -34 3 Human 6.8 pEC50 = 6.8 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
9853471 198427 0 None -389 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL75604 198427 0 None -389 3 Human 5.8 pEC50 = 5.8 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 628 12 6 6 6.7 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(CC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
44331425 4213 0 None -186 3 Human 5.7 pEC50 = 5.7 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
CHEMBL101630 4213 0 None -186 3 Human 5.7 pEC50 = 5.7 Functional
Beta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptorBeta-1 adrenergic receptor agonist activity as increased cAMP levels in CHO cells expressing human Beta-1-adrenoceptor
ChEMBL 576 13 6 8 2.5 CC(C)C[C@H](NC(=O)c1ccc(N2CCC(CNC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)C(=O)O 10.1016/s0960-894x(02)00608-x
45483838 190536 0 None -14 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
CHEMBL566352 190536 0 None -14 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulationAgonist activity at human adrenergic beta 1 expressed in CHO-K1 cells assessed as intracellular cAMP accumulation
ChEMBL 383 7 4 4 3.5 CC(C)(Cc1cccc(C(F)(F)F)c1)NCC(O)c1ccc(O)c(CO)c1 10.1016/j.bmcl.2009.10.013
10302342 109074 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
CHEMBL323258 109074 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
In vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptorIn vitro agonistic activity assessed by measurement of cAMP accumulation level in CHO cells expressing human beta1-AR receptor
ChEMBL 538 14 5 6 4.5 O=C(NCCCC1CCCC1)N1CCC(Nc2ccc(CCNC[C@H](O)COc3ccc(O)cc3)cc2)CC1 10.1016/s0960-894x(01)00645-x
44396488 66185 0 None -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL185703 66185 0 None -14 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 556 12 4 7 3.8 C[C@H](Cc1c[nH]c2c(OCC(=O)N(C)C)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
9831168 198277 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL74085 198277 0 None -2 3 Human 7.7 pEC50 = 7.7 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 552 11 6 6 5.0 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(CC3NCCc4cc(O)c(O)cc43)cc2)cc1 10.1016/s0960-894x(00)00459-5
11005613 119055 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL348269 119055 0 None -1 3 Human 7.7 pEC50 = 7.7 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 501 12 4 5 4.3 Cc1ccc(S(=O)(=O)NCCc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
44441234 93132 0 None -63 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247520 93132 0 None -63 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 414 9 4 5 4.4 C[C@H](CNc1ccc(-c2occc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
44441228 166949 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL430390 166949 0 None -3 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 431 9 4 6 4.3 C[C@H](CNc1ccc(-c2nc(C(=O)O)cs2)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
46832507 13932 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1085638 13932 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
CHEMBL1198915 13932 0 None -12 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 475 17 6 7 2.8 NC(=O)Nc1cccc(COCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm100326d
10203169 13957 0 None -25 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1086536 13957 0 None -25 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
CHEMBL1199300 13957 0 None -25 3 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 minsAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation after 30 to 45 mins
ChEMBL 433 16 5 7 3.0 OCc1cc([C@@H](O)CNCCCCCCOCCOCc2cccc(O)c2)ccc1O 10.1021/jm100326d
44574867 177730 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL467102 177730 0 None -2 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 562 13 3 6 4.4 O=C(Cc1nccn1Cc1ccc(Br)cc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
44579650 184490 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
CHEMBL492005 184490 0 None -15 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 435 10 4 6 3.4 CC(=O)Nc1ccc(Oc2cccc(CCNC[C@H](O)c3cccnc3)c2)cc1C(=O)O 10.1016/j.bmcl.2008.08.009
44580041 187985 0 None -9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
CHEMBL524145 187985 0 None -9 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 530 11 4 5 5.9 O=C(O)c1cc(NC(=O)c2ccccc2)cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)c1 10.1016/j.bmcl.2008.08.009
44127480 190162 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
CHEMBL563810 190162 0 None 6 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as increase in cAMP production after 2 days by radioimmunoassay
ChEMBL 454 11 4 5 3.8 O=C(Cc1ccc(Cl)cc1)Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1 10.1016/j.ejmech.2009.01.022
44560793 186072 0 None -2951 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL507506 186072 0 None -2951 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 434 11 3 5 4.5 CCCOc1cc(-c2ccc(C[C@@H](C)NC[C@H](O)c3cccnc3)cc2)ccc1C(=O)O 10.1021/jm8000345
9873257 84297 9 None -74 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
CHEMBL22375 84297 9 None -74 3 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclaseAgonistic activity against the cloned human Beta-1 adrenergic receptor was measured by its by its ability to stimulate adenylyl cyclase
ChEMBL 591 14 3 10 3.5 O=c1n(CCCC2CCCC2)nnn1-c1ccc(S(=O)(=O)Nc2ccc(CCNC[C@H](O)c3cccnc3)cc2)cc1 10.1016/s0960-894x(99)00182-1
155527926 170427 0 None -8709 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4460095 170427 0 None -8709 2 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 451 11 5 5 3.9 CC(C)CCC(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
56670092 63563 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
CHEMBL1807874 63563 0 None -112 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at adrenergic beta1 receptorAgonist activity at adrenergic beta1 receptor
ChEMBL 445 13 4 7 2.5 CN(CCOCCCNC[C@H](O)c1ccc(O)c2[nH]c(=O)sc12)CCc1ccccc1 10.1016/j.bmcl.2011.05.097
56675509 63955 0 None -79 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
CHEMBL1814270 63955 0 None -79 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CNC(=O)N1c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1016/j.bmc.2011.05.064
53357712 65861 0 None -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1814271 65861 0 None -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
CHEMBL1851848 65861 0 None -251 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 541 17 5 7 3.9 CC1(C)NC(=O)N(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C1=O 10.1016/j.bmc.2011.05.064
56658244 65862 0 None -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1814272 65862 0 None -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
CHEMBL1851849 65862 0 None -79 4 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human adrenergic beta1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 513 17 5 7 3.2 O=C1CN(c2cccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)c2)C(=O)N1 10.1016/j.bmc.2011.05.064
9958539 102407 0 None -5 3 Human 8.7 pEC50 = 8.7 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
CHEMBL307647 102407 0 None -5 3 Human 8.7 pEC50 = 8.7 Functional
Percent adenylyl cyclase activation at 10000 nM of compound concentrationPercent adenylyl cyclase activation at 10000 nM of compound concentration
ChEMBL 527 3 2 5 3.4 COc1c(I)cc(CC2NCCc3nc(N)sc32)cc1I 10.1016/s0960-894x(00)00459-5
443372 9974 16 None 1 8 Guinea pig 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1160723 9974 16 None 1 8 Guinea pig 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL2062275 9974 16 None 1 8 Guinea pig 8.7 pEC50 = 8.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
44392215 65061 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183307 65061 0 None 1 2 Human 8.7 pEC50 = 8.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 465 12 5 6 3.3 COc1ccc(NC(=O)Nc2ccc(C[C@@H](CO)NC[C@H](O)COc3ccccc3)cc2)cc1 10.1016/j.bmcl.2004.11.001
5311116 2207 4 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
544 2207 4 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
CHEMBL207802 2207 4 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 484 15 5 8 2.2 N#Cc1cc(OCCOCC2CC2)ccc1OCC(CNCCNC(=O)Nc1ccc(cc1)O)O 10.1021/jm400348g
56598832 87615 0 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
CHEMBL2348218 87615 0 None 4365 3 Human 8.6 pEC50 = 8.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 527 16 5 7 3.3 O=C(NCCNCC(O)COc1ccc(OCCOCCc2ccc(F)cc2)cc1)Nc1ccc(O)cc1 10.1021/jm400348g
10289065 12272 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL1186683 12272 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
CHEMBL474616 12272 0 None - 1 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1cccc(CCCOCCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)c1 10.1021/jm801016j
42625511 12462 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL1187778 12462 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
CHEMBL520313 12462 0 None -3 4 Guinea pig 8.6 pEC50 = 8.6 Functional
Agonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contractionAgonist activity at beta-1 adrenergic receptor in guinea pig trachea assessed as inhibition of electrical stimulation-induced muscle contraction
ChEMBL 494 17 5 7 2.8 NS(=O)(=O)c1ccccc1CCCCOCCCCCCNC[C@H](O)c1ccc(O)c(CO)c1 10.1021/jm801016j
90645344 111740 0 None -7 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
CHEMBL3298324 111740 0 None -7 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccccc1CN 10.1016/j.bmcl.2014.04.095
10239722 111742 0 None -11 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
CHEMBL3298326 111742 0 None -11 3 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 550 11 6 7 5.0 COc1ccc(Nc2ccc(CCNC[C@H](O)c3ccc(O)c4[nH]c(=O)ccc34)cc2)cc1-c1ccc(CN)cc1 10.1016/j.bmcl.2014.04.095
145984584 165075 0 None -5 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
CHEMBL4249564 165075 0 None -5 3 Human 8.5 pEC50 = 8.5 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 444 10 5 4 4.4 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]ccc23)cc1 10.1016/j.ejmech.2018.03.032
24822643 156851 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
CHEMBL408145 156851 0 None -4 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 413 8 3 3 4.7 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)c(F)c1 10.1021/jm701324c
44392212 167546 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204383 167546 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL434524 167546 0 None 12 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 405 10 4 4 3.9 O=C(Nc1ccccc1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
45271492 188844 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL1203997 188844 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL550906 188844 0 None 16 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 390 10 3 4 3.5 O=C(Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
10113837 65028 0 None -39 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
CHEMBL183129 65028 0 None -39 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptorAgonistic activity was assessed by measuring cAMP accumulation in CHO cell lines expressing cloned human Beta-1 adrenergic receptor
ChEMBL 435 11 5 5 3.3 O=C(Nc1ccccc1)Nc1ccc(C[C@@H](CO)NC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmcl.2004.11.001
44396531 66288 0 None -38 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
CHEMBL186135 66288 0 None -38 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 647 18 4 8 6.4 CCCCCCCCS(=O)(=O)Oc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)c[nH]c12 10.1016/j.bmcl.2004.10.035
24822469 97103 0 None -26 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
CHEMBL271765 97103 0 None -26 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 401 8 3 4 4.6 O=C(O)c1ccc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)s1 10.1021/jm701324c
24950568 186928 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
CHEMBL516002 186928 0 None -234 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 422 6 3 4 4.3 O=C(O)c1ccc(-c2ccc3c(c2)C[C@@H](NC[C@H](O)c2ccc(Cl)nc2)CC3)cc1 10.1021/jm800222k
11625493 194308 0 None -12 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL600007 194308 0 None -12 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 400 8 4 6 2.8 CCOc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
44565908 184459 0 None -1513 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491726 184459 0 None -1513 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 512 11 4 8 2.7 CC(C)Oc1cc(-c2ccc(CCNC[C@H](O)c3cnccc3N)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
10139127 56983 0 None -50 2 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
CHEMBL165893 56983 0 None -50 2 Human 5.7 pEC50 = 5.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 455 9 3 7 2.6 O=C1NC(=O)C(Cc2ccc(N3CCC(NC[C@H](O)COc4ccccc4)CC3)cc2)S1 10.1016/s0960-894x(01)00063-4
44589133 175009 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
CHEMBL458541 175009 0 None -2 3 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at adrenergic beta-1 receptorAgonist activity at adrenergic beta-1 receptor
ChEMBL 354 8 2 4 3.4 CC(C)NCC(O)COc1ccc2c(c1)CCCN2Cc1ccccc1 10.1016/j.bmc.2008.11.030
10145446 3953 0 None -102 2 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
CHEMBL100124 3953 0 None -102 2 Human 5.7 pEC50 = 5.7 Functional
In vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptorIn vitro agonist activity measured by increase in cAMP levels in chinese hamster ovary cells (CHO) cells expressing human Beta-1 adrenergic receptor
ChEMBL 602 14 5 8 3.6 O=C(NCCCc1cccs1)Nc1ccc(S(=O)(=O)N2CCC(CNC[C@H](O)COc3ccc(O)cc3)CC2)cc1 10.1016/s0960-894x(02)00607-8
46232816 194549 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL601858 194549 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 432 7 4 5 4.0 CC(C)(Cc1ccc(-c2ccccc2)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
11632691 195137 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL605372 195137 0 None -3 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 398 7 4 5 3.5 CC(C)c1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
44377523 55735 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
CHEMBL162711 55735 0 None 1 2 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptorAgonistic activity as cAMP accumulation in CHO cells expressing human beta-1-adrenergic receptor
ChEMBL 509 9 3 8 1.0 O=C1N=c2cccc(OC[C@@H](O)CNC3CCN(c4ccc(CC5SC(=O)NC5=O)cc4)CC3)c2=N1 10.1016/s0960-894x(01)00063-4
9933039 162234 0 None -6 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
CHEMBL417613 162234 0 None -6 3 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenolAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay relative to isoproterenol
ChEMBL 442 11 4 6 2.8 O=S(=O)(Nc1ccc(CCNC[C@H](O)COc2ccc(O)cc2)cc1)c1ccccc1 10.1016/j.bmc.2009.06.031
24895563 175899 0 None -173 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
CHEMBL460256 175899 0 None -173 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 435 12 3 5 4.5 CCCOc1cc(-c2ccc(OCCNC[C@H](O)c3ccccc3)cc2)ccc1C(=O)O 10.1021/jm8000345
11668125 194606 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
CHEMBL602258 194606 0 None -4 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 384 7 4 5 2.9 CCc1ccc(CC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)cc1 10.1016/j.bmcl.2009.12.087
155536314 171348 0 None -6025 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
CHEMBL4473515 171348 0 None -6025 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 354 7 5 5 2.2 O=c1ccc2c(C(O)CNCCCc3cccc(O)c3)ccc(O)c2[nH]1 10.1016/j.bmc.2018.10.043
24895789 186042 0 None -72 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
CHEMBL507003 186042 0 None -72 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 375 8 3 3 4.3 C[C@H](Cc1ccc(-c2ccc(C(=O)O)cc2)cc1)NC[C@H](O)c1ccccc1 10.1021/jm8000345
44396715 66898 0 None -20 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
CHEMBL189081 66898 0 None -20 3 Human 7.7 pEC50 = 7.7 Functional
Agonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptorAgonistic activity was determined by measuring cAMP accumulation in CHO cells expressing cloned human Beta-1 adrenergic receptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1016/j.bmcl.2004.10.035
155551006 173111 0 None -44 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
CHEMBL4541169 173111 0 None -44 2 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 423 9 5 5 3.1 CC(C)C(=O)Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1 10.1016/j.bmc.2018.10.043
56598833 87614 0 None 436 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
CHEMBL2348217 87614 0 None 436 3 Human 7.6 pEC50 = 7.6 Functional
Partial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrsPartial agonist activity at human beta1 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
ChEMBL 433 14 5 7 2.0 CCOCCOc1ccc(OCC(O)CNCCNC(=O)Nc2ccc(O)cc2)cc1 10.1021/jm400348g
42639314 12297 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL1186804 12297 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
CHEMBL479341 12297 0 None -575 2 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 550 11 3 6 5.0 CS(=O)(=O)NC(=O)c1ccc(-c2ccc(CCNC[C@H](O)c3ccccc3)cc2)cc1OC1CCCCCC1 10.1021/jm9000709
5808 175941 16 None -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL1257092 175941 16 None -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
CHEMBL460574 175941 16 None -5 5 Guinea pig 5.7 pEC50 = 5.7 Functional
Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.Activity for Beta-1 adrenergic receptor was assessed from ability to stimulate contractions in isolated guinea pig atrium.
ChEMBL 211 4 4 4 1.1 CC(C)NC[C@@H](O)c1ccc(O)c(O)c1 10.1021/jm00019a001
145983266 164717 0 None -66 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
CHEMBL4241176 164717 0 None -66 3 Human 6.7 pEC50 = 6.7 Functional
Antagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assayAntagonist activity at human beta1 adrenergic receptor expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of isoproterenol-induced intercellular calcium mobilization pre-incubated for 10 mins before isoproterenol addition by Fluo-4AM dye-based fluorescence assay
ChEMBL 512 14 5 6 2.7 CC(=O)NCc1cccc(OC[C@@H](O)CNCCc2ccc(NS(=O)(=O)Nc3ccccc3)cc2)c1 10.1016/j.ejmech.2018.03.032
319 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
321 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
444031 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
784 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
CHEMBL1346 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
DB00496 1246 33 None -2290 6 Rat 5.6 pEC50 = 5.6 Functional
Agonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effectAgonist activity at beta1 adrenoceptor in rat left atria assessed as induction of ionotropic effect
ChEMBL 426 7 1 3 4.0 NC(=O)C(c1ccccc1)(c1ccccc1)[C@@H]1CCN(C1)CCc1ccc2c(c1)CCO2 10.1016/j.bmcl.2010.12.096
155543518 174165 0 None -794 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
CHEMBL4566727 174165 0 None -794 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assayAgonist activity at human beta1 adrenergic receptor expressed in HEK293 cells assessed as increase in cAMP accumulation after 60 mins by HTRF assay
ChEMBL 457 9 5 5 3.7 O=C(Nc1cccc(CCCNCC(O)c2ccc(O)c3[nH]c(=O)ccc23)c1)c1ccccc1 10.1016/j.bmc.2018.10.043
45101521 190432 0 None -4 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 570 15 8 9 1.3 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C(N)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
CHEMBL565747 190432 0 None -4 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP levelAgonist activity at human beta-1 adrenoceptor expressed in CHOK1 cell assessed as increase of intracellular cAMP level
ChEMBL 570 15 8 9 1.3 CC(C)(Cc1ccc(NC(=O)CCCNC(=O)C(N)CCCN)cc1)NCC(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.06.104
44560794 172668 0 None -346 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
CHEMBL453056 172668 0 None -346 2 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immuno assay
ChEMBL 474 10 3 5 5.4 C[C@H](Cc1ccc(-c2ccc(C(=O)O)c(OC3CCCCC3)c2)cc1)NC[C@H](O)c1cccnc1 10.1021/jm8000345
44579940 187407 0 None -37 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
CHEMBL519985 187407 0 None -37 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 468 10 4 5 4.7 CC(=O)Nc1cc(Oc2cccc(CCNC[C@H](O)c3cccc(Cl)c3)c2)cc(C(=O)O)c1 10.1016/j.bmcl.2008.08.009
46232857 194354 0 None -19 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
CHEMBL600400 194354 0 None -19 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human recombinant adrenergic beta-1 receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 440 7 4 6 3.3 CC(C)(Cc1ccc(OC(F)(F)F)cc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmcl.2009.12.087
42639654 12365 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL1187156 12365 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
CHEMBL491891 12365 0 None -1258 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 513 11 3 7 3.8 CC(C)Sc1cc(-c2ccc(CCNC[C@H](O)c3cccnc3)cc2)ccc1C(=O)NS(C)(=O)=O 10.1021/jm9000709
9832011 104779 0 None -138 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
CHEMBL312074 104779 0 None -138 3 Human 5.6 pEC50 = 5.6 Functional
Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)Compound was evaluated for its inhibitory activity against human beta-1 adrenergic receptor (AR)
ChEMBL 644 13 6 7 6.5 CCCCCCNC(=O)Nc1ccc(S(=O)(=O)Nc2ccc(-c3ccc(OCC4NCCc5cc(O)c(O)cc54)cc3)cc2)cc1 10.1016/s0960-894x(00)00459-5
11091850 46782 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
CHEMBL154370 46782 0 None -25 3 Human 7.6 pEC50 = 7.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 465 11 4 4 4.6 Cc1ccc(CNC(=O)Cc2ccc(NC[C@@H](C)NC[C@H](O)c3cccc(Cl)c3)cc2)cc1 10.1021/jm0101500
44441232 93131 0 None -19 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
CHEMBL247519 93131 0 None -19 3 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 415 9 4 6 3.8 C[C@H](CNc1ccc(-c2ocnc2C(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1016/j.bmcl.2007.05.069
9892481 69671 6 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
CHEMBL1940832 69671 6 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assayAgonist activity at human beta1 adrenergic receptor expressed in cells by cAMP accumulation assay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2014.04.095
9849126 12167 0 None -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL1185969 12167 0 None -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
CHEMBL443435 12167 0 None -630 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assayAgonist activity at human cloned beta-1 adrenergic receptor expressed in CHO cells assessed as induction of intracellular cAMP accumulation by beta-galactosidase based whole cell assay
ChEMBL 507 18 5 7 2.8 NS(=O)(=O)c1cccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(NC=O)c2)c1 10.1021/jm801016j
9892481 69671 6 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
CHEMBL1940832 69671 6 None -501 4 Human 7.6 pEC50 = 7.6 Functional
Agonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassayAgonist activity at recombinant human beta1-adrenoceptor expressed in whole cells assessed as cAMP accumulation by homogeneous radioimmunoassay
ChEMBL 435 12 6 6 3.0 O=CNc1cc([C@@H](O)CNCCc2ccc(NC[C@H](O)c3ccccc3)cc2)ccc1O 10.1016/j.bmcl.2011.11.072
44574720 177708 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 11 4 5 4.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466923 177708 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 494 11 4 5 4.5 O=C(Cc1ccccn1)Nc1ccc(CCNC[C@H](O)COc2cccc3[nH]c4ccccc4c23)cc1 10.1016/j.bmc.2009.03.044
49861320 54478 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1204003 54478 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
CHEMBL1615579 54478 0 None -6 3 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassayAgonist activity at human cloned adrenergic beta-1 receptor expressed in CHO cells assessed as [125I]cAMP accumulation after 2 days by radioimmunoassay
ChEMBL 426 11 3 5 3.1 O=S(=O)(Nc1ccccc1)c1ccc(CCNC[C@@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.06.031
10048077 97220 6 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
CHEMBL272383 97220 6 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassayAgonist activity at human recombinant beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by enzyme immunoassay
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm9000709
44574757 177643 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
CHEMBL466467 177643 0 None -12 2 Human 5.6 pEC50 = 5.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulationAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation
ChEMBL 511 14 3 6 4.4 O=C(Cc1cccc(OCc2ccccc2)n1)Nc1ccc(CCNC[C@H](O)COc2ccccc2)cc1 10.1016/j.bmc.2009.03.044
10048077 97220 6 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
CHEMBL272383 97220 6 None -52 2 Human 6.6 pEC50 = 6.6 Functional
Agonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIAAgonist activity at human beta-1 adrenergic receptor expressed in CHO cells assessed as cAMP accumulation by EIA
ChEMBL 425 9 3 4 4.6 COc1cc(-c2ccc(CCNC[C@H](O)c3cccc(Cl)c3)cc2)ccc1C(=O)O 10.1021/jm701324c
11003341 45852 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500
CHEMBL153558 45852 0 None -10 3 Human 6.6 pEC50 = 6.6 Functional
Ability to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentrationAbility to cause cAMP accumulation in CHO cells expressing human beta-1 AR expressed as the negative logarithm of the molar drug concentration
ChEMBL 376 10 4 4 3.5 C[C@H](CNc1ccc(CCC(=O)O)cc1)NC[C@H](O)c1cccc(Cl)c1 10.1021/jm0101500