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Ligand source activities (1 row/activity)

Ligand Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors UniProt IUPHAR Species p-value
(-log)		 Activity
Type		 Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
9849126 12151 0 B0FL73 β1-adrenoceptor 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 12151 0 B0FL73 β1-adrenoceptor 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 12151 0 B0FL73 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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
9906822 161213 0 ADRB1 β1-adrenoceptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
CHEMBL416012 161213 0 ADRB1 β1-adrenoceptor Human 9.9 pEC50 = 9.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 358 7 3 3 4.1 COc1cccc2c(CC(C)NC[C@H](O)c3cccc(Cl)c3)c[nH]c12 10.1007/s00044-009-9257-x
11268355 95709 0 ADRB1 β1-adrenoceptor 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 95709 0 ADRB1 β1-adrenoceptor 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 1558 42 B0FL73 β1-adrenoceptor 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 1558 42 B0FL73 β1-adrenoceptor 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 1558 42 B0FL73 β1-adrenoceptor 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 1558 42 B0FL73 β1-adrenoceptor 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 1558 42 B0FL73 β1-adrenoceptor 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 17149 0 ADRB1 β1-adrenoceptor 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 17149 0 ADRB1 β1-adrenoceptor 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
45483813 192255 13 ADRB1 β1-adrenoceptor 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(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
CHEMBL579394 192255 13 ADRB1 β1-adrenoceptor 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(O)c1ccc(O)c2c1OCC(=O)N2 10.1016/j.bmcl.2009.10.013
9891927 183321 4 B0FL73 β1-adrenoceptor 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 183321 4 B0FL73 β1-adrenoceptor 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 183321 4 B0FL73 β1-adrenoceptor 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 183321 4 B0FL73 β1-adrenoceptor 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 190735 0 ADRB1 β1-adrenoceptor 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 190735 0 ADRB1 β1-adrenoceptor 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 9359 38 ADRB1 β1-adrenoceptor 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 9359 38 ADRB1 β1-adrenoceptor 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 9359 38 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 190812 0 ADRB1 β1-adrenoceptor 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 190812 0 ADRB1 β1-adrenoceptor 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 131009 0 ADRB1 β1-adrenoceptor 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 131009 0 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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
44396736 66306 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL186271 66306 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 617 12 4 9 5.1 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccs3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL4645927 177496 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4651239 177496 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
44396715 66883 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL189081 66883 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 612 12 4 9 4.4 C[C@H](Cc1c[nH]c2c(OS(=O)(=O)c3cccnc3)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44392230 65041 0 ADRB1 β1-adrenoceptor 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 65041 0 ADRB1 β1-adrenoceptor 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 97175 0 ADRB1 β1-adrenoceptor 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 97175 0 ADRB1 β1-adrenoceptor 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
CHEMBL4635163 177439 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
CHEMBL4650951 177439 0 ADRB1 β1-adrenoceptor Human 8.9 pEC50 = 8.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1ccccc1CCC(C)(C)NC[C@H](O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
1499 1961 36 ADRB1 β1-adrenoceptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
3779 1961 36 ADRB1 β1-adrenoceptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
536 1961 36 ADRB1 β1-adrenoceptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
CHEMBL434 1961 36 ADRB1 β1-adrenoceptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
DB01064 1961 36 ADRB1 β1-adrenoceptor Human 8.8 pEC50 = 8.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 211 4 4 4 1.1 CC(NCC(c1ccc(c(c1)O)O)O)C 10.1016/j.bmc.2019.115178
90645347 111782 0 ADRB1 β1-adrenoceptor 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 111782 0 ADRB1 β1-adrenoceptor 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 192113 0 ADRB1 β1-adrenoceptor 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 192113 0 ADRB1 β1-adrenoceptor 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 17181 0 ADRB1 β1-adrenoceptor 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 17181 0 ADRB1 β1-adrenoceptor 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
165193 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
2303 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
4946 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
564 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
62882 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
63 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
66366 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
91536 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
CHEMBL27 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
CHEMBL452861 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
DB00571 2992 54 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Displacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cellsDisplacement of [125I]cyanopindolol from human recombinant adrenergic beta-1 receptor expressed in Rex16 cells
ChEMBL 259 6 2 3 2.6 OC(COc1cccc2c1cccc2)CNC(C)C 10.1021/np058114h
9927453 95999 0 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
CHEMBL26393 95999 0 ADRB1 β1-adrenoceptor Human 8.7 pEC50 = 8.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 328 6 3 2 4.1 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(Cl)c1 10.1007/s00044-009-9257-x
9927453 95999 0 ADRB1 β1-adrenoceptor 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 95999 0 ADRB1 β1-adrenoceptor 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 12270 0 B0FL73 β1-adrenoceptor 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 12270 0 B0FL73 β1-adrenoceptor 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 12270 0 B0FL73 β1-adrenoceptor 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 111764 0 ADRB1 β1-adrenoceptor 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 111764 0 ADRB1 β1-adrenoceptor 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
44392457 165131 0 ADRB1 β1-adrenoceptor Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
CHEMBL425161 165131 0 ADRB1 β1-adrenoceptor Human 8.0 pEC50 = 8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 457 11 4 6 3.7 C/C=C/CNc1cccc([C@@H](O)CN[C@H](C)Cc2c[nH]c3c(OS(C)(=O)=O)cccc23)c1 10.1007/s00044-009-9257-x
42625517 12430 0 B0FL73 β1-adrenoceptor 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 12430 0 B0FL73 β1-adrenoceptor 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 12430 0 B0FL73 β1-adrenoceptor 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 111777 0 ADRB1 β1-adrenoceptor 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 111777 0 ADRB1 β1-adrenoceptor 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 66041 0 ADRB1 β1-adrenoceptor 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 66041 0 ADRB1 β1-adrenoceptor 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 66041 0 ADRB1 β1-adrenoceptor 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 189224 0 ADRB1 β1-adrenoceptor 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 189224 0 ADRB1 β1-adrenoceptor 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 189224 0 ADRB1 β1-adrenoceptor 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 111539 0 ADRB1 β1-adrenoceptor 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 111539 0 ADRB1 β1-adrenoceptor 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 3847 25 ADRB1 β1-adrenoceptor 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 3847 25 ADRB1 β1-adrenoceptor 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 3847 25 ADRB1 β1-adrenoceptor 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 3847 25 ADRB1 β1-adrenoceptor 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 3847 25 ADRB1 β1-adrenoceptor 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 49849 0 ADRB1 β1-adrenoceptor 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 49849 0 ADRB1 β1-adrenoceptor 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 63537 0 ADRB1 β1-adrenoceptor 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 63537 0 ADRB1 β1-adrenoceptor 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 63538 0 ADRB1 β1-adrenoceptor 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 63538 0 ADRB1 β1-adrenoceptor 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 63539 0 ADRB1 β1-adrenoceptor 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 63539 0 ADRB1 β1-adrenoceptor 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 63543 0 ADRB1 β1-adrenoceptor 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 63543 0 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 92710 0 ADRB1 β1-adrenoceptor 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 92710 0 ADRB1 β1-adrenoceptor 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 147253 0 ADRB1 β1-adrenoceptor 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 147253 0 ADRB1 β1-adrenoceptor 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 150190 0 ADRB1 β1-adrenoceptor 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 150190 0 ADRB1 β1-adrenoceptor 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 188726 0 ADRB1 β1-adrenoceptor 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 188726 0 ADRB1 β1-adrenoceptor 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 188726 0 ADRB1 β1-adrenoceptor 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 189038 0 ADRB1 β1-adrenoceptor 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 189038 0 ADRB1 β1-adrenoceptor 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 189038 0 ADRB1 β1-adrenoceptor 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 12388 0 ADRB1 β1-adrenoceptor 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 12388 0 ADRB1 β1-adrenoceptor 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 12388 0 ADRB1 β1-adrenoceptor 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 6727 0 ADRB1 β1-adrenoceptor 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 6727 0 ADRB1 β1-adrenoceptor 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 98994 0 ADRB1 β1-adrenoceptor 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 98994 0 ADRB1 β1-adrenoceptor 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
44328703 9953 0 ADRB1 β1-adrenoceptor Human 6.0 pEC50 = 6 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK2 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
CHEMBL1160694 9953 0 ADRB1 β1-adrenoceptor Human 6.0 pEC50 = 6 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK2 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK2 and coelenterazine 400a by BRET assay
ChEMBL 241 6 4 5 0.8 CC(C)NC[C@H](O)COc1ccc(O)c(O)c1 10.1021/acs.jmedchem.9b00349
10347461 105559 0 ADRB1 β1-adrenoceptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3126384 105559 0 ADRB1 β1-adrenoceptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
CHEMBL3139025 105559 0 ADRB1 β1-adrenoceptor Human 6.0 pEC50 = 6 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 547 18 4 7 4.8 O=S(=O)(c1ccc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc1)C1CCCC1 10.1021/jm401532g
1499 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 12430 0 ADRB1 β1-adrenoceptor 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 12430 0 ADRB1 β1-adrenoceptor 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 12430 0 ADRB1 β1-adrenoceptor 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 179558 0 ADRB1 β1-adrenoceptor 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 179558 0 ADRB1 β1-adrenoceptor 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 4190 0 ADRB1 β1-adrenoceptor 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 4190 0 ADRB1 β1-adrenoceptor 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 76624 0 ADRB1 β1-adrenoceptor 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 76624 0 ADRB1 β1-adrenoceptor 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 57711 0 ADRB1 β1-adrenoceptor 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 57711 0 ADRB1 β1-adrenoceptor 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
146025803 175329 0 ADRB1 β1-adrenoceptor Human 5.0 pEC50 = 5 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL4593181 175329 0 ADRB1 β1-adrenoceptor Human 5.0 pEC50 = 5 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 467 14 4 7 3.7 COc1cc(CCNC[C@H](O)COc2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
155517986 169368 0 ADRB1 β1-adrenoceptor 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 169368 0 ADRB1 β1-adrenoceptor 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 103063 0 ADRB1 β1-adrenoceptor 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 103063 0 ADRB1 β1-adrenoceptor 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 2687 57 B0FL73 β1-adrenoceptor 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 2687 57 B0FL73 β1-adrenoceptor 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 2687 57 B0FL73 β1-adrenoceptor 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 2687 57 B0FL73 β1-adrenoceptor 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 2687 57 B0FL73 β1-adrenoceptor 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 102248 0 ADRB1 β1-adrenoceptor 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 102248 0 ADRB1 β1-adrenoceptor 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 164903 0 ADRB1 β1-adrenoceptor 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 164903 0 ADRB1 β1-adrenoceptor 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 190731 0 ADRB1 β1-adrenoceptor 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 190731 0 ADRB1 β1-adrenoceptor 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 194344 0 ADRB1 β1-adrenoceptor 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 194344 0 ADRB1 β1-adrenoceptor 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 3924 0 ADRB1 β1-adrenoceptor 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 3924 0 ADRB1 β1-adrenoceptor 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 4165 0 ADRB1 β1-adrenoceptor 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 4165 0 ADRB1 β1-adrenoceptor 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 194372 0 ADRB1 β1-adrenoceptor 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 194372 0 ADRB1 β1-adrenoceptor 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 197859 0 ADRB1 β1-adrenoceptor 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 197859 0 ADRB1 β1-adrenoceptor 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 109010 0 ADRB1 β1-adrenoceptor 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 109010 0 ADRB1 β1-adrenoceptor 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 166980 0 ADRB1 β1-adrenoceptor 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 166980 0 ADRB1 β1-adrenoceptor 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 97355 0 ADRB1 β1-adrenoceptor 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 97355 0 ADRB1 β1-adrenoceptor 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 190885 0 ADRB1 β1-adrenoceptor 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 190885 0 ADRB1 β1-adrenoceptor 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 175607 0 ADRB1 β1-adrenoceptor 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 175607 0 ADRB1 β1-adrenoceptor 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 171366 0 ADRB1 β1-adrenoceptor 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 171366 0 ADRB1 β1-adrenoceptor 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 188636 0 ADRB1 β1-adrenoceptor 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 188636 0 ADRB1 β1-adrenoceptor 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 188636 0 ADRB1 β1-adrenoceptor 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 190161 0 ADRB1 β1-adrenoceptor 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 190161 0 ADRB1 β1-adrenoceptor 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 17426 0 ADRB1 β1-adrenoceptor 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 17426 0 ADRB1 β1-adrenoceptor 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 189326 0 ADRB1 β1-adrenoceptor 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 189326 0 ADRB1 β1-adrenoceptor 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 172257 0 ADRB1 β1-adrenoceptor 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 172257 0 ADRB1 β1-adrenoceptor 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 56304 0 ADRB1 β1-adrenoceptor 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 56304 0 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 1961 36 ADRB1 β1-adrenoceptor 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 175608 0 ADRB1 β1-adrenoceptor 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 175608 0 ADRB1 β1-adrenoceptor 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 184017 0 ADRB1 β1-adrenoceptor 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 184017 0 ADRB1 β1-adrenoceptor 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 197451 0 ADRB1 β1-adrenoceptor 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 197451 0 ADRB1 β1-adrenoceptor 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 65512 0 ADRB1 β1-adrenoceptor 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 65512 0 ADRB1 β1-adrenoceptor 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 93115 0 ADRB1 β1-adrenoceptor 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 93115 0 ADRB1 β1-adrenoceptor 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
CHEMBL4645694 177420 0 ADRB1 β1-adrenoceptor Human 7.9 pEC50 = 7.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
CHEMBL4650809 177420 0 ADRB1 β1-adrenoceptor Human 7.9 pEC50 = 7.9 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 400 8 4 6 2.8 COc1cccc(CCC(C)(C)NCC(O)c2cc(O)cc3c2OCC(=O)N3)c1 10.1016/j.bmc.2019.115178
2687 843 12 ADRB1 β1-adrenoceptor 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
532 843 12 ADRB1 β1-adrenoceptor 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 843 12 ADRB1 β1-adrenoceptor 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 843 12 ADRB1 β1-adrenoceptor 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 92996 0 ADRB1 β1-adrenoceptor 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 92996 0 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 111748 0 ADRB1 β1-adrenoceptor 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 111748 0 ADRB1 β1-adrenoceptor 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 111772 0 ADRB1 β1-adrenoceptor 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 111772 0 ADRB1 β1-adrenoceptor 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 13905 0 ADRB1 β1-adrenoceptor 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 13905 0 ADRB1 β1-adrenoceptor 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 13905 0 ADRB1 β1-adrenoceptor 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 13914 0 ADRB1 β1-adrenoceptor 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 13914 0 ADRB1 β1-adrenoceptor 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 13914 0 ADRB1 β1-adrenoceptor 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 13917 0 ADRB1 β1-adrenoceptor 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 13917 0 ADRB1 β1-adrenoceptor 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 13917 0 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 1558 42 ADRB1 β1-adrenoceptor 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 172256 0 ADRB1 β1-adrenoceptor 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 172256 0 ADRB1 β1-adrenoceptor 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 64687 0 ADRB1 β1-adrenoceptor 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 64687 0 ADRB1 β1-adrenoceptor 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 97606 0 ADRB1 β1-adrenoceptor 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 97606 0 ADRB1 β1-adrenoceptor 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 99275 0 ADRB1 β1-adrenoceptor 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 99275 0 ADRB1 β1-adrenoceptor 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 165088 0 ADRB1 β1-adrenoceptor 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 165088 0 ADRB1 β1-adrenoceptor 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 3248 73 ADRB1 β1-adrenoceptor 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 3248 73 ADRB1 β1-adrenoceptor 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 3248 73 ADRB1 β1-adrenoceptor 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 3248 73 ADRB1 β1-adrenoceptor 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 3248 73 ADRB1 β1-adrenoceptor 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 63942 0 ADRB1 β1-adrenoceptor 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 63942 0 ADRB1 β1-adrenoceptor 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 63942 0 ADRB1 β1-adrenoceptor 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 65848 0 ADRB1 β1-adrenoceptor 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 65848 0 ADRB1 β1-adrenoceptor 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 65848 0 ADRB1 β1-adrenoceptor 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 12409 0 ADRB1 β1-adrenoceptor 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 12409 0 ADRB1 β1-adrenoceptor 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 12409 0 ADRB1 β1-adrenoceptor 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 76736 0 ADRB1 β1-adrenoceptor 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 76736 0 ADRB1 β1-adrenoceptor 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 92749 0 ADRB1 β1-adrenoceptor 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 92749 0 ADRB1 β1-adrenoceptor 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 12309 0 ADRB1 β1-adrenoceptor 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 12309 0 ADRB1 β1-adrenoceptor 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 12309 0 ADRB1 β1-adrenoceptor 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 183691 0 ADRB1 β1-adrenoceptor 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 183691 0 ADRB1 β1-adrenoceptor 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 164558 0 ADRB1 β1-adrenoceptor 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 164558 0 ADRB1 β1-adrenoceptor 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
76333795 84653 0 ADRB1 β1-adrenoceptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
CHEMBL2260985 84653 0 ADRB1 β1-adrenoceptor Human 7.9 pEC50 = 7.9 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 558 11 5 8 3.1 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccc(N)c2)c1 10.1007/s00044-009-9257-x
24895265 184016 0 ADRB1 β1-adrenoceptor 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 184016 0 ADRB1 β1-adrenoceptor 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 63970 0 ADRB1 β1-adrenoceptor 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 63970 0 ADRB1 β1-adrenoceptor 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 174577 0 ADRB1 β1-adrenoceptor 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 174577 0 ADRB1 β1-adrenoceptor 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 177744 0 ADRB1 β1-adrenoceptor 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 177744 0 ADRB1 β1-adrenoceptor 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 188768 0 ADRB1 β1-adrenoceptor 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 188768 0 ADRB1 β1-adrenoceptor 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 188768 0 ADRB1 β1-adrenoceptor 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 184272 0 ADRB1 β1-adrenoceptor 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 184272 0 ADRB1 β1-adrenoceptor 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 188826 0 ADRB1 β1-adrenoceptor 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 188826 0 ADRB1 β1-adrenoceptor 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 172746 0 ADRB1 β1-adrenoceptor 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 172746 0 ADRB1 β1-adrenoceptor 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 183987 0 ADRB1 β1-adrenoceptor 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 183987 0 ADRB1 β1-adrenoceptor 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 12224 0 ADRB1 β1-adrenoceptor 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 12224 0 ADRB1 β1-adrenoceptor 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 12224 0 ADRB1 β1-adrenoceptor 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 178466 0 ADRB1 β1-adrenoceptor 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 178466 0 ADRB1 β1-adrenoceptor 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 99312 0 ADRB1 β1-adrenoceptor 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 99312 0 ADRB1 β1-adrenoceptor 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 177663 0 ADRB1 β1-adrenoceptor 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 177663 0 ADRB1 β1-adrenoceptor 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 91907 2 ADRB1 β1-adrenoceptor 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 91907 2 ADRB1 β1-adrenoceptor 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 100949 8 ADRB1 β1-adrenoceptor 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 100949 8 ADRB1 β1-adrenoceptor 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
CHEMBL4638864 176604 0 ADRB1 β1-adrenoceptor Human 7.8 pEC50 = 7.8 ADMET
Agonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assayAgonist activity at human beta1 adrenoreceptor overexpressed in human HEK293 cells assessed as cAMP accumulation incubated for 60 mins by HTRF assay
ChEMBL 370 7 4 5 2.8 CC(C)(CCc1ccccc1)NCC(O)c1cc(O)cc2c1OCC(=O)N2 10.1016/j.bmc.2019.115178
9804536 164871 0 ADRB1 β1-adrenoceptor 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 164871 0 ADRB1 β1-adrenoceptor 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 177742 0 ADRB1 β1-adrenoceptor 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 177742 0 ADRB1 β1-adrenoceptor 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 189279 0 ADRB1 β1-adrenoceptor 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 189279 0 ADRB1 β1-adrenoceptor 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 189279 0 ADRB1 β1-adrenoceptor 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 187611 0 ADRB1 β1-adrenoceptor 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 187611 0 ADRB1 β1-adrenoceptor 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 176175 0 ADRB1 β1-adrenoceptor 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 176175 0 ADRB1 β1-adrenoceptor 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 12157 0 ADRB1 β1-adrenoceptor 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 12157 0 ADRB1 β1-adrenoceptor 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 12157 0 ADRB1 β1-adrenoceptor 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 98602 0 ADRB1 β1-adrenoceptor 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 98602 0 ADRB1 β1-adrenoceptor 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 169122 0 ADRB1 β1-adrenoceptor 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 169122 0 ADRB1 β1-adrenoceptor 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 172855 0 ADRB1 β1-adrenoceptor 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 172855 0 ADRB1 β1-adrenoceptor 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 64306 0 ADRB1 β1-adrenoceptor 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 64306 0 ADRB1 β1-adrenoceptor 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 276 64 B0FL73 β1-adrenoceptor 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 276 64 B0FL73 β1-adrenoceptor 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
479 276 64 B0FL73 β1-adrenoceptor 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 276 64 B0FL73 β1-adrenoceptor 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 276 64 B0FL73 β1-adrenoceptor 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 276 64 B0FL73 β1-adrenoceptor 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 170052 0 ADRB1 β1-adrenoceptor 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 170052 0 ADRB1 β1-adrenoceptor 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 173464 0 ADRB1 β1-adrenoceptor 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 173464 0 ADRB1 β1-adrenoceptor 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 189759 0 ADRB1 β1-adrenoceptor 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 189759 0 ADRB1 β1-adrenoceptor 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 189837 0 ADRB1 β1-adrenoceptor 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 189837 0 ADRB1 β1-adrenoceptor 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 183915 0 ADRB1 β1-adrenoceptor 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 183915 0 ADRB1 β1-adrenoceptor 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 186453 0 ADRB1 β1-adrenoceptor 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 186453 0 ADRB1 β1-adrenoceptor 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 178493 0 ADRB1 β1-adrenoceptor 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 178493 0 ADRB1 β1-adrenoceptor 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 185438 0 ADRB1 β1-adrenoceptor 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 185438 0 ADRB1 β1-adrenoceptor 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 54911 0 ADRB1 β1-adrenoceptor 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 54911 0 ADRB1 β1-adrenoceptor 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 63547 0 ADRB1 β1-adrenoceptor 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 63547 0 ADRB1 β1-adrenoceptor 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 65805 0 ADRB1 β1-adrenoceptor 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 65805 0 ADRB1 β1-adrenoceptor 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 65805 0 ADRB1 β1-adrenoceptor 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 147248 0 ADRB1 β1-adrenoceptor 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 147248 0 ADRB1 β1-adrenoceptor 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
10482960 105669 0 ADRB1 β1-adrenoceptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3126383 105669 0 ADRB1 β1-adrenoceptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
CHEMBL3139365 105669 0 ADRB1 β1-adrenoceptor Human 6.8 pEC50 = 6.8 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 561 18 4 7 5.1 Cc1cc(CCCCOCCCCCCNC[C@H](O)c2ccc(O)c(CO)c2)cc(S(=O)(=O)C2CCCC2)c1 10.1021/jm401532g
145981079 165856 0 ADRB1 β1-adrenoceptor 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 165856 0 ADRB1 β1-adrenoceptor 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 185477 0 ADRB1 β1-adrenoceptor 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 185477 0 ADRB1 β1-adrenoceptor 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 12236 0 ADRB1 β1-adrenoceptor 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 12236 0 ADRB1 β1-adrenoceptor 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 12236 0 ADRB1 β1-adrenoceptor 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 64699 0 ADRB1 β1-adrenoceptor 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 64699 0 ADRB1 β1-adrenoceptor 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 57707 0 ADRB1 β1-adrenoceptor 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 57707 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 101480 0 ADRB1 β1-adrenoceptor 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 101480 0 ADRB1 β1-adrenoceptor 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 111276 0 ADRB1 β1-adrenoceptor 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 111276 0 ADRB1 β1-adrenoceptor 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 5808 0 ADRB1 β1-adrenoceptor 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 5808 0 ADRB1 β1-adrenoceptor 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 186447 0 ADRB1 β1-adrenoceptor 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 186447 0 ADRB1 β1-adrenoceptor 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 96929 0 ADRB1 β1-adrenoceptor 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 96929 0 ADRB1 β1-adrenoceptor 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 96929 0 ADRB1 β1-adrenoceptor 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 96929 0 ADRB1 β1-adrenoceptor 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 165131 0 ADRB1 β1-adrenoceptor 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 165131 0 ADRB1 β1-adrenoceptor 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
567 686 6 ADRB1 β1-adrenoceptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
9841972 686 6 ADRB1 β1-adrenoceptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
CHEMBL284782 686 6 ADRB1 β1-adrenoceptor Human 5.8 pEC50 = 5.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 363 9 3 4 3.1 C[C@H](Cc1ccc(cc1)OCC(=O)O)NC[C@@H](c1cccc(c1)Cl)O 10.1007/s00044-009-9257-x
44127677 189002 0 ADRB1 β1-adrenoceptor 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 189002 0 ADRB1 β1-adrenoceptor 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
567 686 6 ADRB1 β1-adrenoceptor 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 686 6 ADRB1 β1-adrenoceptor 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 686 6 ADRB1 β1-adrenoceptor 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 194739 0 ADRB1 β1-adrenoceptor 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 194739 0 ADRB1 β1-adrenoceptor 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 175150 0 ADRB1 β1-adrenoceptor 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 175150 0 ADRB1 β1-adrenoceptor 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
5581 100949 8 B0FL73 β1-adrenoceptor Guinea pig 6.8 pEC50 = 6.8 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compound
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL299175 100949 8 B0FL73 β1-adrenoceptor Guinea pig 6.8 pEC50 = 6.8 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compoundInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria after treatment with the compound
ChEMBL 345 5 3 6 2.6 COc1cc(CC2NCCc3cc(O)c(O)cc32)cc(OC)c1OC 10.1021/jm00081a007
131487 4732 7 B0FL73 β1-adrenoceptor 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 4732 7 B0FL73 β1-adrenoceptor 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
11432806 65638 0 ADRB1 β1-adrenoceptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL184407 65638 0 ADRB1 β1-adrenoceptor Human 7.8 pEC50 = 7.8 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 549 11 4 8 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
24822648 96918 0 ADRB1 β1-adrenoceptor 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 96918 0 ADRB1 β1-adrenoceptor 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 190427 0 ADRB1 β1-adrenoceptor 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 190427 0 ADRB1 β1-adrenoceptor 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 177667 0 ADRB1 β1-adrenoceptor 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 177667 0 ADRB1 β1-adrenoceptor 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 177714 0 ADRB1 β1-adrenoceptor 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 177714 0 ADRB1 β1-adrenoceptor 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 188952 0 ADRB1 β1-adrenoceptor 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 188952 0 ADRB1 β1-adrenoceptor 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 175845 0 ADRB1 β1-adrenoceptor 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 175845 0 ADRB1 β1-adrenoceptor 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 66721 0 ADRB1 β1-adrenoceptor 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 66721 0 ADRB1 β1-adrenoceptor 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 198416 0 ADRB1 β1-adrenoceptor 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 198416 0 ADRB1 β1-adrenoceptor 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 4197 0 ADRB1 β1-adrenoceptor 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 4197 0 ADRB1 β1-adrenoceptor 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 190524 0 ADRB1 β1-adrenoceptor 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 190524 0 ADRB1 β1-adrenoceptor 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 109059 0 ADRB1 β1-adrenoceptor 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 109059 0 ADRB1 β1-adrenoceptor 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
44396568 66721 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL188196 66721 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 529 12 5 7 3.7 C[C@H](Cc1c[nH]c2c(OCC(=O)O)cccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
76315638 84654 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
CHEMBL2260986 84654 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 543 11 4 7 3.6 C[C@H](Cc1c[nH]c2c(OS(C)(=O)=O)cccc12)NC[C@H](O)c1ccc(S(=O)(=O)Nc2ccccc2)cc1 10.1007/s00044-009-9257-x
44396488 66170 0 ADRB1 β1-adrenoceptor 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 66170 0 ADRB1 β1-adrenoceptor 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 198266 0 ADRB1 β1-adrenoceptor 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 198266 0 ADRB1 β1-adrenoceptor 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 119040 0 ADRB1 β1-adrenoceptor 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 119040 0 ADRB1 β1-adrenoceptor 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 93117 0 ADRB1 β1-adrenoceptor 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 93117 0 ADRB1 β1-adrenoceptor 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 166935 0 ADRB1 β1-adrenoceptor 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 166935 0 ADRB1 β1-adrenoceptor 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 13916 0 ADRB1 β1-adrenoceptor 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 13916 0 ADRB1 β1-adrenoceptor 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 13916 0 ADRB1 β1-adrenoceptor 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 13941 0 ADRB1 β1-adrenoceptor 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 13941 0 ADRB1 β1-adrenoceptor 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 13941 0 ADRB1 β1-adrenoceptor 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 177718 0 ADRB1 β1-adrenoceptor 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 177718 0 ADRB1 β1-adrenoceptor 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 184478 0 ADRB1 β1-adrenoceptor 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 184478 0 ADRB1 β1-adrenoceptor 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 187973 0 ADRB1 β1-adrenoceptor 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 187973 0 ADRB1 β1-adrenoceptor 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 190150 0 ADRB1 β1-adrenoceptor 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 190150 0 ADRB1 β1-adrenoceptor 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 186060 0 ADRB1 β1-adrenoceptor 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 186060 0 ADRB1 β1-adrenoceptor 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 84282 9 ADRB1 β1-adrenoceptor 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 84282 9 ADRB1 β1-adrenoceptor 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 170414 0 ADRB1 β1-adrenoceptor 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 170414 0 ADRB1 β1-adrenoceptor 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 63548 0 ADRB1 β1-adrenoceptor 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 63548 0 ADRB1 β1-adrenoceptor 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
2419 3248 73 ADRB1 β1-adrenoceptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
5152 3248 73 ADRB1 β1-adrenoceptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
559 3248 73 ADRB1 β1-adrenoceptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
CHEMBL1263 3248 73 ADRB1 β1-adrenoceptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
DB00938 3248 73 ADRB1 β1-adrenoceptor Human 6.7 pEC50 = 6.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring GFP/Rluc2-tagged beta-arrestin2 assessed as increase in beta-arrestin2 recruitment incubated for 5 mins in presence of GRK5 and coelenterazine 400a by BRET assay
ChEMBL 415 16 4 5 4.1 OCc1cc(ccc1O)C(CNCCCCCCOCCCCc1ccccc1)O 10.1021/acs.jmedchem.9b00349
56675509 63940 0 ADRB1 β1-adrenoceptor 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 63940 0 ADRB1 β1-adrenoceptor 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 65846 0 ADRB1 β1-adrenoceptor 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 65846 0 ADRB1 β1-adrenoceptor 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 65846 0 ADRB1 β1-adrenoceptor 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 65847 0 ADRB1 β1-adrenoceptor 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 65847 0 ADRB1 β1-adrenoceptor 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 65847 0 ADRB1 β1-adrenoceptor 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
127046950 139251 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
CHEMBL3800303 139251 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assayAgonist activity at beta1-adrenergic receptor (unknown origin) expressed in HEK293T cells harboring Rluc2-117-GalphaS/GFP10-Ggamma/Gbeta1 assessed as activation of GalphaS incubated for 5 mins in presence of coelenterazine 400a by BRET assay
ChEMBL 437 12 4 6 4.0 COc1cc(CCNC[C@H](O)c2ccc(O)c(O)c2)ccc1OCCCc1ccccc1 10.1021/acs.jmedchem.9b00349
11318107 105668 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126386 105668 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139364 105668 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 505 16 4 7 3.4 O=S1(=O)CCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
11318358 105712 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3126387 105712 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
CHEMBL3139613 105712 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
Agonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assayAgonist activity at human beta1 adrenoceptor transfected in CHO cells assessed as cyclic AMP accumulation after 45 mins by fluorescence polarization assay
ChEMBL 519 16 4 7 3.8 O=S1(=O)CCCc2ccc(CCCCOCCCCCCNC[C@H](O)c3ccc(O)c(CO)c3)cc21 10.1021/jm401532g
9958539 102392 0 ADRB1 β1-adrenoceptor 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 102392 0 ADRB1 β1-adrenoceptor 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 9958 16 B0FL73 β1-adrenoceptor 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 9958 16 B0FL73 β1-adrenoceptor 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 9958 16 B0FL73 β1-adrenoceptor 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 65046 0 ADRB1 β1-adrenoceptor 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 65046 0 ADRB1 β1-adrenoceptor 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 2197 4 ADRB1 β1-adrenoceptor 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 2197 4 ADRB1 β1-adrenoceptor 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 2197 4 ADRB1 β1-adrenoceptor 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 87600 0 ADRB1 β1-adrenoceptor 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 87600 0 ADRB1 β1-adrenoceptor 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 12256 0 B0FL73 β1-adrenoceptor 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 12256 0 B0FL73 β1-adrenoceptor 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 12256 0 B0FL73 β1-adrenoceptor 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 12446 0 B0FL73 β1-adrenoceptor 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 12446 0 B0FL73 β1-adrenoceptor 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 12446 0 B0FL73 β1-adrenoceptor 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 111725 0 ADRB1 β1-adrenoceptor 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 111725 0 ADRB1 β1-adrenoceptor 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 111727 0 ADRB1 β1-adrenoceptor 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 111727 0 ADRB1 β1-adrenoceptor 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 165061 0 ADRB1 β1-adrenoceptor 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 165061 0 ADRB1 β1-adrenoceptor 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 156837 0 ADRB1 β1-adrenoceptor 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 156837 0 ADRB1 β1-adrenoceptor 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 167532 0 ADRB1 β1-adrenoceptor 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 167532 0 ADRB1 β1-adrenoceptor 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 167532 0 ADRB1 β1-adrenoceptor 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 188832 0 ADRB1 β1-adrenoceptor 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 188832 0 ADRB1 β1-adrenoceptor 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 188832 0 ADRB1 β1-adrenoceptor 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 65013 0 ADRB1 β1-adrenoceptor 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 65013 0 ADRB1 β1-adrenoceptor 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 66273 0 ADRB1 β1-adrenoceptor 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 66273 0 ADRB1 β1-adrenoceptor 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 97088 0 ADRB1 β1-adrenoceptor 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 97088 0 ADRB1 β1-adrenoceptor 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 186916 0 ADRB1 β1-adrenoceptor 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 186916 0 ADRB1 β1-adrenoceptor 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 194297 0 ADRB1 β1-adrenoceptor 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 194297 0 ADRB1 β1-adrenoceptor 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 184447 0 ADRB1 β1-adrenoceptor 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 184447 0 ADRB1 β1-adrenoceptor 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
10393774 119975 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
CHEMBL35500 119975 0 ADRB1 β1-adrenoceptor Human 5.7 pEC50 = 5.7 Binding
In vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptorIn vitro activity to increase cAMP levels in Chinese hamster ovary (CHO) cells expressing the cloned human beta 1 Adrenergic receptor
ChEMBL 598 14 5 9 2.1 CCCCN(c1ccc(N2CCC(NC[C@H](O)c3ccc(O)c(NS(C)(=O)=O)c3)CC2)cc1)S(=O)(=O)CC(=O)O 10.1021/jm000544b
10139127 56967 0 ADRB1 β1-adrenoceptor 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 56967 0 ADRB1 β1-adrenoceptor 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 174997 0 ADRB1 β1-adrenoceptor 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 174997 0 ADRB1 β1-adrenoceptor 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 3937 0 ADRB1 β1-adrenoceptor 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 3937 0 ADRB1 β1-adrenoceptor 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 194538 0 ADRB1 β1-adrenoceptor 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 194538 0 ADRB1 β1-adrenoceptor 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 195126 0 ADRB1 β1-adrenoceptor 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 195126 0 ADRB1 β1-adrenoceptor 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
44396532 66195 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
CHEMBL185836 66195 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 455 9 4 5 4.3 C[C@H](Cc1c[nH]c2ccccc12)NC[C@H](O)c1cccc(NS(=O)(=O)c2cccs2)c1 10.1007/s00044-009-9257-x
44377523 55719 0 ADRB1 β1-adrenoceptor 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 55719 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 162220 0 ADRB1 β1-adrenoceptor 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 175887 0 ADRB1 β1-adrenoceptor 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 175887 0 ADRB1 β1-adrenoceptor 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 194595 0 ADRB1 β1-adrenoceptor 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 194595 0 ADRB1 β1-adrenoceptor 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 171335 0 ADRB1 β1-adrenoceptor 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 171335 0 ADRB1 β1-adrenoceptor 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
76315640 84656 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
CHEMBL2260988 84656 0 ADRB1 β1-adrenoceptor Human 7.7 pEC50 = 7.7 Binding
Agonist activity at Homo sapiens (human) beta1 adrenoreceptorAgonist activity at Homo sapiens (human) beta1 adrenoreceptor
ChEMBL 575 12 3 7 5.8 COc1cccc2c(C[C@@H](C)NC[C@H](O)c3cccc(NS(=O)(=O)c4cccs4)c3)cn(Cc3ccccc3)c12 10.1007/s00044-009-9257-x
24895789 186030 0 ADRB1 β1-adrenoceptor 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 186030 0 ADRB1 β1-adrenoceptor 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 66883 0 ADRB1 β1-adrenoceptor 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 66883 0 ADRB1 β1-adrenoceptor 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 173099 0 ADRB1 β1-adrenoceptor 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 173099 0 ADRB1 β1-adrenoceptor 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 87599 0 ADRB1 β1-adrenoceptor 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 87599 0 ADRB1 β1-adrenoceptor 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 12281 0 ADRB1 β1-adrenoceptor 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 12281 0 ADRB1 β1-adrenoceptor 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 12281 0 ADRB1 β1-adrenoceptor 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 175929 16 B0FL73 β1-adrenoceptor 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 175929 16 B0FL73 β1-adrenoceptor 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 175929 16 B0FL73 β1-adrenoceptor 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 164703 0 ADRB1 β1-adrenoceptor 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 164703 0 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 1239 33 ADRB1 β1-adrenoceptor 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 174153 0 ADRB1 β1-adrenoceptor 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 174153 0 ADRB1 β1-adrenoceptor 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
13720716 62501 0 B0FL73 β1-adrenoceptor Guinea pig 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
CHEMBL1788251 62501 0 B0FL73 β1-adrenoceptor Guinea pig 6.6 pEC50 = 6.6 Binding
Inhibitory activity against Beta-1 adrenergic receptor in guinea pig atriaInhibitory activity against Beta-1 adrenergic receptor in guinea pig atria
ChEMBL 363 5 3 6 2.7 COc1cc(C[C@@H]2NCCc3cc(O)c(O)c(F)c32)cc(OC)c1OC 10.1021/jm00081a007
45101521 190420 0 ADRB1 β1-adrenoceptor 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 190420 0 ADRB1 &bet