Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
138697637 184183 0 None 3 2 Human 11.0 pEC50 = 11 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 551 10 1 10 4.2 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4851100 184183 0 None 3 2 Human 11.0 pEC50 = 11 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 551 10 1 10 4.2 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
138697719 185973 0 None 3 2 Human 11.0 pEC50 = 11 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 555 9 1 10 3.9 COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O 10.1016/j.bmcl.2021.128325
CHEMBL4878056 185973 0 None 3 2 Human 11.0 pEC50 = 11 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 555 9 1 10 3.9 COc1cccc(OC)c1-n1c(COC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O 10.1016/j.bmcl.2021.128325
25085173 209468 25 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2014.08.045
CHEMBL3184840 209468 25 None - 1 Human 10.9 pEC50 = 10.9 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2014.08.045
168274433 189542 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 519 6 1 9 3.1 COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5173464 189542 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 519 6 1 9 3.1 COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137197922 190768 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 537 6 1 9 3.3 COc1cccc(OC)c1-n1c(-c2cnn(C)c2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5192130 190768 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 537 6 1 9 3.3 COc1cccc(OC)c1-n1c(-c2cnn(C)c2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137198123 190853 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 533 6 1 7 4.4 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3c(F)cccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5193130 190853 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 533 6 1 7 4.4 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3c(F)cccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
168293355 191470 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 534 6 1 8 3.8 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@@H](c3ncc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5202635 191470 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 534 6 1 8 3.8 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@@H](c3ncc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137198148 191662 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 515 8 1 8 3.4 CCOCc1nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
CHEMBL5205562 191662 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 515 8 1 8 3.4 CCOCc1nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
137198156 191822 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 537 6 1 9 3.3 COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5208127 191822 0 None - 1 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 537 6 1 9 3.3 COc1cccc(OC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137250580 185065 0 None 1 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 484 9 1 8 4.0 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4864542 185065 0 None 1 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 484 9 1 8 4.0 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
138697675 185571 0 None 1 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 537 9 1 10 3.3 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4872345 185571 0 None 1 2 Human 10.7 pEC50 = 10.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 537 9 1 10 3.3 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
11838 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1016/j.bmcl.2021.128325
137106310 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1016/j.bmcl.2021.128325
CHEMBL4873876 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1016/j.bmcl.2021.128325
164619102 184882 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 9 2 9 3.6 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(C)cn3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4861895 184882 0 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 9 2 9 3.6 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(C)cn3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
11838 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acs.jmedchem.0c01878
137106310 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acs.jmedchem.0c01878
CHEMBL4873876 680 6 None -15 2 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 498 9 2 9 4.0 CCOCc1c(c(c(c(=O)[nH]1)c1nnc(o1)Cc1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acs.jmedchem.0c01878
11837 971 2 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 512 8 1 8 4.0 C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acsmedchemlett.1c00385
162679533 971 2 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 512 8 1 8 4.0 C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acsmedchemlett.1c00385
CHEMBL4854412 971 2 None - 1 Human 10.6 pEC50 = 10.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 512 8 1 8 4.0 C(CCC)c1n(c(c(c(=O)n1)C(=O)N1C[C@@H](CC1)c1ncc(cc1)Cl)O)c1c(cccc1OC)OC 10.1021/acsmedchemlett.1c00385
137198078 189664 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 516 6 1 8 3.6 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ncccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5175424 189664 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 516 6 1 8 3.6 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CCC(c3ncccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137197999 191445 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 554 6 1 9 4.3 COc1cccc(OC)c1-n1c(-c2csc(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5202233 191445 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 554 6 1 9 4.3 COc1cccc(OC)c1-n1c(-c2csc(C)n2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
146222276 183981 0 None 6 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 550 10 2 8 5.0 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4848436 183981 0 None 6 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 550 10 2 8 5.0 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3cccnc3OC)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
132248099 185558 0 None 3 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 570 9 2 8 4.7 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4872192 185558 0 None 3 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 570 9 2 8 4.7 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
139292739 185590 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 604 11 2 10 4.5 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4872583 185590 0 None 1 2 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 604 11 2 10 4.5 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccnc(NC(=O)C4CC4)c3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
164624169 185234 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 512 8 1 8 4.0 CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccc(Cl)cn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4867145 185234 0 None - 1 Human 10.5 pEC50 = 10.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 512 8 1 8 4.0 CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccc(Cl)cn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
168287693 191151 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 515 6 1 7 4.2 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5197398 191151 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 515 6 1 7 4.2 CCc1cccc(CC)c1-n1c(-c2ccn(C)n2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
145419550 185000 0 None 2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 534 9 2 7 5.3 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4863554 185000 0 None 2 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 534 9 2 7 5.3 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccncc3C)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
164620375 185635 0 None 1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 521 9 1 9 4.2 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4873216 185635 0 None 1 2 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 521 9 1 9 4.2 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3cccnc3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL3417385 209909 0 None - 1 Human 10.4 pEC50 = 10.4 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(C(=O)c2ccccc2)cc1)C(=O)O 10.1021/jm501916k
25085173 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.9b01513
CHEMBL3184840 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.9b01513
25078060 433 23 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01504
602 433 23 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01504
605 433 23 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01504
CHEMBL414173 433 23 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL None None None None 10.1021/acs.jmedchem.1c01504
137250573 184163 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 571 9 1 10 3.9 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4850818 184163 0 None -2 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 571 9 1 10 3.9 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-n3cc(Cl)ccc3=O)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
138698137 184502 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 553 9 1 9 4.6 COc1cccc(OC)c1-n1c(CCC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O 10.1016/j.bmcl.2021.128325
CHEMBL4855918 184502 0 None 1 2 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 553 9 1 9 4.6 COc1cccc(OC)c1-n1c(CCC(C)C)nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c1O 10.1016/j.bmcl.2021.128325
25085173 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production and measured by FLIPR assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production and measured by FLIPR assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2022.128882
CHEMBL3184840 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production and measured by FLIPR assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production and measured by FLIPR assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2022.128882
25085173 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acsmedchemlett.1c00385
CHEMBL3184840 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acsmedchemlett.1c00385
25085173 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01878
CHEMBL3184840 209468 25 None - 1 Human 10.3 pEC50 = 10.3 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01878
11836 1015 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 550 6 1 8 4.3 CCc1cccc(CC)c1n1c(O)c(c(=O)nc1c1nn(cc1)C)C(=O)N1CC[C@@H](c2ncc(cc2F)Cl)C1 10.1021/acs.jmedchem.1c01504
140930129 1015 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 550 6 1 8 4.3 CCc1cccc(CC)c1n1c(O)c(c(=O)nc1c1nn(cc1)C)C(=O)N1CC[C@@H](c2ncc(cc2F)Cl)C1 10.1021/acs.jmedchem.1c01504
CHEMBL5170657 1015 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 550 6 1 8 4.3 CCc1cccc(CC)c1n1c(O)c(c(=O)nc1c1nn(cc1)C)C(=O)N1CC[C@@H](c2ncc(cc2F)Cl)C1 10.1021/acs.jmedchem.1c01504
154995949 171595 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 553 9 3 4 7.5 CCC[C@@H](NC(=O)c1ccc(-c2c(Cl)cccc2-c2nc3cc(OC)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4473347 171595 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 553 9 3 4 7.5 CCC[C@@H](NC(=O)c1ccc(-c2c(Cl)cccc2-c2nc3cc(OC)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
156013195 176906 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 1534 44 19 21 -4.6 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)O1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2020.126955
CHEMBL4639193 176906 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 1534 44 19 21 -4.6 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)O1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmcl.2020.126955
168271814 189927 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 497 8 1 8 3.3 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
CHEMBL5179504 189927 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 497 8 1 8 3.3 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
CHEMBL3417389 209911 0 None - 1 Human 10.2 pEC50 = 10.2 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@](C)(Cc1ccccc1)C(=O)O 10.1021/jm501916k
137250546 185716 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 538 9 1 8 4.9 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4874447 185716 0 None 1 2 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 538 9 1 8 4.9 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
137502080 172446 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 553 9 3 4 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(OC)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4518406 172446 0 None - 1 Human 10.1 pEC50 = 10.1 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 553 9 3 4 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(OC)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
10557 975 2 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
137501999 975 2 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
CHEMBL4435973 975 2 None - 1 Human 10.0 pEC50 = 10.0 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
73442763 946 5 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 455 11 2 5 5.7 CCC(n1c(Cc2cccs2)nc2c1ccc(c2)C(=O)N[C@H](CC(=O)O)CC(C)C)CC 10.1021/acs.jmedchem.8b00435
9448 946 5 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 455 11 2 5 5.7 CCC(n1c(Cc2cccs2)nc2c1ccc(c2)C(=O)N[C@H](CC(=O)O)CC(C)C)CC 10.1021/acs.jmedchem.8b00435
CHEMBL4597963 946 5 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulationAgonist activity at APJ receptor (unknown origin) assessed as inhibition of forskolin-induced cAMP accumulation
ChEMBL 455 11 2 5 5.7 CCC(n1c(Cc2cccs2)nc2c1ccc(c2)C(=O)N[C@H](CC(=O)O)CC(C)C)CC 10.1021/acs.jmedchem.8b00435
139557792 189610 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 530 6 2 6 5.9 CCN(c1ccccc1)c1c(-c2cccc(C)c2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
CHEMBL5174457 189610 0 None - 1 Human 10.0 pEC50 = 10 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 530 6 2 6 5.9 CCN(c1ccccc1)c1c(-c2cccc(C)c2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
137197871 185699 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccccn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4874120 185699 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccccn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
137106162 185171 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 497 9 2 8 4.6 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4866313 185171 0 None - 1 Human 9.9 pEC50 = 9.9 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 497 9 2 8 4.6 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
137197878 184386 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.6 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccc(Cl)cc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4854048 184386 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.6 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccc(Cl)cc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL3417378 209902 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(C)cc1)C(=O)O 10.1021/jm501916k
137197871 185699 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccccn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4874120 185699 0 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccccn3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
137106321 185829 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 498 9 2 9 4.0 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)nc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4876050 185829 1 None - 1 Human 9.8 pEC50 = 9.8 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 498 9 2 9 4.0 CCOCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)nc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
154603299 170032 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 503 8 3 3 7.2 CCC[C@@H](NC(=O)c1ccc(-c2c(C)cccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4450702 170032 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 503 8 3 3 7.2 CCC[C@@H](NC(=O)c1ccc(-c2c(C)cccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
155516953 169586 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 576 10 3 5 6.2 COC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4444303 169586 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 576 10 3 5 6.2 COC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
168278529 190278 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 533 6 1 7 4.5 COc1cccc(OC)c1-n1c(-c2ccc(F)cc2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5184730 190278 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 533 6 1 7 4.5 COc1cccc(OC)c1-n1c(-c2ccc(F)cc2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
137198016 191254 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 548 6 1 8 4.2 COc1cccc(OC)c1-n1c(-c2ccc(C)nc2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5199079 191254 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 548 6 1 8 4.2 COc1cccc(OC)c1-n1c(-c2ccc(C)nc2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
138698343 185147 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 458 8 1 8 3.4 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4865954 185147 0 None 1 2 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 458 8 1 8 3.4 CCCCc1nc(=O)c(S(=O)(=O)c2ccc(C)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
10557 975 2 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
137501999 975 2 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
CHEMBL4435973 975 2 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@H](c1ccccc1)NC(=O)c1ccc(c(c1)C(=O)O)c1c(Cl)cccc1c1nc2c([nH]1)cccc2 10.1021/acs.jmedchem.9b01513
137238856 184457 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 477 8 1 7 3.9 CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4855254 184457 0 None - 1 Human 9.7 pEC50 = 9.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 477 8 1 7 3.9 CCCCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL3417377 209901 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(OC)cc1)C(=O)O 10.1021/jm501916k
10061 552 4 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 523 9 1 10 3.7 COc1cccc(c1n1c(nnc1c1cncc(c1)C)NS(=O)(=O)[C@H]([C@@H](c1ncc(cn1)C)C)C)OC 10.1021/acsmedchemlett.1c00385
122702529 552 4 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 523 9 1 10 3.7 COc1cccc(c1n1c(nnc1c1cncc(c1)C)NS(=O)(=O)[C@H]([C@@H](c1ncc(cn1)C)C)C)OC 10.1021/acsmedchemlett.1c00385
CHEMBL4866732 552 4 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 523 9 1 10 3.7 COc1cccc(c1n1c(nnc1c1cncc(c1)C)NS(=O)(=O)[C@H]([C@@H](c1ncc(cn1)C)C)C)OC 10.1021/acsmedchemlett.1c00385
162675419 182777 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assayAgonist activity at human APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 2165 80 25 29 -3.6 CCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(=O)O 10.1016/j.bmcl.2020.127499
CHEMBL4797693 182777 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assayAgonist activity at human APJ receptor stably expressed in CHO cell membranes in presence of [35S]GTPgammaS by scintillation proximity assay
ChEMBL 2165 80 25 29 -3.6 CCCCCCCCCCCCC(=O)N[C@@H](CCC(=O)NCCOCCOCC(=O)NCCOCCOCC(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1c[nH]cn1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(=O)O 10.1016/j.bmcl.2020.127499
139576721 189521 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 496 8 2 6 5.3 CCCCc1nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5173131 189521 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 496 8 2 6 5.3 CCCCc1nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
139576458 189988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 512 8 2 6 5.8 CCCCc1nc(O)c(C(=O)N2CCC(c3ncc(Cl)cc3F)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5180344 189988 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 512 8 2 6 5.8 CCCCc1nc(O)c(C(=O)N2CCC(c3ncc(Cl)cc3F)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL3417383 209907 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCc1ccccc1)C(=O)O 10.1021/jm501916k
137197878 184386 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.6 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccc(Cl)cc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4854048 184386 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 511 8 1 7 4.6 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccc(Cl)cc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
137106334 183839 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 507 7 2 7 5.7 COc1cccc(OC)c1-c1c(C2CCCC2)[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c1O 10.1021/acs.jmedchem.0c01878
CHEMBL4846150 183839 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 507 7 2 7 5.7 COc1cccc(OC)c1-c1c(C2CCCC2)[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c1O 10.1021/acs.jmedchem.0c01878
137198004 185579 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 477 8 1 7 3.9 CCCCc1nc(=O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4872407 185579 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 477 8 1 7 3.9 CCCCc1nc(=O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
139557785 191413 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 494 8 2 6 5.7 CCCCc1nc(O)c(C(=O)N2CCC(c3ccc(Cl)cn3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5201652 191413 0 None - 1 Human 9.6 pEC50 = 9.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 494 8 2 6 5.7 CCCCc1nc(O)c(C(=O)N2CCC(c3ccc(Cl)cn3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
137197947 184982 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3cccnc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4863297 184982 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3cccnc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
138697975 185123 0 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 496 7 1 8 4.3 COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c1O 10.1016/j.bmcl.2021.128325
CHEMBL4865532 185123 0 None 1 2 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 496 7 1 8 4.3 COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(S(=O)(=O)c2ccc(C3CC3)cc2)c1O 10.1016/j.bmcl.2021.128325
25085173 209468 25 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01448
CHEMBL3184840 209468 25 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01448
139557766 190345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 520 6 2 8 4.4 CCN(c1ccccc1)c1c(-c2ccn(C)n2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
CHEMBL5185653 190345 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 520 6 2 8 4.4 CCN(c1ccccc1)c1c(-c2ccn(C)n2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
137197947 184982 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3cccnc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4863297 184982 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3cccnc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
25085173 209468 25 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2019.115237
CHEMBL3184840 209468 25 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2019.115237
154603335 174270 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 557 8 3 3 8.2 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(Cl)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4562873 174270 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 557 8 3 3 8.2 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(Cl)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
155566712 175337 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 574 10 3 4 7.4 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4587131 175337 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 574 10 3 4 7.4 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
129226884 189844 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 561 12 2 5 5.8 CC(C)CN(C)CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1 10.1016/j.bmc.2022.116789
CHEMBL5178250 189844 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 561 12 2 5 5.8 CC(C)CN(C)CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1 10.1016/j.bmc.2022.116789
CHEMBL3417384 209908 0 None - 1 Human 9.5 pEC50 = 9.5 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/jm501916k
137197893 185435 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 479 8 1 8 3.1 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
CHEMBL4870497 185435 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 479 8 1 8 3.1 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.1c01504
137197843 190347 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 491 8 1 8 3.3 COc1cccc(OC)c1-n1c(COC2CC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5185709 190347 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 491 8 1 8 3.3 COc1cccc(OC)c1-n1c(COC2CC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
137106179 184825 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 495 9 2 7 5.4 CCCCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4861053 184825 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 495 9 2 7 5.4 CCCCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
25085173 209468 25 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.04.001
CHEMBL3184840 209468 25 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2014.04.001
137197893 185435 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 479 8 1 8 3.1 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4870497 185435 2 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 479 8 1 8 3.1 CCOCc1nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL3417379 209903 0 None - 1 Human 9.4 pEC50 = 9.4 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccncc1)C(=O)O 10.1021/jm501916k
146222398 184115 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 536 9 2 8 4.1 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4850182 184115 0 None 3 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 536 9 2 8 4.1 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-n3ccccc3=O)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
138697689 185953 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 444 8 1 8 3.1 CCCCc1nc(=O)c(S(=O)(=O)c2ccccc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4877813 185953 0 None 1 2 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 444 8 1 8 3.1 CCCCc1nc(=O)c(S(=O)(=O)c2ccccc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
164627297 185979 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4878158 185979 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
154603359 171622 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 507 8 3 3 7.0 CCC[C@@H](NC(=O)c1ccc(-c2c(F)cccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4473653 171622 0 None - 1 Human 9.3 pEC50 = 9.3 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 507 8 3 3 7.0 CCC[C@@H](NC(=O)c1ccc(-c2c(F)cccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
137198133 191740 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 505 8 1 8 3.7 COc1cccc(OC)c1-n1c(COC2CCC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5206677 191740 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 505 8 1 8 3.7 COc1cccc(OC)c1-n1c(COC2CCC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
154603397 170347 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 537 8 3 3 7.8 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(C)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4454971 170347 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 537 8 3 3 7.8 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3cc(C)ccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
118734778 118216 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL 1541 45 20 19 -3.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C/C=C/c1ccccc1)C(=O)O 10.1021/jm501916k
CHEMBL3417386 118216 0 None - 1 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL 1541 45 20 19 -3.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C/C=C/c1ccccc1)C(=O)O 10.1021/jm501916k
146222358 185650 0 None 7 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 538 9 2 7 5.1 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4873432 185650 0 None 7 2 Human 9.2 pEC50 = 9.2 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 538 9 2 7 5.1 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)nc3)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
11852 1062 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1c2ccccc2ccc1 10.1021/acs.jmedchem.1c01708
162679539 1062 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1c2ccccc2ccc1 10.1021/acs.jmedchem.1c01708
CHEMBL5091501 1062 2 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1c2ccccc2ccc1 10.1021/acs.jmedchem.1c01708
CHEMBL5087847 213347 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
CHEMBL3417390 209912 0 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@](C)(Cc1ccccc1)C(=O)O 10.1021/jm501916k
25078060 433 23 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None None 10.1016/j.bmc.2014.04.001
602 433 23 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None None 10.1016/j.bmc.2014.04.001
605 433 23 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None None 10.1016/j.bmc.2014.04.001
CHEMBL414173 433 23 None - 1 Human 9.1 pEC50 = 9.1 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None None 10.1016/j.bmc.2014.04.001
164612570 184819 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 497 9 2 8 4.2 COCCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4860991 184819 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 497 9 2 8 4.2 COCCc1[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
25085173 209468 25 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01448
CHEMBL3184840 209468 25 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01448
129226756 185271 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 580 12 2 9 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)Nc2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4867710 185271 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 580 12 2 9 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)Nc2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129032236 184219 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2022.128882
CHEMBL4851693 184219 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2022.128882
129032236 184219 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4851693 184219 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
164617525 184629 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1529 44 20 19 -4.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
CHEMBL4857723 184629 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1529 44 20 19 -4.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
164620186 185246 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4867453 185246 0 None - 1 Human 9.0 pEC50 = 9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL3261778 209528 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmc.2014.04.001
118734783 117995 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL 1527 42 20 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC1(C(=O)O)CCc2ccccc21 10.1021/jm501916k
CHEMBL3414601 117995 0 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL 1527 42 20 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC1(C(=O)O)CCc2ccccc21 10.1021/jm501916k
25078060 433 23 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01941
602 433 23 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01941
605 433 23 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01941
CHEMBL414173 433 23 None - 1 Human 9.0 pEC50 = 9.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL None None None None 10.1021/acs.jmedchem.0c01941
CHEMBL5078149 212765 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1Cc2cncn2C/C=C/C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
CHEMBL3417388 209910 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1csc2ccccc12)C(=O)O 10.1021/jm501916k
CHEMBL5091081 213519 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
25085173 209468 25 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm501916k
CHEMBL3184840 209468 25 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/jm501916k
164626262 186032 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cccc(-c2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4879061 186032 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cccc(-c2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
137502125 169073 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4437206 169073 0 None - 1 Human 8.9 pEC50 = 8.9 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
137197918 185768 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccncc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4875108 185768 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccncc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
164626824 185877 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4876632 185877 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
154603363 169605 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 503 8 3 3 7.2 CCC[C@@H](NC(=O)c1ccc(-c2cc(C)ccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4444538 169605 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 503 8 3 3 7.2 CCC[C@@H](NC(=O)c1ccc(-c2cc(C)ccc2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
164610921 184655 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1627 44 20 19 -2.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4858171 184655 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1627 44 20 19 -2.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL3261787 209536 0 None - 1 Human 8.8 pEC50 = 8.8 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@@H]1C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmc.2014.04.001
137198167 190664 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 548 6 1 8 4.2 COc1cccc(OC)c1-n1c(-c2ccc(C)cn2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5190307 190664 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 548 6 1 8 4.2 COc1cccc(OC)c1-n1c(-c2ccc(C)cn2)nc(=O)c(C(=O)N2CCC(c3ccc(F)cc3F)C2)c1O 10.1021/acs.jmedchem.1c01504
129032307 185340 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4869091 185340 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 476 8 2 5 4.7 CCCCc1[nH]c(=O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
102485315 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
155817444 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
16130452 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
3556 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
90488791 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
CHEMBL3234446 434 11 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL None None None None 10.1016/j.ejmech.2019.01.040
CHEMBL3261776 209526 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmc.2014.04.001
137198011 190661 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 531 8 1 7 4.5 COc1cccc(OC)c1-n1c(CCCC(F)(F)F)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5190259 190661 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 531 8 1 7 4.5 COc1cccc(OC)c1-n1c(CCCC(F)(F)F)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
137198114 191127 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 489 6 1 7 4.2 COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
CHEMBL5197115 191127 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysisAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production incubated for 60 mins by fluorescence based analysis
ChEMBL 489 6 1 7 4.2 COc1cccc(OC)c1-n1c(C2CCCC2)nc(=O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c1O 10.1021/acs.jmedchem.1c01504
162670111 181998 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2137 69 32 28 -7.9 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(=O)N1CCCC1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4787992 181998 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2137 69 32 28 -7.9 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(=O)N1CCCC1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL5092604 213605 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCN(S(=O)(=O)c2ccccc2[N+](=O)[O-])C/C=C/C[C@H](N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
164620186 185246 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4867453 185246 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
164629125 185870 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1767 49 22 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4876569 185870 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1767 49 22 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
164616329 184573 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1655 44 20 19 -1.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C(C)(C)C1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4857085 184573 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1655 44 20 19 -1.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C(C)(C)C1C(=O)O 10.1021/acs.jmedchem.0c01941
164626824 185877 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4876632 185877 0 None - 1 Human 8.0 pEC50 = 8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
156013300 176911 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 6 1 6 2.8 CCCSc1nc(=O)cc(O)n1-c1ccccc1OCC 10.1016/j.bmcl.2020.126955
CHEMBL4639234 176911 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 6 1 6 2.8 CCCSc1nc(=O)cc(O)n1-c1ccccc1OCC 10.1016/j.bmcl.2020.126955
156020074 177570 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 276 4 1 5 2.7 CCCSc1nc(=O)cc(O)n1-c1ccccc1C 10.1016/j.bmcl.2020.126955
CHEMBL4648809 177570 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 276 4 1 5 2.7 CCCSc1nc(=O)cc(O)n1-c1ccccc1C 10.1016/j.bmcl.2020.126955
129226556 190026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 585 10 2 5 6.1 O=C(C[C@H](CCN1CC2CCC1CC2)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5180988 190026 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 585 10 2 5 6.1 O=C(C[C@H](CCN1CC2CCC1CC2)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
164609058 183820 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1C[C@@H](OCc2ccccc2)C[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4845895 183820 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1C[C@@H](OCc2ccccc2)C[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
129226760 185070 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 552 12 1 8 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)OC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4864641 185070 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 552 12 1 8 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)OC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226902 177493 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 564 12 2 6 6.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCCC1 10.1016/j.bmc.2019.115237
CHEMBL4647391 177493 0 None - 1 Human 7.0 pEC50 = 7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 564 12 2 6 6.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCCC1 10.1016/j.bmc.2019.115237
129226887 190737 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 570 10 2 4 6.6 O=C(C[C@H](CCc1ccc(F)cc1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5191542 190737 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 570 10 2 4 6.6 O=C(C[C@H](CCc1ccc(F)cc1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
162660992 181269 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1212 31 13 14 -0.2 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
CHEMBL4778604 181269 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1212 31 13 14 -0.2 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1cccc2ccccc12)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
129226279 184153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 565 12 1 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)N(C)C2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4850694 184153 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 565 12 1 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)N(C)C2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
164619379 185390 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cccc(OCc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4869716 185390 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cccc(OCc2ccccc2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
129226903 177319 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 524 13 2 6 5.5 CCCn1nc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)cc1-c1c(OC)cccc1OC 10.1016/j.bmc.2019.115237
CHEMBL4644803 177319 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 524 13 2 6 5.5 CCCn1nc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)cc1-c1c(OC)cccc1OC 10.1016/j.bmc.2019.115237
164617525 184629 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1529 44 20 19 -4.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
CHEMBL4857723 184629 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1529 44 20 19 -4.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
137223238 177370 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 304 6 1 6 2.3 CCCCc1nc(=O)cc(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4645657 177370 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 304 6 1 6 2.3 CCCCc1nc(=O)cc(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2020.126955
129226414 191614 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 595 10 2 5 6.0 O=C(C[C@H](CCN1CCCC(F)(F)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5204722 191614 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 595 10 2 5 6.0 O=C(C[C@H](CCN1CCCC(F)(F)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
164620982 185277 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1616 44 21 19 -3.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)O)C1=O 10.1021/acs.jmedchem.0c01941
CHEMBL4867913 185277 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1616 44 21 19 -3.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)O)C1=O 10.1021/acs.jmedchem.0c01941
164627297 185979 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4878158 185979 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
164627340 186039 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4879304 186039 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
137106246 184269 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 479 7 2 7 4.9 COc1cccc(OC)c1-c1c(C2CC2)[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c1O 10.1021/acs.jmedchem.0c01878
CHEMBL4852391 184269 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 479 7 2 7 4.9 COc1cccc(OC)c1-c1c(C2CC2)[nH]c(=O)c(-c2nnc(Cc3ccc(Cl)cc3)o2)c1O 10.1021/acs.jmedchem.0c01878
155514812 169334 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2437 85 32 27 -0.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL4440817 169334 0 None - 1 Human 8.0 pEC50 = 8.0 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2437 85 32 27 -0.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL5091081 213519 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
164617222 183984 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 436 9 3 5 4.0 CCCCc1[nH]c(=O)c(C(=O)NCc2ccccc2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4848469 183984 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 436 9 3 5 4.0 CCCCc1[nH]c(=O)c(C(=O)NCc2ccccc2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
164616916 184427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 374 7 2 5 2.8 CCCCc1[nH]c(=O)c(C(=O)N(C)C)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4854830 184427 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 374 7 2 5 2.8 CCCCc1[nH]c(=O)c(C(=O)N(C)C)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
164617160 184854 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1667 46 21 20 -1.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4861483 184854 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1667 46 21 20 -1.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
164619966 184944 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1641 44 20 19 -1.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C(C)C1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4862772 184944 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1641 44 20 19 -1.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C(C)C1C(=O)O 10.1021/acs.jmedchem.0c01941
118568981 177535 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 556 15 3 7 5.0 CCC(O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4647996 177535 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 556 15 3 7 5.0 CCC(O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
129226761 185135 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 555 14 2 8 3.8 COCCNC(=O)C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(C2CCCC2)n1 10.1021/acs.jmedchem.0c01448
CHEMBL4865671 185135 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 555 14 2 8 3.8 COCCNC(=O)C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(C2CCCC2)n1 10.1021/acs.jmedchem.0c01448
129226756 185271 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 580 12 2 9 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)Nc2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4867710 185271 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 580 12 2 9 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)Nc2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
139576623 190665 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 459 8 2 5 5.6 CCCCc1nc(O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5190325 190665 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 459 8 2 5 5.6 CCCCc1nc(O)c(C(=O)N2CC[C@@H](c3ccccc3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
129032132 183795 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 11 2 5 5.2 CCCCc1[nH]c(=O)c(C(=O)N(CCC)Cc2ccccc2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4845664 183795 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 11 2 5 5.2 CCCCc1[nH]c(=O)c(C(=O)N(CCC)Cc2ccccc2)c(O)c1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
168290844 191367 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 567 9 2 5 5.2 O=C(C[C@@H](CN1CCC(F)(F)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5201002 191367 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 567 9 2 5 5.2 O=C(C[C@@H](CN1CCC(F)(F)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
137646730 157249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL 1447 35 20 18 -4.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
CHEMBL4083079 157249 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL 1447 35 20 18 -4.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
118568757 177420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 518 12 2 6 4.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCc2ccccc2)C(=O)NC2CCC2)nn1CC(C)C 10.1016/j.bmc.2019.115237
CHEMBL4646232 177420 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 518 12 2 6 4.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCc2ccccc2)C(=O)NC2CCC2)nn1CC(C)C 10.1016/j.bmc.2019.115237
162670561 182266 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1176 32 13 14 -1.0 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCc1ccccc1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
CHEMBL4791473 182266 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1176 32 13 14 -1.0 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCc1ccccc1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
137204225 176556 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 424 9 1 7 3.9 CCCCc1nc(=O)c(Cc2ccc(OC)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4633783 176556 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 424 9 1 7 3.9 CCCCc1nc(=O)c(Cc2ccc(OC)cc2)c(O)n1-c1c(OC)cccc1OC 10.1016/j.bmcl.2020.126955
139557802 190043 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 494 7 2 6 4.9 CCN(c1ccccc1)c1c(CC2CC2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
CHEMBL5181275 190043 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 494 7 2 6 4.9 CCN(c1ccccc1)c1c(CC2CC2)nc(O)c(C(=O)N2CCC(c3ncc(F)cc3F)C2)c1O 10.1016/j.bmcl.2022.128882
142754030 191757 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 459 8 2 5 5.6 CCCCc1nc(O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5207156 191757 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 459 8 2 5 5.6 CCCCc1nc(O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
137106275 184668 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 461 9 2 7 4.7 CCCCc1[nH]c(=O)c(-c2nnc(Cc3ccccc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4858384 184668 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 461 9 2 7 4.7 CCCCc1[nH]c(=O)c(-c2nnc(Cc3ccccc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
129204846 185830 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 521 11 2 8 4.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)Cc2nnc[nH]2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4876051 185830 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 521 11 2 8 4.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)Cc2nnc[nH]2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226364 187965 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 553 12 2 8 3.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCOCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4863277 187965 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 553 12 2 8 3.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCOCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028640 187965 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 553 12 2 8 3.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCOCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
118568534 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assayAgonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4875417 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assayAgonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028970 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assayAgonist activity at Galphaq16-fused human APJ receptor expressed in CHO cells assessed as stimulation of Ca2+ mobilization incubated for 1 hr by Calcium 5-dye based fluorescence based assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
118568534 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
CHEMBL4875417 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
CHEMBL5028970 188015 0 None -13 2 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
129226849 187955 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 486 13 2 7 4.0 CCN(CC)CC[C@@H](CC(=O)O)NC(=O)c1cc(-c2c(OC)cccc2OC)n(C2CCCC2)n1 10.1021/acs.jmedchem.0c01448
CHEMBL4869477 187955 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 486 13 2 7 4.0 CCN(CC)CC[C@@H](CC(=O)O)NC(=O)c1cc(-c2c(OC)cccc2OC)n(C2CCCC2)n1 10.1021/acs.jmedchem.0c01448
CHEMBL5028561 187955 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 486 13 2 7 4.0 CCN(CC)CC[C@@H](CC(=O)O)NC(=O)c1cc(-c2c(OC)cccc2OC)n(C2CCCC2)n1 10.1021/acs.jmedchem.0c01448
CHEMBL5072626 212514 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCNC/C=C/C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
CHEMBL3261777 209527 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CC(=O)N[C@@H](C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmc.2014.04.001
129226384 184223 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 594 12 1 9 5.2 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)N(C)c2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4851755 184223 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 594 12 1 9 5.2 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)N(C)c2nccs2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226423 189324 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 587 11 2 5 6.5 CN(CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C1CCCCC1 10.1016/j.bmc.2022.116789
CHEMBL5169875 189324 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 587 11 2 5 6.5 CN(CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C1CCCCC1 10.1016/j.bmc.2022.116789
164627297 185979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4878158 185979 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1621 47 20 20 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
156016218 177158 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 290 5 1 5 3.0 CCCSc1nc(=O)cc(O)n1-c1ccccc1CC 10.1016/j.bmcl.2020.126955
CHEMBL4642418 177158 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 290 5 1 5 3.0 CCCSc1nc(=O)cc(O)n1-c1ccccc1CC 10.1016/j.bmcl.2020.126955
129226318 191721 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 533 11 2 5 5.8 CC(C)c1ccccc1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
CHEMBL5206392 191721 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 533 11 2 5 5.8 CC(C)c1ccccc1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
156015988 176957 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 5 1 6 2.8 CCCSc1nc(=O)c(C)c(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4640095 176957 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 5 1 6 2.8 CCCSc1nc(=O)c(C)c(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
164611267 184398 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1757 49 20 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(OCc2ccccc2)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4854245 184398 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1757 49 20 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(OCc2ccccc2)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
162667712 181947 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1162 31 13 14 -1.4 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C)[C@@H](C)CC 10.1021/acs.jmedchem.0c01547
CHEMBL4787249 181947 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1162 31 13 14 -1.4 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C)[C@@H](C)CC 10.1021/acs.jmedchem.0c01547
164610312 184564 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1577 44 20 19 -3.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4856918 184564 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1577 44 20 19 -3.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
164624300 185462 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1-c1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4870831 185462 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccccc1-c1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
129226281 184868 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 565 12 2 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2(C)CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4861663 184868 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 565 12 2 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2(C)CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5079665 212861 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
118568985 177520 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 554 15 2 7 5.2 CCC(=O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4647853 177520 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 554 15 2 7 5.2 CCC(=O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
129226474 177517 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 443 10 2 6 4.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)O)nn1C 10.1016/j.bmc.2019.115237
CHEMBL4647813 177517 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 443 10 2 6 4.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)O)nn1C 10.1016/j.bmc.2019.115237
129226887 190737 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 570 10 2 4 6.6 O=C(C[C@H](CCc1ccc(F)cc1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5191542 190737 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 570 10 2 4 6.6 O=C(C[C@H](CCc1ccc(F)cc1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
164610921 184655 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1627 44 20 19 -2.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4858171 184655 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1627 44 20 19 -2.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N1Cc2ccccc2C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
129226902 177493 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 564 12 2 6 6.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCCC1 10.1016/j.bmc.2019.115237
CHEMBL4647391 177493 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 564 12 2 6 6.6 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCCC1 10.1016/j.bmc.2019.115237
129226437 189385 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 573 9 3 5 5.3 O=C(C[C@@H](NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C(=O)NC1CCCCC1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5170879 189385 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 573 9 3 5 5.3 O=C(C[C@@H](NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C(=O)NC1CCCCC1)NC1CCC1 10.1016/j.bmc.2022.116789
162666490 181811 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1212 31 13 14 -0.2 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
CHEMBL4785339 181811 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1212 31 13 14 -0.2 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc2ccccc2c1)C(=O)N1CCC[C@H]1C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
162662912 181380 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1318 37 14 15 1.0 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
CHEMBL4780010 181380 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1318 37 14 15 1.0 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)C(=O)O)C(C)C 10.1021/acs.jmedchem.0c01547
156016005 177030 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 340 4 1 5 3.2 CCCSc1nc(=O)cc(O)n1-c1ccccc1Br 10.1016/j.bmcl.2020.126955
CHEMBL4640808 177030 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 340 4 1 5 3.2 CCCSc1nc(=O)cc(O)n1-c1ccccc1Br 10.1016/j.bmcl.2020.126955
CHEMBL5092962 213622 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCN(C)C/C=C/C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
129226536 190983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 570 10 2 6 5.7 Cc1cc(C)n(CC[C@@H](CC(=O)NC2CCC2)NC(=O)c2cc(-c3ccccc3C(F)(F)F)n(C3CCCC3)n2)n1 10.1016/j.bmc.2022.116789
CHEMBL5195107 190983 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 570 10 2 6 5.7 Cc1cc(C)n(CC[C@@H](CC(=O)NC2CCC2)NC(=O)c2cc(-c3ccccc3C(F)(F)F)n(C3CCCC3)n2)n1 10.1016/j.bmc.2022.116789
118568652 177032 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 556 15 3 7 5.0 CC[C@@H](O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4640815 177032 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 556 15 3 7 5.0 CC[C@@H](O)CNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
129226508 184643 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 587 12 2 7 5.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CC(F)(F)C2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4857978 184643 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 587 12 2 7 5.0 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CC(F)(F)C2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226380 187943 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 565 12 2 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4849104 187943 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 565 12 2 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028491 187943 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 565 12 2 7 5.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
139557852 191169 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 556 9 2 6 6.3 CCCCc1nc(O)c(C(=O)N2CCN(Cc3cccc(Cl)c3Cl)CC2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
CHEMBL5197766 191169 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 556 9 2 6 6.3 CCCCc1nc(O)c(C(=O)N2CCN(Cc3cccc(Cl)c3Cl)CC2)c(O)c1N(CC)c1ccccc1 10.1016/j.bmcl.2022.128882
164617160 184854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1667 46 21 20 -1.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4861483 184854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1667 46 21 20 -1.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
162647219 179141 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2624 85 33 32 -3.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4744024 179141 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2624 85 33 32 -3.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
156013739 176690 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 292 5 1 6 2.4 CCCSc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4636169 176690 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 292 5 1 6 2.4 CCCSc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
156013043 176912 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 280 4 1 5 2.6 CCCSc1nc(=O)cc(O)n1-c1ccccc1F 10.1016/j.bmcl.2020.126955
CHEMBL4639331 176912 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 280 4 1 5 2.6 CCCSc1nc(=O)cc(O)n1-c1ccccc1F 10.1016/j.bmcl.2020.126955
CHEMBL5074959 212571 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)C/C=C\C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccc(OCc3ccccc3)cc2)C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.1c01708
118568534 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
CHEMBL4875417 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
CHEMBL5028970 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1016/j.bmc.2022.116789
118568534 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4875417 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028970 188015 0 None -13 2 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 551 12 2 7 4.7 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226549 191583 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 573 10 2 6 4.6 O=C(C[C@H](CCN1CC2(COC2)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5204090 191583 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 573 10 2 6 4.6 O=C(C[C@H](CCN1CC2(COC2)C1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
118568960 177077 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 534 14 2 7 4.1 CCC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4641474 177077 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 534 14 2 7 4.1 CCC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
129226780 191694 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 525 10 2 5 5.4 O=C(C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2ccccc2Cl)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5206038 191694 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 525 10 2 5 5.4 O=C(C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2ccccc2Cl)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
129226379 187961 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 537 12 2 7 4.3 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4873660 187961 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 537 12 2 7 4.3 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028617 187961 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 537 12 2 7 4.3 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCC2)CC(=O)NC2CCC2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226792 190784 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 575 9 3 6 4.1 O=C(C[C@@H](NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C(=O)NC1CCOCC1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5192313 190784 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 575 9 3 6 4.1 O=C(C[C@@H](NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C(=O)NC1CCOCC1)NC1CCC1 10.1016/j.bmc.2022.116789
146222314 185172 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 537 9 2 6 5.7 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
CHEMBL4866318 185172 0 None 1 2 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assayAgonist activity at human APJ receptor assessed as effect on cAMP accumulation by cAMP-Glo assay
ChEMBL 537 9 2 6 5.7 CCCCc1[nH]c(=O)c(S(=O)(=O)c2ccc(-c3ccc(F)cc3)cc2)c(O)c1-c1c(OC)cccc1OC 10.1016/j.bmcl.2021.128325
164623151 184990 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4863381 184990 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CC[C@H](c2ccccc2)[C@@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
164626895 185996 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1604 47 22 19 -3.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4878369 185996 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1604 47 22 19 -3.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
156014239 176605 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 348 8 1 6 3.8 CCCCc1c(O)n(-c2ccccc2OC)c(SCCC)nc1=O 10.1016/j.bmcl.2020.126955
CHEMBL4634841 176605 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 348 8 1 6 3.8 CCCCc1c(O)n(-c2ccccc2OC)c(SCCC)nc1=O 10.1016/j.bmcl.2020.126955
118569021 177382 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 542 15 2 7 4.8 COCCNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4645790 177382 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 542 15 2 7 4.8 COCCNC(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
155514255 169273 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 1768 54 25 22 -5.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL4439951 169273 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 1768 54 25 22 -5.5 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](N)CCCNC(=N)N)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
129204911 189343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 575 11 3 6 4.0 O=C(C[C@H](CCNC(=O)C1COC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5170198 189343 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assayAgonist activity at human APJ receptor expressed in CHO cells co-expressing Galphaq16 assessed as stimulation of Ca2+ mobilization measured at 1 sec interval for 90 sec by fluorescent Calcium 5-dye based FLIPR-calcium mobilization assay
ChEMBL 575 11 3 6 4.0 O=C(C[C@H](CCNC(=O)C1COC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
164629125 185870 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1767 49 22 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4876569 185870 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1767 49 22 20 0.3 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)N[C@H](Cc1cc(C2CCCC2)c(O)c(C2CCCC2)c1)C(=O)O 10.1021/acs.jmedchem.0c01941
25085173 209468 25 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human APJ receptor stably expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01878
CHEMBL3184840 209468 25 None - 1 Human 7.8 pEC50 = 7.8 Functional
Agonist activity at human APJ receptor stably expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human APJ receptor stably expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01878
164626635 185974 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 481 8 2 7 5.5 CCCCc1[nH]c(=O)c(-c2nnc(-c3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4878068 185974 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 481 8 2 7 5.5 CCCCc1[nH]c(=O)c(-c2nnc(-c3ccc(Cl)cc3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
129226850 184395 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 579 13 3 10 2.9 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NCc2nnn[nH]2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4854216 184395 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assayAgonist activity at human AGTRL1 expressed in CHO-K1 cells assessed as induction of beta-arrestin 2 recruitment incubated for 90 mins by PathHunter assay
ChEMBL 579 13 3 10 2.9 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NCc2nnn[nH]2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226376 187903 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 512 11 2 7 4.5 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4856959 187903 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 512 11 2 7 4.5 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028199 187903 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 512 11 2 7 4.5 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
118568772 177161 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 570 14 1 8 4.7 COC(=O)CN(C)C(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4642445 177161 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assayAgonist activity at human APJ receptor stably expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by Eu-cAMP tracer based TR-FRET assay
ChEMBL 570 14 1 8 4.7 COC(=O)CN(C)C(=O)C[C@H](CCC1CCCCC1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
118568535 177609 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 542 14 3 7 4.3 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NCC(=O)O)nn1CC(C)C 10.1016/j.bmc.2019.115237
CHEMBL4649282 177609 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 542 14 3 7 4.3 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCC2CCCCC2)CC(=O)NCC(=O)O)nn1CC(C)C 10.1016/j.bmc.2019.115237
CHEMBL5089609 213441 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL None None None CC(C)C[C@@H]1NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)C/C=C\C[C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2CCC[C@H]2C(=O)N[C@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@H](CO)NC1=O 10.1021/acs.jmedchem.1c01708
CHEMBL3261767 209521 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCC(N)=O)C(N)=O 10.1016/j.bmc.2014.04.001
CHEMBL5094438 213718 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCN(S(=O)(=O)c2ccccc2[N+](=O)[O-])C/C=C/C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
164626824 185877 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4876632 185877 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1605 46 20 19 -3.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
164627340 186039 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4879304 186039 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
154603343 170758 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 524 8 3 4 6.9 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3ccncc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4461195 170758 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 524 8 3 4 6.9 CCC[C@@H](NC(=O)c1ccc(-c2cc(Cl)ccc2-c2nc3ccncc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
164624998 185142 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1571 44 19 20 -4.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1C[C@@H](OCc2ccccc2)C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4865796 185142 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293 cells co-expressing Rlucll-beta-arrestin2 assessed as induction of beta-arrestin2 recruitment to receptor incubated for 30 mins by BRET assay
ChEMBL 1571 44 19 20 -4.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1C[C@@H](OCc2ccccc2)C[C@@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
129226755 184715 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 578 13 2 9 4.4 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NCc2ncco2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4859298 184715 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 578 13 2 9 4.4 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)NCc2ncco2)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
162671786 182259 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1093 32 13 13 -0.6 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(=O)O)Cc1ccccc1)C(C)C 10.1021/acs.jmedchem.0c01547
CHEMBL4791398 182259 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll assessed as induction of Galpha12 effector (PDZ-RhoGEF) to the cell membrane incubated for 5 mins by BRET assay
ChEMBL 1093 32 13 13 -0.6 CCCC[C@H](N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)N[C@H](CCC(=O)O)Cc1ccccc1)C(C)C 10.1021/acs.jmedchem.0c01547
118715457 114243 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1692 54 21 19 2.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2014.08.045
CHEMBL3338680 114243 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1692 54 21 19 2.4 CCCCCCCCCCCCCCCC(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O 10.1016/j.bmcl.2014.08.045
CHEMBL5080649 212925 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assayAgonist activity at human APJ expressed in HEK293 cells assessed as recruitment of beta-arrestin2 to receptor by BRET-based beta-arrestin2 assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCC[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
156010717 176481 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 288 5 1 5 2.6 CCCCc1nc(=O)cc(O)n1-c1c(C)cccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4632688 176481 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 288 5 1 5 2.6 CCCCc1nc(=O)cc(O)n1-c1c(C)cccc1OC 10.1016/j.bmcl.2020.126955
129226423 189324 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 587 11 2 5 6.5 CN(CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C1CCCCC1 10.1016/j.bmc.2022.116789
CHEMBL5169875 189324 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 587 11 2 5 6.5 CN(CC[C@@H](CC(=O)NC1CCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)C1CCCCC1 10.1016/j.bmc.2022.116789
25085173 209468 25 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2019.115237
CHEMBL3184840 209468 25 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1016/j.bmc.2019.115237
164614785 184820 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4860998 184820 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL3261789 209538 0 None - 1 Human 8.7 pEC50 = 8.7 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(C)=O)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmc.2014.04.001
CHEMBL3417380 209904 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1cccnc1)C(=O)O 10.1021/jm501916k
162644859 178877 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2213 70 32 27 -6.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@](C)(CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4740668 178877 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2213 70 32 27 -6.0 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@](C)(CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CCCCN)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
162674008 182630 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 1533 44 20 20 -5.0 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)C1CCC(=O)N1)C(=O)N1CCCC1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4795982 182630 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 1533 44 20 20 -5.0 CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)C1CCC(=O)N1)C(=O)N1CCCC1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01395
11853 1075 2 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1ccc2ccccc2c1 10.1021/acs.jmedchem.1c01708
162679361 1075 2 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1ccc2ccccc2c1 10.1021/acs.jmedchem.1c01708
CHEMBL5085866 1075 2 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL 1020 21 14 13 -2.4 N[C@@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](C/C=C\C1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](C(=O)O)Cc1ccc2ccccc2c1 10.1021/acs.jmedchem.1c01708
129226783 191347 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 559 10 2 5 5.7 O=C(C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
CHEMBL5200689 191347 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by TR-FRET based LANCE cAMP assay
ChEMBL 559 10 2 5 5.7 O=C(C[C@H](CCN1CCCCC1)NC(=O)c1cc(-c2ccccc2C(F)(F)F)n(C2CCCC2)n1)NC1CCC1 10.1016/j.bmc.2022.116789
164617113 184748 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1543 44 20 19 -3.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
CHEMBL4859698 184748 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1543 44 20 19 -3.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)C(C)(C)c1ccccc1 10.1021/acs.jmedchem.0c01941
155536031 171549 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2756 94 33 35 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL4472749 171549 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2756 94 33 35 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
164609874 184645 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4858007 184645 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1527 41 19 19 -4.4 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N1Cc2ccccc2C[C@H]1C(=O)O 10.1021/acs.jmedchem.0c01941
164620982 185277 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1616 44 21 19 -3.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)O)C1=O 10.1021/acs.jmedchem.0c01941
CHEMBL4867913 185277 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1616 44 21 19 -3.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H]1Cc2c([nH]c3ccccc23)CN([C@H](Cc2ccccc2)C(=O)O)C1=O 10.1021/acs.jmedchem.0c01941
162670284 182111 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2800 97 33 36 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4789383 182111 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2800 97 33 36 -3.2 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCNC(=O)OCC1c2ccccc2-c2ccccc21)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
155550782 173727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2423 85 33 27 -1.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL4550078 173727 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assayActivation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay
ChEMBL 2423 85 33 27 -1.1 CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCCC)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1016/j.ejmech.2019.01.040
CHEMBL5092962 213622 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as dissociation of G alphai1 from the G beta gamma subunit by BRET-based G protein dissociation assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCN(C)C/C=C/C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
137106142 184883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 495 9 2 7 5.4 CCCCc1[nH]c(=O)c(-c2nnc(Cc3cccc(Cl)c3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
CHEMBL4861906 184883 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assayAgonist activity at human APJ receptor expressed in human HEK293 cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 1 hr by TR-FRET assay
ChEMBL 495 9 2 7 5.4 CCCCc1[nH]c(=O)c(-c2nnc(Cc3cccc(Cl)c3)o2)c(O)c1-c1c(OC)cccc1OC 10.1021/acs.jmedchem.0c01878
118715466 114247 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1628 53 20 18 2.1 CCCCCCCCCCCCCCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2014.08.045
CHEMBL3338689 114247 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1628 53 20 18 2.1 CCCCCCCCCCCCCCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2014.08.045
CHEMBL3417382 209906 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](C(=O)O)c1ccccc1 10.1021/jm501916k
137197918 185768 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccncc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
CHEMBL4875108 185768 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assayAgonist activity at human APJ receptor expressed in HEK293T cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins by HTRF assay
ChEMBL 478 8 1 8 3.3 CCCCc1nc(=O)c(C(=O)N2CCC(c3ccncc3)C2)c(O)n1-c1c(OC)cccc1OC 10.1021/acsmedchemlett.1c00385
164618998 185483 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4871150 185483 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing Galphai1 RlucII assessed as dissociation of Galphai1 from Gbetta/gamma subunit measured using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1635 47 20 20 -2.6 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@](C)(Cc1ccc(OCc2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
155516838 169540 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 576 10 3 5 6.2 COC[C@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4443604 169540 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 576 10 3 5 6.2 COC[C@H](NC(=O)c1ccc(-c2cc(Cl)ccc2C(=O)Nc2ccc(OC)c(F)c2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
164613492 184454 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1705 49 21 19 -1.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4855178 184454 0 None - 1 Human 8.6 pEC50 = 8.6 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1705 49 21 19 -1.1 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N[C@H](Cc1cccc2ccccc12)C(=O)NC(Cc1ccccc1)(Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.0c01941
162643410 181066 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2578 94 33 35 -6.8 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCN)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL4775988 181066 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Activation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assayActivation of APJ receptor (unknown origin) expressed in Chem-5 cells assessed as stimulation of Ca2+ mobilization by Calcium 6-GF dye based fluorescence based assay
ChEMBL 2578 94 33 35 -6.8 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCCN)NC(=O)CCOCCOCCOCCOCCOCCOCCOCCN)C(=O)NC(C)(C)C(=O)N[C@@H](Cc1ccc(Br)cc1)C(=O)O 10.1021/acs.jmedchem.0c01395
CHEMBL3417375 209899 0 None - 1 Human 8.5 pEC50 = 8.5 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as inhibition of forskolin-induced intracellular cAMP production incubated for 30 mins by TR-FRET assay
ChEMBL None None None CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)O 10.1021/jm501916k
CHEMBL3261766 209520 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilizationAgonist activity at APJ receptor (unknown origin) expressed in CHO cells co-expressing with Calphaq16 assessed as calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CCC(N)=O)C(=O)N1CCC[C@H]1C(N)=O 10.1016/j.bmc.2014.04.001
156016414 177082 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 6 1 6 2.8 CCCCSc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4641511 177082 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 306 6 1 6 2.8 CCCCSc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
139557818 189488 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 457 6 2 5 5.2 CCCCc1nc(O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1N1CCc2ccccc21 10.1016/j.bmcl.2022.128882
CHEMBL5172676 189488 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assayAgonist activity at human APJ receptor expressed in HEK293 cells assessed as compound stimulated inhibition of forskolin stimulated cAMP production incubated for 30 mins and measured by fluorescence based assay
ChEMBL 457 6 2 5 5.2 CCCCc1nc(O)c(C(=O)N2CC[C@H](c3ccccc3)C2)c(O)c1N1CCc2ccccc21 10.1016/j.bmcl.2022.128882
164614785 184820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
CHEMBL4860998 184820 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assayAgonist activity at human APJ receptor expressed in HEK293T cells co-expressing PDZ-Rho-Gef-RLucll and rGFP-CAAX assessed as induction of recruitment of Galpha12 to cell membrane using coelenterazine luciferase substrate incubated for 5 mins by BRET assay
ChEMBL 1591 45 20 19 -2.9 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1cnc[nH]1)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]1CCC(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@H](Cc1ccc(-c2ccccc2)cc1)C(=O)O 10.1021/acs.jmedchem.0c01941
118568750 177486 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 536 13 2 8 3.2 COC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
CHEMBL4647332 177486 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assayAgonist activity at human APJ receptor stably expressed in CHO cells co-expressing Galphaq16 assessed as increase in intracellular calcium mobilization measured at 1 sec intervals for 90 secs by calcium 5 dye based FLIPR assay
ChEMBL 536 13 2 8 3.2 COC(=O)CNC(=O)[C@H](CCc1ccccc1)NC(=O)c1cc(-c2c(OC)cccc2OC)n(CC(C)C)n1 10.1016/j.bmc.2019.115237
118715463 114245 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1690 54 20 18 3.7 CCCCCCCCCCCCCCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2014.08.045
CHEMBL3338686 114245 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assayAgonist activity at APJ receptor in HEK293 cells assessed as inhibition of forskolin-induced cAMP level incubated for 5 mins prior to forskolin challenge measured after 30 mins by TR-FRET assay
ChEMBL 1690 54 20 18 3.7 CCCCCCCCCCCCCCCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O)[C@@H](C)O)[C@@H](C)O)C(C)C 10.1016/j.bmcl.2014.08.045
155558340 174192 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
CHEMBL4561041 174192 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assayAgonist activity at human APJ-R expressed in HEK293 cells assessed as inhibition of forskolin- stimulated cAMP accumulation incubated for 30 mins by HTRF assay
ChEMBL 523 8 3 3 7.5 CCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2-c2nc3ccccc3[nH]2)c(C(=O)O)c1)c1ccccc1 10.1021/acs.jmedchem.9b01513
118568866 187900 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 498 11 2 7 4.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4852570 187900 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 498 11 2 7 4.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028185 187900 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 498 11 2 7 4.1 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2CCCCC2)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
129226284 187917 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 526 11 2 7 4.9 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2C(C)CCCC2C)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL4858793 187917 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 526 11 2 7 4.9 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2C(C)CCCC2C)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
CHEMBL5028276 187917 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
Agonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assayAgonist activity at human APJ receptor expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation measured after 40 mins by TR-FRET assay
ChEMBL 526 11 2 7 4.9 COc1cccc(OC)c1-c1cc(C(=O)N[C@@H](CCN2C(C)CCCC2C)CC(=O)O)nn1C1CCCC1 10.1021/acs.jmedchem.0c01448
137646730 157249 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL 1447 35 20 18 -4.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
CHEMBL4083079 157249 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assayAgonist activity at human APJ expressed in HEK293 cell membrane assessed as recruitment of PDZ-RhoGEF Galpha12 to cell membrane by BRET-based G protein dissociation assay
ChEMBL 1447 35 20 18 -4.7 CCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)CNC(=O)[C@H](CCCCN)NC(=O)[C@@H]1C/C=C\C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCC(=O)N2)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccccc1)C(=O)O 10.1021/acs.jmedchem.1c01708
156011345 176744 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 274 5 1 5 2.3 CCCCc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
CHEMBL4637001 176744 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
Agonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP productionAgonist activity at human APJ expressed in HEK293 cells assessed as inhibition of forskolin-stimulated cAMP production
ChEMBL 274 5 1 5 2.3 CCCCc1nc(=O)cc(O)n1-c1ccccc1OC 10.1016/j.bmcl.2020.126955
164611267 184398 0 None - 1 Human 7.7 pEC50 = 7.7