Ligand source activities (1 row/activity)





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

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
AssayType

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

10169886 182329 33 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assayAntagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assay
ChEMBL 872 26 14 12 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C)C(=O)O 10.1021/acs.jmedchem.9b01780
CHEMBL4578721 182329 33 None - 1 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assayAntagonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells by cAMP accumulation based assay
ChEMBL 872 26 14 12 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)CC(=O)O)C(C)C)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@H](C)C(=O)O 10.1021/acs.jmedchem.9b01780
5579 7317 49 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation
ChEMBL 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 10.1021/acs.jmedchem.9b01780
9851724 7317 49 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation
ChEMBL 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 10.1021/acs.jmedchem.9b01780
CHEMBL4303593 7317 49 None 2 2 Human 7.7 pIC50 = 7.7 Functional
Agonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulationAgonist activity at N-terminal c-Myc tagged human MasR expressed in HEK293T cells assessed as reduction in forskolin-induced cAMP accumulation
ChEMBL 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 10.1021/acs.jmedchem.9b01780
155817498 9244 0 None - 1 Rat 4.4 pEC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16336942
7038 9244 0 None - 1 Rat 4.4 pEC50 = 4.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 16336942
155817499 7675 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18854305
155817499 7675 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20479330
7040 7675 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18854305
7040 7675 0 None - 1 Human 6.0 pEC50 = 6 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20479330
155817500 7674 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18854305
155817500 7674 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20479330
7041 7674 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 18854305
7041 7674 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 20479330
7039 7242 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 555 8 0 8 3.4 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-] 22003054
89560738 7242 0 None -1 2 Rat 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 555 8 0 8 3.4 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-] 22003054
7039 7242 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 555 8 0 8 3.4 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-] 22003054
89560738 7242 0 None 1 2 Human 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 555 8 0 8 3.4 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccccn1)[N+](=O)[O-] 22003054
123797 9567 25 None -10 3 Mouse 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11551509
1479 9567 25 None -10 3 Mouse 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11551509
CHEMBL429731 9567 25 None -10 3 Mouse 6.4 pEC50 = 6.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 11551509
11279 7241 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 8 0 7 4.1 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccc(cc1)F)[N+](=O)[O-] 29928987
154733032 7241 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 572 8 0 7 4.1 COc1cc(ccc1S(=O)(=O)N1CC(C(C1)c1cccc(c1)F)CN1CCN(CC1)c1ccc(cc1)F)[N+](=O)[O-] 29928987
11280 7244 0 None - 1 Human 8.0 pEC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 480 3 0 2 6.2 Fc1cccc(c1C(=O)N1CC2(c3c1ccc(c3)C(C)(C)C)CCN(CC2)CCC(F)(F)F)F 29928987
15983171 7244 0 None - 1 Human 8.0 pEC50 = 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 480 3 0 2 6.2 Fc1cccc(c1C(=O)N1CC2(c3c1ccc(c3)C(C)(C)C)CCN(CC2)CCC(F)(F)F)F 29928987
59004159 7243 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 0 2 5.2 C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F 22003054
7042 7243 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 0 2 5.2 C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F 22003054
7043 7245 0 None -1 2 Rat 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22003054
59004159 7243 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 0 2 5.2 C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F 22003054
7042 7243 0 None 1 2 Human 6.7 pIC50 = 6.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 416 4 0 2 5.2 C=CCCN1CCC2(CC1)CN(c1c2cc(Cl)cc1)C(=O)c1c(F)cccc1F 22003054
7043 7245 0 None 1 2 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 22003054
5579 7317 49 None -2 2 Mouse 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 15326087
9851724 7317 49 None -2 2 Mouse 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 15326087
CHEMBL4303593 7317 49 None -2 2 Mouse 7.3 pIC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 580 11 2 8 5.4 CCNC(=O)NS(=O)(=O)c1sc(cc1c1ccc(cc1)Cn1c(nc(c1C=O)OC)c1ccccc1)CC(C)C 15326087
123805 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
46878481 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
5578 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
582 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
CHEMBL3545347 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
DB11720 7205 0 None 35 2 Mouse 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
6081 8093 0 None - 1 Mouse 9.5 pIC50 = 9.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity
Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

123805 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
46878481 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
5578 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
582 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
CHEMBL3545347 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
DB11720 7205 0 None - 1 Mouse 9.1 pKd = 9.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 12829792
123805 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
46878481 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
5578 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
582 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
CHEMBL3545347 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
DB11720 7205 0 None - 1 Mouse 7.3 pKi = 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420
6081 8093 0 None - 1 Mouse 8.3 pKi = 8.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 21670420