Ligand source activities (1 row/activity)



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

 Species

 Assay
Type

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
44433913 88739 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL236037 88739 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433903 88799 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 827 25 10 9 1.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL236292 88799 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 827 25 10 9 1.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433904 88800 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 837 25 10 8 1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL236293 88800 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 837 25 10 8 1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433916 90296 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 777 25 10 10 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL238396 90296 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 777 25 10 10 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433914 97180 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 789 25 10 10 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL267729 97180 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 789 25 10 10 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433917 146600 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 792 25 10 10 0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL392253 146600 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 792 25 10 10 0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433905 153767 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 842 25 10 9 2.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL398128 153767 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 842 25 10 9 2.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433912 161900 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL414319 161900 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
137638214 156918 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 435 11 4 6 0.9 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4071278 156918 None 0 Human Functional pEC50 = 7 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 435 11 4 6 0.9 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL235440 212031 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL238015 212848 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(N)=O 10.1016/j.bmcl.2007.08.026
162670571 183857 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4791973 183857 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4793975 183857 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803771 183857 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
49788381 18132 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
CHEMBL1269137 18132 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
156016097 177791 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.2 NC(=O)c1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4641856 177791 None 0 Human Functional pEC50 = 6 6.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.2 NC(=O)c1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
25108280 187490 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccccc1Br 10.1021/jm800754r
CHEMBL493494 187490 None 0 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccccc1Br 10.1021/jm800754r
CHEMBL238078 212849 None 34 Human Functional pEC50 = 5 5.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm800754r
44433910 97145 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 767 26 10 8 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(C)C)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL267389 97145 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 767 26 10 8 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(C)C)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL266796 213158 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL393243 214925 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O 10.1016/j.bmcl.2007.08.026
49788381 18132 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
CHEMBL1269137 18132 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
156018833 178003 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.4 NC(=O)Cc1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4644870 178003 None 0 Human Functional pEC50 = 5.0 5.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.4 NC(=O)Cc1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL236457 212039 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236681 212040 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL266812 213160 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
162661352 181557 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1255 45 6 21 6.0 COc1ccnc(NCCCOc2ccc(C[C@@H](CC(=O)O)NC(=O)c3ccc(OCc4cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC5CCCCC5)NC(=O)c5ccno5)C5CCCCC5)nn4)cc3)cc2)c1 10.1039/d0md00098a
CHEMBL4764373 181557 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1255 45 6 21 6.0 COc1ccnc(NCCCOc2ccc(C[C@@H](CC(=O)O)NC(=O)c3ccc(OCc4cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC5CCCCC5)NC(=O)c5ccno5)C5CCCCC5)nn4)cc3)cc2)c1 10.1039/d0md00098a
162659655 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4763124 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803166 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
162659655 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4763124 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803166 183804 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
25108339 176385 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 411 3 2 3 2.7 O=C1NC[C@@H](c2ccccc2)[C@@H]1C(=O)N/N=C1\CCc2ccc(Br)cc21 10.1021/jm800754r
CHEMBL459509 176385 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 411 3 2 3 2.7 O=C1NC[C@@H](c2ccccc2)[C@@H]1C(=O)N/N=C1\CCc2ccc(Br)cc21 10.1021/jm800754r
49788378 18130 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(C(=O)N2CCC(CN)CC2)CC1 10.1021/jm100984y
CHEMBL1269134 18130 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(C(=O)N2CCC(CN)CC2)CC1 10.1021/jm100984y
49788504 18137 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 671 15 4 8 2.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NC1CCN([C@@H](CC(C)C)C(=O)N2CCC(CN)CC2)C1=O 10.1021/jm100984y
CHEMBL1269142 18137 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 671 15 4 8 2.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NC1CCN([C@@H](CC(C)C)C(=O)N2CCC(CN)CC2)C1=O 10.1021/jm100984y
162668020 183844 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2415 108 20 43 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
CHEMBL4786553 183844 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2415 108 20 43 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
CHEMBL4803624 183844 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2415 108 20 43 -3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
CHEMBL237114 212473 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CCOP(=O)(Cc1ccc(C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(=O)N[C@H](C(N)=O)[C@@H](C)CC)cc1)OCC 10.1016/j.bmcl.2007.08.026
CHEMBL398099 214975 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(OC)c(OC)c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156018888 177889 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.4 NC(=O)Cc1cccc(NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
CHEMBL4643214 177889 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.4 NC(=O)Cc1cccc(NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
49788504 18137 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 671 15 4 8 2.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NC1CCN([C@@H](CC(C)C)C(=O)N2CCC(CN)CC2)C1=O 10.1021/jm100984y
CHEMBL1269142 18137 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 671 15 4 8 2.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NC1CCN([C@@H](CC(C)C)C(=O)N2CCC(CN)CC2)C1=O 10.1021/jm100984y
49788378 18130 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(C(=O)N2CCC(CN)CC2)CC1 10.1021/jm100984y
CHEMBL1269134 18130 None 0 Human Functional pEC50 = 4.9 4.9 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(C(=O)N2CCC(CN)CC2)CC1 10.1021/jm100984y
53326692 58987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 862 29 11 11 0.0 C=CCOC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm1013049
CHEMBL1689558 58987 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 862 29 11 11 0.0 C=CCOC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm1013049
CHEMBL237550 212843 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cc([N+](=O)[O-])c(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL397818 214969 None 0 Human Functional pEC50 = 5.9 5.9 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)c([N+](=O)[O-])c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
51351273 58988 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 695 21 10 10 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689560 58988 None 0 Human Functional pEC50 = 6.9 6.9 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 695 21 10 10 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
44433907 146599 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 838 25 10 9 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1nccc2ccccc12)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL392252 146599 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 838 25 10 9 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1nccc2ccccc12)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
10395438 189185 None 25 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.0c00154
CHEMBL509819 189185 None 25 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.0c00154
44433908 88801 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 863 26 10 8 2.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(-c2ccccc2)cc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236294 88801 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 863 26 10 8 2.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(-c2ccccc2)cc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
44433902 153768 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 776 25 10 9 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL398131 153768 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 776 25 10 9 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
44433915 169009 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 803 25 11 9 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccc1O)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL438512 169009 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 803 25 11 9 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccc1O)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
44433947 159739 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 742 22 9 10 -0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL410365 159739 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 742 22 9 10 -0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
137654325 159005 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.0c00154
CHEMBL4095478 159005 None 12 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.0c00154
CHEMBL398130 214978 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cccc(C#N)c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
49788439 18133 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC(C(=O)N2CCC(CN)CC2)C1 10.1021/jm100984y
CHEMBL1269138 18133 None 0 Human Functional pEC50 = 4.8 4.8 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC(C(=O)N2CCC(CN)CC2)C1 10.1021/jm100984y
51351273 58988 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 695 21 10 10 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689560 58988 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 695 21 10 10 -0.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
137661916 159495 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 461 10 4 6 1.4 NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL4100763 159495 None 0 Human Functional pEC50 = 7.8 7.8 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 461 10 4 6 1.4 NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
44433917 146600 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 792 25 10 10 0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL392253 146600 None 0 Human Functional pEC50 = 6.8 6.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 792 25 10 10 0.1 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL266795 213157 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156014169 177291 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 418 9 3 5 2.5 NC(=O)CC1CCCCC1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4634986 177291 None 0 Human Functional pEC50 = 5.8 5.8 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 418 9 3 5 2.5 NC(=O)CC1CCCCC1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
137661916 159495 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 461 10 4 6 1.4 NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL4100763 159495 None 0 Human Functional pEC50 = 7.7 7.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 461 10 4 6 1.4 NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL410759 215297 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccncc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156016297 177810 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 406 9 3 5 1.4 NC(=O)Cc1ccccc1CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4642100 177810 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 406 9 3 5 1.4 NC(=O)Cc1ccccc1CNC(=O)[C@H](Cc1ccccc1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
49788311 18129 None 7 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/acsmedchemlett.5b00429
CHEMBL1269133 18129 None 7 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/acsmedchemlett.5b00429
137637330 156152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 704 21 9 9 0.2 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4062629 156152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 704 21 9 9 0.2 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/acsmedchemlett.5b00429
9456 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm800754r
9589606 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm800754r
CHEMBL493076 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm800754r
49788440 18134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 594 12 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
CHEMBL1269139 18134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 594 12 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
44433940 97053 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 855 25 10 12 0.5 CC[C@H](C)[C@H](N)C(=O)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC 10.1016/j.bmcl.2007.08.026
CHEMBL266588 97053 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 855 25 10 12 0.5 CC[C@H](C)[C@H](N)C(=O)NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC 10.1016/j.bmcl.2007.08.026
73346321 92579 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 855 26 10 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL2431723 92579 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 855 26 10 11 0.5 CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
44433902 153768 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 776 25 10 9 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL398131 153768 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 776 25 10 9 0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
10395438 189185 None 25 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm400638v
CHEMBL509819 189185 None 25 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm400638v
49788311 18129 None 7 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/acsmedchemlett.5b00429
CHEMBL1269133 18129 None 7 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/acsmedchemlett.5b00429
137637330 156152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 704 21 9 9 0.2 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4062629 156152 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 704 21 9 9 0.2 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/acsmedchemlett.5b00429
9456 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
9589606 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
CHEMBL493076 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
9456 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
9589606 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
CHEMBL493076 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
CHEMBL237960 212844 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccc(F)cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
44433913 88739 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236037 88739 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
44433916 90296 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 777 25 10 10 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL238396 90296 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 777 25 10 10 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
49788440 18134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 594 12 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
CHEMBL1269139 18134 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 594 12 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
156009830 177175 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 384 7 3 5 2.5 NC(=O)c1cccc(NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
CHEMBL4632977 177175 None 0 Human Functional pEC50 = 5.7 5.7 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 384 7 3 5 2.5 NC(=O)c1cccc(NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
156021076 178286 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)[C@@H]1c2ccccc2CCN1C(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4649267 178286 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)[C@@H]1c2ccccc2CCN1C(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL2431720 212923 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human PAR2 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate productionAgonist activity at human PAR2 expressed in African green monkey COS7 cells assessed as stimulation of inositol triphosphate production
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)C(=O)O)[C@@H](C)CC 10.1021/jm400638v
25108340 176657 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 477 4 2 3 3.6 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1cccc(Br)c1)c1cccc(Br)c1 10.1021/jm800754r
CHEMBL459723 176657 None 0 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 477 4 2 3 3.6 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1cccc(Br)c1)c1cccc(Br)c1 10.1021/jm800754r
10395438 189185 None 25 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm800754r
CHEMBL509819 189185 None 25 Human Functional pEC50 = 7.6 7.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm800754r
44433903 88799 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 827 25 10 9 1.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236292 88799 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 827 25 10 9 1.5 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL237969 212847 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(N=[N+]=[N-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
162659655 183804 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4763124 183804 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803166 183804 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
49788311 18129 None 7 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
CHEMBL1269133 18129 None 7 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
25108338 187517 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 405 4 2 4 2.9 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccc(Br)s1 10.1021/jm800754r
CHEMBL493704 187517 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 405 4 2 4 2.9 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccc(Br)s1 10.1021/jm800754r
44433912 161900 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL414319 161900 None 0 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 788 25 10 9 0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
51351274 58989 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)nc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689561 58989 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)nc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
137654325 159005 None 12 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1039/d0md00098a
CHEMBL4095478 159005 None 12 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1039/d0md00098a
49788311 18129 None 7 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
CHEMBL1269133 18129 None 7 Human Functional pEC50 = 6.6 6.6 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1cccc(C(=O)N2CCC(CN)CC2)c1 10.1021/jm100984y
CHEMBL396797 214960 None 0 Human Functional pEC50 = 5.6 5.6 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](COc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
3740 3622 None 16 Human Functional pEC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilizationAntagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
CHEMBL443719 3622 None 16 Human Functional pEC50 = 4.6 4.6 - 1
Antagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilizationAntagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization
ChEMBL None None None None 10.1021/jm900604g
44433914 97180 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 789 25 10 10 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL267729 97180 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 789 25 10 10 -0.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156020881 178267 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 412 9 3 5 2.1 NC(=O)Cc1cccc(CNC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
CHEMBL4649051 178267 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 412 9 3 5 2.1 NC(=O)Cc1cccc(CNC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
25108278 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
9460 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
CHEMBL494502 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
25108278 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
9460 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
CHEMBL494502 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysisAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
CHEMBL235647 212032 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1csc2ccccc12)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236704 212042 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236704 212042 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(Cl)c(Cl)c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
10395438 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL509819 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL238406 212851 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CCc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
10483914 158003 None 33 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 614 21 9 9 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00429
CHEMBL4084322 158003 None 33 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 614 21 9 9 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00429
137654325 159005 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL4095478 159005 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
25108278 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm800754r
9460 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm800754r
CHEMBL494502 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm800754r
156013443 177565 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 384 7 3 5 2.5 NC(=O)c1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4638957 177565 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 384 7 3 5 2.5 NC(=O)c1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
51351274 58989 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)nc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689561 58989 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzerAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels measured every 15 second for 2 hrs by xCelligence real time cell analyzer
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)nc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
49788380 18131 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
CHEMBL1269136 18131 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
10395438 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL509819 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/acsmedchemlett.5b00429
10483914 158003 None 33 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 614 21 9 9 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00429
CHEMBL4084322 158003 None 33 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 614 21 9 9 -2.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(N)=O)C(C)C 10.1021/acsmedchemlett.5b00429
CHEMBL1627325 211270 None 0 Human Functional pEC50 = 4.5 4.5 -933254 8
Antagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilizationAntagonist activity at human recombinant PAR2 expressed in A549 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization
ChEMBL None None None CSCC[C@H](NC(=O)CNC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CO)C(C)(C)C)C(C)C)[C@@H](C)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)O)[C@@H](C)O 10.1021/jm900604g
44433949 159741 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 838 21 9 9 0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL410366 159741 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 838 21 9 9 0.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(I)cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
137654325 159005 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL4095478 159005 None 12 Human Functional pEC50 = 7.5 7.5 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 404 8 3 5 2.3 NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1 10.1021/acsmedchemlett.5b00429
CHEMBL398129 214976 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cccc(OC)c1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156013563 177622 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.2 NC(=O)c1cccc(CNC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
CHEMBL4639745 177622 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 398 8 3 5 2.2 NC(=O)c1cccc(CNC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)c1 10.1021/acsmedchemlett.0c00154
49788380 18131 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
CHEMBL1269136 18131 None 0 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 608 13 4 7 3.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCC(CN)CC2)cc1 10.1021/jm100984y
10395438 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1039/d0md00098a
CHEMBL509819 189185 None 25 Human Functional pEC50 = 6.5 6.5 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1039/d0md00098a
51351408 58990 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689562 58990 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 689 21 10 9 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccc(N)n1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
162659655 183804 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4763124 183804 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803166 183804 None 0 Human Functional pEC50 = 5.5 5.5 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS followed by compound addition in absence of cRGD by Fluo-4-AM dye-based FLIPR assay
ChEMBL 2042 90 12 38 -0.3 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
44433904 88800 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 837 25 10 8 1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236293 88800 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 837 25 10 8 1.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236682 212041 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC1CCCCC1)C(N)=O 10.1016/j.bmcl.2007.08.026
44433905 153767 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 842 25 10 9 2.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL398128 153767 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 842 25 10 9 2.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
137633152 156385 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 378 9 3 5 1.8 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4065387 156385 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 378 9 3 5 1.8 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL2431724 212925 None 0 Human Functional pEC50 = 8.4 8.4 - 1
Agonist activity at PAR2 in human 16HBE14o- cells assessed as increase in intracellular calcium levelAgonist activity at PAR2 in human 16HBE14o- cells assessed as increase in intracellular calcium level
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OCCOCCOCCNCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL396183 214952 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL397820 214970 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL396183 214952 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc([N+](=O)[O-])cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
CHEMBL397820 214970 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
137633152 156385 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 378 9 3 5 1.8 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4065387 156385 None 0 Human Functional pEC50 = 6.4 6.4 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 378 9 3 5 1.8 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL238078 212849 None 34 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL238078 212849 None 34 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm400638v
156012611 177500 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)C1CN(C(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)Cc2ccccc21 10.1021/acsmedchemlett.0c00154
CHEMBL4638185 177500 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)C1CN(C(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)Cc2ccccc21 10.1021/acsmedchemlett.0c00154
44433918 88779 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 868 26 10 10 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc(-c2ccc(C)cc2)on1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236194 88779 None 0 Human Functional pEC50 = 5.4 5.4 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 868 26 10 10 1.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc(-c2ccc(C)cc2)on1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
44433909 88803 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 793 25 10 8 1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)C1CCCCC1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236295 88803 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 793 25 10 8 1.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)C1CCCCC1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156012611 177500 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)C1CN(C(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)Cc2ccccc21 10.1021/acsmedchemlett.0c00154
CHEMBL4638185 177500 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 424 6 2 5 2.4 NC(=O)C1CN(C(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)Cc2ccccc21 10.1021/acsmedchemlett.0c00154
25108342 176992 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 453 5 1 3 4.5 CC(C)=CN1C[C@@H](c2ccccc2)[C@H](C(=O)N/N=C(\C)c2cccc(Br)c2)C1=O 10.1021/jm800754r
CHEMBL461639 176992 None 0 Human Functional pEC50 = 7.3 7.3 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 453 5 1 3 4.5 CC(C)=CN1C[C@@H](c2ccccc2)[C@H](C(=O)N/N=C(\C)c2cccc(Br)c2)C1=O 10.1021/jm800754r
CHEMBL396184 214953 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(Cl)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL395357 214945 None 0 Human Functional pEC50 = 5.3 5.3 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(C(=O)O)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
162643417 183720 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1382 45 12 23 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4776148 183720 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1382 45 12 23 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4802303 183720 None 0 Human Functional pEC50 = 6.3 6.3 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1382 45 12 23 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
44433906 169149 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 826 25 11 8 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2[nH]1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL439563 169149 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 826 25 11 8 1.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2[nH]1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
156018869 178033 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 412 9 3 5 2.1 NC(=O)Cc1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4645377 178033 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 412 9 3 5 2.1 NC(=O)Cc1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL236099 212034 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc([N+](=O)[O-])cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL237961 212845 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccc(O)cc1)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL237968 212846 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(I)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL278937 213296 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(C(C)(C)C)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
52948093 18136 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 659 11 3 9 1.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CC(=O)N2C(C1)SCC2C(=O)N1CCC(CN)CC1 10.1021/jm100984y
CHEMBL1269141 18136 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 659 11 3 9 1.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CC(=O)N2C(C1)SCC2C(=O)N1CCC(CN)CC1 10.1021/jm100984y
162675462 183889 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1755 63 20 28 -3.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
CHEMBL4798456 183889 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1755 63 20 28 -3.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
CHEMBL4804056 183889 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1755 63 20 28 -3.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCn1cc(C[C@H]2CN[C@@H](CCCNC(=N)N)C(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@H](Cc3ccccc3)C(=O)N2)nn1 10.1039/d0md00098a
137641156 157148 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 617 16 8 8 0.2 N=C(N)NCCC[C@H](NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4073996 157148 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 617 16 8 8 0.2 N=C(N)NCCC[C@H](NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
137641156 157148 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 617 16 8 8 0.2 N=C(N)NCCC[C@H](NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4073996 157148 None 0 Human Functional pEC50 = 7.2 7.2 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 617 16 8 8 0.2 N=C(N)NCCC[C@H](NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
52948093 18136 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 659 11 3 9 1.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CC(=O)N2C(C1)SCC2C(=O)N1CCC(CN)CC1 10.1021/jm100984y
CHEMBL1269141 18136 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 659 11 3 9 1.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CC(=O)N2C(C1)SCC2C(=O)N1CCC(CN)CC1 10.1021/jm100984y
9457 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 10.1021/jm800754r
9696680 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 10.1021/jm800754r
CHEMBL494303 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 10.1021/jm800754r
25108341 176658 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 413 4 1 3 3.2 C/C(=N\N(C)C(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 10.1021/jm800754r
CHEMBL459724 176658 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 413 4 1 3 3.2 C/C(=N\N(C)C(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 10.1021/jm800754r
156014169 177291 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 418 9 3 5 2.5 NC(=O)CC1CCCCC1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
CHEMBL4634986 177291 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 418 9 3 5 2.5 NC(=O)CC1CCCCC1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 10.1021/acsmedchemlett.0c00154
156019141 178055 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 426 9 3 5 2.4 Cc1cc(C(=O)N[C@@H](CC2CCCCC2)C(=O)NCc2ccccc2CC(N)=O)on1 10.1021/acsmedchemlett.0c00154
CHEMBL4645730 178055 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 426 9 3 5 2.4 Cc1cc(C(=O)N[C@@H](CC2CCCCC2)C(=O)NCc2ccccc2CC(N)=O)on1 10.1021/acsmedchemlett.0c00154
51351409 58991 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 688 21 10 8 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL1689563 58991 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 688 21 10 8 -0.2 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc(N)cc1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm1013049
CHEMBL438676 216247 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL438676 216247 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
56640611 143337 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 578 9 2 7 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1021/acsmedchemlett.6b00306
CHEMBL3896632 143337 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 578 9 2 7 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)CC(=O)c1ccccc1O2 10.1021/acsmedchemlett.6b00306
134147747 149727 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 562 9 2 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)c1ccccc1C1OC12 10.1021/acsmedchemlett.6b00306
CHEMBL3947297 149727 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 562 9 2 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)c1ccccc1C1OC12 10.1021/acsmedchemlett.6b00306
56640610 150888 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 564 9 2 7 4.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)OC(=O)c1ccccc12 10.1021/acsmedchemlett.6b00306
CHEMBL3956750 150888 None 0 Human Functional pEC50 = 6.2 6.2 - 1
Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release incubated for 30 mins measured for 60 secs by Fluo-3 AM dye based FLIPR assay relative to 2f-LIGRLO-NH2
ChEMBL 564 9 2 7 4.0 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CC1)OC(=O)c1ccccc12 10.1021/acsmedchemlett.6b00306
49788441 18135 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCCC1C(=O)N1CCC(CN)CC1 10.1021/jm100984y
CHEMBL1269140 18135 None 0 Human Functional pEC50 = 5.2 5.2 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCCC1C(=O)N1CCC(CN)CC1 10.1021/jm100984y
162664662 183832 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1181 49 11 20 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCn1cc(COC)nn1 10.1039/d0md00098a
CHEMBL4782345 183832 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1181 49 11 20 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCn1cc(COC)nn1 10.1039/d0md00098a
CHEMBL4803431 183832 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1181 49 11 20 -0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(=O)NCCOCCOCCOCCOCCOCCOCCn1cc(COC)nn1 10.1039/d0md00098a
137654661 158687 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 591 17 8 8 -0.4 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4092076 158687 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 591 17 8 8 -0.4 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acsmedchemlett.5b00429
137653967 158775 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 730 20 9 9 0.7 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4093061 158775 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 730 20 9 9 0.7 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
49788441 18135 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCCC1C(=O)N1CCC(CN)CC1 10.1021/jm100984y
CHEMBL1269140 18135 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release
ChEMBL 586 11 3 7 2.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCCC1C(=O)N1CCC(CN)CC1 10.1021/jm100984y
25108279 187652 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccc(Br)cc1 10.1021/jm800754r
CHEMBL494503 187652 None 0 Human Functional pEC50 = 5.1 5.1 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay
ChEMBL 399 4 2 3 2.8 C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccc(Br)cc1 10.1021/jm800754r
137654661 158687 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 591 17 8 8 -0.4 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4092076 158687 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 591 17 8 8 -0.4 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(N)=O 10.1021/acsmedchemlett.5b00429
137653967 158775 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 730 20 9 9 0.7 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4093061 158775 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 730 20 9 9 0.7 CC(C)C[C@H](NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)C(NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C1CCCCC1)C(N)=O 10.1021/acsmedchemlett.5b00429
44433911 88804 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 787 25 10 8 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
CHEMBL236296 88804 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL 787 25 10 8 0.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccc1)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
162670571 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4791973 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4793975 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803771 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
53326692 58987 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 862 29 11 11 0.0 C=CCOC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm1013049
CHEMBL1689558 58987 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assayAgonist activity at PAR2 in human 16HBE14o cells assessed as increase in intracellular calcium levels by in vitro physiological response assay
ChEMBL 862 29 11 11 0.0 C=CCOC(=O)NCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)[C@@H](C)CC)C(N)=O 10.1021/jm1013049
162670571 183857 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4791973 183857 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4793975 183857 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803771 183857 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
162644186 181906 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 807 31 3 15 2.5 COCc1cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)C2CCCCC2)nn1 10.1039/d0md00098a
CHEMBL4778041 181906 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 807 31 3 15 2.5 COCc1cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC2CCCCC2)NC(=O)c2ccno2)C2CCCCC2)nn1 10.1039/d0md00098a
162670571 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4791973 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4793975 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL4803771 183857 None 0 Human Functional pEC50 = 7.1 7.1 - 1
Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay
ChEMBL 1470 51 12 25 -0.6 N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O 10.1039/d0md00098a
CHEMBL236305 212035 None 0 Human Functional pEC50 = 6.1 6.1 - 1
Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccc(C#N)cc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O 10.1016/j.bmcl.2007.08.026
137638214 156918 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 435 11 4 6 0.9 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O 10.1021/acsmedchemlett.5b00429
CHEMBL4071278 156918 None 0 Human Functional pEC50 = 7.0 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay
ChEMBL 435 11 4 6 0.9 CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O 10.1021/acsmedchemlett.5b00429
156012496 177498 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 440 10 3 5 2.7 CCc1cc(C(=O)N[C@@H](CC2CCCCC2)C(=O)NCc2ccccc2CC(N)=O)on1 10.1021/acsmedchemlett.0c00154
CHEMBL4638162 177498 None 0 Human Functional pEC50 = 6.0 6.0 - 1
Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay
ChEMBL 440 10 3 5 2.7 CCc1cc(C(=O)N[C@@H](CC2CCCCC2)C(=O)NCc2ccccc2CC(N)=O)on1 10.1021/acsmedchemlett.0c00154
56640042 92577 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assayAgonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 7 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assayAgonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
155534488 172061 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4470628 172061 None 0 Human Functional pIC50 = 7 7.0 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
57330164 1783 None 20 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/jm400638v
6658 1783 None 20 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/jm400638v
73755230 1783 None 20 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/jm400638v
CHEMBL2431617 1783 None 20 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/jm400638v
CHEMBL2431719 212922 None 0 Human Functional pIC50 = 6 6.0 - 1
Antagonist activity at human PAR2 expressed in African green monkey COS7 cells assessed as inhibition of SLIGKV-NH2-induced inositol triphosphate productionAntagonist activity at human PAR2 expressed in African green monkey COS7 cells assessed as inhibition of SLIGKV-NH2-induced inositol triphosphate production
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC 10.1021/jm400638v
134137699 147614 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 575 10 3 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(CN)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3930659 147614 None 0 Human Functional pIC50 = 5 5.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 575 10 3 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(CN)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
56640042 92577 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assayAgonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 7.0 7.0 - 1
Agonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assayAgonist activity at human PAR2 expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation incubated for 20 mins followed by forskolin addition for 10 mins measured after 1 hr by LANCE assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
57330164 1783 None 20 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
6658 1783 None 20 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
73755230 1783 None 20 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
CHEMBL2431617 1783 None 20 Human Functional pIC50 = 6.0 6.0 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
56640547 144058 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 561 9 3 6 4.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(N)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3902670 144058 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 561 9 3 6 4.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(N)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
56640547 144058 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 561 9 3 6 4.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(N)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3902670 144058 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 561 9 3 6 4.4 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(N)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431719 212922 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Partial agonist activity at PAR2 in human SW620 cells assessed as increase in intracellular calcium releasePartial agonist activity at PAR2 in human SW620 cells assessed as increase in intracellular calcium release
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC 10.1021/jm400638v
57330164 1783 None 20 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
6658 1783 None 20 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
73755230 1783 None 20 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
CHEMBL2431617 1783 None 20 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
56639666 92578 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by SLIGKV-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by SLIGKV-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmc.2018.04.016
CHEMBL2431717 92578 None 0 Human Functional pIC50 = 5.8 5.8 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by SLIGKV-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization pretreated for 15 mins followed by SLIGKV-NH2 addition measured at 5 secs interval for 250 secs by Fluo-4/AM dye based fluorescence assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmc.2018.04.016
56640474 151184 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 564 9 2 6 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3959120 151184 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 564 9 2 6 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1021/acsmedchemlett.6b00306
56639666 92578 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium release
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1021/jm400638v
CHEMBL2431717 92578 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium release
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1021/jm400638v
56640474 151184 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 564 9 2 6 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3959120 151184 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 564 9 2 6 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc3O2)CC1 10.1021/acsmedchemlett.6b00306
117978042 121497 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582248 121497 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
117991137 121499 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 505 5 0 6 4.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)Cc4ccsc4)[C@@H](C)C3)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582250 121499 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 505 5 0 6 4.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)Cc4ccsc4)[C@@H](C)C3)nc12 10.1021/acsmedchemlett.5b00147
155534488 172061 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of trypsin-induced intracellular calcium mobilization preincubated for 15 mins followed by trypsin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of trypsin-induced intracellular calcium mobilization preincubated for 15 mins followed by trypsin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4470628 172061 None 0 Human Functional pIC50 = 8.7 8.7 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of trypsin-induced intracellular calcium mobilization preincubated for 15 mins followed by trypsin addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of trypsin-induced intracellular calcium mobilization preincubated for 15 mins followed by trypsin addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
49788574 18324 None 9 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 548 9 2 5 4.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm400638v
CHEMBL1270720 18324 None 9 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 548 9 2 5 4.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm400638v
56640042 92577 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 5.7 5.7 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
127036298 136515 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assayAntagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assay
ChEMBL 417 5 1 5 6.4 Cc1ccoc1CNc1nc(Oc2cc(Cl)cc(Cl)c2)nc2ccc(F)cc12 10.1016/j.bmc.2015.11.016
CHEMBL3735493 136515 None 0 Human Functional pIC50 = 5.6 5.6 - 1
Antagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assayAntagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assay
ChEMBL 417 5 1 5 6.4 Cc1ccoc1CNc1nc(Oc2cc(Cl)cc(Cl)c2)nc2ccc(F)cc12 10.1016/j.bmc.2015.11.016
134143255 145813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 9 3 4 4.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1c[nH]cn1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3916411 145813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 9 3 4 4.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1c[nH]cn1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
134143255 145813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 9 3 4 4.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1c[nH]cn1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3916411 145813 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 9 3 4 4.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1c[nH]cn1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
117990832 121498 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
CHEMBL3582249 121498 None 0 Human Functional pIC50 = 5.5 5.5 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
155549751 174022 None 0 Human Functional pIC50 = 5.5 5.5 -16 2
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 174022 None 0 Human Functional pIC50 = 5.5 5.5 -16 2
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
6737869 92575 None 2 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium release
ChEMBL 467 4 1 5 4.4 COc1ccc(Br)c(C(=O)Nn2c(-c3ccc(F)cc3)nc3ccccc3c2=O)c1 10.1021/jm400638v
CHEMBL2431619 92575 None 2 Human Functional pIC50 = 4.5 4.5 - 1
Antagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium release
ChEMBL 467 4 1 5 4.4 COc1ccc(Br)c(C(=O)Nn2c(-c3ccc(F)cc3)nc3ccccc3c2=O)c1 10.1021/jm400638v
155549751 174022 None 0 Human Functional pIC50 = 5.5 5.5 -16 2
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4540591 174022 None 0 Human Functional pIC50 = 5.5 5.5 -16 2
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 2446 97 6 39 9.5 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)NCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCn4cc(CCC(=O)NCC[C@H](NC(=O)[C@H](Cc5ccc(F)c(F)c5)NC(=O)Nc5ccc6c(CN7CCCC7)nn(Cc7c(Cl)cccc7Cl)c6c5)C(=O)NCc5ccccc5)nn4)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
57330164 1783 None 20 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
6658 1783 None 20 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
73755230 1783 None 20 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
CHEMBL2431617 1783 None 20 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1021/acsmedchemlett.6b00306
56640042 92577 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium release
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/jm400638v
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced intracellular calcium release
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/jm400638v
117977940 121500 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 509 2 0 6 5.3 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(C)(C)C)c3n2)C(C)(C)C1 10.1021/acsmedchemlett.5b00147
CHEMBL3582251 121500 None 0 Human Functional pIC50 = 8.4 8.4 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of SLIGKV-induced Ca2+ responses pre-incubated for 30 mins before SLIGKV stimulation by FLIPR assay
ChEMBL 509 2 0 6 5.3 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(C)(C)C)c3n2)C(C)(C)C1 10.1021/acsmedchemlett.5b00147
117977940 121500 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 509 2 0 6 5.3 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(C)(C)C)c3n2)C(C)(C)C1 10.1021/acsmedchemlett.5b00147
CHEMBL3582251 121500 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 509 2 0 6 5.3 CC(C)(C)OC(=O)N1CCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(C)(C)C)c3n2)C(C)(C)C1 10.1021/acsmedchemlett.5b00147
56639666 92578 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium release
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1021/jm400638v
CHEMBL2431717 92578 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium release
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1021/jm400638v
126961334 540 None 12 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 10.1016/j.bmcl.2018.05.032
9585 540 None 12 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 10.1016/j.bmcl.2018.05.032
CHEMBL4127372 540 None 12 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 10.1016/j.bmcl.2018.05.032
117990832 121498 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
CHEMBL3582249 121498 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
56640042 92577 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human PC3 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by stimulation measured for 60 secs by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human PC3 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by stimulation measured for 60 secs by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Antagonist activity at PAR2 in human PC3 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by stimulation measured for 60 secs by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human PC3 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by stimulation measured for 60 secs by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
155534488 172061 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
CHEMBL4470628 172061 None 0 Human Functional pIC50 = 6.3 6.3 - 1
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 495 6 1 6 3.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)CCC(=O)O)CC3(C)C)nc12 10.1021/acsmedchemlett.8b00538
117990832 121498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
CHEMBL3582249 121498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
117978042 121497 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582248 121497 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
117991137 121499 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 505 5 0 6 4.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)Cc4ccsc4)[C@@H](C)C3)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582250 121499 None 0 Human Functional pIC50 = 8.3 8.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of trypsin-induced Ca2+ responses pre-incubated for 30 mins before trypsin stimulation by FLIPR assay
ChEMBL 505 5 0 6 4.6 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)Cc4ccsc4)[C@@H](C)C3)nc12 10.1021/acsmedchemlett.5b00147
117978042 121497 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582248 121497 None 0 Human Functional pIC50 = 4.3 4.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
117990832 121498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
CHEMBL3582249 121498 None 0 Human Functional pIC50 = 5.3 5.3 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of thrombin-induced Ca2+ responses pre-incubated for 30 mins before thrombin stimulation by FLIPR assay
ChEMBL 478 4 0 6 4.4 CCOC(=O)[C@H]1CCCN(C(=O)c2cn3nc(-c4ccc(F)cc4)cc(C(F)(F)F)c3n2)[C@@H]1C 10.1021/acsmedchemlett.5b00147
49788505 18138 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 581 12 3 7 3.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCOCC2)cc1 10.1021/jm400638v
CHEMBL1269143 18138 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilizationAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of agonist-induced calcium mobilization
ChEMBL 581 12 3 7 3.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCOCC2)cc1 10.1021/jm400638v
49788505 18138 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium releaseAntagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium release
ChEMBL 581 12 3 7 3.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCOCC2)cc1 10.1021/jm100984y
CHEMBL1269143 18138 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium releaseAntagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium release
ChEMBL 581 12 3 7 3.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)Nc1ccc(CC(=O)N2CCOCC2)cc1 10.1021/jm100984y
145962815 161608 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human HEK293 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 15 mins followed by trypsin addition by Fluo-8 dye based fluorescence assayAntagonist activity at PAR2 in human HEK293 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 15 mins followed by trypsin addition by Fluo-8 dye based fluorescence assay
ChEMBL 341 7 2 4 3.9 O[C@@H](CCc1ccc(F)cc1)C[C@H](O)c1cc(-c2ccccc2)on1 10.1016/j.bmcl.2018.05.032
CHEMBL4128225 161608 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human HEK293 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 15 mins followed by trypsin addition by Fluo-8 dye based fluorescence assayAntagonist activity at PAR2 in human HEK293 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 15 mins followed by trypsin addition by Fluo-8 dye based fluorescence assay
ChEMBL 341 7 2 4 3.9 O[C@@H](CCc1ccc(F)cc1)C[C@H](O)c1cc(-c2ccccc2)on1 10.1016/j.bmcl.2018.05.032
56640042 92577 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human PC3 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human PC3 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human PC3 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human PC3 cells assessed as inhibition of endogenous trypsin-stimulated intracellular calcium release by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
126961335 538 None 36 Human Functional pIC50 = 5.2 5.2 5 2
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1016/j.bmcl.2018.05.032
9560 538 None 36 Human Functional pIC50 = 5.2 5.2 5 2
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1016/j.bmcl.2018.05.032
CHEMBL4128763 538 None 36 Human Functional pIC50 = 5.2 5.2 5 2
Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assayAntagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1016/j.bmcl.2018.05.032
10149969 161473 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 in human HEK293 cells assessed as inhibition of SLIGRL-induced intracellular calcium flux preincubated for 10 mins followed by SLIGRL-induction measured after 24 hrs by Fluo4-AM dye-based fluorescence assayAntagonist activity at PAR2 in human HEK293 cells assessed as inhibition of SLIGRL-induced intracellular calcium flux preincubated for 10 mins followed by SLIGRL-induction measured after 24 hrs by Fluo4-AM dye-based fluorescence assay
ChEMBL 340 10 0 4 3.8 COc1ccc(CCC(=O)CC(=O)CCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.05.032
CHEMBL4126288 161473 None 0 Human Functional pIC50 = 4.2 4.2 - 1
Antagonist activity at PAR2 in human HEK293 cells assessed as inhibition of SLIGRL-induced intracellular calcium flux preincubated for 10 mins followed by SLIGRL-induction measured after 24 hrs by Fluo4-AM dye-based fluorescence assayAntagonist activity at PAR2 in human HEK293 cells assessed as inhibition of SLIGRL-induced intracellular calcium flux preincubated for 10 mins followed by SLIGRL-induction measured after 24 hrs by Fluo4-AM dye-based fluorescence assay
ChEMBL 340 10 0 4 3.8 COc1ccc(CCC(=O)CC(=O)CCc2ccc(OC)cc2)cc1 10.1016/j.bmcl.2018.05.032
53318281 58680 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assayAntagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assay
ChEMBL 328 8 2 5 4.6 CCCCCNc1nc(NCc2ccco2)c2cc(F)ccc2n1 10.1016/j.bmc.2015.11.016
CHEMBL1684609 58680 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assayAntagonist activity at protease-activated receptor 2 (unknown origin) expressed in CHO-K1 cells assessed as inhibition of trypsin-induced calcium flux by FLIPR assay
ChEMBL 328 8 2 5 4.6 CCCCCNc1nc(NCc2ccco2)c2cc(F)ccc2n1 10.1016/j.bmc.2015.11.016
56640042 92577 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium release
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/jm400638v
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced intracellular calcium release
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/jm400638v
56640042 92577 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 6.2 6.2 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
155567301 176091 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1074 41 1 20 3.2 COCc1cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCC(=O)N2CCN(C(=O)c3cn4nc(-c5ccc(F)cc5)cc(C(C)C)c4n3)C(C)(C)C2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4588926 176091 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human EAhy926 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1074 41 1 20 3.2 COCc1cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCC(=O)N2CCN(C(=O)c3cn4nc(-c5ccc(F)cc5)cc(C(C)C)c4n3)C(C)(C)C2)nn1 10.1021/acsmedchemlett.8b00538
56848369 92576 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Antagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium release
ChEMBL 430 3 0 4 4.2 Cc1nc2ccc(C(=O)N3CCN(C(=O)C4CCCCC4)CC3)cn2c1-c1ccccc1 10.1021/jm400638v
CHEMBL2431715 92576 None 0 Human Functional pIC50 = 4.1 4.1 - 1
Antagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium releaseAntagonist activity at PAR2 in human HCT15 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium release
ChEMBL 430 3 0 4 4.2 Cc1nc2ccc(C(=O)N3CCN(C(=O)C4CCCCC4)CC3)cn2c1-c1ccccc1 10.1021/jm400638v
56640042 92577 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
56640398 145565 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 10 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC[C@H]1C(=O)NC(C)(C)C 10.1021/acsmedchemlett.6b00306
CHEMBL3914547 145565 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 10 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC[C@H]1C(=O)NC(C)(C)C 10.1021/acsmedchemlett.6b00306
49788574 18324 None 9 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium releaseAntagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium release
ChEMBL 548 9 2 5 4.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm100984y
CHEMBL1270720 18324 None 9 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium releaseAntagonist activity at PAR2 receptor in human HT-29 cells assessed as inhibition of intracellular calcium release
ChEMBL 548 9 2 5 4.8 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC2(CCc3ccccc32)CC1 10.1021/jm100984y
155567301 176091 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1074 41 1 20 3.2 COCc1cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCC(=O)N2CCN(C(=O)c3cn4nc(-c5ccc(F)cc5)cc(C(C)C)c4n3)C(C)(C)C2)nn1 10.1021/acsmedchemlett.8b00538
CHEMBL4588926 176091 None 0 Human Functional pIC50 = 6.1 6.1 - 1
Antagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assayAntagonist activity at PAR2 in human MDA-MB-231 cells assessed as inhibition of SLIGKV-NH2-induced intracellular calcium mobilization preincubated for 15 mins followed by SLIGKV-NH2 addition by Fluo-4-AM dye based fluorescence assay
ChEMBL 1074 41 1 20 3.2 COCc1cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)CCC(=O)N2CCN(C(=O)c3cn4nc(-c5ccc(F)cc5)cc(C(C)C)c4n3)C(C)(C)C2)nn1 10.1021/acsmedchemlett.8b00538
56640398 145565 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 10 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC[C@H]1C(=O)NC(C)(C)C 10.1021/acsmedchemlett.6b00306
CHEMBL3914547 145565 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 545 10 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCCC[C@H]1C(=O)NC(C)(C)C 10.1021/acsmedchemlett.6b00306
134137699 147614 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 575 10 3 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(CN)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL3930659 147614 None 0 Human Functional pIC50 = 5.1 5.1 - 1
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-stimulated intracellular calcium release preincubated for 30 mins followed by 2f-LIGRLO-NH2 stimulation measured for 60 sec by Fluo-3 AM dye based FLIPR assay
ChEMBL 575 10 3 6 4.3 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1cc(CN)no1)C(=O)N1CCC2(C=Cc3ccccc32)CC1 10.1021/acsmedchemlett.6b00306
117978042 121497 None 0 Human Functional pIC50 = 4.0 4.0 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
CHEMBL3582248 121497 None 0 Human Functional pIC50 = 4.0 4.0 - 1
Antagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assayAntagonist activity against PAR2 in human HT29 cells assessed as inhibition of UTP-induced Ca2+ responses pre-incubated for 30 mins before UTP stimulation by FLIPR assay
ChEMBL 495 3 0 6 5.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)OC(C)(C)C)CC3(C)C)nc12 10.1021/acsmedchemlett.5b00147
12490 537 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Determined in an IP1 assayDetermined in an IP1 assay
Guide to Pharmacology 542 9 3 6 3.9 CNC(=O)[C@H]1CCC(NC(=O)[C@H](CC2CCCCC2)NC(=O)C3=CN(CC4=CC=CC=C4)N=N3)C5=C1C=CC=C5 33335291
167993644 537 None 0 Human Functional pEC50 = 6.7 6.7 - 1
Determined in an IP1 assayDetermined in an IP1 assay
Guide to Pharmacology 542 9 3 6 3.9 CNC(=O)[C@H]1CCC(NC(=O)[C@H](CC2CCCCC2)NC(=O)C3=CN(CC4=CC=CC=C4)N=N3)C5=C1C=CC=C5 33335291
9457 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 18720984
9696680 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 18720984
CHEMBL494303 246 None 0 Human Functional pEC50 = 5.2 5.2 - 1
UnclassifiedUnclassified
Guide to Pharmacology 327 4 2 4 2.1 O=C([C@@H]1C(=O)NC[C@H]1c1ccccc1)N/N=C(/c1cccs1)\C 18720984
49843508 1781 None 0 Human Functional pEC50 = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 608 13 4 7 3.4 NCC1CCN(CC1)C(=O)c1cccc(c1)CNC(=O)[C@H](C(CC)C)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1 20873792
6657 1781 None 0 Human Functional pEC50 = 6.6 6.6 - 1
UnclassifiedUnclassified
Guide to Pharmacology 608 13 4 7 3.4 NCC1CCN(CC1)C(=O)c1cccc(c1)CNC(=O)[C@H](C(CC)C)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1 20873792
9456 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 18720984
9589606 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 18720984
CHEMBL493076 243 None 27 Human Functional pEC50 = 6.7 6.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 18720984
9455 533 None 0 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26819675
25108278 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 18720984
9460 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 18720984
CHEMBL494502 240 None 8 Human Functional pEC50 = 7.5 7.5 - 1
UnclassifiedUnclassified
Guide to Pharmacology 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 18720984
12493 2097 None 0 Human Functional pEC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None C[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C2=CC=NO2)C3=CC=CC=C3)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]4=C(/C=C/C=C/C=C\5/N(C)C6=C(C=C(C=C6)S([O-])(=O)=O)C5(C)C)C(C)(C)C7=C4C=CC(=C7)S([O-])(=O)=O)C(N)=O 31312406
167993645 2097 None 0 Human Functional pEC50 = 7.8 7.8 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None C[C@H](NC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)C2=CC=NO2)C3=CC=CC=C3)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCNC(=O)CCCCC[N+]4=C(/C=C/C=C/C=C\5/N(C)C6=C(C=C(C=C6)S([O-])(=O)=O)C5(C)C)C(C)(C)C7=C4C=CC(=C7)S([O-])(=O)=O)C(N)=O 31312406
12492 2096 None 0 Human Functional pEC50 = 7.9 7.9 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 36527934
126970682 766 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonism of 2-at-LIGRL-NH2-induced ERK phosphorylation in 16HBE14o- cells.Antagonism of 2-at-LIGRL-NH2-induced ERK phosphorylation in 16HBE14o- cells.
Guide to Pharmacology 767 18 6 10 0.8 NCCCC[C@H](N1CC2N(CC1=O)C(=O)[C@H](CN2C(=O)c1ccco1)NC(=O)CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccc(cc1)O)CC(C)C 26140338
9570 766 None 0 Human Functional pIC50 = 4.8 4.8 - 1
Antagonism of 2-at-LIGRL-NH2-induced ERK phosphorylation in 16HBE14o- cells.Antagonism of 2-at-LIGRL-NH2-induced ERK phosphorylation in 16HBE14o- cells.
Guide to Pharmacology 767 18 6 10 0.8 NCCCC[C@H](N1CC2N(CC1=O)C(=O)[C@H](CN2C(=O)c1ccco1)NC(=O)CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccc(cc1)O)CC(C)C 26140338
129320516 539 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonism of SLIGRL-NH2-induced IP1 formation.Antagonism of SLIGRL-NH2-induced IP1 formation.
Guide to Pharmacology 262 2 1 1 3.4 O=CN1c2ccccc2CC1c1c[nH]c2c1cccc2 28445455
9586 539 None 0 Human Functional pIC50 = 5.2 5.2 - 1
Antagonism of SLIGRL-NH2-induced IP1 formation.Antagonism of SLIGRL-NH2-induced IP1 formation.
Guide to Pharmacology 262 2 1 1 3.4 O=CN1c2ccccc2CC1c1c[nH]c2c1cccc2 28445455
126961335 538 None 36 Human Functional pIC50 = 7.6 7.6 5 2
Antagonism of SLIGRL-NH2-induced IP1 formation.Antagonism of SLIGRL-NH2-induced IP1 formation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
9560 538 None 36 Human Functional pIC50 = 7.6 7.6 5 2
Antagonism of SLIGRL-NH2-induced IP1 formation.Antagonism of SLIGRL-NH2-induced IP1 formation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
CHEMBL4128763 538 None 36 Human Functional pIC50 = 7.6 7.6 5 2
Antagonism of SLIGRL-NH2-induced IP1 formation.Antagonism of SLIGRL-NH2-induced IP1 formation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
126970682 766 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonism of peptidomimetic-induced PAR2 Ca2+ signalling in 16HBE14o- cells.Antagonism of peptidomimetic-induced PAR2 Ca2+ signalling in 16HBE14o- cells.
Guide to Pharmacology 767 18 6 10 0.8 NCCCC[C@H](N1CC2N(CC1=O)C(=O)[C@H](CN2C(=O)c1ccco1)NC(=O)CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccc(cc1)O)CC(C)C 26140338
9570 766 None 0 Human Functional pIC50 = 5.9 5.9 - 1
Antagonism of peptidomimetic-induced PAR2 Ca2+ signalling in 16HBE14o- cells.Antagonism of peptidomimetic-induced PAR2 Ca2+ signalling in 16HBE14o- cells.
Guide to Pharmacology 767 18 6 10 0.8 NCCCC[C@H](N1CC2N(CC1=O)C(=O)[C@H](CN2C(=O)c1ccco1)NC(=O)CC(C)C)C(=O)N[C@H](C(=O)N[C@H](C(=O)O)Cc1ccc(cc1)O)CC(C)C 26140338
126961334 540 None 12 Human Functional pIC50 = 5.6 5.6 - 1
In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
9585 540 None 12 Human Functional pIC50 = 5.6 5.6 - 1
In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
CHEMBL4127372 540 None 12 Human Functional pIC50 = 5.6 5.6 - 1
In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
126961335 538 None 36 Human Functional pIC50 = 8.3 8.3 5 2
In a FLIPR calcium accumulation assay, vs. SLIGRL activation.In a FLIPR calcium accumulation assay, vs. SLIGRL activation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
9560 538 None 36 Human Functional pIC50 = 8.3 8.3 5 2
In a FLIPR calcium accumulation assay, vs. SLIGRL activation.In a FLIPR calcium accumulation assay, vs. SLIGRL activation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
CHEMBL4128763 538 None 36 Human Functional pIC50 = 8.3 8.3 5 2
In a FLIPR calcium accumulation assay, vs. SLIGRL activation.In a FLIPR calcium accumulation assay, vs. SLIGRL activation.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
12491 1962 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of Gα13 activation in hPAR2-HEK293 cellsInhibition of Gα13 activation in hPAR2-HEK293 cells
Guide to Pharmacology 564 4 1 6 6.4 CC(C)(C)C1=CC(=NC2=C1OC(=C2)C(=O)N3CCN(CC3(C)C)C4=CC=C(C=N4)C(O)=O)C5=CC=C(Cl)C(F)=C5 33247181
134296695 1962 None 0 Human Functional pIC50 = 6.4 6.4 - 1
Inhibition of Gα13 activation in hPAR2-HEK293 cellsInhibition of Gα13 activation in hPAR2-HEK293 cells
Guide to Pharmacology 564 4 1 6 6.4 CC(C)(C)C1=CC(=NC2=C1OC(=C2)C(=O)N3CCN(CC3(C)C)C4=CC=C(C=N4)C(O)=O)C5=CC=C(Cl)C(F)=C5 33247181
12491 1962 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of Gαq activation in hPAR2-HEK293 cellsInhibition of Gαq activation in hPAR2-HEK293 cells
Guide to Pharmacology 564 4 1 6 6.4 CC(C)(C)C1=CC(=NC2=C1OC(=C2)C(=O)N3CCN(CC3(C)C)C4=CC=C(C=N4)C(O)=O)C5=CC=C(Cl)C(F)=C5 33247181
134296695 1962 None 0 Human Functional pIC50 = 7.1 7.1 - 1
Inhibition of Gαq activation in hPAR2-HEK293 cellsInhibition of Gαq activation in hPAR2-HEK293 cells
Guide to Pharmacology 564 4 1 6 6.4 CC(C)(C)C1=CC(=NC2=C1OC(=C2)C(=O)N3CCN(CC3(C)C)C4=CC=C(C=N4)C(O)=O)C5=CC=C(Cl)C(F)=C5 33247181
126961334 540 None 12 Human Functional pIC50 = 5.8 5.8 - 1
Measuring SLIGRL-NH2-induced IP1 formationMeasuring SLIGRL-NH2-induced IP1 formation
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
9585 540 None 12 Human Functional pIC50 = 5.8 5.8 - 1
Measuring SLIGRL-NH2-induced IP1 formationMeasuring SLIGRL-NH2-induced IP1 formation
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
CHEMBL4127372 540 None 12 Human Functional pIC50 = 5.8 5.8 - 1
Measuring SLIGRL-NH2-induced IP1 formationMeasuring SLIGRL-NH2-induced IP1 formation
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
6659 2985 None 0 Human Functional pIC50 = 5.4 5.4 - 1
Measuring antagonism of calcium flux induced by PAR2 agonist SLIGRL.Measuring antagonism of calcium flux induced by PAR2 agonist SLIGRL.
Guide to Pharmacology None None None None None
57330164 1783 None 20 Human Functional pIC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 21806599
6658 1783 None 20 Human Functional pIC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 21806599
73755230 1783 None 20 Human Functional pIC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 21806599
CHEMBL2431617 1783 None 20 Human Functional pIC50 = 5.7 5.7 - 1
UnclassifiedUnclassified
Guide to Pharmacology 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 21806599
10268 1961 None 0 Human Functional pIC50 = 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 5 3.2 Fc1ccc(cc1)c1nn2cc(nc2c(c1)C(C)(C)C)C(=O)N1CCNC(=O)C1(C)C 29263243
117977934 1961 None 0 Human Functional pIC50 = 7.1 7.1 - 1
UnclassifiedUnclassified
Guide to Pharmacology 423 2 1 5 3.2 Fc1ccc(cc1)c1nn2cc(nc2c(c1)C(C)(C)C)C(=O)N1CCNC(=O)C1(C)C 29263243


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

 Species

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

 Mol
weight		 Rot
Bonds		 H don

 H acc

 LogP

 Smiles

 DOI
CHEMBL2431724 212925 None 0 Human Binding pEC50 = 8 8.0 - 0
Agonist activity at PAR2 in human 16HBE14o- cells assessed as increase in MAPK levelAgonist activity at PAR2 in human 16HBE14o- cells assessed as increase in MAPK level
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)OCCOCCOCCNCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)[C@@H](C)CC)C(N)=O 10.1021/jm400638v
56640042 92577 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
9456 243 None 27 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
9589606 243 None 27 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
CHEMBL493076 243 None 27 Human Binding pEC50 = 6.7 6.7 - 0
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 517 6 3 5 3.7 Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C 10.1021/jm400638v
56640042 92577 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
CHEMBL2431716 92577 None 0 Human Binding pEC50 = 5.7 5.7 - 0
Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs
ChEMBL 522 10 2 5 4.7 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 10.1021/acsmedchemlett.6b00306
25108278 240 None 8 Human Binding pEC50 = 7.5 7.5 - 2
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
9460 240 None 8 Human Binding pEC50 = 7.5 7.5 - 2
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
CHEMBL494502 240 None 8 Human Binding pEC50 = 7.5 7.5 - 2
Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay
ChEMBL 399 4 2 3 2.8 Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C 10.1021/jm400638v
CHEMBL238078 212849 None 34 Human Binding pEC50 = 5.3 5.3 - 0
Agonist activity at PAR2 (unknown origin) by cell-based assayAgonist activity at PAR2 (unknown origin) by cell-based assay
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm400638v
CHEMBL2431718 212921 None 0 Human Binding pEC50 = 5.1 5.1 - 0
Agonist activity at PAR2 in human platelets by platelet aggregation assay in presence of SFLLRNAgonist activity at PAR2 in human platelets by platelet aggregation assay in presence of SFLLRN
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C 10.1021/jm400638v
117991201 193892 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system methodInhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system method
ChEMBL 509 5 1 6 4.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)[C@H](O)CC(C)(C)C)[C@@H](C)C3)nc12 10.1016/j.ejmech.2021.113867
CHEMBL5273903 193892 None 0 Human Binding pIC50 = 9.2 9.2 - 0
Inhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system methodInhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system method
ChEMBL 509 5 1 6 4.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)[C@H](O)CC(C)(C)C)[C@@H](C)C3)nc12 10.1016/j.ejmech.2021.113867
10395438 189185 None 25 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysis
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm400638v
CHEMBL509819 189185 None 25 Human Binding pIC50 = 7 7.0 - 0
Displacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysis
ChEMBL 777 26 11 10 -0.9 CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O 10.1021/jm400638v
57330164 1783 None 20 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
6658 1783 None 20 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
73755230 1783 None 20 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
CHEMBL2431617 1783 None 20 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
71511553 137369 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 540 14 3 6 4.8 CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC 10.1016/j.bmcl.2015.12.048
CHEMBL3752235 137369 None 0 Human Binding pIC50 = 6 6.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 540 14 3 6 4.8 CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC 10.1016/j.bmcl.2015.12.048
57330164 1783 None 20 Human Binding pIC50 = 5 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
6658 1783 None 20 Human Binding pIC50 = 5 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
73755230 1783 None 20 Human Binding pIC50 = 5 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
CHEMBL2431617 1783 None 20 Human Binding pIC50 = 5 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
11557006 92580 None 8 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/jm400638v
CHEMBL2431727 92580 None 8 Human Binding pIC50 = 6.0 6.0 - 1
Antagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assay
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/jm400638v
57330164 1783 None 20 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
6658 1783 None 20 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
73755230 1783 None 20 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
CHEMBL2431617 1783 None 20 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
71511553 137369 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 540 14 3 6 4.8 CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC 10.1016/j.bmcl.2015.12.048
CHEMBL3752235 137369 None 0 Human Binding pIC50 = 5.9 5.9 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 540 14 3 6 4.8 CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC 10.1016/j.bmcl.2015.12.048
107985 177463 None 47 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay
ChEMBL 360 1 1 6 1.1 CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O 10.1021/jm400638v
CHEMBL463763 177463 None 47 Human Binding pIC50 = 7.9 7.9 - 0
Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay
ChEMBL 360 1 1 6 1.1 CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O 10.1021/jm400638v
CHEMBL2431721 212924 None 0 Human Binding pIC50 = 6.9 6.9 - 0
Antagonist activity at PAR2 in human neutrophils assessed as inhibition of chemotactic migration of cells towards trypsin/SLIGRL-NH2Antagonist activity at PAR2 in human neutrophils assessed as inhibition of chemotactic migration of cells towards trypsin/SLIGRL-NH2
ChEMBL None None None CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC 10.1021/jm400638v
56639666 92578 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431717 92578 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
56639666 92578 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431717 92578 None 0 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
57330164 1783 None 20 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin)
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmc.2015.11.016
6658 1783 None 20 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin)
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmc.2015.11.016
73755230 1783 None 20 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin)
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmc.2015.11.016
CHEMBL2431617 1783 None 20 Human Binding pIC50 = 5.7 5.7 - 0
Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin)
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmc.2015.11.016
126961335 538 None 36 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin)
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.3c01861
9560 538 None 36 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin)
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.3c01861
CHEMBL4128763 538 None 36 Human Binding pIC50 = 7.6 7.6 - 1
Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin)
ChEMBL 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 10.1021/acs.jmedchem.3c01861
134819117 196746 None 4 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cellsAntagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cells
ChEMBL 570 5 1 6 7.5 CC(C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 10.1016/j.ejmech.2022.115079
CHEMBL5431335 196746 None 4 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cellsAntagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cells
ChEMBL 570 5 1 6 7.5 CC(C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 10.1016/j.ejmech.2022.115079
107985 177463 None 47 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISAAntagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA
ChEMBL 360 1 1 6 1.1 CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O 10.1021/jm400638v
CHEMBL463763 177463 None 47 Human Binding pIC50 = 7.6 7.6 - 0
Antagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISAAntagonist activity at human PAR2 expressed in human A549 cells coexpressing TACR1 assessed as inhibition of substance P-induced IL-8 production by ELISA
ChEMBL 360 1 1 6 1.1 CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O 10.1021/jm400638v
56639666 92578 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of europium-labeled 2f-LIGRLO-NH2 from human PAR2 expressed in CHO cells after 1 to 2 hrsDisplacement of europium-labeled 2f-LIGRLO-NH2 from human PAR2 expressed in CHO cells after 1 to 2 hrs
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431717 92578 None 0 Human Binding pIC50 = 5.4 5.4 - 0
Displacement of europium-labeled 2f-LIGRLO-NH2 from human PAR2 expressed in CHO cells after 1 to 2 hrsDisplacement of europium-labeled 2f-LIGRLO-NH2 from human PAR2 expressed in CHO cells after 1 to 2 hrs
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
56639666 92578 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431717 92578 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431725 212926 None 25 Rat Binding pIC50 = 4.3 4.3 - 0
Antagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activationAntagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activation
ChEMBL None None None CC(C)C[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O 10.1021/jm400638v
CHEMBL2431726 212927 None 0 Rat Binding pIC50 = 4.3 4.3 - 0
Antagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activationAntagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activation
ChEMBL None None None CC[C@H](C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC(C)C)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O 10.1021/jm400638v
56639666 92578 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
CHEMBL2431717 92578 None 0 Human Binding pIC50 = 6.3 6.3 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 498 12 3 6 3.6 CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC 10.1016/j.bmcl.2015.12.048
172444139 195501 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin)
ChEMBL 539 5 1 5 7.1 C[C@@H](c1ccccc1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccccc3)ccc21 10.1021/acs.jmedchem.3c01861
CHEMBL5404935 195501 None 0 Human Binding pIC50 = 7.1 7.1 - 0
Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin)
ChEMBL 539 5 1 5 7.1 C[C@@H](c1ccccc1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccccc3)ccc21 10.1021/acs.jmedchem.3c01861
57330164 1783 None 20 Human Binding pIC50 = 5.0 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
6658 1783 None 20 Human Binding pIC50 = 5.0 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
73755230 1783 None 20 Human Binding pIC50 = 5.0 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
CHEMBL2431617 1783 None 20 Human Binding pIC50 = 5.0 5.0 - 0
Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay
ChEMBL 546 9 2 5 4.9 CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C 10.1016/j.bmcl.2015.12.048
127035718 136502 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cellsDisplacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cells
ChEMBL 796 16 6 7 5.9 NCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@H](Cc1ccccc1)C(=O)Nc1ccccc1 10.1016/j.bmc.2015.11.016
CHEMBL3735405 136502 None 0 Human Binding pKi = 5.7 5.7 - 1
Displacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cellsDisplacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cells
ChEMBL 796 16 6 7 5.9 NCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@H](Cc1ccccc1)C(=O)Nc1ccccc1 10.1016/j.bmc.2015.11.016
11557006 92580 None 8 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells by scintillation counting analysisDisplacement of [3H]2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells by scintillation counting analysis
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/jm400638v
CHEMBL2431727 92580 None 8 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells by scintillation counting analysisDisplacement of [3H]2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells by scintillation counting analysis
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/jm400638v
127035910 136463 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cellsDisplacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cells
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2015.11.016
CHEMBL3735057 136463 None 0 Human Binding pKi = 6.2 6.2 - 1
Displacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cellsDisplacement of [3H]furoyl-LIGRL-NH2 from human protease-activated receptor 2 in NCTC-2544 cells
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1016/j.bmc.2015.11.016
11557006 92580 None 8 Human Binding pKi = 6.2 6.2 - 1
Binding affinity to PAR2 (unknown origin) assessed as inhibition constantBinding affinity to PAR2 (unknown origin) assessed as inhibition constant
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c01861
CHEMBL2431727 92580 None 8 Human Binding pKi = 6.2 6.2 - 1
Binding affinity to PAR2 (unknown origin) assessed as inhibition constantBinding affinity to PAR2 (unknown origin) assessed as inhibition constant
ChEMBL 914 20 6 7 8.0 NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 10.1021/acs.jmedchem.3c01861
126961335 538 None 36 Human Binding pKd = 7.9 7.9 - 1
In a BIACORE assay.In a BIACORE assay.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
9560 538 None 36 Human Binding pKd = 7.9 7.9 - 1
In a BIACORE assay.In a BIACORE assay.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
CHEMBL4128763 538 None 36 Human Binding pKd = 7.9 7.9 - 1
In a BIACORE assay.In a BIACORE assay.
Guide to Pharmacology 570 5 1 6 7.5 N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br 28445455
126961334 540 None 12 Human Binding pKd = 6.5 6.5 - 1
Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
9585 540 None 12 Human Binding pKd = 6.5 6.5 - 1
Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
CHEMBL4127372 540 None 12 Human Binding pKd = 6.5 6.5 - 1
Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.Saturation binding of [<sup>3</sup>H]-AZ8838 antagonist to wild-type PAR2.
Guide to Pharmacology 234 4 2 2 2.6 CCCc1cc(F)ccc1[C@@H](c1ncc[nH]1)O 28445455
3851 63 None 0 Human Binding pKi = 5.4 5.4 - 1
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14976230