Ligand source activities (1 row/activity)



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Ligands Receptor Assay information Chemical information
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name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Potency)		 # tested GPCRs
(Potency)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
44433913 88277 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 88277 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 88337 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 88337 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 88338 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 88338 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 89831 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 89831 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 96679 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 96679 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 145979 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 145979 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 153144 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 153144 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 161257 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 161257 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 156284 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 156284 0 None - 1 Human 7.0 pEC50 = 7 Functional
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 207827 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 208644 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 183169 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 183169 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 183169 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 183169 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 17941 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 17941 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 177112 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 177112 0 None - 1 Human 6.0 pEC50 = 6 Functional
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 186801 0 None - 1 Human 5.0 pEC50 = 5 Functional
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 186801 0 None - 1 Human 5.0 pEC50 = 5 Functional
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 208645 31 None - 1 Human 5.0 pEC50 = 5 Functional
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 96645 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 96645 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 208954 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 210718 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 17941 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 17941 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 177324 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 177324 0 None - 1 Human 5.0 pEC50 = 5.0 Functional
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 207835 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 207836 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 208956 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 180869 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 180869 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 183116 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 175706 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 175706 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 17939 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17939 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17946 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17946 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 183156 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 183156 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 183156 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 208269 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 210768 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177210 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 177210 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 17946 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17946 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17939 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 17939 0 None - 1 Human 4.9 pEC50 = 4.9 Functional
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 58662 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 58662 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 208639 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 210762 0 None - 1 Human 5.9 pEC50 = 5.9 Functional
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 58663 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 58663 0 None - 1 Human 6.9 pEC50 = 6.9 Functional
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 145978 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 145978 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 188488 21 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 188488 21 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 88339 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 88339 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 153145 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 153145 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 168340 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 168340 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 159098 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 159098 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158367 5 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 158367 5 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 210771 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 17942 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 17942 0 None - 1 Human 4.8 pEC50 = 4.8 Functional
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 58663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 58663 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 158854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 158854 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 145979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 145979 0 None - 1 Human 6.8 pEC50 = 6.8 Functional
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 208953 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176612 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 176612 0 None - 1 Human 5.8 pEC50 = 5.8 Functional
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 158854 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 158854 0 None - 1 Human 7.7 pEC50 = 7.7 Functional
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 211090 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 177131 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 177131 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 17938 3 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 17938 3 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 155520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 155520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 17943 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 17943 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 96552 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 96552 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 92095 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 92095 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 153145 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 153145 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 188488 21 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 188488 21 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 17938 3 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 17938 3 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 155520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 155520 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 208640 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 88277 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 88277 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 89831 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 89831 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 17943 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 17943 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 176496 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 176496 0 None - 1 Human 5.7 pEC50 = 5.7 Functional
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 177607 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 177607 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 208719 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 175978 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 175978 0 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 188488 21 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 188488 21 None - 1 Human 7.6 pEC50 = 7.6 Functional
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 88337 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 88337 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 208643 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 183116 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 183116 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 183116 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 17938 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 17938 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 186828 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 186828 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 161257 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 161257 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 58664 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 58664 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 158367 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 158367 5 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 17938 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 17938 3 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 210753 0 None - 1 Human 5.6 pEC50 = 5.6 Functional
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 3565 11 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 3565 11 None - 1 Human 4.6 pEC50 = 4.6 Functional
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 96679 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 96679 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 177588 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 177588 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 207828 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 207838 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 207838 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 208647 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 157369 32 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 157369 32 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 158367 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 158367 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 176886 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 176886 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 58664 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 58664 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 17940 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 17940 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 157369 32 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 157369 32 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 207068 0 None -933254 8 Human 4.5 pEC50 = 4.5 Functional
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 159100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 159100 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 158367 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 158367 5 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 210769 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 176943 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 176943 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 17940 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 17940 0 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 188488 21 None - 1 Human 6.5 pEC50 = 6.5 Functional
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 58665 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 58665 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 183116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 183116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 183116 0 None - 1 Human 5.5 pEC50 = 5.5 Functional
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 88338 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 88338 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 207837 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 153144 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 153144 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 208721 0 None - 1 Human 8.4 pEC50 = 8.4 Functional
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 210745 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 210763 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 210745 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 210763 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 155753 0 None - 1 Human 6.4 pEC50 = 6.4 Functional
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 208645 31 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 208645 31 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 176821 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 176821 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 88317 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 88317 0 None - 1 Human 5.4 pEC50 = 5.4 Functional
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 88341 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 88341 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 176821 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 176821 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 176313 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 176313 0 None - 1 Human 7.3 pEC50 = 7.3 Functional
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 210746 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 210738 0 None - 1 Human 5.3 pEC50 = 5.3 Functional
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 183032 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 183032 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 183032 0 None - 1 Human 6.3 pEC50 = 6.3 Functional
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 168480 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 168480 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 177354 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 177354 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 207830 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 208641 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 208642 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 209092 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 17945 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 17945 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 183201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 183201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 183201 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 156514 0 None - 1 Human 7.2 pEC50 = 7.2 Functional
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 17945 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 17945 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 175979 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 175979 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 176612 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 176612 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 177376 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 177376 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 58666 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 58666 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 212038 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 212038 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 142718 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 142718 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 149107 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 149107 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 150266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 150266 0 None - 1 Human 6.2 pEC50 = 6.2 Functional
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 17944 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 17944 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 183144 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183144 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183144 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158049 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158049 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158137 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158137 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 17944 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 17944 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 186963 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 186963 0 None - 1 Human 5.1 pEC50 = 5.1 Functional
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 158049 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158049 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158137 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 158137 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 88342 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 88342 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 58662 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 58662 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 181218 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 181218 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 183169 0 None - 1 Human 7.1 pEC50 = 7.1 Functional
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 207831 0 None - 1 Human 6.1 pEC50 = 6.1 Functional
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 156284 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 156284 0 None - 1 Human 7.0 pEC50 = 7.0 Functional
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 176819 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 176819 0 None - 1 Human 6.0 pEC50 = 6.0 Functional
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 92093 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 92093 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 171392 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 171392 0 None - 1 Human 7.0 pIC50 = 7 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6 Functional
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 208718 0 None - 1 Human 6.0 pIC50 = 6 Functional
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 146993 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 146993 0 None - 1 Human 5.0 pIC50 = 5 Functional
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 92093 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 92093 0 None - 1 Human 7.0 pIC50 = 7.0 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 1753 11 None - 1 Human 6.0 pIC50 = 6.0 Functional
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 143439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 143439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 143439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 143439 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 208718 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
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 1753 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 1753 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 1753 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 1753 11 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 92094 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 92094 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 150563 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 150563 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92094 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92094 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 150563 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 150563 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 120919 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 120919 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 120921 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 120921 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 171392 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 171392 0 None - 1 Human 8.7 pIC50 = 8.7 Functional
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 18133 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 18133 6 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92093 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 92093 0 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 135905 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 135905 0 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 145192 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 145192 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 145192 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 145192 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 120920 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 120920 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
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 173346 0 None -16 2 Human 5.5 pIC50 = 5.5 Functional
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 173346 0 None -16 2 Human 5.5 pIC50 = 5.5 Functional
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 92091 4 None - 1 Human 4.5 pIC50 = 4.5 Functional
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 92091 4 None - 1 Human 4.5 pIC50 = 4.5 Functional
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 173346 0 None -16 2 Human 5.5 pIC50 = 5.5 Functional
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 173346 0 None -16 2 Human 5.5 pIC50 = 5.5 Functional
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 1753 11 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 1753 11 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 1753 11 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 1753 11 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92093 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92093 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 120922 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 120922 0 None - 1 Human 8.4 pIC50 = 8.4 Functional
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 120922 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 120922 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 92094 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 92094 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 535 5 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 535 5 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 535 5 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 120920 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 120920 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92093 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 92093 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 171392 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 171392 0 None - 1 Human 6.3 pIC50 = 6.3 Functional
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 120920 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 120920 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 120919 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 120919 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 120921 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 120921 0 None - 1 Human 8.3 pIC50 = 8.3 Functional
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 120919 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
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 120919 0 None - 1 Human 4.3 pIC50 = 4.3 Functional
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 120920 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 120920 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 17947 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 17947 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 17947 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 17947 0 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 160967 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 160967 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 92093 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 92093 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 533 31 None 4 2 Human 5.2 pIC50 = 5.2 Functional
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 533 31 None 4 2 Human 5.2 pIC50 = 5.2 Functional
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 533 31 None 4 2 Human 5.2 pIC50 = 5.2 Functional
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 160832 1 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 160832 1 None - 1 Human 4.2 pIC50 = 4.2 Functional
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 58355 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 58355 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92093 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92093 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92093 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 92093 0 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 175414 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 175414 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 92092 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
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 92092 0 None - 1 Human 4.1 pIC50 = 4.1 Functional
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 92093 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 92093 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 144944 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 144944 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 18133 6 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 18133 6 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 175414 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 175414 0 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 144944 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 144944 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 146993 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 146993 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
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 120919 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
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 120919 0 None - 1 Human 4.0 pIC50 = 4.0 Functional
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 532 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 532 0 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 244 0 None - 1 Human 5.2 pEC50 = 5.2 Functional
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 1751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 1751 0 None - 1 Human 6.6 pEC50 = 6.6 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 241 39 None - 1 Human 6.7 pEC50 = 6.7 Functional
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 528 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26819675
25108278 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 238 12 None - 1 Human 7.5 pEC50 = 7.5 Functional
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 2066 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 2066 0 None - 1 Human 7.8 pEC50 = 7.8 Functional
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 2065 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 36527934
126970682 754 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
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 754 0 None - 1 Human 4.8 pIC50 = 4.8 Functional
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 534 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 534 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
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 533 31 None 4 2 Human 7.6 pIC50 = 7.6 Functional
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 533 31 None 4 2 Human 7.6 pIC50 = 7.6 Functional
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 533 31 None 4 2 Human 7.6 pIC50 = 7.6 Functional
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 754 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 754 0 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 535 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 535 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 535 5 None - 1 Human 5.6 pIC50 = 5.6 Functional
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 533 31 None 4 2 Human 8.3 pIC50 = 8.3 Functional
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 533 31 None 4 2 Human 8.3 pIC50 = 8.3 Functional
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 533 31 None 4 2 Human 8.3 pIC50 = 8.3 Functional
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 1931 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 1931 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
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 1931 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 1931 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 535 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 535 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 535 5 None - 1 Human 5.8 pIC50 = 5.8 Functional
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 2937 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 1753 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 1753 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 1753 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 1753 11 None - 1 Human 5.7 pIC50 = 5.7 Functional
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 1930 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 1930 0 None - 1 Human 7.1 pIC50 = 7.1 Functional
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 Receptor Assay information Chemical information
Sel. page Common
name		 GPCRdb ID #Vendors Reference
ligand		 Fold selectivity
(Affinity)		 # tested GPCRs
(Affinity)		 Species p-value
(-log)		 Type Activity
Relation		 Activity
Value		 Assay Type Assay Description Source Mol
weight		 Rot
Bonds		 H don H acc LogP Smiles DOI
CHEMBL2431724 208721 0 None - 0 Human 8.0 pEC50 = 8 Binding
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 92093 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 92093 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 241 39 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 241 39 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 241 39 None - 0 Human 6.7 pEC50 = 6.7 Binding
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 92093 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 92093 0 None - 0 Human 5.7 pEC50 = 5.7 Binding
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 238 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 238 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 238 12 None - 0 Human 7.5 pEC50 = 7.5 Binding
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 208645 31 None - 0 Human 5.3 pEC50 = 5.3 Binding
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 208717 0 None - 0 Human 5.1 pEC50 = 5.1 Binding
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
10395438 188488 21 None - 0 Human 7.0 pIC50 = 7 Binding
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 188488 21 None - 0 Human 7.0 pIC50 = 7 Binding
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 1753 11 None - 0 Human 6.0 pIC50 = 6 Binding
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 1753 11 None - 0 Human 6.0 pIC50 = 6 Binding
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 1753 11 None - 0 Human 6.0 pIC50 = 6 Binding
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 1753 11 None - 0 Human 6.0 pIC50 = 6 Binding
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 136758 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 136758 0 None - 0 Human 6.0 pIC50 = 6 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5 Binding
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 92096 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
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 92096 4 None - 1 Human 6.0 pIC50 = 6.0 Binding
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 1753 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 1753 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 1753 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 1753 11 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 136758 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 136758 0 None - 0 Human 5.9 pIC50 = 5.9 Binding
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 176784 69 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 176784 69 None - 0 Human 7.9 pIC50 = 7.9 Binding
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 208720 0 None - 0 Human 6.9 pIC50 = 6.9 Binding
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 92094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 92094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 92094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 92094 0 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 1753 11 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 1753 11 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 1753 11 None - 0 Human 5.7 pIC50 = 5.7 Binding
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 1753 11 None - 0 Human 5.7 pIC50 = 5.7 Binding
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
107985 176784 69 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 176784 69 None - 0 Human 7.6 pIC50 = 7.6 Binding
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 92094 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 92094 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
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 92094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 92094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 208722 21 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 208723 0 None - 0 Rat 4.3 pIC50 = 4.3 Binding
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 92094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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 92094 0 None - 0 Human 6.3 pIC50 = 6.3 Binding
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
57330164 1753 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
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 1753 11 None - 0 Human 5.0 pIC50 = 5.0 Binding
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 135892 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 135892 0 None - 1 Human 5.7 pKi = 5.7 Binding
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 92096 4 None - 1 Human 6.2 pKi = 6.2 Binding
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 92096 4 None - 1 Human 6.2 pKi = 6.2 Binding
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 135853 0 None - 1 Human 6.2 pKi = 6.2 Binding
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 135853 0 None - 1 Human 6.2 pKi = 6.2 Binding
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
126961335 533 31 None - 1 Human 7.9 pKd = 7.9 Binding
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 533 31 None - 1 Human 7.9 pKd = 7.9 Binding
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 533 31 None - 1 Human 7.9 pKd = 7.9 Binding
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 535 5 None - 1 Human 6.5 pKd = 6.5 Binding
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 535 5 None - 1 Human 6.5 pKd = 6.5 Binding
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 535 5 None - 1 Human 6.5 pKd = 6.5 Binding
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 0 None - 1 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14976230