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 95480 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 95480 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 95540 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 95540 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 95541 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 95541 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 97037 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 97037 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 103902 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 103902 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 153290 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 153290 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 160457 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 160457 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 168585 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 168585 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 163605 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 163605 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 216351 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 217168 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 190530 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 190530 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 190530 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 190530 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 24897 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 24897 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 184465 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 184465 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 194163 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 194163 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 217169 37 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 103867 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 103867 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 217478 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 219244 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 24897 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 24897 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 184677 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 184677 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 216359 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 216360 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 217480 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 188230 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 188230 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 190477 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 190477 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 190477 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 190477 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 190477 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 190477 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 183059 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 183059 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 24895 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 24895 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 24902 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 24902 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 190517 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 190517 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 190517 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 216793 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 219294 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 184563 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 184563 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 24902 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 24902 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 24895 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 24895 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 65744 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 65744 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 217163 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 219288 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 65745 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 65745 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 153289 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 153289 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 195855 26 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 195855 26 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 95542 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 95542 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 160458 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 160458 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 175685 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 175685 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 166424 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 166424 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 165692 11 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 165692 11 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 219297 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 24898 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 24898 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 65745 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 65745 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 166180 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 166180 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 153290 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 153290 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 217477 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 183965 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 183965 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 166180 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 166180 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 219616 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 184484 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 184484 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 24894 6 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 24894 6 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 162840 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 162840 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 7031 41 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 7031 41 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 7031 41 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 24899 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 24899 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 103775 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 103775 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 99302 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 99302 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 160458 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 160458 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 195855 26 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 195855 26 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 24894 6 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 24894 6 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 162840 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 162840 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 7031 41 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 7031 41 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 7031 41 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 7031 41 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 7031 41 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 7031 41 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 217164 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 95480 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 95480 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 97037 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 97037 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 24899 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 24899 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 183849 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 183849 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 184960 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 184960 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 217243 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 183331 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 183331 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 195855 26 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 195855 26 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 95540 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 95540 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 217167 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 190477 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 190477 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 190477 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 24894 6 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 24894 6 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 194190 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 194190 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 168585 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 168585 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 65746 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 65746 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 165692 11 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 165692 11 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 24894 6 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 24894 6 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 219279 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 10394 15 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 10394 15 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 103902 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 103902 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 184941 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 184941 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 7028 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 7028 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 7028 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 7028 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 7028 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 7028 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 216352 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 216362 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 216362 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 195855 26 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 195855 26 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 217171 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 164690 38 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 164690 38 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 165692 11 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 165692 11 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 7028 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 7028 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 7028 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 184239 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 184239 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 65746 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 65746 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 24896 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 24896 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 195855 26 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 195855 26 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 164690 38 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 164690 38 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 215590 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 166426 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 166426 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 165692 11 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 165692 11 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 219295 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 184296 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 184296 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 24896 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 24896 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 195855 26 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 195855 26 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 65747 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 65747 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 190477 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 190477 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 190477 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 95541 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 95541 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 216361 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 160457 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 160457 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 163073 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 163073 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 217245 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 219271 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 219289 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 219271 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 219289 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 163073 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 163073 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 217169 37 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 217169 37 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 184174 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 184174 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 95520 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 95520 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 95544 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 95544 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 184174 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 184174 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 183666 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 183666 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 219272 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 219264 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 190393 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 190393 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 190393 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 175825 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 175825 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 184707 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 184707 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 216354 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 217165 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 217166 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 217616 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 24901 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 24901 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 190562 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 190562 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 190562 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 163835 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 163835 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 163835 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 163835 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 24901 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 24901 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 7034 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 7034 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 7034 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 183332 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 183332 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 183965 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 183965 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 184729 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 184729 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 65748 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 65748 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 220565 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 220565 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 150028 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 150028 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 156418 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 156418 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 157578 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 157578 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 24900 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 24900 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 190505 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 190505 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 190505 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 165374 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 165374 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 165462 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 165462 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 24900 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 24900 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 194325 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 194325 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 165374 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 165374 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 165462 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 165462 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 95545 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 95545 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 190530 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 190530 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 190530 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 190530 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 65744 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 65744 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 190530 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 190530 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 190530 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 190530 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 188579 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 188579 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 190530 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 190530 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 190530 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 190530 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 216355 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 163605 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 163605 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 184172 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 184172 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 99300 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 99300 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 178737 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 178737 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 217242 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 154304 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 154304 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 99300 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 99300 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 150749 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 150749 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 150749 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 150749 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 217242 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 99301 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 99301 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 157874 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 157874 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 99301 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 99301 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 157874 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 157874 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 128211 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 128211 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 128213 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 128213 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 178737 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 178737 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 25089 8 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 25089 8 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 99300 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 99300 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 143206 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 143206 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 152503 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 152503 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 152503 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 152503 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 128212 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 128212 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 180697 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 180697 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 99298 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 99298 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 180697 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 180697 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 99300 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 99300 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 128214 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 128214 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 128214 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 128214 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 99301 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 99301 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 7328 9 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 7328 9 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 7328 9 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 128212 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 128212 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 99300 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 99300 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 178737 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 178737 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 128212 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 128212 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 128211 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 128211 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 128213 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 128213 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 128211 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 128211 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 128212 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 128212 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 24903 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 24903 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 24903 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 24903 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 168293 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 168293 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 99300 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 99300 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 7326 35 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 7326 35 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 7326 35 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 168158 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 168158 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 65437 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 65437 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 99300 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 99300 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 99300 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 99300 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 182766 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 182766 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 99299 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 99299 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 99300 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 99300 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 152255 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 152255 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 25089 8 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 25089 8 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 182766 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 182766 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 152255 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 152255 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 154304 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 154304 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 128211 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 128211 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 7325 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 7325 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 7034 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 7034 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 7034 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 8562 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 8562 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 7031 41 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 7031 41 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 7031 41 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 7321 0 None - 1 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 26819675
25108278 7028 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 7028 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 7028 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 8878 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 8878 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 8877 0 None - 1 Human 7.9 pEC50 = 7.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology None None None None 36527934
126970682 7553 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 7553 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 7327 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 7327 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 7326 35 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 7326 35 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 7326 35 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 7553 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 7553 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 7328 9 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 7328 9 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 7328 9 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 7326 35 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 7326 35 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 7326 35 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 8743 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 8743 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 8743 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 8743 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 7328 9 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 7328 9 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 7328 9 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 9759 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 8742 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 8742 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 217245 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 99300 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 99300 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 7031 41 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 7031 41 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 7031 41 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 99300 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 99300 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 7028 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 7028 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 7028 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 217169 37 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 217241 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
CHEMBL5273903 200563 0 None - 0 Human 9.2 pIC50 = 9.2 Binding
Inhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system methodInhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system method
ChEMBL 509 5 1 6 4.1 CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)[C@H](O)CC(C)(C)C)[C@@H](C)C3)nc12 10.1016/j.ejmech.2021.113867
10395438 195855 26 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 195855 26 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 144060 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 144060 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 99303 6 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 99303 6 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 144060 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 144060 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 184137 73 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 184137 73 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 217244 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 99301 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 99301 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 99301 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 99301 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 184137 73 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 184137 73 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 99301 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 99301 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 99301 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 99301 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 217246 25 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 217247 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 99301 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 99301 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 8564 16 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 8564 16 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 8564 16 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 8564 16 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 143193 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 143193 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 99303 6 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 99303 6 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 143154 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 143154 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 7326 35 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 7326 35 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 7326 35 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 7328 9 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 7328 9 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 7328 9 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 6851 0 None - 1 Human 5.4 pKi = 5.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology None None None None 14976230