Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 44433913 | 88739 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 788 | 25 | 10 | 9 | 0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL236037 | 88739 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 788 | 25 | 10 | 9 | 0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cccnc1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433903 | 88799 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 827 | 25 | 10 | 9 | 1.5 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL236292 | 88799 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 827 | 25 | 10 | 9 | 1.5 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2o1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433904 | 88800 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 837 | 25 | 10 | 8 | 1.9 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL236293 | 88800 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 837 | 25 | 10 | 8 | 1.9 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccc2ccccc2c1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433916 | 90296 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 777 | 25 | 10 | 10 | -0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL238396 | 90296 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 777 | 25 | 10 | 10 | -0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccno1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433914 | 97180 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 789 | 25 | 10 | 10 | -0.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL267729 | 97180 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 789 | 25 | 10 | 10 | -0.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cnccn1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433917 | 146600 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 792 | 25 | 10 | 10 | 0.1 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL392253 | 146600 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 792 | 25 | 10 | 10 | 0.1 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1coc(C)n1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433905 | 153767 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 842 | 25 | 10 | 9 | 2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL398128 | 153767 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 842 | 25 | 10 | 9 | 2.0 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1cc2ccccc2s1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 44433912 | 161900 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 788 | 25 | 10 | 9 | 0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL414319 | 161900 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium releaseAgonist activity at PAR2 in human HT-29 cells assessed as increase in intracellular calcium release |
ChEMBL | 788 | 25 | 10 | 9 | 0.2 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccccn1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||
| 137638214 | 156918 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay |
ChEMBL | 435 | 11 | 4 | 6 | 0.9 | CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O | 10.1021/acsmedchemlett.5b00429 | ||
| CHEMBL4071278 | 156918 | None | 0 | Human | Functional | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assayAgonist activity at human PAR2 expressed in CHO cells assessed as induction of intracellular calcium release measured for 300 secs by Fluo-3 AM dye-based fluorescence assay |
ChEMBL | 435 | 11 | 4 | 6 | 0.9 | CC[C@H](C)[C@H](NC(=O)C(CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCC(N)=O | 10.1021/acsmedchemlett.5b00429 | ||
| CHEMBL235440 | 212031 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| CHEMBL238015 | 212848 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCc1ccccc1)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| 162670571 | 183857 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1470 | 51 | 12 | 25 | -0.6 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4791973 | 183857 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1470 | 51 | 12 | 25 | -0.6 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4793975 | 183857 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1470 | 51 | 12 | 25 | -0.6 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4803771 | 183857 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in HUVEC cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1470 | 51 | 12 | 25 | -0.6 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| 49788381 | 18132 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release |
ChEMBL | 608 | 13 | 4 | 7 | 3.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 | 10.1021/jm100984y | ||
| CHEMBL1269137 | 18132 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release |
ChEMBL | 608 | 13 | 4 | 7 | 3.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 | 10.1021/jm100984y | ||
| 156016097 | 177791 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay |
ChEMBL | 398 | 8 | 3 | 5 | 2.2 | NC(=O)c1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 | 10.1021/acsmedchemlett.0c00154 | ||
| CHEMBL4641856 | 177791 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay |
ChEMBL | 398 | 8 | 3 | 5 | 2.2 | NC(=O)c1ccccc1CNC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 | 10.1021/acsmedchemlett.0c00154 | ||
| 25108280 | 187490 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay |
ChEMBL | 399 | 4 | 2 | 3 | 2.8 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccccc1Br | 10.1021/jm800754r | ||
| CHEMBL493494 | 187490 | None | 0 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay |
ChEMBL | 399 | 4 | 2 | 3 | 2.8 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1ccccc1Br | 10.1021/jm800754r | ||
| CHEMBL238078 | 212849 | None | 34 | Human | Functional | pEC50 | = | 5 | 5.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O | 10.1021/jm800754r | ||||
| 44433910 | 97145 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | 767 | 26 | 10 | 8 | 0.5 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(C)C)[C@@H](C)CC)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||
| CHEMBL267389 | 97145 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | 767 | 26 | 10 | 8 | 0.5 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)CC(C)C)[C@@H](C)CC)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||
| CHEMBL266796 | 213158 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](Cc1cccnc1)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| CHEMBL393243 | 214925 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1cccc2ccccc12)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| 49788381 | 18132 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release |
ChEMBL | 608 | 13 | 4 | 7 | 3.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 | 10.1021/jm100984y | ||
| CHEMBL1269137 | 18132 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium releaseAgonist activity at PAR2 receptor in human HT-29 cells assessed as induction of intracellular calcium release |
ChEMBL | 608 | 13 | 4 | 7 | 3.4 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccc(C(=O)N2CCC(CN)CC2)cc1 | 10.1021/jm100984y | ||
| 156018833 | 178003 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay |
ChEMBL | 398 | 8 | 3 | 5 | 2.4 | NC(=O)Cc1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 | 10.1021/acsmedchemlett.0c00154 | ||
| CHEMBL4644870 | 178003 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as induction of Galphaq-stimulated IP1 formation incubated for 2 hrs by FRET assay |
ChEMBL | 398 | 8 | 3 | 5 | 2.4 | NC(=O)Cc1ccccc1NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1 | 10.1021/acsmedchemlett.0c00154 | ||
| CHEMBL236457 | 212039 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| CHEMBL236681 | 212040 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)[C@@H](C)CC)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| CHEMBL266812 | 213160 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium releaseAgonist activity at PAR2 expressed in human HT29 cells assessed as intracellular calcium release |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccc(O)cc1)C(N)=O | 10.1016/j.bmcl.2007.08.026 | ||||
| 162661352 | 181557 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1255 | 45 | 6 | 21 | 6.0 | COc1ccnc(NCCCOc2ccc(C[C@@H](CC(=O)O)NC(=O)c3ccc(OCc4cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC5CCCCC5)NC(=O)c5ccno5)C5CCCCC5)nn4)cc3)cc2)c1 | 10.1039/d0md00098a | ||
| CHEMBL4764373 | 181557 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 1255 | 45 | 6 | 21 | 6.0 | COc1ccnc(NCCCOc2ccc(C[C@@H](CC(=O)O)NC(=O)c3ccc(OCc4cn(CCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC5CCCCC5)NC(=O)c5ccno5)C5CCCCC5)nn4)cc3)cc2)c1 | 10.1039/d0md00098a | ||
| 162659655 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4763124 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4803166 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization preincubated for 2 hrs with LPS and 30 mins with cRGD followed by compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| 162659655 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4763124 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
| CHEMBL4803166 | 183804 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assayAgonist activity at PAR2 in human EA.hy926 cells assessed as stimulation of calcium mobilization treated with cRGD for 30 mins prior to compound addition by Fluo-4-AM dye-based FLIPR assay |
ChEMBL | 2042 | 90 | 12 | 38 | -0.3 | N=C(N)NCCC[C@@H]1NC[C@H](Cc2cn(CCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCNC(=O)[C@@H](NC(=O)[C@H](CC3CCCCC3)NC(=O)c3ccno3)C3CCCCC3)nn2)NC(=O)[C@@H](Cc2ccccc2)NC(=O)[C@H](CC(=O)O)NC(=O)CNC1=O | 10.1039/d0md00098a | ||
Showing 1 to 50 of 499 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| CHEMBL2431724 | 212925 | None | 0 | Human | Binding | pEC50 | = | 8 | 8.0 | - | 0 | Agonist activity at PAR2 in human 16HBE14o- cells assessed as increase in MAPK levelAgonist activity at PAR2 in human 16HBE14o- cells assessed as increase in MAPK level |
ChEMBL | None | None | None | CCCCCCCCCCCCCCCC(=O)OCCOCCOCCNCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)c1csc(N)n1)[C@@H](C)CC)C(N)=O | 10.1021/jm400638v | ||||
| 56640042 | 92577 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs |
ChEMBL | 522 | 10 | 2 | 5 | 4.7 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | 10.1021/acsmedchemlett.6b00306 | ||
| CHEMBL2431716 | 92577 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs |
ChEMBL | 522 | 10 | 2 | 5 | 4.7 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | 10.1021/acsmedchemlett.6b00306 | ||
| 9456 | 243 | None | 27 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 517 | 6 | 3 | 5 | 3.7 | Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C | 10.1021/jm400638v | ||
| 9589606 | 243 | None | 27 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 517 | 6 | 3 | 5 | 3.7 | Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C | 10.1021/jm400638v | ||
| CHEMBL493076 | 243 | None | 27 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 517 | 6 | 3 | 5 | 3.7 | Brc1cccc(c1)/C(=N/NC(=O)C(c1n[nH]c(=O)c2c1cccc2)NC(=O)c1ccccc1)/C | 10.1021/jm400638v | ||
| 56640042 | 92577 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs |
ChEMBL | 522 | 10 | 2 | 5 | 4.7 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | 10.1021/acsmedchemlett.6b00306 | ||
| CHEMBL2431716 | 92577 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrsAgonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs |
ChEMBL | 522 | 10 | 2 | 5 | 4.7 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | 10.1021/acsmedchemlett.6b00306 | ||
| 25108278 | 240 | None | 8 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 2 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 399 | 4 | 2 | 3 | 2.8 | Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C | 10.1021/jm400638v | ||
| 9460 | 240 | None | 8 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 2 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 399 | 4 | 2 | 3 | 2.8 | Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C | 10.1021/jm400638v | ||
| CHEMBL494502 | 240 | None | 8 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 2 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assayAgonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay |
ChEMBL | 399 | 4 | 2 | 3 | 2.8 | Brc1cccc(c1)/C(=N/NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)/C | 10.1021/jm400638v | ||
| CHEMBL238078 | 212849 | None | 34 | Human | Binding | pEC50 | = | 5.3 | 5.3 | - | 0 | Agonist activity at PAR2 (unknown origin) by cell-based assayAgonist activity at PAR2 (unknown origin) by cell-based assay |
ChEMBL | None | None | None | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](N)CO)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(N)=O | 10.1021/jm400638v | ||||
| CHEMBL2431718 | 212921 | None | 0 | Human | Binding | pEC50 | = | 5.1 | 5.1 | - | 0 | Agonist activity at PAR2 in human platelets by platelet aggregation assay in presence of SFLLRNAgonist activity at PAR2 in human platelets by platelet aggregation assay in presence of SFLLRN |
ChEMBL | None | None | None | CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CS)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](C)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O)C(C)C | 10.1021/jm400638v | ||||
| 117991201 | 193892 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Inhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system methodInhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system method |
ChEMBL | 509 | 5 | 1 | 6 | 4.1 | CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)[C@H](O)CC(C)(C)C)[C@@H](C)C3)nc12 | 10.1016/j.ejmech.2021.113867 | ||
| CHEMBL5273903 | 193892 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | Inhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system methodInhibition of PAR2 expressed in human HT-29 cells incubated for 30 mins by FLIPR Tetra system method |
ChEMBL | 509 | 5 | 1 | 6 | 4.1 | CC(C)c1cc(-c2ccc(F)cc2)nn2cc(C(=O)N3CCN(C(=O)[C@H](O)CC(C)(C)C)[C@@H](C)C3)nc12 | 10.1016/j.ejmech.2021.113867 | ||
| 10395438 | 189185 | None | 25 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysis |
ChEMBL | 777 | 26 | 11 | 10 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O | 10.1021/jm400638v | ||
| CHEMBL509819 | 189185 | None | 25 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysisDisplacement of [3H]-2-furoyl-LIGRL-NH2 from human PAR2 expressed in human NCTC-2544 cells after 60 mins by scintillation counting analysis |
ChEMBL | 777 | 26 | 11 | 10 | -0.9 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(=O)c1ccco1)C(=O)NCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCN)C(N)=O | 10.1021/jm400638v | ||
| 57330164 | 1783 | None | 20 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 6658 | 1783 | None | 20 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 73755230 | 1783 | None | 20 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL2431617 | 1783 | None | 20 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 71511553 | 137369 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 540 | 14 | 3 | 6 | 4.8 | CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL3752235 | 137369 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 540 | 14 | 3 | 6 | 4.8 | CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC | 10.1016/j.bmcl.2015.12.048 | ||
| 57330164 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 6658 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 73755230 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL2431617 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 11557006 | 92580 | None | 8 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assay |
ChEMBL | 914 | 20 | 6 | 7 | 8.0 | NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 | 10.1021/jm400638v | ||
| CHEMBL2431727 | 92580 | None | 8 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 1 | Antagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human NCTC-2544 cells assessed as inhibition of SLIGKV-NH2-induced NFkappaB activation preincubated for 15 to 30 mins followed by SLIGKV-NH2 addition measured after 6 hrs by luciferase reporter gene assay |
ChEMBL | 914 | 20 | 6 | 7 | 8.0 | NCCCC[C@H](NC(=O)CNC(=O)Nc1ccc2c(c1)c(CN1CCCC1)cn2Cc1c(Cl)cccc1Cl)C(=O)N[C@@H](Cc1ccccc1)C(=O)NC(c1ccccc1)c1ccccc1 | 10.1021/jm400638v | ||
| 57330164 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 6658 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 73755230 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL2431617 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmcl.2015.12.048 | ||
| 71511553 | 137369 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 540 | 14 | 3 | 6 | 4.8 | CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL3752235 | 137369 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of 2f-LIGRLO-NH2-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 540 | 14 | 3 | 6 | 4.8 | CCC(C)Oc1ccccc1CNC(=O)[C@@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)[C@@H](C)CC | 10.1016/j.bmcl.2015.12.048 | ||
| 107985 | 177463 | None | 47 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay |
ChEMBL | 360 | 1 | 1 | 6 | 1.1 | CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O | 10.1021/jm400638v | ||
| CHEMBL463763 | 177463 | None | 47 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Antagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assayAntagonist activity at human PAR2 expressed in human A549 cells assessed as inhibition of 2f-LIGRLO-NH2-induced NFkappaB activation by luciferase reporter gene assay |
ChEMBL | 360 | 1 | 1 | 6 | 1.1 | CC(C)[C@]12O[C@H]1[C@@H]1O[C@@]13[C@@]1(C)CCC4=C(COC4=O)[C@@H]1C[C@@H]1O[C@@]13[C@@H]2O | 10.1021/jm400638v | ||
| CHEMBL2431721 | 212924 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Antagonist activity at PAR2 in human neutrophils assessed as inhibition of chemotactic migration of cells towards trypsin/SLIGRL-NH2Antagonist activity at PAR2 in human neutrophils assessed as inhibition of chemotactic migration of cells towards trypsin/SLIGRL-NH2 |
ChEMBL | None | None | None | CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(=O)O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CO)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)O)[C@@H](C)CC | 10.1021/jm400638v | ||||
| 56639666 | 92578 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 498 | 12 | 3 | 6 | 3.6 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL2431717 | 92578 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 498 | 12 | 3 | 6 | 3.6 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | 10.1016/j.bmcl.2015.12.048 | ||
| 56639666 | 92578 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 498 | 12 | 3 | 6 | 3.6 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | 10.1016/j.bmcl.2015.12.048 | ||
| CHEMBL2431717 | 92578 | None | 0 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assayAntagonist activity at PAR2 in human HT-29 cells assessed as inhibition of trypsin-induced ca2+ release preincubated for 15 mins measured after 1 hr by FLIPR assay |
ChEMBL | 498 | 12 | 3 | 6 | 3.6 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | 10.1016/j.bmcl.2015.12.048 | ||
| 57330164 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin) |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmc.2015.11.016 | ||
| 6658 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin) |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmc.2015.11.016 | ||
| 73755230 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin) |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmc.2015.11.016 | ||
| CHEMBL2431617 | 1783 | None | 20 | Human | Binding | pIC50 | = | 5.7 | 5.7 | - | 0 | Antagonist activity at protease-activated receptor 2 (unknown origin)Antagonist activity at protease-activated receptor 2 (unknown origin) |
ChEMBL | 546 | 9 | 2 | 5 | 4.9 | CC[C@H]([C@@H](C(=O)N1CCC2(CC1)C=Cc1c2cccc1)NC(=O)[C@@H](NC(=O)c1ccno1)CC1CCCCC1)C | 10.1016/j.bmc.2015.11.016 | ||
| 126961335 | 538 | None | 36 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 1 | Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin) |
ChEMBL | 570 | 5 | 1 | 6 | 7.5 | N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br | 10.1021/acs.jmedchem.3c01861 | ||
| 9560 | 538 | None | 36 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 1 | Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin) |
ChEMBL | 570 | 5 | 1 | 6 | 7.5 | N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br | 10.1021/acs.jmedchem.3c01861 | ||
| CHEMBL4128763 | 538 | None | 36 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 1 | Antagonist activity at PAR2 (unknown origin)Antagonist activity at PAR2 (unknown origin) |
ChEMBL | 570 | 5 | 1 | 6 | 7.5 | N#Cc1ccc(cc1)NC(=O)c1ccc2c(c1)nc(n2[C@H](C1CCCCC1)C)c1cc2OCOc2cc1Br | 10.1021/acs.jmedchem.3c01861 | ||
| 134819117 | 196746 | None | 4 | Human | Binding | pIC50 | = | 7.6 | 7.6 | - | 0 | Antagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cellsAntagonist activity at PAR2 (unknown origin) expressed in human 1321N1 cells |
ChEMBL | 570 | 5 | 1 | 6 | 7.5 | CC(C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | 10.1016/j.ejmech.2022.115079 | ||
Showing 1 to 50 of 82 entries