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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
2-furoyl-LIGRLO-amide | 63 | None | 0 | Human | Binding | pKi | = | - | 5.40 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/14976230 | |
AC-55541 | 243 | None | 27 | Human | Binding | EC50 | = | 200.00 | 6.70 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay | ChEMBL | 517.1 | 6 | 3 | 5 | 3.70 | C/C(=N\NC(=O)C(NC(=O)c1ccccc1)c1n[nH]c(=O)c2ccccc12)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AC264613 | 240 | None | 8 | Human | Binding | EC50 | = | 30.00 | 7.52 | - | 3 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of cell proliferation after 5 days by beta-galactosidase assay | ChEMBL | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AZ3451 | 538 | None | 36 | Human | Binding | IC50 | = | 23.00 | 7.64 | - | 2 | Antagonist activity at PAR2 (unknown origin) | ChEMBL | 570.1 | 5 | 1 | 6 | 7.46 | C[C@@H](C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | https://dx.doi.org/10.1021/acs.jmedchem.3c01861 | |
AZ3451 | 538 | None | 36 | Human | Binding | pKd | = | - | 7.87 | - | 2 | In a BIACORE assay. | Guide to Pharmacology | 570.1 | 5 | 1 | 6 | 7.46 | C[C@@H](C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
AZ8838 | 540 | None | 12 | Human | Binding | pKd | = | - | 6.46 | - | 1 | Saturation binding of [3H]-AZ8838 antagonist to wild-type PAR2. | Guide to Pharmacology | 234.1 | 4 | 2 | 2 | 2.58 | CCCc1cc(F)ccc1[C@H](O)c1ncc[nH]1 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
CHEMBL238078 | 212849 | None | 34 | Human | Binding | EC50 | = | 5000.00 | 5.30 | - | 1 | Agonist activity at PAR2 (unknown origin) by cell-based assay | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431716 | 92577 | None | 0 | Human | Binding | EC50 | = | 2200.00 | 5.66 | - | 1 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs | ChEMBL | 522.3 | 10 | 2 | 5 | 4.68 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00306 | |
CHEMBL2431716 | 92577 | None | 0 | Human | Binding | EC50 | = | 1995.26 | 5.70 | - | 1 | Agonist activity at human PAR2 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation incubated for 10 mins measured after 2 hrs | ChEMBL | 522.3 | 10 | 2 | 5 | 4.68 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)N1CCC(c2ccccc2)CC1 | https://dx.doi.org/10.1021/acsmedchemlett.6b00306 | |
CHEMBL2431717 | 92578 | None | 0 | Human | Binding | IC50 | = | 4500.00 | 5.35 | - | 1 | Displacement of europium-labeled 2f-LIGRLO-NH2 from human PAR2 expressed in CHO cells after 1 to 2 hrs | ChEMBL | 498.3 | 12 | 3 | 6 | 3.60 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2015.12.048 | |
CHEMBL2431717 | 92578 | None | 0 | Human | Binding | IC50 | = | 1995.26 | 5.70 | - | 1 | 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 assay | ChEMBL | 498.3 | 12 | 3 | 6 | 3.60 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2015.12.048 | |
CHEMBL2431717 | 92578 | None | 0 | Human | Binding | IC50 | = | 1900.00 | 5.72 | - | 1 | 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 assay | ChEMBL | 498.3 | 12 | 3 | 6 | 3.60 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2015.12.048 | |
CHEMBL2431717 | 92578 | None | 0 | Human | Binding | IC50 | = | 501.19 | 6.30 | - | 1 | 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 assay | ChEMBL | 498.3 | 12 | 3 | 6 | 3.60 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2015.12.048 | |
CHEMBL2431717 | 92578 | None | 0 | Human | Binding | IC50 | = | 500.00 | 6.30 | - | 1 | 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 assay | ChEMBL | 498.3 | 12 | 3 | 6 | 3.60 | CC[C@H](C)[C@H](NC(=O)[C@H](CC1CCCCC1)NC(=O)c1ccno1)C(=O)NCc1ccccc1OC | https://dx.doi.org/10.1016/j.bmcl.2015.12.048 | |
CHEMBL2431718 | 212921 | None | 0 | Human | Binding | EC50 | = | 8000.00 | 5.10 | - | 2 | Agonist activity at PAR2 in human platelets by platelet aggregation assay in presence of SFLLRN | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431721 | 212924 | None | 0 | Human | Binding | IC50 | = | 140.00 | 6.85 | - | 1 | Antagonist activity at PAR2 in human neutrophils assessed as inhibition of chemotactic migration of cells towards trypsin/SLIGRL-NH2 | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431724 | 212925 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 1 | Agonist activity at PAR2 in human 16HBE14o- cells assessed as increase in MAPK level | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431725 | 212926 | None | 25 | Rat | Binding | IC50 | = | 50000.00 | 4.30 | - | 1 | Antagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activation | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431726 | 212927 | None | 0 | Rat | Binding | IC50 | = | 50000.00 | 4.30 | - | 1 | Antagonist activity at rat PAR2 expressed in rat KNRK cells assessed as inhibition of trypsin-induced receptor activation | ChEMBL | - | - | - | - | - | 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 | https://dx.doi.org/10.1021/jm400638v | |
CHEMBL2431727 | 92580 | None | 8 | Human | Binding | IC50 | = | 1100.00 | 5.96 | - | 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 assay | ChEMBL | 914.4 | 20 | 6 | 7 | 7.96 | 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 | https://dx.doi.org/10.1021/jm400638v |
Showing 1 to 20 of 37 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
AC-55541 | 243 | None | 27 | Human | Functional | pEC50 | = | - | 6.70 | - | 1 | Unclassified | Guide to Pharmacology | 517.1 | 6 | 3 | 5 | 3.70 | C/C(=N\NC(=O)C(NC(=O)c1ccccc1)c1n[nH]c(=O)c2ccccc12)c1cccc(Br)c1 | https://pubmed.ncbi.nlm.nih.gov/18720984 | |
AC-55541 | 243 | None | 27 | Human | Functional | EC50 | = | 199.53 | 6.70 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | ChEMBL | 517.1 | 6 | 3 | 5 | 3.70 | C/C(=N\NC(=O)C(NC(=O)c1ccccc1)c1n[nH]c(=O)c2ccccc12)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm800754r | |
AC-55541 | 243 | None | 27 | Human | Functional | EC50 | = | 200.00 | 6.70 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis | ChEMBL | 517.1 | 6 | 3 | 5 | 3.70 | C/C(=N\NC(=O)C(NC(=O)c1ccccc1)c1n[nH]c(=O)c2ccccc12)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AC-55541 | 243 | None | 27 | Human | Functional | EC50 | = | 200.00 | 6.70 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay | ChEMBL | 517.1 | 6 | 3 | 5 | 3.70 | C/C(=N\NC(=O)C(NC(=O)c1ccccc1)c1n[nH]c(=O)c2ccccc12)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AC-98170 | 246 | None | 0 | Human | Functional | pEC50 | = | - | 5.20 | - | 1 | Unclassified | Guide to Pharmacology | 327.1 | 4 | 2 | 4 | 2.12 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccs1 | https://pubmed.ncbi.nlm.nih.gov/18720984 | |
AC-98170 | 246 | None | 0 | Human | Functional | EC50 | = | 6309.57 | 5.20 | - | 1 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | ChEMBL | 327.1 | 4 | 2 | 4 | 2.12 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccs1 | https://dx.doi.org/10.1021/jm800754r | |
AC264613 | 240 | None | 8 | Human | Functional | pEC50 | = | - | 7.50 | - | 3 | Unclassified | Guide to Pharmacology | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://pubmed.ncbi.nlm.nih.gov/18720984 | |
AC264613 | 240 | None | 8 | Human | Functional | EC50 | = | 30.00 | 7.52 | - | 3 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as stimulation of phosphatidylinositol hydrolysis after 45 mins by scintillation counting analysis | ChEMBL | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AC264613 | 240 | None | 8 | Human | Functional | EC50 | = | 30.00 | 7.52 | - | 3 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as increase in intracellular calcium level by bioluminescence assay | ChEMBL | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm400638v | |
AC264613 | 240 | None | 8 | Human | Functional | EC50 | = | 31.62 | 7.50 | - | 3 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | ChEMBL | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm800754r | |
AC264613 | 240 | None | 8 | Human | Functional | EC50 | = | 31.62 | 7.50 | - | 3 | Agonist activity at human PAR2 expressed in HEK293T cells assessed as effect on intracellular calcium mobilization by R-SAT assay | ChEMBL | 399.1 | 4 | 2 | 3 | 2.82 | C/C(=N\NC(=O)[C@@H]1C(=O)NC[C@H]1c1ccccc1)c1cccc(Br)c1 | https://dx.doi.org/10.1021/jm800754r | |
AY77 | 533 | None | 0 | Human | Functional | pEC50 | = | - | 7.48 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/26819675 | |
AZ2429 | 537 | None | 0 | Human | Functional | pEC50 | = | - | 6.70 | - | 1 | Determined in an IP1 assay | Guide to Pharmacology | 542.3 | 9 | 3 | 6 | 3.88 | CNC(=O)[C@H]1CCC(NC(=O)[C@H](CC2CCCCC2)NC(=O)c2cn(Cc3ccccc3)nn2)c2ccccc21 | https://pubmed.ncbi.nlm.nih.gov/33335291 | |
AZ3451 | 538 | None | 36 | Human | Functional | pIC50 | = | - | 7.64 | 5 | 2 | Antagonism of SLIGRL-NH2-induced IP1 formation. | Guide to Pharmacology | 570.1 | 5 | 1 | 6 | 7.46 | C[C@@H](C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
AZ3451 | 538 | None | 36 | Human | Functional | IC50 | = | 6600.00 | 5.18 | 5 | 2 | Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay | ChEMBL | 570.1 | 5 | 1 | 6 | 7.46 | C[C@@H](C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | https://dx.doi.org/10.1016/j.bmcl.2018.05.032 | |
AZ3451 | 538 | None | 36 | Human | Functional | pIC50 | = | - | 8.27 | 5 | 2 | In a FLIPR calcium accumulation assay, vs. SLIGRL activation. | Guide to Pharmacology | 570.1 | 5 | 1 | 6 | 7.46 | C[C@@H](C1CCCCC1)n1c(-c2cc3c(cc2Br)OCO3)nc2cc(C(=O)Nc3ccc(C#N)cc3)ccc21 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
AZ7188 | 539 | None | 0 | Human | Functional | pIC50 | = | - | 5.22 | - | 1 | Antagonism of SLIGRL-NH2-induced IP1 formation. | Guide to Pharmacology | 262.1 | 2 | 1 | 1 | 3.43 | O=CN1c2ccccc2CC1c1c[nH]c2ccccc12 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
AZ8838 | 540 | None | 12 | Human | Functional | pIC50 | = | - | 5.64 | - | 1 | In a FLIPR assay measuring SLIGRL-NH2-induced calcium mobilisation. | Guide to Pharmacology | 234.1 | 4 | 2 | 2 | 2.58 | CCCc1cc(F)ccc1[C@H](O)c1ncc[nH]1 | https://pubmed.ncbi.nlm.nih.gov/28445455 | |
AZ8838 | 540 | None | 12 | Human | Functional | IC50 | = | 4200.00 | 5.38 | - | 1 | Antagonist activity at PAR2 in human 1321N1 cells assessed as inhibition of trypsin-induced intracellular calcium flux pretreated for 60 mins followed by trypsin addition by Fluo-8 NW dye based FLIPR assay | ChEMBL | 234.1 | 4 | 2 | 2 | 2.58 | CCCc1cc(F)ccc1[C@H](O)c1ncc[nH]1 | https://dx.doi.org/10.1016/j.bmcl.2018.05.032 | |
AZ8838 | 540 | None | 12 | Human | Functional | pIC50 | = | - | 5.82 | - | 1 | Measuring SLIGRL-NH2-induced IP1 formation | Guide to Pharmacology | 234.1 | 4 | 2 | 2 | 2.58 | CCCc1cc(F)ccc1[C@H](O)c1ncc[nH]1 | https://pubmed.ncbi.nlm.nih.gov/28445455 |
Showing 1 to 20 of 253 entries