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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 | |
CHEMBL115478 | 210960 | None | 0 | Human | Binding | IC50 | = | 280.00 | 6.55 | - | 1 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL115478 | 210960 | None | 0 | Human | Binding | IC50 | = | 12.00 | 7.92 | - | 1 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@@H](CCCN=C(N)N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL116851 | 210994 | None | 0 | Human | Binding | IC50 | = | 14000.00 | 4.85 | - | 1 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(N)=O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL116851 | 210994 | None | 0 | Human | Binding | IC50 | = | 500.00 | 6.30 | - | 1 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](CCCN=C(N)N)C(N)=O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL1169838 | 210996 | None | 0 | Human | Binding | IC50 | = | 1700.00 | 5.77 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1169838 | 210996 | None | 0 | Human | Binding | IC50 | = | 1584.89 | 5.80 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170025 | 210997 | None | 0 | Human | Binding | IC50 | = | 560.00 | 6.25 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170025 | 210997 | None | 0 | Human | Binding | IC50 | = | 501.19 | 6.30 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170026 | 210998 | None | 0 | Human | Binding | IC50 | = | 2000.00 | 5.70 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170026 | 210998 | None | 0 | Human | Binding | IC50 | = | 1995.26 | 5.70 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170027 | 210999 | None | 0 | Human | Binding | IC50 | = | 29000.00 | 4.54 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170027 | 210999 | None | 0 | Human | Binding | IC50 | = | 31622.78 | 4.50 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@H](CC(=O)O)N(C)C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170029 | 211001 | None | 0 | Human | Binding | IC50 | = | 4700.00 | 5.33 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL1170029 | 211001 | None | 0 | Human | Binding | IC50 | = | 5011.87 | 5.30 | - | 2 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | https://dx.doi.org/10.1021/jm1003705 | |
CHEMBL117143 | 211037 | None | 0 | Human | Binding | IC50 | = | 11000.00 | 4.96 | - | 1 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm9806594 | |
CHEMBL117143 | 211037 | None | 0 | Human | Binding | IC50 | = | 11000.00 | 4.96 | - | 1 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL117143 | 211037 | None | 0 | Human | Binding | IC50 | = | 700.00 | 6.16 | - | 1 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL118072 | 211050 | None | 0 | Human | Binding | IC50 | = | 1800.00 | 5.75 | - | 1 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL118072 | 211050 | None | 0 | Human | Binding | IC50 | = | 14000.00 | 4.85 | - | 1 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a | ChEMBL | - | - | - | - | - | CN[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC1CCCCC1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm9800651 | |
CHEMBL127385 | 211131 | None | 0 | Human | Binding | Ki | = | 2100.00 | 5.68 | - | 1 | Inhibitory activity against [125I]-rC5a binding to C5a anaphylatoxin chemotactic receptor in human polymorphonuclear leukocyte (PMNL) membranes | ChEMBL | - | - | - | - | - | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](N)Cc1cccs1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCN=C(N)N)C(=O)O | https://dx.doi.org/10.1021/jm00080a030 |
Showing 1 to 20 of 223 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 | |
AcPhe-Orn-Pro-D-Cha-Trp-Arg | 263 | None | 0 | Human | Functional | pIC50 | = | - | 7.90 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9719594 | |
ACT-1014-6470 | 270 | None | 0 | Human | Functional | pIC50 | = | - | 7.96 | - | 1 | Unclassified | Guide to Pharmacology | 565.2 | 6 | 0 | 4 | 6.62 | Cc1cccc(F)c1N1CCC(N2Cc3cn(CC(C)(F)F)nc3N(Cc3ccccc3C(F)(F)F)C2=O)CC1 | https://pubmed.ncbi.nlm.nih.gov/36285509 | |
avacopan | 527 | None | 0 | Human | Functional | pIC50 | = | - | 9.70 | - | 1 | Unclassified | Guide to Pharmacology | 581.3 | 6 | 2 | 3 | 8.05 | Cc1ccc(NC(=O)[C@H]2CCCN(C(=O)c3c(C)cccc3F)[C@H]2c2ccc(NC3CCCC3)cc2)cc1C(F)(F)F | https://pubmed.ncbi.nlm.nih.gov/27768695 | |
BM213 | 667 | None | 0 | Human | Functional | pEC50 | = | - | 7.23 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/34762432 | |
BM221 | 668 | None | 0 | Human | Functional | pEC50 | = | - | 8.24 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/34762432 | |
C089 | 762 | None | 0 | Human | Functional | pIC50 | = | - | 6.70 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/7930622 | |
C5a | 771 | None | 0 | Human | Functional | pIC50 | = | - | 9.15 | 1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15661745 | |
C5a | 771 | None | 0 | Human | Functional | pIC50 | = | - | 9.15 | 1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10602324 | |
C5a | 771 | None | 0 | Human | Functional | pEC50 | = | - | 8.50 | 1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10602324 | |
C5a | 771 | None | 0 | Human | Functional | pEC50 | = | - | 8.50 | 1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/9881961 | |
C5a des-Arg | 774 | None | 0 | Human | Functional | pIC50 | = | - | 6.30 | -69 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11773063 | |
CHEMBL214024 | 211737 | None | 0 | Human | Functional | IC50 | = | 19.00 | 7.72 | - | 1 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CC#N)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL214456 | 211739 | None | 0 | Human | Functional | IC50 | = | 6900.00 | 5.16 | - | 1 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](C)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL219236 | 211869 | None | 0 | Human | Functional | IC50 | = | 490.00 | 6.31 | - | 1 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL219386 | 211873 | None | 0 | Human | Functional | IC50 | = | 146.00 | 6.84 | - | 1 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | ChEMBL | - | - | - | - | - | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@H]1CCCNC(=O)[C@H](CCC2CCCCC2)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C1=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL2371928 | 212613 | None | 0 | Human | Functional | IC50 | = | 39.00 | 7.41 | 12 | 4 | Antagonist activity at human C5aR in CD88 transfected RBL cells assessed as inhibition of C5a-induced glucosaminidase release | ChEMBL | - | - | - | - | - | CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL2371928 | 212613 | None | 0 | Human | Functional | IC50 | = | 41.00 | 7.39 | 12 | 4 | Antagonist activity at human C5aR expressed in human PMN cells assessed as inhibition of glucosaminidase release | ChEMBL | - | - | - | - | - | CC(C)CC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1CC(=O)NC(=O)N1)C(=O)N[C@@H](Cc1ccc(F)cc1)C(=O)N[C@H](Cc1ccccc1)C(N)=O | https://dx.doi.org/10.1016/j.bmcl.2006.07.036 | |
CHEMBL257128 | 95504 | None | 0 | Human | Functional | IC50 | = | 820.00 | 6.09 | - | 1 | Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization | ChEMBL | 440.3 | 6 | 1 | 3 | 6.93 | CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@H]1CCCc2ccccc21 | https://dx.doi.org/10.1016/j.bmcl.2008.03.049 | |
CHEMBL257128 | 95504 | None | 0 | Human | Functional | IC50 | = | 5500.00 | 5.26 | - | 1 | Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization | ChEMBL | 440.3 | 6 | 1 | 3 | 6.93 | CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@H]1CCCc2ccccc21 | https://dx.doi.org/10.1016/j.bmcl.2008.03.049 | |
CHEMBL257175 | 95518 | None | 0 | Human | Functional | IC50 | = | 1900.00 | 5.72 | - | 1 | Antagonist activity at human C5a receptor in U937 cells assessed as inhibition of anaphylatoxin-induced intracellular calcium mobilization | ChEMBL | 440.3 | 6 | 1 | 3 | 6.93 | CCc1cccc(CC)c1-c1cc(OC)c2c(n1)CCCC2N[C@@H]1CCCc2ccccc21 | https://dx.doi.org/10.1016/j.bmcl.2008.03.049 |
Showing 1 to 20 of 382 entries