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
| |
| CHEMBL217378 | 211834 | None | 0 | Human | Functional | pEC50 | = | 8.9 | 8.9 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5082686 | 217309 | None | 0 | Human | Functional | pEC50 | = | 8.8 | 8.8 | 275 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC[C@@H](C)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5080234 | 217159 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 3 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL217378 | 211834 | None | 0 | Human | Functional | pEC50 | = | 7.9 | 7.9 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL265884 | 213127 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| 44590341 | 179157 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Antagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS bindingAntagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS binding |
ChEMBL | 476 | 8 | 1 | 4 | 5.3 | COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1 | 10.1016/j.bmcl.2008.12.104 | ||
| CHEMBL471412 | 179157 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Antagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS bindingAntagonist activity at human recombinant C5a receptor expressed in HEK cells assessed as inhibition of C5a-induced [35S]GTPgammaS binding |
ChEMBL | 476 | 8 | 1 | 4 | 5.3 | COc1ccc(N(C(=O)c2ccccc2)C(C(=O)NC2CCCC2)c2ccccc2F)c(OC)c1 | 10.1016/j.bmcl.2008.12.104 | ||
| CHEMBL5078171 | 217027 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 436 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5083558 | 217359 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL427936 | 215856 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5085196 | 217444 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | 3 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@H](C)NC(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5081287 | 217227 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | -30 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](C)N)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL262653 | 213003 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5092578 | 217866 | None | 0 | Human | Functional | pEC50 | = | 8.6 | 8.6 | 295 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CCC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL269480 | 213248 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL429535 | 215999 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL412680 | 215475 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5071478 | 216747 | None | 8 | Mouse | Functional | pEC50 | = | 4.6 | 4.6 | -389 | 3 | Agonist activity at C5aR1 in mouse RAW264.7 cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at C5aR1 in mouse RAW264.7 cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL268322 | 213205 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL5075364 | 216858 | None | 0 | Mouse | Functional | pEC50 | = | 5.6 | 5.6 | -398 | 3 | Agonist activity at C5aR1 in mouse RAW264.7 cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at C5aR1 in mouse RAW264.7 cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5076900 | 216956 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | -2 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](N)Cc1ccccc1)[C@@H](C)O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL414361 | 215587 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL408796 | 215193 | None | 0 | Human | Functional | pEC50 | = | 4.6 | 4.6 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL408796 | 215193 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL265884 | 213127 | None | 0 | Human | Functional | pEC50 | = | 4.5 | 4.5 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL5092461 | 217860 | None | 0 | Human | Functional | pEC50 | = | 7.5 | 7.5 | 2041 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5080381 | 217169 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | 47 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL406011 | 215052 | None | 2 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5080181 | 217156 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | 3 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5093227 | 217907 | None | 0 | Human | Functional | pEC50 | = | 8.4 | 8.4 | 99 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL406011 | 215052 | None | 2 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL438728 | 216251 | None | 0 | Human | Functional | pEC50 | = | 5.4 | 5.4 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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](Cc1ccccc1)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL412680 | 215475 | None | 0 | Human | Functional | pEC50 | = | 4.4 | 4.4 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5081621 | 217244 | None | 0 | Human | Functional | pEC50 | = | 7.4 | 7.4 | -4 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5087896 | 217615 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(N)=O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL414361 | 215587 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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)N1CCC[C@@H]1C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL386427 | 214842 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL269480 | 213248 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL5075364 | 216858 | None | 0 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 398 | 3 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC[C@H](NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccccc1)NC(C)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL435318 | 216125 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL405966 | 215049 | None | 0 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL406011 | 215052 | None | 2 | Human | Functional | pEC50 | = | 4.3 | 4.3 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | None | 10.1021/jm00018a028 | ||||
| CHEMBL412249 | 215441 | None | 0 | Human | Functional | pEC50 | = | 5.3 | 5.3 | - | 1 | Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN)Ability to induce shape change (polarization) in human polymorphonuclear leukocytes (PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL429535 | 215999 | None | 0 | Human | Functional | pEC50 | = | 4.2 | 4.2 | - | 1 | Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN)Release of beta-glucuronidase from human polymorphonuclear leukocytes(PMN) |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=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](CCCN=C(N)N)C(=O)O | 10.1021/jm00018a028 | ||||
| CHEMBL5071478 | 216747 | None | 8 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 389 | 3 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5075511 | 216869 | None | 0 | Human | Functional | pEC50 | = | 6.2 | 6.2 | - | 1 | Agonist activity at C5aR1 in human MDM cells assessed as induction of intracellular calcium mobilization pretreated with antagonist PMX53 for 30 mins followed by compound treatment for 10 mins by Fluo-4 dye based assayAgonist activity at C5aR1 in human MDM cells assessed as induction of intracellular calcium mobilization pretreated with antagonist PMX53 for 30 mins followed by compound treatment for 10 mins by Fluo-4 dye based assay |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H](N)Cc1ccccc1)C(=O)N[C@@H](C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.1c01174 | ||||
| CHEMBL5087237 | 217570 | None | 0 | Human | Functional | pEC50 | = | 8.2 | 8.2 | 446 | 2 | Agonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assayAgonist activity at human C5aR1 expressed in CHO cells assessed as induction of ERK1/2 phosphorylation at Thr202/Tyr204 residues incubated for 10 mins by AlphaLISA assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCCN)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C(=O)N[C@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)C(C)C | 10.1021/acs.jmedchem.1c01174 | ||||
| 1599 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -354 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
| 3955 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -354 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
| 3955.0 | 2341 | None | 28 | Human | Functional | pEC50 | = | 6.2 | 6.2 | -354 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
Showing 1 to 50 of 686 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
| |
| 44589819 | 185939 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 455 | 7 | 0 | 3 | 5.9 | CC(C)Cc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL486749 | 185939 | None | 0 | Human | Binding | pIC50 | = | 8.8 | 8.8 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 455 | 7 | 0 | 3 | 5.9 | CC(C)Cc1ccccc1C(=O)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.106 | ||
| 44383980 | 60000 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937 |
ChEMBL | 359 | 7 | 2 | 2 | 4.7 | C/N=C(/N)Nc1ccc(OCCCc2ccccc2)c(-c2ccccc2)c1 | 10.1016/S0960-894X(97)00124-8 | ||
| CHEMBL173394 | 60000 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937 |
ChEMBL | 359 | 7 | 2 | 2 | 4.7 | C/N=C(/N)Nc1ccc(OCCCc2ccccc2)c(-c2ccccc2)c1 | 10.1016/S0960-894X(97)00124-8 | ||
| 44384139 | 60012 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937 |
ChEMBL | 351 | 6 | 2 | 2 | 5.1 | C/N=C(/N)Nc1ccc(OCCC2CCCCC2)c(-c2ccccc2)c1 | 10.1016/S0960-894X(97)00124-8 | ||
| CHEMBL173442 | 60012 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937Binding affinity against C5a anaphylatoxin chemotactic receptor assayed on human monocyte cell line U937 |
ChEMBL | 351 | 6 | 2 | 2 | 5.1 | C/N=C(/N)Nc1ccc(OCCC2CCCCC2)c(-c2ccccc2)c1 | 10.1016/S0960-894X(97)00124-8 | ||
| 44589629 | 186065 | None | 9 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 490 | 10 | 0 | 3 | 6.1 | COc1ccc(CCCN2CCC(N(CCc3ccc(Cl)cc3)C(=O)c3ccccc3)CC2)cc1 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL486959 | 186065 | None | 9 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 490 | 10 | 0 | 3 | 6.1 | COc1ccc(CCCN2CCC(N(CCc3ccc(Cl)cc3)C(=O)c3ccccc3)CC2)cc1 | 10.1016/j.bmcl.2008.08.106 | ||
| 44589782 | 194497 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 429 | 6 | 0 | 4 | 4.7 | COc1cccc(C(=O)N(CCc2ccc(Cl)cc2)C2CCC3(CC2)OCCO3)c1 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL528767 | 194497 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 429 | 6 | 0 | 4 | 4.7 | COc1cccc(C(=O)N(CCc2ccc(Cl)cc2)C2CCC3(CC2)OCCO3)c1 | 10.1016/j.bmcl.2008.08.106 | ||
| 44308973 | 206366 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 497 | 9 | 4 | 5 | 1.9 | N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCN(c3ccccc3)CC2)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL69007 | 206366 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 497 | 9 | 4 | 5 | 1.9 | N=C(N)NCCC[C@H]1NC(=O)N([C@H](CC2CCCCC2)C(=O)N2CCN(c3ccccc3)CC2)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL291792 | 213342 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | None | None | None | NC(N)=NCC[C@@H]1NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@@H](CC2CCCCC2)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@@H](N)Cc2ccccc2)CNC1=O | 10.1021/jm9806594 | ||||
| 579 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2006.07.036 | ||||
| 6918468 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2006.07.036 | ||||
| CHEMBL41547 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells |
ChEMBL | None | None | None | None | 10.1016/j.bmcl.2006.07.036 | ||||
| 44589863 | 179109 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 450 | 5 | 0 | 4 | 5.3 | O=C(c1cccc2cnccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL471009 | 179109 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 450 | 5 | 0 | 4 | 5.3 | O=C(c1cccc2cnccc12)N(CCc1ccc(Cl)cc1)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL117143 | 211037 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) |
ChEMBL | None | None | None | 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 | 10.1021/jm9800651 | ||||
| CHEMBL117143 | 211037 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | None | None | None | 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 | 10.1021/jm9806594 | ||||
| 44309233 | 103876 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 566 | 8 | 4 | 4 | 3.4 | N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2cccc3ccccc23)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL309154 | 103876 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 566 | 8 | 4 | 4 | 3.4 | N=C(N)NCCC[C@H]1NC(=O)N([C@H](Cc2cccc3ccccc23)C(=O)N2CCC3(CCc4ccccc43)CC2)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL2371928 | 212613 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of C5a binding to human C5aR expressed in HEK293 cellsInhibition of C5a binding to human C5aR expressed in HEK293 cells |
ChEMBL | None | None | None | 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 | 10.1016/j.bmcl.2006.07.036 | ||||
| CHEMBL115478 | 210960 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a |
ChEMBL | None | None | None | 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 | 10.1021/jm9800651 | ||||
| 44581545 | 189537 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 499 | 7 | 0 | 5 | 5.9 | COCC(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| CHEMBL513344 | 189537 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 499 | 7 | 0 | 5 | 5.9 | COCC(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| 118719110 | 115506 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | 2082 | 70 | 27 | 26 | -1.2 | CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[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)C(C)C | 10.1021/jm9806594 | ||
| CHEMBL3350746 | 115506 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | 2082 | 70 | 27 | 26 | -1.2 | CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[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)C(C)C | 10.1021/jm9806594 | ||
| 56658522 | 63225 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations |
ChEMBL | 482 | 8 | 3 | 4 | 1.9 | CC[C@@H](C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL1790511 | 63225 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Tested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparationsTested for its ability to compete with [125I]C5a for binding to C5a anaphylatoxin chemotactic receptor of human neutrophil membrane preparations |
ChEMBL | 482 | 8 | 3 | 4 | 1.9 | CC[C@@H](C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| 44309496 | 164162 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 468 | 7 | 3 | 4 | 1.5 | CC(C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| CHEMBL420926 | 164162 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Tested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparationsTested for the ability to compete with [125I]-CO13 ([125I]-Y-F-K-A-Cha-G-L-dF-R) for binding to C5a anaphylatoxin chemotactic receptor from human neutrophil membrane preparations |
ChEMBL | 468 | 7 | 3 | 4 | 1.5 | CC(C)[C@H](C(=O)N1CCC2(CCc3ccccc32)CC1)N1C(=O)N[C@H](CCCN=C(N)N)C1=O | 10.1016/S0960-894X(96)00606-3 | ||
| 118719110 | 115506 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | 2082 | 70 | 27 | 26 | -1.2 | CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[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)C(C)C | 10.1021/jm9806594 | ||
| CHEMBL3350746 | 115506 | None | 0 | Human | Binding | pIC50 | = | 5.9 | 5.9 | - | 0 | Inhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptorInhibition of binding of [125I]C5a to human polymorphonuclear leukocyte C5a receptor |
ChEMBL | 2082 | 70 | 27 | 26 | -1.2 | CC(C)[C@H](NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H](N)CCCCN)C(=O)N[C@H](C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(=O)NCCCCC(=O)N[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)C(C)C | 10.1021/jm9806594 | ||
| 25110775 | 190834 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 407 | 5 | 1 | 2 | 5.5 | O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1 | 10.1016/j.bmcl.2008.08.101 | ||
| CHEMBL518254 | 190834 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 407 | 5 | 1 | 2 | 5.5 | O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1 | 10.1016/j.bmcl.2008.08.101 | ||
| 25110775 | 190834 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 407 | 5 | 1 | 2 | 5.5 | O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1 | 10.1016/j.bmcl.2008.08.106 | ||
| CHEMBL518254 | 190834 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cellsDisplacement of [125I]r-hC5a from C5a receptor in cAMP differentiated human U937 cells |
ChEMBL | 407 | 5 | 1 | 2 | 5.5 | O=C(c1cccc2ccccc12)N(CCc1ccc(Cl)cc1)[C@H]1CC[C@H](O)CC1 | 10.1016/j.bmcl.2008.08.106 | ||
| 25193057 | 178831 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 506 | 7 | 0 | 4 | 5.8 | CN(C)CC(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| CHEMBL468430 | 178831 | None | 0 | Human | Binding | pIC50 | = | 7.9 | 7.9 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 506 | 7 | 0 | 4 | 5.8 | CN(C)CC(Cc1ccc(Cl)cc1)N(C(=O)c1cccc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| CHEMBL116851 | 210994 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | 50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs)50% reduction in binding of [125I]C5a to human polymorphonuclear cells (PMNs) |
ChEMBL | None | None | None | 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 | 10.1021/jm9800651 | ||||
| CHEMBL118072 | 211050 | None | 0 | Human | Binding | pIC50 | = | 4.9 | 4.9 | - | 0 | 50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a50% reduction in myeloperoxidase secretion from human PMNs mediated by 100 nM C5a |
ChEMBL | None | None | None | 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 | 10.1021/jm9800651 | ||||
| 1351023 | 202563 | None | 11 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr |
ChEMBL | 443 | 5 | 0 | 3 | 4.8 | Cc1ccc(S(=O)(=O)N(C)c2ccc(Br)cc2C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2009.11.058 | ||
| CHEMBL596055 | 202563 | None | 11 | Human | Binding | pIC50 | = | 4.8 | 4.8 | - | 0 | Displacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hrDisplacement of [125I]human anaphylatoxin C5a from human C5a receptor expressed in CHO cells co-expressed with Galpha16 after 1 hr |
ChEMBL | 443 | 5 | 0 | 3 | 4.8 | Cc1ccc(S(=O)(=O)N(C)c2ccc(Br)cc2C(=O)c2ccccc2)cc1 | 10.1016/j.bmcl.2009.11.058 | ||
| 579 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
| 6918468 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
| CHEMBL41547 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
| 44581482 | 189729 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 513 | 6 | 0 | 6 | 5.5 | COC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| CHEMBL514872 | 189729 | None | 0 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assayDisplacement of [125I]C5a from C5a receptor in cAMP differentiated human U937 cells by filtration assay |
ChEMBL | 513 | 6 | 0 | 6 | 5.5 | COC(=O)C(Cc1ccc(Cl)cc1)N(C(=O)c1csc2ccccc12)C1CCC2(CC1)OCCO2 | 10.1016/j.bmcl.2008.08.101 | ||
| 579 | 3144 | None | 18 | Human | Binding | pIC50 | = | 7.8 | 7.8 | - | 0 | Displacement of [125I-C5a] from C5a receptor in human PBMC by scintillation countingDisplacement of [125I-C5a] from C5a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
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