Ligand source activities (1 row/activity)
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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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
| |
CHEMBL2064011 | 211630 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@H](C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O | 10.1021/jm201609k | ||||
CHEMBL1170042 | 211007 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170045 | 211010 | None | 0 | Human | Functional | pEC50 | = | 6 | 6.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)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/jm1003705 | ||||
CHEMBL1170640 | 211030 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170231 | 211017 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O | 10.1021/jm1003705 | ||||
CHEMBL5081621 | 217244 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 4 | 2 | Agonist activity at human C3aR 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 C3aR 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 | ||||
CHEMBL1170045 | 211010 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCc1ccccc1)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/jm1003705 | ||||
CHEMBL1170231 | 211017 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | CC(C)C[C@H](NC(=O)[C@@H](N)CCc1ccccc1)C(=O)N[C@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)[C@@H](C)O | 10.1021/jm1003705 | ||||
1599 | 2341 | None | 28 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
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 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
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 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
7215 | 2341 | None | 28 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
CHEMBL841 | 2341 | None | 28 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
DB00836 | 2341 | None | 28 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -630 | 32 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1GPCR PRESTO-Tango dose-response in antagonist mode with target: C3AR1 |
ChEMBL | 476 | 7 | 1 | 3 | 5.1 | Clc1ccc(cc1)C1(O)CCN(CC1)CCC(C(=O)N(C)C)(c1ccccc1)c1ccccc1 | 10.6019/CHEMBL5442687 | ||
CHEMBL1170635 | 211025 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170635 | 211025 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
101886248 | 115038 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a |
ChEMBL | 434 | 10 | 6 | 4 | 2.0 | N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342688 | 115038 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a |
ChEMBL | 434 | 10 | 6 | 4 | 2.0 | N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O | 10.1021/jm500956p | ||
44426497 | 85769 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells |
ChEMBL | 502 | 10 | 5 | 4 | 4.2 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL229006 | 85769 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at C3a receptor expressed on HMC1 cellsAgonist activity at C3a receptor expressed on HMC1 cells |
ChEMBL | 502 | 10 | 5 | 4 | 4.2 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2ccc(Cl)cc2)c2ccc(Cl)cc2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL1170026 | 210998 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 48 | 2 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | 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 | 10.1021/jm1003705 | ||||
3915 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
49799079 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
5760 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
91933514 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170024 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170027 | 210999 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 30 | 2 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | 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 | 10.1021/jm1003705 | ||||
44426495 | 85768 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 470 | 10 | 5 | 4 | 3.2 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL229005 | 85768 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 470 | 10 | 5 | 4 | 3.2 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(C(c2cccc(F)c2)c2cccc(F)c2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL5080181 | 217156 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -3 | 2 | Agonist activity at human C3aR 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 C3aR 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 | ||||
101886248 | 115038 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a |
ChEMBL | 434 | 10 | 6 | 4 | 2.0 | N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342688 | 115038 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3aAgonist activity against C3AR in HMDMs assessed as increase in intracellular calcium release by Fluo-3 AM dye based FLIPR assay relative to 1 uM C3a |
ChEMBL | 434 | 10 | 6 | 4 | 2.0 | N=C(N)NCCC[C@H](NC(=O)c1c[nH]c(C(c2ccccc2)c2ccccc2)n1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL1170026 | 210998 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | 48 | 2 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | 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 | 10.1021/jm1003705 | ||||
3915 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
49799079 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
5760 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
91933514 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170024 | 1525 | None | 14 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170027 | 210999 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | 30 | 2 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | 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 | 10.1021/jm1003705 | ||||
CHEMBL5075364 | 216858 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -2511 | 3 | Agonist activity at human C3aR 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 C3aR 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 | ||||
CHEMBL2064020 | 211639 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assayAgonist activity at human C3a receptor expressed in RBL-2H3 cells assessed as beta-hexosaminidase activity in cell supernatant by degranulation assay |
ChEMBL | None | None | None | CC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/jm201609k | ||||
122392665 | 165536 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release |
ChEMBL | 457 | 10 | 6 | 5 | 3.3 | N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O | 10.1021/acs.jmedchem.7b00882 | ||
CHEMBL4239035 | 165536 | None | 0 | Human | Functional | pEC50 | = | 7.8 | 7.8 | - | 1 | Agonist activity at C3aR in HMDM assessed as induction of Ca2+ releaseAgonist activity at C3aR in HMDM assessed as induction of Ca2+ release |
ChEMBL | 457 | 10 | 6 | 5 | 3.3 | N=C(N)NCCC[C@H](Nc1nccc2[nH]c(C(c3ccccc3)c3ccccc3)nc12)C(=O)O | 10.1021/acs.jmedchem.7b00882 | ||
17753143 | 85974 | None | 3 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 434 | 10 | 5 | 4 | 2.9 | N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL230034 | 85974 | None | 3 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 434 | 10 | 5 | 4 | 2.9 | N=C(N)NCCC[C@H](NC(=O)c1ccc(C(c2ccccc2)c2ccccc2)o1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
44430551 | 88038 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 483 | 7 | 1 | 3 | 5.6 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL234305 | 88038 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorinAgonist activity at human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 483 | 7 | 1 | 3 | 5.6 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1ccc2ccccc2c1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL1170025 | 210997 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -1 | 2 | Agonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium releaseAgonist activity at human C3a receptor in human U937 cells assessed as induction of intracellular calcium release |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
44426475 | 144757 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 394 | 8 | 5 | 4 | 2.5 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL390834 | 144757 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | - | 1 | Antagonist activity at C3aRAntagonist activity at C3aR |
ChEMBL | 394 | 8 | 5 | 4 | 2.5 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)s1)C(=O)O | 10.1016/j.bmcl.2007.04.022 |
Showing 1 to 50 of 468 entries
Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
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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
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Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
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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
| |
CHEMBL1170042 | 211007 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
155534696 | 172082 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition |
ChEMBL | 464 | 10 | 5 | 4 | 3.7 | Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.9b00927 | ||
CHEMBL4470864 | 172082 | None | 0 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Antagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a additionAntagonist at C3a receptor in human LAD2 cells assessed as inhibition of C3a-induced beta-hexosaminidase release preincubated for 30 mins followed by C3a addition |
ChEMBL | 464 | 10 | 5 | 4 | 3.7 | Cc1cc(C(c2ccccc2)c2ccccc2)sc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/acs.jmedchem.9b00927 | ||
3915 | 1525 | None | 14 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
49799079 | 1525 | None | 14 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
5760 | 1525 | None | 14 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
91933514 | 1525 | None | 14 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
CHEMBL1170024 | 1525 | None | 14 | Human | Binding | pIC50 | = | 8.7 | 8.7 | - | 0 | Displacement of [125I-C3a] from C3a receptor in human PBMC by scintillation countingDisplacement of [125I-C3a] from C3a receptor in human PBMC by scintillation counting |
ChEMBL | None | None | None | None | 10.1021/jm1003705 | ||||
8381 | 1029 | None | 7 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 448 | 10 | 6 | 4 | 2.3 | O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N | 10.1021/jm500956p | ||
91827354 | 1029 | None | 7 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 448 | 10 | 6 | 4 | 2.3 | O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N | 10.1021/jm500956p | ||
CHEMBL3342689 | 1029 | None | 7 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 448 | 10 | 6 | 4 | 2.3 | O=C(c1nc([nH]c1C)C(c1ccccc1)c1ccccc1)N[C@H](C(=O)O)CCCNC(=N)N | 10.1021/jm500956p | ||
3529 | 3517 | None | 6 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 412 | 12 | 4 | 4 | 1.5 | O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 | 10.1021/jm500956p | ||
5311120 | 3517 | None | 6 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 412 | 12 | 4 | 4 | 1.5 | O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 | 10.1021/jm500956p | ||
CHEMBL389348 | 3517 | None | 6 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 412 | 12 | 4 | 4 | 1.5 | O=C(N[C@H](C(=O)O)CCCN=C(N)N)COCC(c1ccccc1)c1ccccc1 | 10.1021/jm500956p | ||
89570442 | 115036 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 449 | 10 | 5 | 5 | 2.6 | Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342686 | 115036 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 449 | 10 | 5 | 5 | 2.6 | Cc1oc(C(c2ccccc2)c2ccccc2)nc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/jm500956p | ||
127035774 | 136524 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 1 | Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells |
ChEMBL | 413 | 12 | 4 | 4 | 1.9 | NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3735614 | 136524 | None | 0 | Human | Binding | pIC50 | = | 8 | 8.0 | - | 1 | Displacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cellsDisplacement of [125I]-C3a from human C3aR expressed in rat RBL-2H3 cells |
ChEMBL | 413 | 12 | 4 | 4 | 1.9 | NC(=O)NCCC[C@H](NC(=O)COCC(c1ccccc1)c1ccccc1)C(=O)O | 10.1016/j.bmcl.2015.10.038 | ||
118716617 | 115027 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 410 | 12 | 5 | 3 | 2.8 | N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342677 | 115027 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 410 | 12 | 5 | 3 | 2.8 | N=C(N)NCCC[C@H](NC(=O)CCCC(c1ccccc1)c1ccccc1)C(=O)O | 10.1021/jm500956p | ||
101886251 | 115029 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 449 | 10 | 5 | 5 | 2.6 | Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342679 | 115029 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 449 | 10 | 5 | 5 | 2.6 | Cc1nc(C(c2ccccc2)c2ccccc2)oc1C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | 10.1021/jm500956p | ||
101886252 | 115033 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 511 | 11 | 5 | 5 | 4.0 | N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342683 | 115033 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 511 | 11 | 5 | 5 | 4.0 | N=C(N)NCCC[C@H](NC(=O)c1oc(C(c2ccccc2)c2ccccc2)nc1-c1ccccc1)C(=O)O | 10.1021/jm500956p | ||
44430549 | 151355 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 487 | 7 | 1 | 3 | 4.9 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL396030 | 151355 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 487 | 7 | 1 | 3 | 4.9 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(c1cc(F)c(F)c(F)c1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
117634981 | 115032 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 436 | 10 | 5 | 6 | 1.7 | N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O | 10.1021/jm500956p | ||
CHEMBL3342682 | 115032 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3AR in HMDMs by scintillation counting methodDisplacement of [125I]-C3a from C3AR in HMDMs by scintillation counting method |
ChEMBL | 436 | 10 | 5 | 6 | 1.7 | N=C(N)NCCC[C@H](NC(=O)c1nnc(C(c2ccccc2)c2ccccc2)o1)C(=O)O | 10.1021/jm500956p | ||
44430552 | 88039 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 439 | 7 | 1 | 3 | 4.9 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL234306 | 88039 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 439 | 7 | 1 | 3 | 4.9 | O=C(NC1CCN(C(=O)CCc2cccnc2)CC1)C(C1CCCCC1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
44430556 | 88085 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 431 | 6 | 1 | 3 | 4.6 | O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL234523 | 88085 | None | 0 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 431 | 6 | 1 | 3 | 4.6 | O=C(NC1CCN(C(=O)/C=C/c2cccnc2)CC1)C(c1ccccc1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
44430526 | 144323 | None | 1 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 461 | 7 | 1 | 3 | 5.1 | CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL390464 | 144323 | None | 1 | Human | Binding | pIC50 | = | 6 | 6.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 461 | 7 | 1 | 3 | 5.1 | CC1(C)CCC(C(C(=O)NC2CCN(C(=O)CCc3cccnc3)CC2)c2ccccc2)CC1 | 10.1016/j.bmcl.2007.04.023 | ||
44430559 | 88204 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 454 | 6 | 1 | 2 | 5.0 | O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
CHEMBL234730 | 88204 | None | 0 | Human | Binding | pIC50 | = | 5 | 5.0 | - | 0 | Displacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorinDisplacement of [125I]C3a from human C3a receptor expressed in HMC1 cells co-expressing aequorin |
ChEMBL | 454 | 6 | 1 | 2 | 5.0 | O=C(NC1CCN(C(=O)Cc2cccc(F)c2F)CC1)C(c1ccccc1)C1CCCCC1 | 10.1016/j.bmcl.2007.04.023 | ||
44426471 | 85737 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay |
ChEMBL | 388 | 8 | 5 | 3 | 2.5 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
CHEMBL228846 | 85737 | None | 0 | Human | Binding | pIC50 | = | 4 | 4.0 | - | 0 | Inhibition of human C3a receptor expressed on HMC1 cells by SPA assayInhibition of human C3a receptor expressed on HMC1 cells by SPA assay |
ChEMBL | 388 | 8 | 5 | 3 | 2.5 | N=C(N)NCCC[C@@H](NC(=O)c1ccc(-c2cccc(Cl)c2)cc1)C(=O)O | 10.1016/j.bmcl.2007.04.022 | ||
117634952 | 136621 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 490 | 13 | 6 | 6 | 1.7 | CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736505 | 136621 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 490 | 13 | 6 | 6 | 1.7 | CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
117634952 | 136621 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 490 | 13 | 6 | 6 | 1.7 | CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736505 | 136621 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 490 | 13 | 6 | 6 | 1.7 | CC(C)C[C@H](NC(=O)Cc1ccc(F)cc1)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
127034743 | 136620 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 542 | 15 | 6 | 6 | 3.3 | CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736489 | 136620 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 542 | 15 | 6 | 6 | 3.3 | CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 | 10.1016/j.bmcl.2015.10.038 | ||
127034743 | 136620 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 542 | 15 | 6 | 6 | 3.3 | CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736489 | 136620 | None | 0 | Human | Binding | pIC50 | = | 6.0 | 6.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 542 | 15 | 6 | 6 | 3.3 | CC(C)Cc1ccc(C(C)C(=O)N[C@@H](CC(C)C)c2nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co2)cc1 | 10.1016/j.bmcl.2015.10.038 | ||
89570392 | 136564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 512 | 12 | 6 | 6 | 2.4 | CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736020 | 136564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 512 | 12 | 6 | 6 | 2.4 | CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
89570392 | 136564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 512 | 12 | 6 | 6 | 2.4 | CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 | ||
CHEMBL3736020 | 136564 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Displacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysisDisplacement of [125I]-C3a from C3aR in human MDM cells after 60 mins by microbeta scintillation counting analysis |
ChEMBL | 512 | 12 | 6 | 6 | 2.4 | CC[C@H](C)[C@H](NC(=O)C1CCCc2ccccc21)c1nc(C(=O)N[C@@H](CCCNC(=N)N)C(=O)O)co1 | 10.1016/j.bmcl.2015.10.038 |
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