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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
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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 | |
CHEMBL4518532 | 173123 | None | 2 | Human | Binding | EC50 | = | 5900.00 | 5.23 | - | 1 | Partial agonist activity at C5a2 receptor (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 1 hr by BRET assay | ChEMBL | 1118.5 | 29 | 17 | 13 | -0.90 | CC(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](Cc1cnc[nH]1)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N1CCC[C@H]1C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | - | |
CHEMBL4550325 | 174415 | None | 0 | Human | Binding | Ki | = | 48000.00 | 4.32 | - | 1 | Displacement of [125I]-C5a from C5a2 receptor (unknown origin) expressed in Flp-In CHO cell membranes incubated for 1 hr by microbeta scintillation counting assay | ChEMBL | 897.6 | 28 | 14 | 9 | 0.39 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | - | |
CHEMBL4550325 | 174415 | None | 0 | Human | Binding | EC50 | = | 7600.00 | 5.12 | - | 1 | Partial agonist activity at C5a2 receptor (unknown origin) expressed in HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 1 hr by BRET assay | ChEMBL | 897.6 | 28 | 14 | 9 | 0.39 | CC[C@H](C)[C@H](NC(=O)[C@H](CC(C)C)NC(C)=O)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCNC(=N)N)C(=O)O | - | |
P32 [PMID: 27108698] | 2987 | None | 0 | Human | Binding | pKi | = | - | 3.65 | - | 1 | Binding assay | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/27108698 | |
P59 [PMID: 27108698] | 2989 | None | 0 | Human | Binding | pKi | = | - | 4.19 | - | 1 | Binding assay | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/27108698 |
Showing 1 to 5 of 5 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 | |
A8Δ71-73 | 213 | None | 0 | Mouse | Functional | pIC50 | ~ | - | 6.00 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/14570896 | |
C5a | 771 | None | 0 | Human | Functional | pIC50 | = | - | 8.30 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11773063 | |
C5a | 771 | None | 0 | Human | Functional | pIC50 | = | - | 8.30 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12899627 | |
C5a | 771 | None | 0 | Human | Functional | pEC50 | = | - | 8.85 | -1 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11773063 | |
C5a des-Arg | 774 | None | 0 | Human | Functional | pEC50 | = | - | 8.64 | 69 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | - | |
C5a des-Arg | 774 | None | 0 | Human | Functional | pIC50 | = | - | 7.65 | 69 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11773063 | |
C5a des-Arg | 774 | None | 0 | Human | Functional | pIC50 | = | - | 7.65 | 69 | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12899627 | |
C5a hexapeptide analogue | 775 | None | 0 | Human | Functional | pIC50 | = | - | 4.74 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12899627 | |
C5apep | 776 | None | 0 | Human | Functional | pEC50 | = | - | 6.15 | - | 1 | β-arrestin recruitment determined in a BRET assay | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/31036565 | |
CHIPS-(28-149) | 914 | None | 0 | Human | Functional | pIC50 | = | - | 6.60 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/17258808 | |
loperamide | 2341 | None | 28 | Human | Functional | EC50 | = | 1251.33 | 5.90 | -676 | 40 | GPCR PRESTO-Tango dose-response in antagonist mode with target: C5AR2 | ChEMBL | 476.2 | 7 | 1 | 3 | 5.09 | CN(C)C(=O)C(CCN1CCC(O)(c2ccc(Cl)cc2)CC1)(c1ccccc1)c1ccccc1 | https://dx.doi.org/10.6019/CHEMBL5442687 |
Showing 1 to 11 of 11 entries