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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Common name | GPCRdb ID | Reference ligand | Vendors | Species | Assay Type | Activity Type | Activity Relation | Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description | Source | Mol weight | Rot Bonds | H don | H acc | LogP | Smiles | DOI | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Binding | pKi | = | - | 7.68 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11850634 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Binding | EC50 | = | 50.00 | 7.30 | - | 3 | Agonist activity at human MrgprX1 | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.9b01003 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Binding | EC50 | = | 50.12 | 7.30 | - | 3 | Agonist activity at human MrgX1 transfected in HEK293 cells by FLIPR assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Binding | pKd | = | - | 7.99 | - | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11850634 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Mouse | Binding | EC50 | = | 300.00 | 6.52 | - | 3 | Agonist activity at mouse MRGPRC11 | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.9b01003 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Mouse | Binding | EC50 | = | 251.19 | 6.60 | - | 3 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Rat | Binding | EC50 | = | 300.00 | 6.52 | - | 3 | Agonist activity at rat MRGPRC | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1021/acs.jmedchem.9b01003 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Rat | Binding | EC50 | = | 316.23 | 6.50 | - | 3 | Agonist activity at rat MrgX1 transfected in HEK293 cells by FLIPR assay | ChEMBL | - | - | - | - | - | - | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL145103 | 36926 | None | 0 | Human | Binding | IC50 | = | 1850.00 | 5.73 | - | 3 | Binding affinity to recombinant MrgX1 (unknown origin) by chromatography-based technique | ChEMBL | 408.2 | 6 | 0 | 3 | 5.37 | N#Cc1ccc(COC2C3CCN(CC3)C2C(c2ccccc2)c2ccccc2)cc1 | - | |
| CHEMBL1494771 | 41979 | None | 7 | Human | Binding | EC50 | = | 14500.00 | 4.84 | - | 1 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay | ChEMBL | 242.1 | 2 | 0 | 4 | 3.79 | Cc1ccccc1Oc1ncnc2sccc12 | https://dx.doi.org/10.1021/acs.jmedchem.1c01709 | |
| CHEMBL1762707 | 61045 | None | 0 | Human | Binding | IC50 | = | 50.00 | 7.30 | - | 1 | Antagonist activity at human MrgX1 transfected in HEK293 cells by FLIPR assay | ChEMBL | 660.2 | 13 | 1 | 9 | 4.36 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(CCCN1CCOCC1)Cc1c(Cl)cncc1Cl | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL179938 | 63509 | None | 0 | Human | Binding | EC50 | = | 510.00 | 6.29 | - | 1 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay | ChEMBL | 361.2 | 8 | 3 | 4 | 4.17 | COc1cc(CNc2ccc(C(=N)N)cc2)ccc1OCc1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.9b01003 | |
| CHEMBL3343987 | 115209 | None | 0 | Mouse | Binding | EC50 | = | 7943.28 | 5.10 | - | 1 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 318.2 | 6 | 6 | 4 | -1.59 | N=C(N)N[C@@H]1CN[C@H](C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343988 | 115210 | None | 0 | Mouse | Binding | EC50 | = | 794.33 | 6.10 | - | 2 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 346.2 | 6 | 5 | 4 | -0.87 | N=C(N)N1CCC(C(N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CC1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343988 | 115210 | None | 0 | Rat | Binding | EC50 | = | 3981.07 | 5.40 | - | 2 | Agonist activity at rat MrgX1 transfected in HEK293 cells by FLIPR assay | ChEMBL | 346.2 | 6 | 5 | 4 | -0.87 | N=C(N)N1CCC(C(N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)CC1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343990 | 115211 | None | 18 | Mouse | Binding | EC50 | = | 501.19 | 6.30 | - | 2 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 320.2 | 9 | 6 | 4 | -1.21 | N=C(N)NCCC[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343990 | 115211 | None | 18 | Rat | Binding | EC50 | = | 6309.57 | 5.20 | - | 2 | Agonist activity at rat MrgX1 transfected in HEK293 cells by FLIPR assay | ChEMBL | 320.2 | 9 | 6 | 4 | -1.21 | N=C(N)NCCC[C@H](N)C(=O)N[C@@H](Cc1ccccc1)C(N)=O | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343991 | 115212 | None | 0 | Mouse | Binding | EC50 | = | 501.19 | 6.30 | - | 1 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 332.2 | 7 | 6 | 4 | -1.34 | N=C(N)NC[C@@H]1CN[C@H](C(=O)N[C@@H](Cc2ccccc2)C(N)=O)C1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343992 | 115213 | None | 0 | Mouse | Binding | EC50 | = | 31622.78 | 4.50 | - | 1 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 354.2 | 7 | 6 | 4 | 0.20 | N=C(N)Nc1cccc(C(N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
| CHEMBL3343992 | 115213 | None | 0 | Mouse | Binding | EC50 | = | 31622.78 | 4.50 | - | 1 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay | ChEMBL | 354.2 | 7 | 6 | 4 | 0.20 | N=C(N)Nc1cccc(C(N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)c1 | https://dx.doi.org/10.1016/j.bmc.2014.09.025 | |
Showing 1 to 20 of 113 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 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Functional | pEC50 | = | - | 6.55 | 2 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/15163697 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Functional | pEC50 | = | - | 6.55 | 2 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11850634 | |
| bovine adrenal medulla peptide 8-22 | 707 | None | 24 | Human | Functional | pEC50 | = | - | 6.55 | 2 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/23396314 | |
| CHEMBL145103 | 36926 | None | 0 | Human | Functional | IC50 | = | 556.00 | 6.25 | -1 | 3 | Antagonist activity at MrgX1 (unknown origin) by beta-lactamase reporter gene assay | ChEMBL | 408.2 | 6 | 0 | 3 | 5.37 | N#Cc1ccc(COC2C3CCN(CC3)C2C(c2ccccc2)c2ccccc2)cc1 | - | |
| CHEMBL145103 | 36926 | None | 0 | Rat | Functional | IC50 | = | 632.00 | 6.20 | -1 | 3 | Antagonist activity at MrgX1 in mouse or rat DRG neurons assessed as intracellular Ca2+ level by FLIPR assay | ChEMBL | 408.2 | 6 | 0 | 3 | 5.37 | N#Cc1ccc(COC2C3CCN(CC3)C2C(c2ccccc2)c2ccccc2)cc1 | - | |
| CHEMBL145103 | 36926 | None | 0 | Rat | Functional | IC50 | = | 5600.00 | 5.25 | -1 | 3 | Antagonist activity at MrgX1 in mouse or rat DRG neurons assessed as action potential by whole-cell patch clamp method | ChEMBL | 408.2 | 6 | 0 | 3 | 5.37 | N#Cc1ccc(COC2C3CCN(CC3)C2C(c2ccccc2)c2ccccc2)cc1 | - | |
| CHEMBL1760000 | 60592 | None | 0 | Human | Functional | IC50 | = | 77.00 | 7.11 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 561.2 | 10 | 1 | 7 | 4.66 | CCN(Cc1c(Cl)cncc1Cl)C(=O)CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762693 | 61030 | None | 0 | Human | Functional | IC50 | = | 530.00 | 6.28 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 627.3 | 11 | 2 | 8 | 4.00 | CC(CN(C)C)NC(=O)C1CCN(S(=O)(=O)c2ccc3nc(NCCc4ccc(Cl)cc4)nc(N4CCCC4)c3c2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762694 | 61031 | None | 1 | Human | Functional | IC50 | = | 8060.00 | 5.09 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 352.1 | 5 | 1 | 4 | 4.54 | Clc1ccc(CCNc2nc(N3CCCC3)c3ccccc3n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762695 | 61032 | None | 0 | Human | Functional | IC50 | = | 640.00 | 6.19 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 481.1 | 9 | 3 | 6 | 4.24 | NS(=O)(=O)c1ccc(CCNc2nc(NCCc3ccc(Cl)cc3)nc3ccccc23)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762696 | 61033 | None | 0 | Human | Functional | IC50 | = | 301.00 | 6.52 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 431.1 | 9 | 3 | 6 | 3.09 | NS(=O)(=O)c1ccc(CCNc2ccnc(NCCc3ccc(Cl)cc3)n2)cc1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762697 | 61034 | None | 0 | Human | Functional | IC50 | = | 758.00 | 6.12 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 442.2 | 7 | 1 | 6 | 2.92 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N1CCCCC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762698 | 61035 | None | 0 | Human | Functional | IC50 | = | 20.00 | 7.70 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 545.2 | 11 | 1 | 8 | 4.12 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(Cc1ccncc1)Cc1ccco1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762699 | 61036 | None | 0 | Human | Functional | IC50 | = | 22.00 | 7.66 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 555.3 | 11 | 1 | 7 | 4.53 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(Cc1ccccc1)Cc1ccncc1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762700 | 61038 | None | 0 | Human | Functional | IC50 | = | 24.00 | 7.62 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 624.2 | 11 | 1 | 8 | 5.23 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(Cc1ccncc1)Cc1c(Cl)cncc1Cl | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762701 | 61039 | None | 0 | Human | Functional | IC50 | = | 40.00 | 7.40 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 549.3 | 11 | 1 | 8 | 3.51 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(Cc1ccncc1)CC1CCCO1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762702 | 61040 | None | 0 | Human | Functional | IC50 | = | 88.00 | 7.06 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 537.3 | 13 | 1 | 8 | 3.37 | COCCCN(Cc1ccncc1)C(=O)CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762703 | 61041 | None | 0 | Human | Functional | IC50 | = | 244.00 | 6.61 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 493.2 | 10 | 1 | 7 | 3.35 | CCN(Cc1ccncc1)C(=O)CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762704 | 61042 | None | 0 | Human | Functional | IC50 | = | 295.00 | 6.53 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 519.3 | 11 | 1 | 7 | 3.74 | O=C(CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1)N(Cc1ccncc1)CC1CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
| CHEMBL1762705 | 61043 | None | 0 | Human | Functional | IC50 | = | 108.00 | 6.97 | - | 1 | Antagonist activity at SNSR4 in human HEK293 cells by FLIPR assay | ChEMBL | 571.1 | 10 | 1 | 7 | 4.11 | CCN(Cc1ccncc1Br)C(=O)CN1CCN(c2ccnc(NCCc3ccc(Cl)cc3)n2)CC1 | https://dx.doi.org/10.1016/j.bmcl.2011.01.138 | |
Showing 1 to 20 of 110 entries