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
| |
| 25209535 | 172697 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 570 | 7 | 1 | 8 | 4.5 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5C[C@H]6C[C@H]5CN6C)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| CHEMBL448975 | 172697 | None | 0 | Human | Functional | pEC50 | = | 7.0 | 7.0 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 570 | 7 | 1 | 8 | 4.5 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5C[C@H]6C[C@H]5CN6C)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| 25209192 | 175613 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 527 | 7 | 2 | 6 | 4.4 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C(c1ccccc1)c1ccccc1 | 10.1021/jm800962k | ||
| CHEMBL457789 | 175613 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 527 | 7 | 2 | 6 | 4.4 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C(c1ccccc1)c1ccccc1 | 10.1021/jm800962k | ||
| 25208898 | 180565 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 558 | 7 | 1 | 8 | 4.3 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCN(C)CC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| CHEMBL475282 | 180565 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 558 | 7 | 1 | 8 | 4.3 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCN(C)CC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| 44581974 | 175808 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 513 | 6 | 2 | 6 | 4.6 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/jm800962k | ||
| CHEMBL458220 | 175808 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 513 | 6 | 2 | 6 | 4.6 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/jm800962k | ||
| 136036260 | 180150 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 623 | 7 | 2 | 7 | 5.9 | CC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)N4CCN(c5ccc(F)cc5)CC4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| CHEMBL474761 | 180150 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 623 | 7 | 2 | 7 | 5.9 | CC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)N4CCN(c5ccc(F)cc5)CC4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| 25208894 | 172717 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 564 | 6 | 2 | 7 | 5.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccc3ncccc3c2)cc1 | 10.1021/jm800962k | ||
| CHEMBL449189 | 172717 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 564 | 6 | 2 | 7 | 5.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccc3ncccc3c2)cc1 | 10.1021/jm800962k | ||
| 25209194 | 181740 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 519 | 6 | 2 | 7 | 4.6 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccsc2)cc1 | 10.1021/jm800962k | ||
| CHEMBL477432 | 181740 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 519 | 6 | 2 | 7 | 4.6 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2ccsc2)cc1 | 10.1021/jm800962k | ||
| 25209050 | 181696 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 479 | 6 | 2 | 6 | 3.9 | Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/jm800962k | ||
| CHEMBL477008 | 181696 | None | 0 | Human | Functional | pEC50 | = | 7.7 | 7.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 479 | 6 | 2 | 6 | 3.9 | Cc1c(Cn2ncc(N3CCNCC3)cc2=O)cccc1NC(=O)c1ccc(-c2ccccc2)cc1 | 10.1021/jm800962k | ||
| 59819672 | 135020 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 604 | 13 | 4 | 7 | 4.5 | CN(CCc1ccccn1)C(=O)c1ccc2c(c1)nc(-c1cccc(Oc3ccccc3)c1)n2[C@@H](CCCNC(=N)N)C(N)=O | nan | ||
| CHEMBL3719266 | 135020 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 604 | 13 | 4 | 7 | 4.5 | CN(CCc1ccccn1)C(=O)c1ccc2c(c1)nc(-c1cccc(Oc3ccccc3)c1)n2[C@@H](CCCNC(=N)N)C(N)=O | nan | ||
| 136036261 | 188860 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 10 | 2 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 632 | 9 | 3 | 6 | 7.1 | CCC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| CHEMBL505263 | 188860 | None | 0 | Human | Functional | pEC50 | = | 6.7 | 6.7 | 10 | 2 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 632 | 9 | 3 | 6 | 7.1 | CCC(C)[C@H]1C(=O)Nc2ccc(NCCN3CCCCC3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| 25208743 | 175611 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 438 | 5 | 2 | 7 | 2.3 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1cccnc1 | 10.1021/jm800962k | ||
| CHEMBL457788 | 175611 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 438 | 5 | 2 | 7 | 2.3 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1cccnc1 | 10.1021/jm800962k | ||
| 25209191 | 189650 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 455 | 5 | 2 | 6 | 3.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccccc1F | 10.1021/jm800962k | ||
| CHEMBL514267 | 189650 | None | 0 | Human | Functional | pEC50 | = | 4.7 | 4.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 455 | 5 | 2 | 6 | 3.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccccc1F | 10.1021/jm800962k | ||
| 25209048 | 179889 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 558 | 8 | 2 | 8 | 4.4 | CNC1CCN(c2cnn(Cc3cccc(NC(=O)c4ccc(-c5ccc(OC)nc5)cc4)c3C)c(=O)c2Cl)C1 | 10.1021/jm800962k | ||
| CHEMBL474470 | 179889 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 558 | 8 | 2 | 8 | 4.4 | CNC1CCN(c2cnn(Cc3cccc(NC(=O)c4ccc(-c5ccc(OC)nc5)cc4)c3C)c(=O)c2Cl)C1 | 10.1021/jm800962k | ||
| 25209356 | 179891 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 544 | 7 | 2 | 8 | 4.0 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| CHEMBL474473 | 179891 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 544 | 7 | 2 | 8 | 4.0 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCNCC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| 59819658 | 134057 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 658 | 11 | 4 | 7 | 5.4 | Cc1cccc(N2CCN(C(=O)c3ccc4c(c3)nc(-c3cccc(Oc5ccccc5)c3)n4[C@@H](CCCNC(=N)N)C(N)=O)CC2C)c1 | nan | ||
| CHEMBL3716029 | 134057 | None | 0 | Human | Functional | pEC50 | = | 7.6 | 7.6 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 658 | 11 | 4 | 7 | 5.4 | Cc1cccc(N2CCN(C(=O)c3ccc4c(c3)nc(-c3cccc(Oc5ccccc5)c3)n4[C@@H](CCCNC(=N)N)C(N)=O)CC2C)c1 | nan | ||
| 59819634 | 134535 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 648 | 11 | 4 | 7 | 4.9 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCN(c4ccc(F)cc4)CC3)ccc21 | nan | ||
| CHEMBL3717645 | 134535 | None | 0 | Human | Functional | pEC50 | = | 6.6 | 6.6 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 648 | 11 | 4 | 7 | 4.9 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCN(c4ccc(F)cc4)CC3)ccc21 | nan | ||
| 136036258 | 188794 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 623 | 5 | 2 | 7 | 4.7 | CC(=O)NC1CCN(c2ccc3c(c2)-c2nc4cc(C(=O)N5CCN(c6ccc(F)cc6)CC5)ccc4n2[C@@H](C(C)C)C(=O)N3)C1 | 10.1016/j.bmcl.2009.01.085 | ||
| CHEMBL504032 | 188794 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 623 | 5 | 2 | 7 | 4.7 | CC(=O)NC1CCN(c2ccc3c(c2)-c2nc4cc(C(=O)N5CCN(c6ccc(F)cc6)CC5)ccc4n2[C@@H](C(C)C)C(=O)N3)C1 | 10.1016/j.bmcl.2009.01.085 | ||
| 25208742 | 175023 | None | 0 | Human | Functional | pEC50 | = | 4.6 | 4.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 443 | 5 | 2 | 6 | 3.2 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C1CCCCC1 | 10.1021/jm800962k | ||
| CHEMBL456481 | 175023 | None | 0 | Human | Functional | pEC50 | = | 4.6 | 4.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 443 | 5 | 2 | 6 | 3.2 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C1CCCCC1 | 10.1021/jm800962k | ||
| 25208744 | 190052 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 545 | 6 | 2 | 8 | 3.4 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C1CCN(c2ccc(C#N)cc2)CC1 | 10.1021/jm800962k | ||
| CHEMBL517029 | 190052 | None | 0 | Human | Functional | pEC50 | = | 5.6 | 5.6 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 545 | 6 | 2 | 8 | 3.4 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)C1CCN(c2ccc(C#N)cc2)CC1 | 10.1021/jm800962k | ||
| 25209355 | 173028 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 564 | 6 | 2 | 7 | 5.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2cccc3cccnc23)cc1 | 10.1021/jm800962k | ||
| CHEMBL451657 | 173028 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 564 | 6 | 2 | 7 | 5.1 | Cc1c(Cn2ncc(N3CCNCC3)c(Cl)c2=O)cccc1NC(=O)c1ccc(-c2cccc3cccnc23)cc1 | 10.1021/jm800962k | ||
| 25209047 | 181660 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 532 | 10 | 3 | 8 | 4.2 | CNCCNc1cnn(Cc2cccc(NC(=O)c3ccc(-c4ccc(OC)nc4)cc3)c2C)c(=O)c1Cl | 10.1021/jm800962k | ||
| CHEMBL476627 | 181660 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 532 | 10 | 3 | 8 | 4.2 | CNCCNc1cnn(Cc2cccc(NC(=O)c3ccc(-c4ccc(OC)nc4)cc3)c2C)c(=O)c1Cl | 10.1021/jm800962k | ||
| 136036262 | 178548 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 652 | 14 | 4 | 8 | 5.6 | CCC(C)[C@H]1C(=O)Nc2ccc(NCCOCCOCCN)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| CHEMBL466116 | 178548 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | - | 1 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 652 | 14 | 4 | 8 | 5.6 | CCC(C)[C@H]1C(=O)Nc2ccc(NCCOCCOCCN)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| 136036237 | 188746 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 2 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 632 | 7 | 3 | 6 | 5.9 | CCC(C)[C@H]1C(=O)Nc2ccc(N3CCC(NC(C)=O)C3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| CHEMBL503202 | 188746 | None | 0 | Human | Functional | pEC50 | = | 6.5 | 6.5 | 3 | 2 | Agonist activity at human MrgX1 receptorAgonist activity at human MrgX1 receptor |
ChEMBL | 632 | 7 | 3 | 6 | 5.9 | CCC(C)[C@H]1C(=O)Nc2ccc(N3CCC(NC(C)=O)C3)cc2-c2nc3cc(C(=O)NCc4cccc(C(F)(F)F)c4)ccc3n21 | 10.1016/j.bmcl.2009.01.085 | ||
| 25209704 | 188377 | None | 0 | Human | Functional | pEC50 | = | 4.5 | 4.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 586 | 7 | 1 | 8 | 4.2 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCN(C(C)=O)CC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| CHEMBL499944 | 188377 | None | 0 | Human | Functional | pEC50 | = | 4.5 | 4.5 | - | 1 | Agonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at human MrgX1 receptor expressed in HEK293 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 586 | 7 | 1 | 8 | 4.2 | COc1ccc(-c2ccc(C(=O)Nc3cccc(Cn4ncc(N5CCN(C(C)=O)CC5)c(Cl)c4=O)c3C)cc2)cn1 | 10.1021/jm800962k | ||
| 59819673 | 134544 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 590 | 13 | 5 | 7 | 4.2 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)NCCc3ccccn3)ccc21 | nan | ||
| CHEMBL3717681 | 134544 | None | 0 | Human | Functional | pEC50 | = | 6.4 | 6.4 | - | 1 | Activation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assayActivation of human MrgX1 receptor expressed in CHOK1/HEK293 cells assessed as stimulation of intracellular calcium mobilization by Fura-2 dye based fluorescence assay |
ChEMBL | 590 | 13 | 5 | 7 | 4.2 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)NCCc3ccccn3)ccc21 | nan | ||
Showing 1 to 50 of 228 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
| |
| 155543843 | 175039 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 411 | 7 | 3 | 5 | 3.9 | COc1ccccc1S(=O)(=O)Nc1ccc(C)cc1Oc1ccc(C(=N)N)cc1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL4565294 | 175039 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 1 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 411 | 7 | 3 | 5 | 3.9 | COc1ccccc1S(=O)(=O)Nc1ccc(C)cc1Oc1ccc(C(=N)N)cc1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL5084093 | 217384 | None | 3 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | None | None | None | CC(C)(C)c1sc2ncnc(Oc3ccccc3OC(F)(F)F)c2c1-c1ccc(Cl)c(Cl)c1 | 10.1021/acs.jmedchem.1c01709 | ||||
| 59819634 | 134535 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 648 | 11 | 4 | 7 | 4.9 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCN(c4ccc(F)cc4)CC3)ccc21 | nan | ||
| CHEMBL3717645 | 134535 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 648 | 11 | 4 | 7 | 4.9 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCN(c4ccc(F)cc4)CC3)ccc21 | nan | ||
| 59819672 | 135020 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 604 | 13 | 4 | 7 | 4.5 | CN(CCc1ccccn1)C(=O)c1ccc2c(c1)nc(-c1cccc(Oc3ccccc3)c1)n2[C@@H](CCCNC(=N)N)C(N)=O | nan | ||
| CHEMBL3719266 | 135020 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 604 | 13 | 4 | 7 | 4.5 | CN(CCc1ccccn1)C(=O)c1ccc2c(c1)nc(-c1cccc(Oc3ccccc3)c1)n2[C@@H](CCCNC(=N)N)C(N)=O | nan | ||
| 168291043 | 192012 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 374 | 7 | 2 | 4 | 3.6 | CCOc1ccccc1NC(=O)c1cc(C)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5200001 | 192012 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 374 | 7 | 2 | 4 | 3.6 | CCOc1ccccc1NC(=O)c1cc(C)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 168289487 | 191535 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 370 | 5 | 2 | 4 | 3.9 | Cc1cc2cccc(NC(=O)c3ccccc3NS(=O)(=O)C3CC3)c2o1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5192837 | 191535 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 370 | 5 | 2 | 4 | 3.9 | Cc1cc2cccc(NC(=O)c3ccccc3NS(=O)(=O)C3CC3)c2o1 | 10.1021/acsmedchemlett.2c00100 | ||
| 168277932 | 190791 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 404 | 9 | 2 | 5 | 3.6 | CCOc1ccc(NC(=O)c2ccccc2NS(=O)(=O)C2CC2)c(OCC)c1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5181857 | 190791 | None | 0 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 404 | 9 | 2 | 5 | 3.6 | CCOc1ccc(NC(=O)c2ccccc2NS(=O)(=O)C2CC2)c(OCC)c1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5082858 | 217317 | None | 7 | Human | Binding | pEC50 | = | 6.0 | 6.0 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | None | None | None | Cc1sc2ncnc(Oc3ccc(F)cc3)c2c1C | 10.1021/acs.jmedchem.1c01709 | ||||
| 71598556 | 190488 | None | 33 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 360 | 7 | 2 | 4 | 3.2 | CCOc1ccccc1NC(=O)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5177388 | 190488 | None | 33 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 360 | 7 | 2 | 4 | 3.2 | CCOc1ccccc1NC(=O)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 118717468 | 115215 | None | 1 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assayAgonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay |
ChEMBL | 368 | 8 | 6 | 4 | 0.1 | N=C(N)Nc1ccc(C[C@@H](N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 | 10.1016/j.bmc.2014.09.025 | ||
| CHEMBL3343994 | 115215 | None | 1 | Mouse | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assayAgonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay |
ChEMBL | 368 | 8 | 6 | 4 | 0.1 | N=C(N)Nc1ccc(C[C@@H](N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 | 10.1016/j.bmc.2014.09.025 | ||
| 168287582 | 191695 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 396 | 7 | 2 | 4 | 3.5 | CCOc1ccc(F)cc1NC(=O)c1cc(F)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5195160 | 191695 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 396 | 7 | 2 | 4 | 3.5 | CCOc1ccc(F)cc1NC(=O)c1cc(F)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 168274093 | 190414 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 386 | 8 | 2 | 4 | 3.6 | O=C(Nc1ccccc1OCC1CC1)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5176049 | 190414 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 386 | 8 | 2 | 4 | 3.6 | O=C(Nc1ccccc1OCC1CC1)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 168273467 | 190213 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 378 | 7 | 2 | 4 | 3.4 | CCOc1ccc(F)cc1NC(=O)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5172913 | 190213 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 378 | 7 | 2 | 4 | 3.4 | CCOc1ccc(F)cc1NC(=O)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 168275005 | 190473 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 420 | 7 | 2 | 4 | 3.8 | CCS(=O)(=O)Nc1ccccc1C(=O)Nc1ccc(F)cc1OCC(F)(F)F | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5177134 | 190473 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 420 | 7 | 2 | 4 | 3.8 | CCS(=O)(=O)Nc1ccccc1C(=O)Nc1ccc(F)cc1OCC(F)(F)F | 10.1021/acsmedchemlett.2c00100 | ||
| 168297110 | 192634 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 356 | 5 | 2 | 4 | 3.6 | O=C(Nc1cccc2occc12)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5209542 | 192634 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 356 | 5 | 2 | 4 | 3.6 | O=C(Nc1cccc2occc12)c1ccccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 710974 | 41979 | None | 7 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | 242 | 2 | 0 | 4 | 3.8 | Cc1ccccc1Oc1ncnc2sccc12 | 10.1021/acs.jmedchem.1c01709 | ||
| CHEMBL1494771 | 41979 | None | 7 | Human | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | 242 | 2 | 0 | 4 | 3.8 | Cc1ccccc1Oc1ncnc2sccc12 | 10.1021/acs.jmedchem.1c01709 | ||
| 155524924 | 171030 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 465 | 7 | 3 | 5 | 4.8 | Cc1ccc(NS(=O)(=O)c2ccccc2OC(F)(F)F)c(Oc2ccc(C(=N)N)cc2)c1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL4455263 | 171030 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 465 | 7 | 3 | 5 | 4.8 | Cc1ccc(NS(=O)(=O)c2ccccc2OC(F)(F)F)c(Oc2ccc(C(=N)N)cc2)c1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL5078077 | 217022 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | None | None | None | Cc1cc2c(Oc3ccccc3F)ncnc2s1 | 10.1021/acs.jmedchem.1c01709 | ||||
| 59819673 | 134544 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 590 | 13 | 5 | 7 | 4.2 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)NCCc3ccccn3)ccc21 | nan | ||
| CHEMBL3717681 | 134544 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 590 | 13 | 5 | 7 | 4.2 | N=C(N)NCCC[C@@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)NCCc3ccccn3)ccc21 | nan | ||
| 89224504 | 135028 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 555 | 10 | 4 | 7 | 3.3 | N=C(N)NCCC[C@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCOCC3)ccc21 | nan | ||
| CHEMBL3719296 | 135028 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Activation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assayActivation of human MrgX1 receptor expressed in NIH/3T3 cells incubated for 5 days by beta-galactosidase reporter gene assay |
ChEMBL | 555 | 10 | 4 | 7 | 3.3 | N=C(N)NCCC[C@H](C(N)=O)n1c(-c2cccc(Oc3ccccc3)c2)nc2cc(C(=O)N3CCOCC3)ccc21 | nan | ||
| 118717467 | 115214 | None | 0 | Mouse | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assayAgonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay |
ChEMBL | 368 | 8 | 6 | 4 | 0.1 | N=C(N)Nc1ccc(C[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 | 10.1016/j.bmc.2014.09.025 | ||
| CHEMBL3343993 | 115214 | None | 0 | Mouse | Binding | pEC50 | = | 4.8 | 4.8 | - | 0 | Agonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assayAgonist activity at mouse MrgC11 transfected in HEK293 cells by FLIPR assay |
ChEMBL | 368 | 8 | 6 | 4 | 0.1 | N=C(N)Nc1ccc(C[C@H](N)C(=O)N[C@@H](Cc2ccccc2)C(N)=O)cc1 | 10.1016/j.bmc.2014.09.025 | ||
| 155551191 | 174045 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 395 | 6 | 3 | 4 | 4.2 | Cc1ccc(S(=O)(=O)Nc2ccc(C)cc2Oc2ccc(C(=N)N)cc2)cc1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL4541091 | 174045 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 395 | 6 | 3 | 4 | 4.2 | Cc1ccc(S(=O)(=O)Nc2ccc(C)cc2Oc2ccc(C(=N)N)cc2)cc1 | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL5070279 | 216719 | None | 7 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | None | None | None | Cc1sc2ncnc(Oc3ccccc3)c2c1C | 10.1021/acs.jmedchem.1c01709 | ||||
| CHEMBL5075377 | 216859 | None | 0 | Human | Binding | pEC50 | = | 5.8 | 5.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 transfected in HEK293 cells in presence of BAM8-22 by Fulo4AM dye based FLIPR assay |
ChEMBL | None | None | None | Cc1csc2ncnc(Oc3ccccc3F)c12 | 10.1021/acs.jmedchem.1c01709 | ||||
| 168297286 | 192587 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 378 | 7 | 2 | 4 | 3.4 | CCOc1ccccc1NC(=O)c1cc(F)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5208855 | 192587 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 378 | 7 | 2 | 4 | 3.4 | CCOc1ccccc1NC(=O)c1cc(F)ccc1NS(=O)(=O)C1CC1 | 10.1021/acsmedchemlett.2c00100 | ||
| 155530228 | 171616 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 341 | 9 | 3 | 4 | 4.0 | COc1cc(CNc2ccc(C(=N)N)cc2)ccc1OCCC(C)C | 10.1021/acs.jmedchem.9b01003 | ||
| CHEMBL4464063 | 171616 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 341 | 9 | 3 | 4 | 4.0 | COc1cc(CNc2ccc(C(=N)N)cc2)ccc1OCCC(C)C | 10.1021/acs.jmedchem.9b01003 | ||
| 168289095 | 191410 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 400 | 7 | 2 | 4 | 3.9 | CCOc1ccc(F)cc1NC(=O)c1cc(Cl)ccc1NS(=O)(=O)CC | 10.1021/acsmedchemlett.2c00100 | ||
| CHEMBL5191110 | 191410 | None | 0 | Human | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Positive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assayPositive allosteric modulator activity at human MRGPRX1 expressed in HEK293 cells in presence of BAM8-22 by Fluo4-dye based FLIPR assay |
ChEMBL | 400 | 7 | 2 | 4 | 3.9 | CCOc1ccc(F)cc1NC(=O)c1cc(Cl)ccc1NS(=O)(=O)CC | 10.1021/acsmedchemlett.2c00100 | ||
| 155563230 | 175411 | None | 0 | Human | Binding | pEC50 | = | 5.7 | 5.7 | - | 0 | Agonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assayAgonist activity at human MrgprX1 expressed in HEK293 cells incubated for 2 mins by Fluo4AM dye based FLIPR assay |
ChEMBL | 399 | 6 | 3 | 4 | 4.0 | Cc1ccc(NS(=O)(=O)c2ccc(F)cc2)c(Oc2ccc(C(=N)N)cc2)c1 | 10.1021/acs.jmedchem.9b01003 | ||
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