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
| |
5311263 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -29 | 7 | Agonist activity at LPA3 expressed in human chem1 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at LPA3 expressed in human chem1 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1016/j.bmc.2009.12.020 | ||
CHEMBL117021 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -29 | 7 | Agonist activity at LPA3 expressed in human chem1 cells assessed as intracellular calcium mobilization by FLIPR assayAgonist activity at LPA3 expressed in human chem1 cells assessed as intracellular calcium mobilization by FLIPR assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1016/j.bmc.2009.12.020 | ||
6610239 | 67636 | None | 20 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 423 | 19 | 4 | 4 | 4.1 | CCCCCCCCCCCCCCCC(=O)N[C@@H](COP(=O)(O)O)C(=O)O | 10.1021/jm049609r | ||
CHEMBL190328 | 67636 | None | 20 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 423 | 19 | 4 | 4 | 4.1 | CCCCCCCCCCCCCCCC(=O)N[C@@H](COP(=O)(O)O)C(=O)O | 10.1021/jm049609r | ||
5311263 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.6 | 6.6 | -29 | 7 | Agonistic activity against lysophosphatidic acid receptor 3 using [35S]GTP-gamma-S as radioligand tested in vitroAgonistic activity against lysophosphatidic acid receptor 3 using [35S]GTP-gamma-S as radioligand tested in vitro |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1016/j.bmcl.2004.04.061 | ||
CHEMBL117021 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.6 | 6.6 | -29 | 7 | Agonistic activity against lysophosphatidic acid receptor 3 using [35S]GTP-gamma-S as radioligand tested in vitroAgonistic activity against lysophosphatidic acid receptor 3 using [35S]GTP-gamma-S as radioligand tested in vitro |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1016/j.bmcl.2004.04.061 | ||
2906 | 2355 | None | 15 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -36 | 12 | Agonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assayAgonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O | 10.1021/acs.jmedchem.6b01270 | ||
5395 | 2355 | None | 15 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -36 | 12 | Agonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assayAgonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O | 10.1021/acs.jmedchem.6b01270 | ||
5497152 | 2355 | None | 15 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -36 | 12 | Agonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assayAgonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O | 10.1021/acs.jmedchem.6b01270 | ||
CHEMBL1222042 | 2355 | None | 15 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -36 | 12 | Agonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assayAgonist activity at LPA3 receptor (unknown origin) expressed in rat RH7777 cells assessed as increase in intracellular calcium level measured every 3.42 secs for 70 secs by Fura-2-AM dye based fluorescence assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O | 10.1021/acs.jmedchem.6b01270 | ||
11473989 | 67142 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -2 | 3 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 364 | 17 | 2 | 2 | 6.3 | CCCCCCCC/C=C/CCCCCCCCOP(O)(O)=S | 10.1021/jm049609r | ||
CHEMBL187459 | 67142 | None | 0 | Human | Functional | pEC50 | = | 6.3 | 6.3 | -2 | 3 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 364 | 17 | 2 | 2 | 6.3 | CCCCCCCC/C=C/CCCCCCCCOP(O)(O)=S | 10.1021/jm049609r | ||
122191543 | 123768 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 12 | 2 | Agonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysisAgonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis |
ChEMBL | 452 | 22 | 2 | 4 | 6.3 | CCCCCCCC/C=C\CCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1039/C4MD00333K | ||
CHEMBL3621961 | 123768 | None | 0 | Human | Functional | pEC50 | = | 7.2 | 7.2 | 12 | 2 | Agonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysisAgonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis |
ChEMBL | 452 | 22 | 2 | 4 | 6.3 | CCCCCCCC/C=C\CCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1039/C4MD00333K | ||
2913 | 347 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 8 | 2 | Agonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysisAgonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis |
ChEMBL | 452 | 22 | 2 | 4 | 6.3 | CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC | 10.1039/C4MD00333K | ||
56947064 | 347 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 8 | 2 | Agonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysisAgonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis |
ChEMBL | 452 | 22 | 2 | 4 | 6.3 | CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC | 10.1039/C4MD00333K | ||
CHEMBL3621962 | 347 | None | 0 | Human | Functional | pEC50 | = | 7.1 | 7.1 | 8 | 2 | Agonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysisAgonist activity at human LPA3 receptor transfected in RH7777 cells assessed as mobilization of Ca2+ by fluorometric analysis |
ChEMBL | 452 | 22 | 2 | 4 | 6.3 | CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC | 10.1039/C4MD00333K | ||
5311263 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.1 | 6.1 | -29 | 7 | Agonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assayAgonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1021/jm5007116 | ||
CHEMBL117021 | 4157 | None | 20 | Human | Functional | pEC50 | = | 6.1 | 6.1 | -29 | 7 | Agonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assayAgonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay |
ChEMBL | 436 | 20 | 3 | 5 | 5.0 | CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O | 10.1021/jm5007116 | ||
11312382 | 67378 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | 21 | 3 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 292 | 13 | 2 | 2 | 4.6 | CC/C=C/CCCCCCCCCCOP(=O)(O)O | 10.1021/jm049609r | ||
CHEMBL188591 | 67378 | None | 0 | Human | Functional | pIC50 | = | 7.0 | 7.0 | 21 | 3 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 292 | 13 | 2 | 2 | 4.6 | CC/C=C/CCCCCCCCCCOP(=O)(O)O | 10.1021/jm049609r | ||
122191544 | 123770 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -4 | 4 | Antagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization by Fura-2 AM probe-based fluorometric analysisAntagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization by Fura-2 AM probe-based fluorometric analysis |
ChEMBL | 484 | 18 | 3 | 4 | 5.4 | CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O | 10.1039/C4MD00333K | ||
CHEMBL3621964 | 123770 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -4 | 4 | Antagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization by Fura-2 AM probe-based fluorometric analysisAntagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization by Fura-2 AM probe-based fluorometric analysis |
ChEMBL | 484 | 18 | 3 | 4 | 5.4 | CCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O | 10.1039/C4MD00333K | ||
81309 | 67282 | None | 42 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 222 | 9 | 2 | 1 | 3.3 | CCCCCCCCCCP(=O)(O)O | 10.1021/jm049609r | ||
88299705 | 67282 | None | 42 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 222 | 9 | 2 | 1 | 3.3 | CCCCCCCCCCP(=O)(O)O | 10.1021/jm049609r | ||
CHEMBL188083 | 67282 | None | 42 | Human | Functional | pIC50 | = | 5.9 | 5.9 | - | 1 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 222 | 9 | 2 | 1 | 3.3 | CCCCCCCCCCP(=O)(O)O | 10.1021/jm049609r | ||
44454369 | 155704 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -239 | 2 | Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assayAntagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay |
ChEMBL | 322 | 4 | 1 | 4 | 5.0 | Cc1noc(-c2ccccc2)c1NC(=O)OC(C)c1ccccc1 | 10.1016/j.bmcl.2007.12.024 | ||
CHEMBL404575 | 155704 | None | 0 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -239 | 2 | Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assayAntagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay |
ChEMBL | 322 | 4 | 1 | 4 | 5.0 | Cc1noc(-c2ccccc2)c1NC(=O)OC(C)c1ccccc1 | 10.1016/j.bmcl.2007.12.024 | ||
11242245 | 67219 | None | 3 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 37 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 254 | 10 | 2 | 2 | 3.4 | CCCCCCCCCCOP(O)(O)=S | 10.1021/jm049609r | ||
CHEMBL187795 | 67219 | None | 3 | Human | Functional | pIC50 | = | 6.9 | 6.9 | 37 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 254 | 10 | 2 | 2 | 3.4 | CCCCCCCCCCOP(O)(O)=S | 10.1021/jm049609r | ||
2260227 | 184193 | None | 8 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -138 | 3 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentrationAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration |
ChEMBL | 488 | 10 | 4 | 6 | 4.4 | O=C(O)/C=C/C(=O)Nc1ccc(Oc2cccc(Oc3ccc(NC(=O)/C=C/C(=O)O)cc3)c2)cc1 | 10.1016/j.bmc.2008.04.035 | ||
CHEMBL482498 | 184193 | None | 8 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -138 | 3 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentrationAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration |
ChEMBL | 488 | 10 | 4 | 6 | 4.4 | O=C(O)/C=C/C(=O)Nc1ccc(Oc2cccc(Oc3ccc(NC(=O)/C=C/C(=O)O)cc3)c2)cc1 | 10.1016/j.bmc.2008.04.035 | ||
2260227 | 184193 | None | 8 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -138 | 3 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium responseAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium response |
ChEMBL | 488 | 10 | 4 | 6 | 4.4 | O=C(O)/C=C/C(=O)Nc1ccc(Oc2cccc(Oc3ccc(NC(=O)/C=C/C(=O)O)cc3)c2)cc1 | 10.1016/j.bmc.2009.09.022 | ||
CHEMBL482498 | 184193 | None | 8 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -138 | 3 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium responseAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium response |
ChEMBL | 488 | 10 | 4 | 6 | 4.4 | O=C(O)/C=C/C(=O)Nc1ccc(Oc2cccc(Oc3ccc(NC(=O)/C=C/C(=O)O)cc3)c2)cc1 | 10.1016/j.bmc.2009.09.022 | ||
16043259 | 79840 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -1 | 2 | Activity at human LPA3 receptor expressed in RH7777 cells by calcium mobilization assayActivity at human LPA3 receptor expressed in RH7777 cells by calcium mobilization assay |
ChEMBL | 434 | 18 | 1 | 4 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 | 10.1021/jm060351+ | ||
CHEMBL212029 | 79840 | None | 0 | Human | Functional | pIC50 | = | 5.9 | 5.9 | -1 | 2 | Activity at human LPA3 receptor expressed in RH7777 cells by calcium mobilization assayActivity at human LPA3 receptor expressed in RH7777 cells by calcium mobilization assay |
ChEMBL | 434 | 18 | 1 | 4 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 | 10.1021/jm060351+ | ||
71457480 | 83160 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | -2 | 2 | Antagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assayAntagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assay |
ChEMBL | 550 | 7 | 2 | 6 | 6.6 | C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 | 10.1021/jm301022v | ||
CHEMBL2182046 | 83160 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | -2 | 2 | Antagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assayAntagonist activity at human recombinant LPA3 expressed in chem-1 cells assessed as inhibition of LPA-induced intracellular calcium mobilization incubated for 30 mins prior to LPA-challenge measured over 100 secs by FLIPR assay |
ChEMBL | 550 | 7 | 2 | 6 | 6.6 | C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 | 10.1021/jm301022v | ||
71457480 | 83160 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | -2 | 2 | Calcium Flux Assay Using Fluorometric Imaging Plate Reader (FLIPR) Assay: Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilutions, 10 mM stocks of compounds were prepared in 100% DMSO. The compound dilution plate was set up as follows: well #1 received 29 μL of stock compound and 31 μL DMSO. Wells 2-10 received 40 μL of DMSO. After mixing, 20 μL of solution from well #1 was transferred into well #2, followed by 1:3 serial dilutions out 10 steps. 2 μL of diluted compound was transferred into duplicate wells of 384 well "assay plate" and then 90 μL of buffer was added. After incubation, both the cell and "assay" plates were brought to the FLIPR and 20 μL of the diluted compounds were transferred to the cell plates by the FLIPR. Compound addition was monitored by the FLIPR to detect any agonist activity of the compounds. Plates were then incubated for 30 minutes at room temperature protected from light. After the incubation, plates were returned to the FLIPR and 20 μL of 4.5× concentrated agonist was added to the cell plates. During the assay, fluorescence readings were taken simultaneously from all 384 wells of the cell plate every 1.5 seconds. Five readings were taken to establish a stable baseline, then 20 μL of sample was rapidly (30 μL/sec) and simultaneously added to each well of the cell plate. The fluorescence was continuously monitored before, during and after sample addition for a total elapsed time of 100 seconds.Calcium Flux Assay Using Fluorometric Imaging Plate Reader (FLIPR) Assay: Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilutions, 10 mM stocks of compounds were prepared in 100% DMSO. The compound dilution plate was set up as follows: well #1 received 29 μL of stock compound and 31 μL DMSO. Wells 2-10 received 40 μL of DMSO. After mixing, 20 μL of solution from well #1 was transferred into well #2, followed by 1:3 serial dilutions out 10 steps. 2 μL of diluted compound was transferred into duplicate wells of 384 well "assay plate" and then 90 μL of buffer was added. After incubation, both the cell and "assay" plates were brought to the FLIPR and 20 μL of the diluted compounds were transferred to the cell plates by the FLIPR. Compound addition was monitored by the FLIPR to detect any agonist activity of the compounds. Plates were then incubated for 30 minutes at room temperature protected from light. After the incubation, plates were returned to the FLIPR and 20 μL of 4.5× concentrated agonist was added to the cell plates. During the assay, fluorescence readings were taken simultaneously from all 384 wells of the cell plate every 1.5 seconds. Five readings were taken to establish a stable baseline, then 20 μL of sample was rapidly (30 μL/sec) and simultaneously added to each well of the cell plate. The fluorescence was continuously monitored before, during and after sample addition for a total elapsed time of 100 seconds. |
ChEMBL | 550 | 7 | 2 | 6 | 6.6 | C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 | nan | ||
CHEMBL2182046 | 83160 | None | 0 | Human | Functional | pIC50 | = | 6.9 | 6.9 | -2 | 2 | Calcium Flux Assay Using Fluorometric Imaging Plate Reader (FLIPR) Assay: Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilutions, 10 mM stocks of compounds were prepared in 100% DMSO. The compound dilution plate was set up as follows: well #1 received 29 μL of stock compound and 31 μL DMSO. Wells 2-10 received 40 μL of DMSO. After mixing, 20 μL of solution from well #1 was transferred into well #2, followed by 1:3 serial dilutions out 10 steps. 2 μL of diluted compound was transferred into duplicate wells of 384 well "assay plate" and then 90 μL of buffer was added. After incubation, both the cell and "assay" plates were brought to the FLIPR and 20 μL of the diluted compounds were transferred to the cell plates by the FLIPR. Compound addition was monitored by the FLIPR to detect any agonist activity of the compounds. Plates were then incubated for 30 minutes at room temperature protected from light. After the incubation, plates were returned to the FLIPR and 20 μL of 4.5× concentrated agonist was added to the cell plates. During the assay, fluorescence readings were taken simultaneously from all 384 wells of the cell plate every 1.5 seconds. Five readings were taken to establish a stable baseline, then 20 μL of sample was rapidly (30 μL/sec) and simultaneously added to each well of the cell plate. The fluorescence was continuously monitored before, during and after sample addition for a total elapsed time of 100 seconds.Calcium Flux Assay Using Fluorometric Imaging Plate Reader (FLIPR) Assay: Test compounds were prepared by adding 90 μL of HBSS/20 mM HEPES/0.1% BSA buffer to 2 μL of serially diluted compounds. To prepare serial dilutions, 10 mM stocks of compounds were prepared in 100% DMSO. The compound dilution plate was set up as follows: well #1 received 29 μL of stock compound and 31 μL DMSO. Wells 2-10 received 40 μL of DMSO. After mixing, 20 μL of solution from well #1 was transferred into well #2, followed by 1:3 serial dilutions out 10 steps. 2 μL of diluted compound was transferred into duplicate wells of 384 well "assay plate" and then 90 μL of buffer was added. After incubation, both the cell and "assay" plates were brought to the FLIPR and 20 μL of the diluted compounds were transferred to the cell plates by the FLIPR. Compound addition was monitored by the FLIPR to detect any agonist activity of the compounds. Plates were then incubated for 30 minutes at room temperature protected from light. After the incubation, plates were returned to the FLIPR and 20 μL of 4.5× concentrated agonist was added to the cell plates. During the assay, fluorescence readings were taken simultaneously from all 384 wells of the cell plate every 1.5 seconds. Five readings were taken to establish a stable baseline, then 20 μL of sample was rapidly (30 μL/sec) and simultaneously added to each well of the cell plate. The fluorescence was continuously monitored before, during and after sample addition for a total elapsed time of 100 seconds. |
ChEMBL | 550 | 7 | 2 | 6 | 6.6 | C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 | nan | ||
1105689 | 184192 | None | 32 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -489 | 2 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentrationAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration |
ChEMBL | 380 | 7 | 4 | 4 | 2.5 | O=C(O)/C=C/C(=O)Nc1ccc(-c2ccc(NC(=O)/C=C/C(=O)O)cc2)cc1 | 10.1016/j.bmc.2008.04.035 | ||
CHEMBL482497 | 184192 | None | 32 | Human | Functional | pIC50 | = | 4.9 | 4.9 | -489 | 2 | Antagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentrationAntagonist activity at LPA3 receptor expressed in rat RH7777 cells assessed as inhibition of LPA-induced intracellular calcium concentration |
ChEMBL | 380 | 7 | 4 | 4 | 2.5 | O=C(O)/C=C/C(=O)Nc1ccc(-c2ccc(NC(=O)/C=C/C(=O)O)cc2)cc1 | 10.1016/j.bmc.2008.04.035 | ||
11393306 | 67436 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 1 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 328 | 14 | 2 | 1 | 5.8 | CCCCCCCCCCCCCCC(F)(F)P(=O)(O)O | 10.1021/jm049609r | ||
CHEMBL188859 | 67436 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 1 | 2 | Inhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptorInhibition of LPA-induced calcium transients in RH7777 rat hepatoma cells expressing LPA3 receptor |
ChEMBL | 328 | 14 | 2 | 1 | 5.8 | CCCCCCCCCCCCCCC(F)(F)P(=O)(O)O | 10.1021/jm049609r | ||
10367662 | 2186 | None | 58 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -3 | 4 | Antagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assayAntagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assay |
ChEMBL | 474 | 9 | 2 | 6 | 6.3 | OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C | 10.1021/acs.jmedchem.2c00046 | ||
2907 | 2186 | None | 58 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -3 | 4 | Antagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assayAntagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assay |
ChEMBL | 474 | 9 | 2 | 6 | 6.3 | OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C | 10.1021/acs.jmedchem.2c00046 | ||
CHEMBL361501 | 2186 | None | 58 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -3 | 4 | Antagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assayAntagonist activity at LPA3 receptor (unknown origin) expressed in cells assessed as blockade of LPA-induced calcium mobilization measured after 120 secs by Fluo-4 NW dye based assay |
ChEMBL | 474 | 9 | 2 | 6 | 6.3 | OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C | 10.1021/acs.jmedchem.2c00046 | ||
2905 | 389 | None | 41 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -89 | 7 | Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysisAntagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis |
ChEMBL | 490 | 7 | 2 | 5 | 6.9 | OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C | 10.1039/C4MD00333K | ||
46240292 | 389 | None | 41 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -89 | 7 | Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysisAntagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis |
ChEMBL | 490 | 7 | 2 | 5 | 6.9 | OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C | 10.1039/C4MD00333K | ||
CHEMBL3621966 | 389 | None | 41 | Human | Functional | pIC50 | = | 5.8 | 5.8 | -89 | 7 | Antagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysisAntagonist activity at human LPA3 receptor expressed in CHO cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 30 mins followed by LPA induction by FLIPR Calcium 4 dye-based fluorometric analysis |
ChEMBL | 490 | 7 | 2 | 5 | 6.9 | OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C | 10.1039/C4MD00333K |
Showing 1 to 50 of 270 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
| |
11496444 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335051 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2364959 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
11496444 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335051 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2364959 | 89093 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
11648176 | 87560 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335052 | 87560 | None | 0 | Human | Binding | pEC50 | = | 9.7 | 9.7 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
11648176 | 87560 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335052 | 87560 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOCC(COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
10322404 | 121145 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL357053 | 121145 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
10322404 | 121145 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL357053 | 121145 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
46223906 | 73546 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2017139 | 73546 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC | 10.1016/j.bmcl.2013.01.002 | ||
46223906 | 73546 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2017139 | 73546 | None | 0 | Human | Binding | pEC50 | = | 9.6 | 9.6 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.9 | CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)S)OC | 10.1016/j.bmcl.2013.01.002 | ||
71569054 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335049 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2365070 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
71569054 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335049 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2365070 | 89102 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 426 | 21 | 2 | 4 | 5.7 | CCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
71720690 | 87558 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335047 | 87558 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
71720690 | 87558 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335047 | 87558 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
71599962 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335050 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2365071 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
71599962 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335050 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2365071 | 89103 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 440 | 22 | 2 | 4 | 6.1 | CCCCCCCCCCCCCCCCCOC(COC)COP(O)(O)=S | 10.1016/j.bmcl.2013.01.002 | ||
44368508 | 45745 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL153043 | 45745 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
44368508 | 45745 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL153043 | 45745 | None | 0 | Human | Binding | pEC50 | = | 9.4 | 9.4 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 468 | 22 | 2 | 5 | 6.0 | CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
71719457 | 87559 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335048 | 87559 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
71719457 | 87559 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
CHEMBL2335048 | 87559 | None | 0 | Human | Binding | pEC50 | = | 9.0 | 9.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assayAgonist activity at human LPA3 receptor transfected in HEK293 cells after 1 hr by TGFalpha shedding assay |
ChEMBL | 454 | 23 | 2 | 4 | 6.5 | CCCCCCCCCCCCCCCCCCOC[C@H](COP(O)(O)=S)OC | 10.1016/j.bmcl.2013.01.002 | ||
10432221 | 123765 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assayAgonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assay |
ChEMBL | 419 | 19 | 3 | 3 | 5.6 | CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](C)COP(=O)(O)O | 10.1039/C4MD00333K | ||
CHEMBL3621958 | 123765 | None | 0 | Human | Binding | pEC50 | = | 7.0 | 7.0 | - | 0 | Agonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assayAgonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assay |
ChEMBL | 419 | 19 | 3 | 3 | 5.6 | CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](C)COP(=O)(O)O | 10.1039/C4MD00333K | ||
16045222 | 74122 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells |
ChEMBL | 440 | 18 | 2 | 6 | 4.4 | CCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC(=O)CCCCCCC | 10.1016/j.bmcl.2005.10.031 | ||
CHEMBL202242 | 74122 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells |
ChEMBL | 440 | 18 | 2 | 6 | 4.4 | CCCCCCCC(=O)OC[C@@H](COP(O)(O)=S)OC(=O)CCCCCCC | 10.1016/j.bmcl.2005.10.031 | ||
44406645 | 14881 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line |
ChEMBL | 436 | 18 | 2 | 4 | 6.0 | CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@H](COP(O)(O)=S)O1 | 10.1016/j.bmcl.2005.08.096 | ||
CHEMBL1207670 | 14881 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line |
ChEMBL | 436 | 18 | 2 | 4 | 6.0 | CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@H](COP(O)(O)=S)O1 | 10.1016/j.bmcl.2005.08.096 | ||
CHEMBL427014 | 14881 | None | 0 | Rat | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line |
ChEMBL | 436 | 18 | 2 | 4 | 6.0 | CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@H](COP(O)(O)=S)O1 | 10.1016/j.bmcl.2005.08.096 | ||
44407397 | 74123 | None | 0 | Human | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells |
ChEMBL | 396 | 20 | 2 | 4 | 5.2 | CCCCCCCCOC[C@H](COP(=O)(O)O)OCCCCCCCC | 10.1016/j.bmcl.2005.10.031 |
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