Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Potency)
# tested GPCRs
(Potency)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
5311263 4078 18 None -29 7 Human 6.9 pEC50 = 6.9 Functional
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 4078 18 None -29 7 Human 6.9 pEC50 = 6.9 Functional
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 67258 24 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 67258 24 None 1 2 Human 5.8 pEC50 = 5.8 Functional
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 4078 18 None -29 7 Human 6.6 pEC50 = 6.6 Functional
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 4078 18 None -29 7 Human 6.6 pEC50 = 6.6 Functional
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 2313 14 None -36 12 Human 6.5 pEC50 = 6.5 Functional
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 2313 14 None -36 12 Human 6.5 pEC50 = 6.5 Functional
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 2313 14 None -36 12 Human 6.5 pEC50 = 6.5 Functional
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 2313 14 None -36 12 Human 6.5 pEC50 = 6.5 Functional
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 66770 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
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 66770 0 None -2 3 Human 6.3 pEC50 = 6.3 Functional
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 123171 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
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 123171 0 None 12 2 Human 7.2 pEC50 = 7.2 Functional
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 344 0 None 8 2 Human 7.1 pEC50 = 7.1 Functional
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 344 0 None 8 2 Human 7.1 pEC50 = 7.1 Functional
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 344 0 None 8 2 Human 7.1 pEC50 = 7.1 Functional
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 4078 18 None -29 7 Human 6.1 pEC50 = 6.1 Functional
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 4078 18 None -29 7 Human 6.1 pEC50 = 6.1 Functional
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 67005 1 None 21 3 Human 7.0 pIC50 = 7.0 Functional
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 67005 1 None 21 3 Human 7.0 pIC50 = 7.0 Functional
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 123173 0 None -4 4 Human 5.9 pIC50 = 5.9 Functional
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 123173 0 None -4 4 Human 5.9 pIC50 = 5.9 Functional
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 66910 65 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 66910 65 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 66910 65 None - 1 Human 5.9 pIC50 = 5.9 Functional
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 155062 0 None -239 2 Human 4.9 pIC50 = 4.9 Functional
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 155062 0 None -239 2 Human 4.9 pIC50 = 4.9 Functional
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 66847 5 None 37 2 Human 6.9 pIC50 = 6.9 Functional
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 66847 5 None 37 2 Human 6.9 pIC50 = 6.9 Functional
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 183495 9 None -138 3 Human 5.9 pIC50 = 5.9 Functional
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 183495 9 None -138 3 Human 5.9 pIC50 = 5.9 Functional
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 183495 9 None -138 3 Human 5.9 pIC50 = 5.9 Functional
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 183495 9 None -138 3 Human 5.9 pIC50 = 5.9 Functional
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 79384 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
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 79384 0 None -1 2 Human 5.9 pIC50 = 5.9 Functional
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 82701 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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 82701 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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 82701 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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 82701 0 None -2 2 Human 6.9 pIC50 = 6.9 Functional
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 183494 34 None -489 2 Human 4.9 pIC50 = 4.9 Functional
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 183494 34 None -489 2 Human 4.9 pIC50 = 4.9 Functional
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 67063 1 None 1 2 Human 5.8 pIC50 = 5.8 Functional
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 67063 1 None 1 2 Human 5.8 pIC50 = 5.8 Functional
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 2146 82 None -4 5 Human 5.8 pIC50 = 5.8 Functional
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 2146 82 None -4 5 Human 5.8 pIC50 = 5.8 Functional
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 2146 82 None -4 5 Human 5.8 pIC50 = 5.8 Functional
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 386 41 None -89 7 Human 5.8 pIC50 = 5.8 Functional
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 386 41 None -89 7 Human 5.8 pIC50 = 5.8 Functional
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 386 41 None -89 7 Human 5.8 pIC50 = 5.8 Functional
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
11312936 67131 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
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 310 14 2 2 4.9 CCCCCCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL189296 67131 0 None 15 2 Human 6.8 pIC50 = 6.8 Functional
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 310 14 2 2 4.9 CCCCCCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
10393842 168622 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL440696 168622 0 None -1 2 Human 6.8 pIC50 = 6.8 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.03.076
72704618 159356 0 None -4 2 Human 4.7 pIC50 = 4.7 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3cccc(C4(C(=O)O)CC4)c3)cc2)nnn1C)c1ccccc1 nan
CHEMBL4107074 159356 0 None -4 2 Human 4.7 pIC50 = 4.7 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3cccc(C4(C(=O)O)CC4)c3)cc2)nnn1C)c1ccccc1 nan
71457482 82705 0 None -165 2 Human 4.7 pIC50 = 4.7 Functional
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 462 7 2 6 5.5 C[C@@H](OC(=O)Nc1c(-c2ccc(C3CCC(CC(=O)O)CC3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182051 82705 0 None -165 2 Human 4.7 pIC50 = 4.7 Functional
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 462 7 2 6 5.5 C[C@@H](OC(=O)Nc1c(-c2ccc(C3CCC(CC(=O)O)CC3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
71457482 82705 0 None -165 2 Human 4.7 pIC50 = 4.7 Functional
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 462 7 2 6 5.5 C[C@@H](OC(=O)Nc1c(-c2ccc(C3CCC(CC(=O)O)CC3)cc2)nnn1C)c1ccccc1 nan
CHEMBL2182051 82705 0 None -165 2 Human 4.7 pIC50 = 4.7 Functional
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 462 7 2 6 5.5 C[C@@H](OC(=O)Nc1c(-c2ccc(C3CCC(CC(=O)O)CC3)cc2)nnn1C)c1ccccc1 nan
71453960 82697 0 None -162 2 Human 4.7 pIC50 = 4.7 Functional
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 456 7 2 6 5.1 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182042 82697 0 None -162 2 Human 4.7 pIC50 = 4.7 Functional
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 456 7 2 6 5.1 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
71453960 82697 0 None -162 2 Human 4.7 pIC50 = 4.7 Functional
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 456 7 2 6 5.1 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)nnn1C)c1ccccc1 nan
CHEMBL2182042 82697 0 None -162 2 Human 4.7 pIC50 = 4.7 Functional
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 456 7 2 6 5.1 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(CC(=O)O)cc3)cc2)nnn1C)c1ccccc1 nan
70856266 82698 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182043 82698 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
70856266 82698 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1ccccc1 nan
CHEMBL2182043 82698 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 482 7 2 6 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1ccccc1 nan
122191545 123174 0 None -17 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 1 min followed by LPA induction measured for 15 secs 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 preincubated for 1 min followed by LPA induction measured for 15 secs by Fura-2 AM probe-based fluorometric analysis
ChEMBL 446 8 2 6 5.6 CC(OC(=O)Nc1cnoc1-c1ccc(CSCC(=O)O)cc1)c1ccccc1Cl 10.1039/C4MD00333K
CHEMBL3621965 123174 0 None -17 2 Human 5.6 pIC50 = 5.6 Functional
Antagonist activity at human LPA3 receptor expressed in RH7777 cells assessed as inhibition of LPA-induced calcium mobilization preincubated for 1 min followed by LPA induction measured for 15 secs 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 preincubated for 1 min followed by LPA induction measured for 15 secs by Fura-2 AM probe-based fluorometric analysis
ChEMBL 446 8 2 6 5.6 CC(OC(=O)Nc1cnoc1-c1ccc(CSCC(=O)O)cc1)c1ccccc1Cl 10.1039/C4MD00333K
71452129 82703 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 559 8 2 8 4.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182049 82703 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 559 8 2 8 4.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1ccccc1 10.1021/jm301022v
71452129 82703 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 559 8 2 8 4.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1ccccc1 nan
CHEMBL2182049 82703 0 None -120 2 Human 5.6 pIC50 = 5.6 Functional
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 559 8 2 8 4.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1ccccc1 nan
44325401 105625 0 None 1 2 Human 5.6 pIC50 = 5.6 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 627 23 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL313413 105625 0 None 1 2 Human 5.6 pIC50 = 5.6 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 627 23 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OC2Cc3ccccc3C2)cc1 10.1016/j.bmcl.2004.03.076
11849496 79181 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
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 406 16 1 4 6.1 CCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 10.1021/jm060351+
CHEMBL211465 79181 0 None -2 2 Human 5.6 pIC50 = 5.6 Functional
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 406 16 1 4 6.1 CCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 10.1021/jm060351+
CHEMBL2372286 208455 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 None None None NCC(=O)N[C@@H](CSc1ccc([N+](=O)[O-])cc1[N+](=O)[O-])C(=O)N[C@@H](CCC(=O)O)C(=O)O 10.1016/j.bmc.2008.04.035
CHEMBL2372286 208455 1 None - 1 Human 7.6 pIC50 = 7.6 Functional
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 None None None NCC(=O)N[C@@H](CSc1ccc([N+](=O)[O-])cc1[N+](=O)[O-])C(=O)N[C@@H](CCC(=O)O)C(=O)O 10.1016/j.bmc.2009.09.022
44325681 106399 0 None 2 2 Human 5.6 pIC50 = 5.6 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 626 23 4 4 9.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(Oc2cc3ccccc3[nH]2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL314554 106399 0 None 2 2 Human 5.6 pIC50 = 5.6 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 626 23 4 4 9.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(Oc2cc3ccccc3[nH]2)cc1 10.1016/j.bmcl.2004.03.076
11208266 67275 1 None 25 2 Human 7.6 pIC50 = 7.6 Functional
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 280 11 2 2 3.9 CC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL190484 67275 1 None 25 2 Human 7.6 pIC50 = 7.6 Functional
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 280 11 2 2 3.9 CC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
71455703 82699 0 None -1445 2 Human 4.6 pIC50 = 4.6 Functional
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 500 7 2 6 5.7 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2F)nnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182044 82699 0 None -1445 2 Human 4.6 pIC50 = 4.6 Functional
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 500 7 2 6 5.7 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2F)nnn1C)c1ccccc1 10.1021/jm301022v
71455703 82699 0 None -1445 2 Human 4.6 pIC50 = 4.6 Functional
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 500 7 2 6 5.7 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2F)nnn1C)c1ccccc1 nan
CHEMBL2182044 82699 0 None -1445 2 Human 4.6 pIC50 = 4.6 Functional
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 500 7 2 6 5.7 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2F)nnn1C)c1ccccc1 nan
72704617 151707 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 CC(OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 nan
CHEMBL3969018 151707 0 None -6 2 Human 6.6 pIC50 = 6.6 Functional
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 CC(OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 nan
10468943 1424 5 None 35 3 Human 7.6 pIC50 = 7.6 Functional
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 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
6990 1424 5 None 35 3 Human 7.6 pIC50 = 7.6 Functional
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 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
CHEMBL191365 1424 5 None 35 3 Human 7.6 pIC50 = 7.6 Functional
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 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
11220562 66758 0 None 16 2 Human 7.6 pIC50 = 7.6 Functional
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 308 13 2 2 4.7 CCCC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL187402 66758 0 None 16 2 Human 7.6 pIC50 = 7.6 Functional
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 308 13 2 2 4.7 CCCC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
753410 200262 9 None -4 2 Human 5.5 pIC50 = 5.5 Functional
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 311 4 1 4 2.5 Cc1ccc(Oc2ccc3c(c2)C(=O)N(CC(=O)O)C3=O)cc1 10.1016/j.bmc.2009.09.022
CHEMBL607806 200262 9 None -4 2 Human 5.5 pIC50 = 5.5 Functional
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 311 4 1 4 2.5 Cc1ccc(Oc2ccc3c(c2)C(=O)N(CC(=O)O)C3=O)cc1 10.1016/j.bmc.2009.09.022
5861754 184175 2 None 11 2 Human 7.5 pIC50 = 7.5 Functional
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 348 7 5 5 0.5 O=C(O)/C=C/C(=O)Nc1cccc(NC(=O)/C=C/C(=O)O)c1C(=O)O 10.1016/j.bmc.2008.04.035
CHEMBL485119 184175 2 None 11 2 Human 7.5 pIC50 = 7.5 Functional
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 348 7 5 5 0.5 O=C(O)/C=C/C(=O)Nc1cccc(NC(=O)/C=C/C(=O)O)c1C(=O)O 10.1016/j.bmc.2008.04.035
5861754 184175 2 None 11 2 Human 7.5 pIC50 = 7.5 Functional
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 348 7 5 5 0.5 O=C(O)/C=C/C(=O)Nc1cccc(NC(=O)/C=C/C(=O)O)c1C(=O)O 10.1016/j.bmc.2009.09.022
CHEMBL485119 184175 2 None 11 2 Human 7.5 pIC50 = 7.5 Functional
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 348 7 5 5 0.5 O=C(O)/C=C/C(=O)Nc1cccc(NC(=O)/C=C/C(=O)O)c1C(=O)O 10.1016/j.bmc.2009.09.022
10367662 2146 82 None -4 5 Human 6.5 pIC50 = 6.5 Functional
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 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
2907 2146 82 None -4 5 Human 6.5 pIC50 = 6.5 Functional
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 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
CHEMBL361501 2146 82 None -4 5 Human 6.5 pIC50 = 6.5 Functional
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 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
78401 67490 54 None 1 2 Human 5.5 pIC50 = 5.5 Functional
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 278 13 2 1 4.9 CCCCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
CHEMBL190999 67490 54 None 1 2 Human 5.5 pIC50 = 5.5 Functional
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 278 13 2 1 4.9 CCCCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
11219269 67260 1 None 22 2 Human 7.5 pIC50 = 7.5 Functional
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 264 11 2 2 3.8 CC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL190349 67260 1 None 22 2 Human 7.5 pIC50 = 7.5 Functional
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 264 11 2 2 3.8 CC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44325366 205682 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 591 26 3 4 8.0 C#CCCCCOc1ccc(C[C@H](COP(=O)(O)O)NC(=O)CCCCCCC/C=C\CCCCCCCC)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL94034 205682 0 None - 1 Human 5.5 pIC50 = 5.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 591 26 3 4 8.0 C#CCCCCOc1ccc(C[C@H](COP(=O)(O)O)NC(=O)CCCCCCC/C=C\CCCCCCCC)cc1 10.1016/j.bmcl.2004.03.076
11288209 123858 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 252 10 2 2 3.1 C=CCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL363935 123858 2 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 252 10 2 2 3.1 C=CCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
2230607 95940 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 310 5 3 3 2.5 O=C(O)/C=C\C(=O)Nc1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmc.2008.04.035
CHEMBL261872 95940 4 None - 1 Human 6.5 pIC50 = 6.5 Functional
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 310 5 3 3 2.5 O=C(O)/C=C\C(=O)Nc1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmc.2008.04.035
44325391 205192 0 None 30 2 Human 7.5 pIC50 = 7.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 631 25 3 5 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL91058 205192 0 None 30 2 Human 7.5 pIC50 = 7.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 631 25 3 5 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
44325365 111847 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 581 25 3 4 8.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCCC(C)C)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL329422 111847 0 None - 1 Human 6.5 pIC50 = 6.5 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 581 25 3 4 8.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCCC(C)C)cc1 10.1016/j.bmcl.2004.03.076
4030 1326 15 None 6 2 Human 6.4 pIC50 = 6.4 Functional
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 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
62532 1326 15 None 6 2 Human 6.4 pIC50 = 6.4 Functional
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 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL361255 1326 15 None 6 2 Human 6.4 pIC50 = 6.4 Functional
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 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
75816 66822 50 None 7 3 Human 6.4 pIC50 = 6.4 Functional
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 266 12 2 2 4.0 CCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL187711 66822 50 None 7 3 Human 6.4 pIC50 = 6.4 Functional
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 266 12 2 2 4.0 CCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
9958483 97375 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
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 525 12 1 5 6.5 COc1cc(OC)cc(C(=O)N(CCCc2ccccc2)Cc2ccc(Oc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmcl.2007.12.024
CHEMBL272087 97375 0 None 2 2 Human 7.4 pIC50 = 7.4 Functional
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 525 12 1 5 6.5 COc1cc(OC)cc(C(=O)N(CCCc2ccccc2)Cc2ccc(Oc3ccccc3C(=O)O)cc2)c1 10.1016/j.bmcl.2007.12.024
44325390 111838 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 607 24 3 4 8.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCC2CCCCC2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL329378 111838 0 None - 1 Human 5.4 pIC50 = 5.4 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 607 24 3 4 8.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCC2CCCCC2)cc1 10.1016/j.bmcl.2004.03.076
82327 66808 13 None 5 2 Human 6.4 pIC50 = 6.4 Functional
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 294 14 2 2 4.8 CCCCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL187633 66808 13 None 5 2 Human 6.4 pIC50 = 6.4 Functional
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 294 14 2 2 4.8 CCCCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44325400 105624 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 705 26 3 8 8.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OC(=O)c2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL313412 105624 0 None - 1 Human 6.4 pIC50 = 6.4 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 705 26 3 8 8.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OC(=O)c2cc(OC)c(OC)c(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
869604 200593 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 342 5 1 6 2.1 O=C(O)CN1C(=O)c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2C1=O 10.1016/j.bmc.2009.09.022
CHEMBL610179 200593 9 None - 1 Human 5.4 pIC50 = 5.4 Functional
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 342 5 1 6 2.1 O=C(O)CN1C(=O)c2ccc(Oc3cccc([N+](=O)[O-])c3)cc2C1=O 10.1016/j.bmc.2009.09.022
10051843 1396 1 None 24 2 Human 6.3 pIC50 = 6.3 Functional
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 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
2916 1396 1 None 24 2 Human 6.3 pIC50 = 6.3 Functional
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 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
CHEMBL191055 1396 1 None 24 2 Human 6.3 pIC50 = 6.3 Functional
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 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
71462858 82680 0 None -11 2 Human 6.3 pIC50 = 6.3 Functional
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 549 7 2 5 7.2 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
CHEMBL2182023 82680 0 None -11 2 Human 6.3 pIC50 = 6.3 Functional
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 549 7 2 5 7.2 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
11755685 67155 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 499 20 4 4 5.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1ccc(OP(=O)(O)O)cc1)C(=O)O 10.1021/jm049609r
CHEMBL189515 67155 0 None - 1 Human 5.3 pIC50 = 5.3 Functional
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 499 20 4 4 5.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1ccc(OP(=O)(O)O)cc1)C(=O)O 10.1021/jm049609r
71452130 82713 0 None -239 2 Human 5.2 pIC50 = 5.2 Functional
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 499 7 2 5 6.3 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccccc1F 10.1021/jm301022v
CHEMBL2182064 82713 0 None -239 2 Human 5.2 pIC50 = 5.2 Functional
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 499 7 2 5 6.3 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccccc1F 10.1021/jm301022v
44325364 205461 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 581 25 3 4 8.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCCC(C)C)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL92593 205461 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 581 25 3 4 8.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCCC(C)C)cc1 10.1016/j.bmcl.2004.03.076
71455704 82702 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
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
CHEMBL2182047 82702 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
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
71455704 82702 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
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
CHEMBL2182047 82702 0 None -2 2 Human 5.2 pIC50 = 5.2 Functional
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
44325370 205690 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 539 23 3 4 7.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCC)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL94089 205690 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 539 23 3 4 7.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCC)cc1 10.1016/j.bmcl.2004.03.076
11599847 204999 0 None 8 2 Human 6.2 pIC50 = 6.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 631 25 3 5 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL89937 204999 0 None 8 2 Human 6.2 pIC50 = 6.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 631 25 3 5 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
5311306 96087 2 None -1 2 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL262906 96087 2 None -1 2 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.03.076
71457481 82704 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
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 627 8 2 8 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
CHEMBL2182050 82704 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
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 627 8 2 8 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
71457481 82704 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
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 627 8 2 8 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 nan
CHEMBL2182050 82704 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
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 627 8 2 8 5.6 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)NS(C)(=O)=O)CC4)cc3)cc2)nnn1C)c1cccc(C(F)(F)F)c1 nan
78816 123511 51 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 250 11 2 1 4.1 CCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
CHEMBL363067 123511 51 None - 1 Human 6.2 pIC50 = 6.2 Functional
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 250 11 2 1 4.1 CCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
3114900 113087 51 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assayAntagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay
ChEMBL 391 6 1 4 4.3 O=C(O)c1ccccc1SCCCN1C(=O)c2cccc3cccc(c23)C1=O 10.1021/jm5007116
CHEMBL3322500 113087 51 None -1 2 Human 5.2 pIC50 = 5.2 Functional
Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assayAntagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay
ChEMBL 391 6 1 4 4.3 O=C(O)c1ccccc1SCCCN1C(=O)c2cccc3cccc(c23)C1=O 10.1021/jm5007116
44325421 168660 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 575 23 3 4 7.9 CCCCCCCCCCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL441066 168660 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 575 23 3 4 7.9 CCCCCCCCCCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1016/j.bmcl.2004.03.076
71455702 82688 0 None -39 2 Human 5.2 pIC50 = 5.2 Functional
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 6.7 Cc1nnn(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)c1NC(=O)O[C@H](C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
CHEMBL2182032 82688 0 None -39 2 Human 5.2 pIC50 = 5.2 Functional
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 6.7 Cc1nnn(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)c1NC(=O)O[C@H](C)c1cccc(C(F)(F)F)c1 10.1021/jm301022v
44325351 162839 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 539 23 3 4 7.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCC)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL419507 162839 0 None - 1 Human 5.2 pIC50 = 5.2 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 539 23 3 4 7.3 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCC)cc1 10.1016/j.bmcl.2004.03.076
44325422 106622 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 605 24 3 5 7.9 CCCCCCCCCCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL316067 106622 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 605 24 3 5 7.9 CCCCCCCCCCCCCCCC(=O)NC(COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)c2)cc1 10.1016/j.bmcl.2004.03.076
1365686 199713 31 None -8 3 Human 6.1 pIC50 = 6.1 Functional
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 404 5 1 6 3.9 O=C(O)c1ccc2c(c1)C(=O)N(c1cccc(Oc3ccc([N+](=O)[O-])cc3)c1)C2=O 10.1016/j.bmc.2009.09.022
CHEMBL604677 199713 31 None -8 3 Human 6.1 pIC50 = 6.1 Functional
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 404 5 1 6 3.9 O=C(O)c1ccc2c(c1)C(=O)N(c1cccc(Oc3ccc([N+](=O)[O-])cc3)c1)C2=O 10.1016/j.bmc.2009.09.022
11447695 123834 2 None 4 2 Human 6.1 pIC50 = 6.1 Functional
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 236 10 2 2 3.0 C=CCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL363776 123834 2 None 4 2 Human 6.1 pIC50 = 6.1 Functional
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 236 10 2 2 3.0 C=CCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44414925 77713 0 None -72 2 Human 5.1 pIC50 = 5.1 Functional
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 436 18 1 4 7.1 CCCCCCCCCCCCCCCCCC(=O)OC[C@@H]1CC(F)P(=O)(O)O1 10.1021/jm060351+
CHEMBL210117 77713 0 None -72 2 Human 5.1 pIC50 = 5.1 Functional
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 436 18 1 4 7.1 CCCCCCCCCCCCCCCCCC(=O)OC[C@@H]1CC(F)P(=O)(O)O1 10.1021/jm060351+
71452131 82714 0 None -144 2 Human 5.1 pIC50 = 5.1 Functional
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 499 7 2 5 6.3 CC(OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccc(F)cc1 10.1021/jm301022v
CHEMBL2182065 82714 0 None -144 2 Human 5.1 pIC50 = 5.1 Functional
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 499 7 2 5 6.3 CC(OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccc(F)cc1 10.1021/jm301022v
11276402 66909 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 236 9 2 2 3.0 CCCCC/C=C/CCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL188081 66909 1 None - 1 Human 6.1 pIC50 = 6.1 Functional
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 236 9 2 2 3.0 CCCCC/C=C/CCCOP(=O)(O)O 10.1021/jm049609r
66553162 82712 1 None -407 2 Human 5.1 pIC50 = 5.1 Functional
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 481 7 2 5 6.2 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccccc1 10.1021/jm301022v
CHEMBL2182063 82712 1 None -407 2 Human 5.1 pIC50 = 5.1 Functional
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 481 7 2 5 6.2 C[C@@H](OC(=O)Nc1c(-c2ccc(-c3ccc(C4(C(=O)O)CC4)cc3)cc2)cnn1C)c1ccccc1 10.1021/jm301022v
44325680 205458 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 626 23 4 4 9.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(Oc2cc3ccccc3[nH]2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL92584 205458 0 None - 1 Human 5.0 pIC50 = 5.0 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 626 23 4 4 9.1 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(Oc2cc3ccccc3[nH]2)cc1 10.1016/j.bmcl.2004.03.076
44325682 106400 1 None -1 2 Human 6.0 pIC50 = 6.0 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.03.076
CHEMBL314555 106400 1 None -1 2 Human 6.0 pIC50 = 6.0 Functional
In vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell linesIn vitro antagonism of LPA-evoked [35S]GTP-gamma-S binding to lysophosphatidic acid receptor 3 in HEK293T cell lines
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.03.076
11197104 67269 1 None 4 3 Human 7.0 pIC50 = 7.0 Functional
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 CCCC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL190430 67269 1 None 4 3 Human 7.0 pIC50 = 7.0 Functional
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 CCCC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
11849496 79181 0 None -2 2 Human 5.9 pKi = 5.9 Functional
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 406 16 1 4 6.1 CCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 10.1021/jm060351+
CHEMBL211465 79181 0 None -2 2 Human 5.9 pKi = 5.9 Functional
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 406 16 1 4 6.1 CCCCCCCCCCCCCCCC(=O)OCC1CCP(O)(=S)O1 10.1021/jm060351+
16725999 720 1 None - 2 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 486 19 3 4 5.7 CCCCCCCCCCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)Br)O 10.1039/C4MD00255E
6985 720 1 None - 2 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 486 19 3 4 5.7 CCCCCCCCCCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)Br)O 10.1039/C4MD00255E
CHEMBL3621357 720 1 None - 2 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 486 19 3 4 5.7 CCCCCCCCCCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)Br)O 10.1039/C4MD00255E
87470750 123286 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 512 20 3 4 6.2 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O 10.1039/C4MD00255E
CHEMBL3621353 123286 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 512 20 3 4 6.2 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O 10.1039/C4MD00255E
CHEMBL3623936 123286 0 None - 0 Human 6.8 pKi = 6.8 Functional
Antagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assayAntagonist activity at human LPA3 receptor expressed in RG7777 cells assessed as inhibition of LPA-induced Ca2+ mobilization by FURA-2AM dye based fluorescence assay
ChEMBL 512 20 3 4 6.2 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)CC(Br)P(=O)(O)O 10.1039/C4MD00255E
2260227 183495 9 None -138 3 Human 6.5 pKi = 6.5 Functional
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 183495 9 None -138 3 Human 6.5 pKi = 6.5 Functional
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
2230607 95940 4 None - 1 Human 6.5 pKi = 6.5 Functional
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 310 5 3 3 2.5 O=C(O)/C=C\C(=O)Nc1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmc.2008.04.035
CHEMBL261872 95940 4 None - 1 Human 6.5 pKi = 6.5 Functional
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 310 5 3 3 2.5 O=C(O)/C=C\C(=O)Nc1cccc(NC(=O)c2ccccc2)c1 10.1016/j.bmc.2008.04.035
44414925 77713 0 None -72 2 Human 5.5 pKi = 5.5 Functional
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 436 18 1 4 7.1 CCCCCCCCCCCCCCCCCC(=O)OC[C@@H]1CC(F)P(=O)(O)O1 10.1021/jm060351+
CHEMBL210117 77713 0 None -72 2 Human 5.5 pKi = 5.5 Functional
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 436 18 1 4 7.1 CCCCCCCCCCCCCCCCCC(=O)OC[C@@H]1CC(F)P(=O)(O)O1 10.1021/jm060351+
90665720 108766 0 None - 0 Human 7.3 pKi = 7.3 Functional
Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation countingCompetitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 702 27 3 6 9.0 CCCCCCCCCCCCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1039/c0md00273a
CHEMBL3218459 108766 0 None - 0 Human 7.3 pKi = 7.3 Functional
Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation countingCompetitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 702 27 3 6 9.0 CCCCCCCCCCCCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1039/c0md00273a
23725184 108767 1 None - 0 Human 6.3 pKi = 6.3 Functional
Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation countingCompetitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 670 24 3 5 8.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](/C=C/P(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1039/c0md00273a
CHEMBL3218460 108767 1 None - 0 Human 6.3 pKi = 6.3 Functional
Competitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation countingCompetitive antagonist activity at N-terminal 3XHA-tagged human LPA3 receptor overexpressed in CHO cells assessed as inhibition of LPA-induced [35S]GTPgammaS binding by liquid scintillation counting
ChEMBL 670 24 3 5 8.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](/C=C/P(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1039/c0md00273a
16043259 79384 0 None -1 2 Human 6.2 pKi = 6.2 Functional
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 79384 0 None -1 2 Human 6.2 pKi = 6.2 Functional
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+
1105689 183494 34 None -489 2 Human 5.2 pKi = 5.2 Functional
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 183494 34 None -489 2 Human 5.2 pKi = 5.2 Functional
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
6983 2863 0 None -2 4 Mouse 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 907 48 0 7 19.6 CCCCCCCC/C=C\CCCCCCCC(=O)OP(=O)(SC(=O)CCCCCCC/C=C\CCCCCCCC)OC(=O)CCCCCCC/C=C\CCCCCCCC 16033271
73755251 2863 0 None -2 4 Mouse 6.3 pEC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 907 48 0 7 19.6 CCCCCCCC/C=C\CCCCCCCC(=O)OP(=O)(SC(=O)CCCCCCC/C=C\CCCCCCCC)OC(=O)CCCCCCC/C=C\CCCCCCCC 16033271
2906 2313 14 None -31 12 Mouse 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 18781939
5395 2313 14 None -31 12 Mouse 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 18781939
5497152 2313 14 None -31 12 Mouse 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 18781939
CHEMBL1222042 2313 14 None -31 12 Mouse 6.6 pEC50 = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 18781939
16078994 2871 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 12554733
2912 2871 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 12554733
CHEMBL1395060 2871 2 None - 1 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 12554733
11313 1172 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 261 5 1 3 3.4 CCN([C@H](c1cccc2c1oc(c2C)C)CO)CC 32409422
154733034 1172 0 None -1 3 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 261 5 1 3 3.4 CCN([C@H](c1cccc2c1oc(c2C)C)CO)CC 32409422
2913 344 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 22 2 4 6.3 CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC 16892372
56947064 344 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 22 2 4 6.3 CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC 16892372
CHEMBL3621962 344 0 None 8 2 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 452 22 2 4 6.3 CCCCCCCC/C=C\CCCCCCCCOC[C@@H](COP(=S)(O)O)OC 16892372
11314 1174 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 3.7 CCN([C@H](c1cccc2c1oc(c2C)CC)CO)CC 32409422
154733035 1174 0 None 1 3 Human 7.7 pEC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 275 6 1 3 3.7 CCN([C@H](c1cccc2c1oc(c2C)CC)CO)CC 32409422
10074712 3651 0 None 1000 2 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 19 1 6 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(S[Na])O 18781939
23701997 3651 0 None 1000 2 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 19 1 6 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(S[Na])O 18781939
6984 3651 0 None 1000 2 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 19 1 6 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(S[Na])O 18781939
73755252 3651 0 None 1000 2 Mouse 9.3 pEC50 = 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 500 19 1 6 6.7 CCCCCCCC/C=C\CCCCCCCC(=O)O[C@@H]1COCC[C@@H]1OP(=O)(S[Na])O 18781939
17757220 2663 0 None -165 3 Mouse 5.3 pEC50 > 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 405 19 3 3 5.2 CCCCCCCC/C=C/CCCCCCCC(=O)NCCOP(=O)(O)O 18781939
6982 2663 0 None -165 3 Mouse 5.3 pEC50 > 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 405 19 3 3 5.2 CCCCCCCC/C=C/CCCCCCCC(=O)NCCOP(=O)(O)O 18781939
CHEMBL1574292 2663 0 None -165 3 Mouse 5.3 pEC50 > 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 405 19 3 3 5.2 CCCCCCCC/C=C/CCCCCCCC(=O)NCCOP(=O)(O)O 18781939
2936 85 0 None -1 4 Human 8.0 pEC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC(COP(=O)(O)O)CO 10922489
56947016 85 0 None -1 4 Human 8.0 pEC50 None 8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC(COP(=O)(O)O)CO 10922489
2915 356 0 None - 1 Human 9.3 pEC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 4 6.4 CCCCCCCC/C=C/CCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)F)OC 15857137
44400349 356 0 None - 1 Human 9.3 pEC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 4 6.4 CCCCCCCC/C=C/CCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)F)OC 15857137
CHEMBL190717 356 0 None - 1 Human 9.3 pEC50 None 9.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 466 21 2 4 6.4 CCCCCCCC/C=C/CCCCCCCC(=O)OC[C@H](CC(P(=O)(O)O)F)OC 15857137
6989 964 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 297 2 1 4 3.1 Cc1ccc(cc1)Oc1ccc2c(c1)C(=O)N(C2=O)C(=O)O 19800804
73755253 964 0 None - 1 Mouse 5.5 pIC50 = 5.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 297 2 1 4 3.1 Cc1ccc(cc1)Oc1ccc2c(c1)C(=O)N(C2=O)C(=O)O 19800804
10282223 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
10282223 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 18781939
2909 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
2909 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 18781939
CHEMBL327240 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
CHEMBL327240 3935 3 None -5 3 Human 5.8 pIC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 18781939
6579 1867 0 None -138 2 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 10 2 6 4.7 O=C/C=C\C(=O)Nc1ccc(cc1)Oc1cccc(c1)Oc1ccc(cc1)NC(=O)/C=C\C=O 19800804
73755226 1867 0 None -138 2 Human 5.9 pIC50 = 5.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 456 10 2 6 4.7 O=C/C=C\C(=O)Nc1ccc(cc1)Oc1cccc(c1)Oc1ccc(cc1)NC(=O)/C=C\C=O 19800804
2908 3939 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
44392752 3939 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
CHEMBL184055 3939 0 None -1 3 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
11132720 1585 0 None 4 4 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 19366702
2910 1585 0 None 4 4 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 19366702
DB07780 1585 0 None 4 4 Human 6.8 pIC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 19366702
10051843 1396 1 None 24 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
2916 1396 1 None 24 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
CHEMBL191055 1396 1 None 24 2 Human 7.0 pIC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
2905 386 41 None -89 7 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573
46240292 386 41 None -89 7 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573
CHEMBL3621966 386 41 None -89 7 Human 5.7 pIC50 None 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573
2911 1586 0 None -10 4 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 9 2 2 4.5 C/C(=C/CC/C(=C\COP(=O)(O)O)/C)/CCC=C(C)C 19366702
6440220 1586 0 None -10 4 Human 6.3 pIC50 None 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 302 9 2 2 4.5 C/C(=C/CC/C(=C\COP(=O)(O)O)/C)/CCC=C(C)C 19366702
2908 3939 0 None -1 3 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
44392752 3939 0 None -1 3 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
CHEMBL184055 3939 0 None -1 3 Human 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 15125924
2905 386 41 None -7 7 Mouse 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573
46240292 386 41 None -7 7 Mouse 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573
CHEMBL3621966 386 41 None -7 7 Mouse 6.8 pIC50 None 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 490 7 2 5 6.9 OC(=O)Cc1ccc(cc1)c1ccc(cc1)c1onc(c1NC(=O)O[C@@H](c1ccccc1Cl)C)C 20649573




Ligands Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb ID #Vendors Reference
ligand
Fold selectivity
(Affinity)
# tested GPCRs
(Affinity)
Species p-value
(-log)
Type Activity
Relation
Activity
Value
Assay Type Assay Description Source Mol
weight
Rot
Bonds
H don H acc LogP Smiles DOI
11496444 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 88616 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 87084 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 87084 0 None - 0 Human 9.7 pEC50 = 9.7 Binding
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 87084 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 87084 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 120555 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 120555 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 120555 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 120555 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 73159 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 73159 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 73159 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 73159 0 None - 0 Human 9.6 pEC50 = 9.6 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88625 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 87082 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 87082 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 87082 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 87082 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 88626 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 45459 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 45459 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 45459 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 45459 0 None - 0 Human 9.4 pEC50 = 9.4 Binding
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 87083 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
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 87083 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
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 87083 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
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 87083 0 None - 0 Human 9.0 pEC50 = 9.0 Binding
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 123168 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 123168 0 None - 0 Human 7.0 pEC50 = 7.0 Binding
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 73733 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 73733 0 None - 0 Human 6.9 pEC50 = 6.9 Binding
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 14691 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 14691 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 14691 0 None - 0 Rat 6.9 pEC50 = 6.9 Binding
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 73734 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
CHEMBL202243 73734 0 None - 0 Human 6.8 pEC50 = 6.8 Binding
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
16044834 14513 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
CHEMBL1206092 14513 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
CHEMBL199400 14513 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
16044830 14515 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
CHEMBL1206094 14515 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
CHEMBL200003 14515 0 None - 0 Rat 6.7 pEC50 = 6.7 Binding
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
16044832 14690 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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
CHEMBL1207662 14690 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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
CHEMBL425218 14690 0 None - 0 Rat 6.6 pEC50 = 6.6 Binding
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
16078994 2871 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 10.1039/C4MD00333K
2912 2871 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 10.1039/C4MD00333K
CHEMBL1395060 2871 2 None - 0 Human 6.6 pEC50 = 6.6 Binding
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 466 21 2 5 5.8 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](COP(=S)(O)O)OC 10.1039/C4MD00333K
11625765 73023 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@H](COP(O)(O)=S)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL201482 73023 0 None - 0 Human 8.5 pEC50 = 8.5 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@H](COP(O)(O)=S)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
58787991 123166 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 435 20 4 4 4.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CO)COP(=O)(O)O 10.1039/C4MD00333K
CHEMBL3621956 123166 0 None - 0 Human 6.5 pEC50 = 6.5 Binding
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 435 20 4 4 4.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CO)COP(=O)(O)O 10.1039/C4MD00333K
6419701 125269 12 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 410 19 3 5 4.5 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
CHEMBL364797 125269 12 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 410 19 3 5 4.5 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
6419701 125269 12 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 410 19 3 5 4.5 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
CHEMBL364797 125269 12 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 410 19 3 5 4.5 CCCCCCCCCCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
16044826 14514 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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/CCCCCCCCC1OCC(COP(O)(O)=S)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1206093 14514 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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/CCCCCCCCC1OCC(COP(O)(O)=S)O1 10.1016/j.bmcl.2005.08.096
CHEMBL199472 14514 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
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/CCCCCCCCC1OCC(COP(O)(O)=S)O1 10.1016/j.bmcl.2005.08.096
10410675 123167 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 434 20 4 4 4.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CN)COP(=O)(O)O 10.1039/C4MD00333K
CHEMBL3621957 123167 0 None - 0 Human 6.2 pEC50 = 6.2 Binding
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 434 20 4 4 4.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CN)COP(=O)(O)O 10.1039/C4MD00333K
11497157 14511 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 472 17 2 4 6.1 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(O)(O)=S)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL1206088 14511 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 472 17 2 4 6.1 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(O)(O)=S)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL198406 14511 0 None - 0 Rat 6.2 pEC50 = 6.2 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 472 17 2 4 6.1 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(O)(O)=S)O2)cc1 10.1016/j.bmcl.2005.08.096
44406650 14637 0 None - 0 Rat 5.1 pEC50 = 5.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 416 16 2 4 5.4 C/C=C/C/C=C/C/C=C/CCCCCCCCC1OCC(COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207268 14637 0 None - 0 Rat 5.1 pEC50 = 5.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 416 16 2 4 5.4 C/C=C/C/C=C/C/C=C/CCCCCCCCC1OCC(COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL383362 14637 0 None - 0 Rat 5.1 pEC50 = 5.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 416 16 2 4 5.4 C/C=C/C/C=C/C/C=C/CCCCCCCCC1OCC(COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
5311263 4078 18 None - 1 Human 7.1 pEC50 = 7.1 Binding
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 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
CHEMBL117021 4078 18 None - 1 Human 7.1 pEC50 = 7.1 Binding
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 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
5311263 4078 18 None - 1 Human 7.1 pEC50 = 7.1 Binding
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 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
CHEMBL117021 4078 18 None - 1 Human 7.1 pEC50 = 7.1 Binding
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 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OC[C@@H](O)COP(=O)(O)O 10.1016/j.bmcl.2013.01.002
11568387 73875 0 None 72 2 Human 8.0 pIC50 = 8.0 Binding
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
CHEMBL202361 73875 0 None 72 2 Human 8.0 pIC50 = 8.0 Binding
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
16044836 14698 0 None - 1 Rat 6.9 pIC50 = 6.9 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207755 14698 0 None - 1 Rat 6.9 pIC50 = 6.9 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL436763 14698 0 None - 1 Rat 6.9 pIC50 = 6.9 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
44407394 75038 0 None 9 2 Human 6.8 pIC50 = 6.8 Binding
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
CHEMBL203986 75038 0 None 9 2 Human 6.8 pIC50 = 6.8 Binding
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
23629653 183497 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of LPA3 receptorInhibition of LPA3 receptor
ChEMBL 396 16 2 6 3.5 CCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCC 10.1016/j.bmc.2008.04.035
CHEMBL482505 183497 1 None - 0 Human 6.8 pIC50 = 6.8 Binding
Inhibition of LPA3 receptorInhibition of LPA3 receptor
ChEMBL 396 16 2 6 3.5 CCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCC 10.1016/j.bmc.2008.04.035
10393842 168622 0 None -9 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assayAntagonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assay
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1039/C4MD00333K
CHEMBL440696 168622 0 None -9 2 Human 6.8 pIC50 = 6.8 Binding
Antagonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assayAntagonist activity at human LPA3 receptor transfected in HEK293T cells after 30 mins by GTP[gamma-35S] binding assay
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1039/C4MD00333K
44407389 2852 0 None 2 2 Human 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
6995 2852 0 None 2 2 Human 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL427017 2852 0 None 2 2 Human 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
44586491 183498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of LPA3 receptorInhibition of LPA3 receptor
ChEMBL 412 16 2 6 3.6 CCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC(=O)CCCCCC 10.1016/j.bmc.2008.04.035
CHEMBL482506 183498 0 None - 0 Human 6.7 pIC50 = 6.7 Binding
Inhibition of LPA3 receptorInhibition of LPA3 receptor
ChEMBL 412 16 2 6 3.6 CCCCCCC(=O)OC[C@H](COP(O)(O)=S)OC(=O)CCCCCC 10.1016/j.bmc.2008.04.035
11101949 140716 0 None 1 2 Human 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL383095 140716 0 None 1 2 Human 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44406681 14631 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207238 14631 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL370846 14631 0 None - 1 Rat 6.7 pIC50 = 6.7 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
44407386 168573 0 None 1 2 Human 6.6 pIC50 = 6.6 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL440396 168573 0 None 1 2 Human 6.6 pIC50 = 6.6 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44407485 138768 0 None 24 2 Human 6.5 pIC50 = 6.5 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL379248 138768 0 None 24 2 Human 6.5 pIC50 = 6.5 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44394293 75046 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL204037 75046 0 None - 1 Human 6.4 pIC50 = 6.4 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44406676 14636 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207267 14636 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL382116 14636 0 None - 1 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
44406670 14512 0 None 11 2 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL1206091 14512 0 None 11 2 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL199380 14512 0 None 11 2 Rat 6.3 pIC50 = 6.3 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
9960370 111048 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human LPA3 receptor transfected in HEK293T cellsAntagonist activity at human LPA3 receptor transfected in HEK293T cells
ChEMBL 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1039/C4MD00333K
CHEMBL328016 111048 1 None - 0 Human 5.2 pIC50 = 5.2 Binding
Antagonist activity at human LPA3 receptor transfected in HEK293T cellsAntagonist activity at human LPA3 receptor transfected in HEK293T cells
ChEMBL 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1039/C4MD00333K
128167 73628 11 None 10 2 Human 7.1 pIC50 = 7.1 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL202185 73628 11 None 10 2 Human 7.1 pIC50 = 7.1 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44407385 73736 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL202251 73736 0 None - 1 Human 6.0 pIC50 = 6.0 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44392791 96461 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL265967 96461 0 None - 1 Human 7.0 pKi = 7.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
44392834 121863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 574 23 3 4 7.7 CCCCCCCCCCCCCCCC(=O)N[C@H](CCP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360064 121863 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 574 23 3 4 7.7 CCCCCCCCCCCCCCCC(=O)N[C@H](CCP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
753410 200262 9 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to LPA3Binding affinity to LPA3
ChEMBL 311 4 1 4 2.5 Cc1ccc(Oc2ccc3c(c2)C(=O)N(CC(=O)O)C3=O)cc1 10.1016/j.bmc.2009.09.022
CHEMBL607806 200262 9 None -3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity to LPA3Binding affinity to LPA3
ChEMBL 311 4 1 4 2.5 Cc1ccc(Oc2ccc3c(c2)C(=O)N(CC(=O)O)C3=O)cc1 10.1016/j.bmc.2009.09.022
44392780 204145 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)n2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL83782 204145 0 None - 1 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)n2)cc1 10.1016/j.bmcl.2004.05.023
78401 67490 54 None 3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 278 13 2 1 4.9 CCCCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
CHEMBL190999 67490 54 None 3 2 Human 6.0 pKi = 6.0 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 278 13 2 1 4.9 CCCCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
44392725 122521 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 682 25 3 6 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)c3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360928 122521 0 None - 1 Human 5.9 pKi = 5.9 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 682 25 3 6 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)c3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
44407386 168573 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL440396 168573 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44407485 138768 0 None 24 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL379248 138768 0 None 24 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 438 18 4 4 3.5 CCCCCCCCNC(=O)[C@@H](COP(O)(O)=S)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
11101949 140716 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL383095 140716 0 None 1 2 Human 6.9 pKi = 6.9 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
4030 1326 15 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
62532 1326 15 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL361255 1326 15 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 238 10 2 2 3.2 CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
75816 66822 50 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 266 12 2 2 4.0 CCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL187711 66822 50 None 11 2 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 266 12 2 2 4.0 CCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
11288209 123858 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 252 10 2 2 3.1 C=CCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL363935 123858 2 None - 1 Human 6.9 pKi = 6.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 252 10 2 2 3.1 C=CCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
10468943 1424 5 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
6990 1424 5 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
CHEMBL191365 1424 5 None -1 2 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 10.1021/jm049609r
11220562 66758 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 308 13 2 2 4.7 CCCC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL187402 66758 0 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 308 13 2 2 4.7 CCCC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
11208266 67275 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 280 11 2 2 3.9 CC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL190484 67275 1 None - 1 Human 7.9 pKi = 7.9 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 280 11 2 2 3.9 CC/C=C/CCCCCCCCOP(O)(O)=S 10.1021/jm049609r
10367662 2146 82 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
2907 2146 82 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
CHEMBL361501 2146 82 None 1 3 Human 6.8 pKi = 6.8 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 10.1021/jm049609r
44392835 64911 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 658 25 3 5 8.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](CCP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL182773 64911 0 None - 1 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 658 25 3 5 8.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](CCP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
44392794 100042 0 None -25 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 27 3 6 8.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL291229 100042 0 None -25 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 27 3 6 8.6 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
2908 3939 0 None -95 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 10.1016/j.bmcl.2004.05.023
44392752 3939 0 None -95 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 10.1016/j.bmcl.2004.05.023
CHEMBL184055 3939 0 None -95 2 Human 5.8 pKi = 5.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1cccnc1)COP(=O)(O)O 10.1016/j.bmcl.2004.05.023
44406670 14512 0 None 11 2 Rat 6.8 pKi = 6.8 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL1206091 14512 0 None 11 2 Rat 6.8 pKi = 6.8 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
CHEMBL199380 14512 0 None 11 2 Rat 6.8 pKi = 6.8 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 456 17 2 4 5.9 CCCCCCCCc1ccc(CCCCCCC2OCC(COP(=O)(O)O)O2)cc1 10.1016/j.bmcl.2005.08.096
10393842 168622 0 None -9 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL440696 168622 0 None -9 2 Human 6.8 pKi = 6.8 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
44394293 75046 0 None - 1 Human 6.7 pKi = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL204037 75046 0 None - 1 Human 6.7 pKi = 6.7 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
10051843 1396 1 None 15 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
2916 1396 1 None 15 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
CHEMBL191055 1396 1 None 15 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 10.1021/jm049609r
44392769 122133 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccncc2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360399 122133 0 None - 1 Human 5.7 pKi = 5.7 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccncc2)cc1 10.1016/j.bmcl.2004.05.023
82327 66808 13 None 5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 294 14 2 2 4.8 CCCCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL187633 66808 13 None 5 2 Human 6.7 pKi = 6.7 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 294 14 2 2 4.8 CCCCCCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
1365686 199713 31 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to LPA3Binding affinity to LPA3
ChEMBL 404 5 1 6 3.9 O=C(O)c1ccc2c(c1)C(=O)N(c1cccc(Oc3ccc([N+](=O)[O-])cc3)c1)C2=O 10.1016/j.bmc.2009.09.022
CHEMBL604677 199713 31 None -4 3 Human 6.6 pKi = 6.6 Binding
Binding affinity to LPA3Binding affinity to LPA3
ChEMBL 404 5 1 6 3.9 O=C(O)c1ccc2c(c1)C(=O)N(c1cccc(Oc3ccc([N+](=O)[O-])cc3)c1)C2=O 10.1016/j.bmc.2009.09.022
44392848 64236 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 615 24 4 4 8.2 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)CC(O)P(=O)(O)O 10.1016/j.bmcl.2004.05.023
CHEMBL181612 64236 0 None - 1 Human 6.6 pKi = 6.6 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 615 24 4 4 8.2 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](Cc1ccc(OCc2ccccc2)cc1)CC(O)P(=O)(O)O 10.1016/j.bmcl.2004.05.023
11755685 67155 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 499 20 4 4 5.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1ccc(OP(=O)(O)O)cc1)C(=O)O 10.1021/jm049609r
CHEMBL189515 67155 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 499 20 4 4 5.8 CCCCCCCCCCCCCCCC(=O)N[C@@H](Cc1ccc(OP(=O)(O)O)cc1)C(=O)O 10.1021/jm049609r
44406676 14636 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207267 14636 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL382116 14636 0 None - 1 Rat 6.6 pKi = 6.6 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
44392726 64647 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 682 25 3 6 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)c3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL182302 64647 0 None - 1 Human 5.6 pKi = 5.6 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 682 25 3 6 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OC)c3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
11219269 67260 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 264 11 2 2 3.8 CC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL190349 67260 1 None - 1 Human 7.6 pKi = 7.6 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 264 11 2 2 3.8 CC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
78816 123511 51 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 250 11 2 1 4.1 CCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
CHEMBL363067 123511 51 None - 1 Human 6.5 pKi = 6.5 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 250 11 2 1 4.1 CCCCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
11276402 66909 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 236 9 2 2 3.0 CCCCC/C=C/CCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL188081 66909 1 None - 1 Human 6.4 pKi = 6.4 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 236 9 2 2 3.0 CCCCC/C=C/CCCOP(=O)(O)O 10.1021/jm049609r
128167 73628 11 None 10 2 Human 7.4 pKi = 7.4 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL202185 73628 11 None 10 2 Human 7.4 pKi = 7.4 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 424 18 2 6 4.3 CCCCCCCC(=O)OC[C@H](COP(=O)(O)O)OC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
44392792 65226 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 646 26 3 6 8.2 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL183143 65226 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 646 26 3 6 8.2 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
44392796 123133 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 25 3 6 8.5 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL362053 123133 0 None -1 2 Human 7.4 pKi = 7.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 25 3 6 8.5 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
11312382 67005 1 None 11 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 292 13 2 2 4.6 CC/C=C/CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL188591 67005 1 None 11 2 Human 7.4 pKi = 7.4 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 292 13 2 2 4.6 CC/C=C/CCCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44392836 127010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 658 25 3 5 8.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CCP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL366292 127010 0 None - 1 Human 5.4 pKi = 5.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 658 25 3 5 8.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](CCP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
44392795 64824 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 676 28 3 7 7.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCOC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL182446 64824 0 None -12 2 Human 6.4 pKi = 6.4 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 676 28 3 7 7.9 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCCOC)ccn2)cc1 10.1016/j.bmcl.2004.05.023
44392779 66304 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)n2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL185287 66304 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 632 25 3 6 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cccc(OC)n2)cc1 10.1016/j.bmcl.2004.05.023
44392793 65239 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 700 26 3 6 8.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL183221 65239 0 None -2 2 Human 7.3 pKi = 7.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 700 26 3 6 8.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2cc(OCC(F)(F)F)ccn2)cc1 10.1016/j.bmcl.2004.05.023
44407385 73736 0 None - 1 Human 6.3 pKi = 6.3 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL202251 73736 0 None - 1 Human 6.3 pKi = 6.3 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 422 18 4 4 3.4 CCCCCCCCNC(=O)[C@@H](COP(=O)(O)O)NC(=O)CCCCCCC 10.1016/j.bmcl.2005.10.031
11242245 66847 5 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 254 10 2 2 3.4 CCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL187795 66847 5 None - 1 Human 7.3 pKi = 7.3 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 254 10 2 2 3.4 CCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
11568387 73875 0 None 72 2 Human 8.3 pKi = 8.3 Binding
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
CHEMBL202361 73875 0 None 72 2 Human 8.3 pKi = 8.3 Binding
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
44407394 75038 0 None 9 2 Human 7.3 pKi = 7.3 Binding
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
CHEMBL203986 75038 0 None 9 2 Human 7.3 pKi = 7.3 Binding
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
11447695 123834 2 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 236 10 2 2 3.0 C=CCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL363776 123834 2 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 236 10 2 2 3.0 C=CCCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44392798 122012 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 652 24 3 5 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccc3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360131 122012 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 652 24 3 5 9.0 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@@H](COP(=O)(O)O)Cc1ccc(OCc2ccc3ccccc3n2)cc1 10.1016/j.bmcl.2004.05.023
44392797 64420 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 25 3 6 8.5 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL181917 64420 0 None - 1 Human 6.3 pKi = 6.3 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 660 25 3 6 8.5 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ncc(C)c(OC)c2C)cc1 10.1016/j.bmcl.2004.05.023
11393306 67063 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 328 14 2 1 5.8 CCCCCCCCCCCCCCC(F)(F)P(=O)(O)O 10.1021/jm049609r
CHEMBL188859 67063 1 None 1 2 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 328 14 2 1 5.8 CCCCCCCCCCCCCCC(F)(F)P(=O)(O)O 10.1021/jm049609r
11197104 67269 1 None 19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 292 13 2 2 4.6 CCCC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
CHEMBL190430 67269 1 None 19 2 Human 7.2 pKi = 7.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 292 13 2 2 4.6 CCCC/C=C/CCCCCCCCOP(=O)(O)O 10.1021/jm049609r
44397968 67676 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 603 25 3 4 8.7 CCCCCCCCCCCCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1021/jm049609r
CHEMBL191411 67676 0 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 603 25 3 4 8.7 CCCCCCCCCCCCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccc2)cc1 10.1021/jm049609r
44392762 122420 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccnc2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360727 122420 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2cccnc2)cc1 10.1016/j.bmcl.2004.05.023
44407389 2852 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
6995 2852 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
CHEMBL427017 2852 0 None 2 2 Human 7.2 pKi = 7.2 Binding
Activity at LPA3 receptor transfected RH7777 cellsActivity at LPA3 receptor transfected RH7777 cells
ChEMBL 412 20 2 4 5.3 CCCCCCCCOC[C@@H](COP(=S)(O)O)OCCCCCCCC 10.1016/j.bmcl.2005.10.031
81309 66910 65 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 222 9 2 1 3.3 CCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
88299705 66910 65 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 222 9 2 1 3.3 CCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
CHEMBL188083 66910 65 None - 1 Human 6.2 pKi = 6.2 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 222 9 2 1 3.3 CCCCCCCCCCP(=O)(O)O 10.1021/jm049609r
44392778 122132 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccncc2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL360397 122132 0 None - 1 Human 5.2 pKi = 5.2 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccncc2)cc1 10.1016/j.bmcl.2004.05.023
11312936 67131 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 310 14 2 2 4.9 CCCCCCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
CHEMBL189296 67131 0 None - 1 Human 7.1 pKi = 7.1 Binding
Binding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cellsBinding affinity for Lysophosphatidic acid receptor 3 expressed in RH7777 rat hepatoma cells
ChEMBL 310 14 2 2 4.9 CCCCCCCCCCCCCCOP(O)(O)=S 10.1021/jm049609r
44406681 14631 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207238 14631 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL370846 14631 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@H]1OC[C@@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
16044836 14698 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL1207755 14698 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
CHEMBL436763 14698 0 None - 1 Rat 7.1 pKi = 7.1 Binding
Activity at LPA3 receptor in RH7777 rat hepatoma cell lineActivity at LPA3 receptor in RH7777 rat hepatoma cell line
ChEMBL 420 18 2 4 5.9 CCCCCCC/C=C/CCCCCCCC[C@@H]1OC[C@H](COP(=O)(O)O)O1 10.1016/j.bmcl.2005.08.096
44325682 106400 1 None -6 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
CHEMBL314555 106400 1 None -6 2 Human 6.0 pKi = 6.0 Binding
Binding affinity towards Lysophosphatidic acid 3 (LPA3) receptorBinding affinity towards Lysophosphatidic acid 3 (LPA3) receptor
ChEMBL 602 24 3 5 7.8 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](COP(=O)(O)O)Cc1ccc(OCc2ccccn2)cc1 10.1016/j.bmcl.2004.05.023
2906 2313 14 None -31 4 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 10488122
5395 2313 14 None -31 4 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 10488122
5497152 2313 14 None -31 4 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 10488122
CHEMBL1222042 2313 14 None -31 4 Human 6.7 pKd None 6.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 436 20 3 5 5.0 CCCCCCCC/C=C\CCCCCCCC(=O)OCC(COP(=O)(O)O)O 10488122
11132720 1585 0 None - 1 Human 6.8 pKd None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 17092771
2910 1585 0 None - 1 Human 6.8 pKd None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 17092771
DB07780 1585 0 None - 1 Human 6.8 pKd None 6.8 Binding
UnclassifiedUnclassified
Guide to Pharmacology 382 11 3 4 4.6 C/C(=C/COP(=O)(OP(=O)(O)O)O)/CC/C=C(\CCC=C(C)C)/C 17092771
2911 1586 0 None - 1 Human 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 9 2 2 4.5 C/C(=C/CC/C(=C\COP(=O)(O)O)/C)/CCC=C(C)C 17092771
6440220 1586 0 None - 1 Human 7.3 pKd None 7.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 302 9 2 2 4.5 C/C(=C/CC/C(=C\COP(=O)(O)O)/C)/CCC=C(C)C 17092771
None 214616 0 35S-GTPGammaS -38 3 Human 6.6 pKi = 6.6 Binding
NoneNone
PDSP KiDatabase 436 20 3 5 5.0 CCCCCCCCC=CCCCCCCCC(=O)OCC(COP(=O)(O)O)O None
None 214617 0 35S-GTPGammaS -125 3 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 252 4 0 4 3.8 COP(=O)(OC)SC1=CC=C(C=C1)Cl None
10051843 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
10051843 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 14500756
2916 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
2916 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 14500756
CHEMBL191055 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 11562440
CHEMBL191055 1396 1 None 15 2 Human 6.3 pKi = 6.3 Binding
UnclassifiedUnclassified
Guide to Pharmacology 504 20 3 8 4.4 CCCCCCCC(=O)OC[C@@H](OC(=O)CCCCCCC)COP(=O)(OP(=O)(O)O)O 14500756
10282223 3935 3 None 2 2 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
2909 3935 3 None 2 2 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
CHEMBL327240 3935 3 None 2 2 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 601 24 3 4 8.4 CCCCCCCC/C=C\CCCCCCCC(=O)N[C@H](Cc1ccc(cc1)OCc1ccccc1)COP(=O)(O)O 11723223
10367662 2146 82 None 1 3 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 14500756
2907 2146 82 None 1 3 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 14500756
CHEMBL361501 2146 82 None 1 3 Human 6.4 pKi = 6.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 474 9 2 6 6.3 OC(=O)CCSCc1ccc(cc1)c1onc(c1NC(=O)OC(c1ccccc1Cl)C)C 14500756
1550836 1423 0 None - 1 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 12 0 4 2.8 CCCCCCCCCCCCOP(=O)([O-])[O-] 12695531
4031 1423 0 None - 1 Human 7.1 pKi = 7.1 Binding
UnclassifiedUnclassified
Guide to Pharmacology 264 12 0 4 2.8 CCCCCCCCCCCCOP(=O)([O-])[O-] 12695531
10468943 1424 5 None 1 2 Mouse 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 16033271
6990 1424 5 None 1 2 Mouse 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 16033271
CHEMBL191365 1424 5 None 1 2 Mouse 7.9 pKi = 7.9 Binding
UnclassifiedUnclassified
Guide to Pharmacology 282 12 2 2 4.1 CCCCCCCCCCCCOP(=S)(O)O 16033271