Ligand source activities (1 row/activity)





Ligands Receptor Assay information Chemical information
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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 10929 22 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 10929 22 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 74389 27 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 74389 27 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 10929 22 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 10929 22 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 9134 18 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 9134 18 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 9134 18 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 9134 18 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 73895 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 73895 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 130479 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 130479 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 7135 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 7135 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 7135 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 10929 22 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 10929 22 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 74131 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 74131 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 130481 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 130481 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 74035 68 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 74035 68 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 74035 68 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 162393 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 162393 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 73972 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 73972 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 190866 10 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 190866 10 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 190866 10 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 190866 10 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 86584 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 86584 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 89903 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 89903 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 89903 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 89903 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 190865 38 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 190865 38 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 74189 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 74189 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 8967 91 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 8967 91 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 8967 91 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 7177 49 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 7177 49 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 7177 49 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 74260 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 74260 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 175978 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 175978 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 166694 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 166694 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 89907 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 89907 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 89907 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 89907 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 89899 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 89899 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 89899 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 89899 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 89900 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 89900 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 89900 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 89900 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 130482 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 130482 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 89905 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 89905 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 89905 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 89905 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 112895 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 112895 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 86381 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 86381 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 216989 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 216989 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 113672 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 113672 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 74406 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 74406 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 89901 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 89901 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 89901 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 89901 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 159030 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 159030 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 8239 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 8239 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 8239 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 73883 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 73883 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 208735 10 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 208735 10 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 191547 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 191547 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 191547 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 191547 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 8967 91 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 8967 91 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 8967 91 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 74622 60 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 74622 60 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 74391 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 74391 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 214204 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 214204 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 131168 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 131168 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 103175 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 103175 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 213708 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 213708 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 119129 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 119129 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 8140 19 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 8140 19 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 8140 19 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 73947 53 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 73947 53 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 104613 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 104613 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 119120 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 119120 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 73933 14 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 73933 14 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 112894 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 112894 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 209068 10 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 209068 10 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 8211 2 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 8211 2 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 8211 2 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 89882 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 89882 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 74284 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 74284 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 89915 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 89915 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 213979 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 213979 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 89904 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 89904 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 89904 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 89904 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 214212 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 214212 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 213515 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 213515 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 103322 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 103322 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 89906 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 89906 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 89906 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 89906 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 130820 56 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 130820 56 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 120376 57 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 120376 57 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 176016 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 176016 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 89890 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 89890 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 170182 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 170182 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 113896 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 113896 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 208187 36 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 208187 36 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 131144 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 131144 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 84857 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 84857 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 89916 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 89916 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 74034 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 74034 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 89914 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 89914 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 213976 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 213976 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 113673 3 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 113673 3 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 74400 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 74400 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 86381 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 86381 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 7518 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 7518 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 7518 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 130595 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 130595 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 130595 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 190866 10 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 190866 10 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 103175 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 103175 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 84857 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 84857 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 116043 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 116043 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 116044 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 116044 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 86584 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 86584 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 190865 38 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 190865 38 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 9693 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 9693 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 9134 18 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 9134 18 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 9134 18 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 9134 18 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 9701 3 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 9701 3 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 9701 3 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 7983 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 7983 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 7135 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 7135 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 7135 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 7985 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 7985 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 10493 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 10493 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 10493 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 10493 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 9490 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 9490 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 9490 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 6873 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 6873 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 7147 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 7147 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 7147 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 7767 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 7767 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 10782 4 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 10782 4 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 10782 4 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 10782 4 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 10782 4 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 10782 4 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 8687 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 8687 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 10786 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 10786 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 10786 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 8403 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 8403 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 8403 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 8211 2 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 8211 2 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 8211 2 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 7177 49 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 7177 49 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 7177 49 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 8404 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 8404 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 10786 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 10786 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 10786 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 7177 49 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 7177 49 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 7177 49 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 95834 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 95834 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 95834 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 95834 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 95834 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 95834 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 94301 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 94301 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 94301 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 94301 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 127859 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 127859 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 127859 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 127859 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 80296 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 80296 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 80296 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 80296 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 95843 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 95843 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 95843 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 95843 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 95843 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 95843 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 94299 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 94299 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 94299 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 94299 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 95844 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 95844 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 95844 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 95844 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 95844 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 95844 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 52505 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 52505 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 52505 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 52505 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 94300 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 94300 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 94300 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 94300 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 130476 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 130476 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 80871 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 80871 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 21647 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 21647 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 21647 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 80872 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 80872 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 21469 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 21469 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 21469 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 21471 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 21471 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 21471 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 21646 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 21646 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 21646 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 9701 3 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 9701 3 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 9701 3 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 80160 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 80160 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 130474 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 130474 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 132581 17 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 132581 17 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 132581 17 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 132581 17 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 21470 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 21470 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 21470 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 130475 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 130475 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 21467 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 21467 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 21467 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 21593 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 21593 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 21593 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 10929 22 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 10929 22 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 10929 22 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 10929 22 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 81013 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 81013 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 21654 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 21654 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 21654 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 82178 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 82178 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 190868 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 190868 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 175978 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 175978 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 9683 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 9683 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 9683 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 190869 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 190869 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 148038 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 148038 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 21587 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 21587 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 21587 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 175929 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 175929 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 146089 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 146089 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 82186 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 82186 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 21592 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 21592 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 21592 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 21468 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 21468 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 21468 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 118326 2 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 118326 2 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 80766 12 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 80766 12 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 80874 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 80874 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 103697 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 103697 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 129169 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 129169 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 208735 10 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 208735 10 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 212649 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 212649 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 74622 60 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 74622 60 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 129828 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 129828 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 175929 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 175929 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 146089 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 146089 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 148038 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 148038 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 8140 19 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 8140 19 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 8140 19 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 73947 53 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 73947 53 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 131168 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 131168 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 8239 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 8239 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 8239 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 73883 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 73883 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 74406 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 74406 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 8967 91 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 8967 91 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 8967 91 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 72031 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 72031 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 107297 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 107297 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 10786 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 10786 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 10786 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 21468 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 21468 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 21468 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 175978 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 175978 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 82186 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 82186 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 8211 2 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 8211 2 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 8211 2 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 129439 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 129439 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 73933 14 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 73933 14 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 208187 36 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 208187 36 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 71356 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 71356 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 74284 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 74284 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 21592 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 21592 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 21592 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 71767 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 71767 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 74391 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 74391 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 130820 56 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 130820 56 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 74034 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 74034 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 80766 12 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 80766 12 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 72346 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 72346 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 130441 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 130441 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 74131 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 74131 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 134323 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 134323 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 71944 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 71944 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 73426 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 73426 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 72359 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 72359 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 80874 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 80874 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 73972 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 73972 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 81013 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 81013 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 82178 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 82178 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 131144 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 131144 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 129318 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 129318 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 71540 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 71540 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 74189 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 74189 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 74400 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 74400 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 74808 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 74808 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 129726 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 129726 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 9683 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 9683 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 9683 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 74035 68 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 74035 68 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 74035 68 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 129438 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 129438 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 74260 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 74260 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 21587 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 21587 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 21587 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 21654 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 21654 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 21654 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 113673 3 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 113673 3 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 9134 18 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 9134 18 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 9134 18 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 9134 18 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 8403 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 8403 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 8403 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 8404 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 8404 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 223155 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 223156 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 8211 2 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 8211 2 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 8211 2 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 8211 2 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 8211 2 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 8211 2 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 10782 4 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 10782 4 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 10782 4 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 8967 91 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 8967 91 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 8967 91 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 8238 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 8238 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 8239 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 8239 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 8239 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