Ligand source activities (1 row/activity)





Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
AssayType

Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

3352 2371 28 None -2041 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
5280879 2371 28 None -2041 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
5863 2371 28 None -2041 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
CHEMBL509456 2371 28 None -2041 4 Human 6.5 pEC50 = 6.5 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
5280878 100273 27 None -2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@@H](SC[C@H](N)C(=O)NCC(=O)O)[C@@H](O)CCCC(=O)O 10.1021/acs.jmedchem.1c01078
CHEMBL288943 100273 27 None -2 2 Human 8.4 pEC50 = 8.4 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@@H](SC[C@H](N)C(=O)NCC(=O)O)[C@@H](O)CCCC(=O)O 10.1021/acs.jmedchem.1c01078
3354 2369 26 None -23 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
5280493 2369 26 None -23 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
CHEMBL451509 2369 26 None -23 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
DB08855 2369 26 None -23 4 Human 8.1 pEC50 = 8.1 Functional
Agonist activity at human CysLT2 receptorAgonist activity at human CysLT2 receptor
ChEMBL 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10.1021/acs.jmedchem.1c01078
11455387 117919 0 None 77 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 531 14 2 6 5.6 O=C(O)CCCN1CC(C(=O)O)Oc2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403187 117919 0 None 77 2 Human 9.5 pIC50 = 9.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 531 14 2 6 5.6 O=C(O)CCCN1CC(C(=O)O)Oc2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
11398820 117787 0 None 1 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 556 13 3 8 4.7 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401689 117787 0 None 1 2 Human 9.3 pIC50 = 9.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 556 13 3 8 4.7 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
11307317 115031 0 None 194 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 14 3 6 5.2 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342959 115031 0 None 194 2 Human 9.2 pIC50 = 9.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 14 3 6 5.2 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
11398475 115036 4 None 19 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1C[C@@H](C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342964 115036 4 None 19 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1C[C@@H](C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
122183753 122214 0 None -3 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597618 122214 0 None -3 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183751 122212 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 543 10 2 4 6.4 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597616 122212 0 None -1 2 Human 9.1 pIC50 = 9.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 543 10 2 4 6.4 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183687 122189 0 None 2 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 579 14 2 4 7.4 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)ccc(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597530 122189 0 None 2 2 Human 9.0 pIC50 = 9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 579 14 2 4 7.4 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)ccc(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
122183689 122191 0 None -1 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4cc(F)c(F)c(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597532 122191 0 None -1 2 Human 8.8 pIC50 = 8.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4cc(F)c(F)c(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
46830961 122225 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2ccc(F)c3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597628 122225 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2ccc(F)c3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
46830963 122229 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 641 14 2 4 7.7 Cc1c(CCCC(=O)O)c2c(F)ccc(C#Cc3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CCCC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597632 122229 0 None -3 3 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 641 14 2 4 7.7 Cc1c(CCCC(=O)O)c2c(F)ccc(C#Cc3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CCCC(=O)O 10.1021/acs.jmedchem.5b00741
122183683 122185 0 None -4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 543 14 2 4 7.2 Cc1c(F)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)cn(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597526 122185 0 None -4 2 Human 7.9 pIC50 = 7.9 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 543 14 2 4 7.2 Cc1c(F)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)cn(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183686 122188 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 555 15 2 5 7.0 COc1ccccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597529 122188 0 None 3 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 555 15 2 5 7.0 COc1ccccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183758 122220 0 None -19 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597623 122220 0 None -19 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
11353238 117917 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 541 14 2 7 5.2 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(CCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403185 117917 0 None 2 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 541 14 2 7 5.2 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(CCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
23124741 115032 0 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 520 12 3 7 3.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342960 115032 0 None 1 2 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 520 12 3 7 3.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
127043618 140525 0 None -2570 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 523 7 3 4 6.9 COc1cccc2c(/C=C/C(=O)Nc3cccc(/C=C/c4ccc5ccc(Cl)cc5n4)c3)c(C(=O)O)[nH]c12 10.1021/acsmedchemlett.5b00482
CHEMBL3810210 140525 0 None -2570 2 Human 4.8 pIC50 = 4.8 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 523 7 3 4 6.9 COc1cccc2c(/C=C/C(=O)Nc3cccc(/C=C/c4ccc5ccc(Cl)cc5n4)c3)c(C(=O)O)[nH]c12 10.1021/acsmedchemlett.5b00482
23124716 115033 0 None 18 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 534 13 3 7 4.3 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342961 115033 0 None 18 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 534 13 3 7 4.3 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
23124707 117786 0 None 5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 517 14 2 5 5.4 O=C(O)CCCN1CC(C(=O)O)Oc2c(CCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401688 117786 0 None 5 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 517 14 2 5 5.4 O=C(O)CCCN1CC(C(=O)O)Oc2c(CCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
11227280 117788 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 609 14 3 8 3.8 CS(=O)(=O)NC(=O)C1CN(CCCC(=O)O)c2cccc(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)c2O1 10.1016/j.bmc.2015.03.011
CHEMBL3401690 117788 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 609 14 3 8 3.8 CS(=O)(=O)NC(=O)C1CN(CCCC(=O)O)c2cccc(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)c2O1 10.1016/j.bmc.2015.03.011
11284237 115034 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 548 14 3 7 4.7 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342962 115034 0 None 1 2 Human 7.8 pIC50 = 7.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 548 14 3 7 4.7 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1021/ml500298y
118716777 115028 1 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 14 3 6 5.2 O=C(O)CCCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342956 115028 1 None -3 2 Human 6.8 pIC50 = 6.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 14 3 6 5.2 O=C(O)CCCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
23124672 115025 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 560 13 3 6 4.8 O=C(O)CCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342953 115025 0 None - 1 Human 5.8 pIC50 = 5.8 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 560 13 3 6 4.8 O=C(O)CCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
122183682 122184 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 565 14 2 4 7.1 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4c(F)ccc(F)c4F)cc3)cccc12 10.1021/acs.jmedchem.5b00741
CHEMBL3597525 122184 0 None -2 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 565 14 2 4 7.1 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4c(F)ccc(F)c4F)cc3)cccc12 10.1021/acs.jmedchem.5b00741
87131159 122192 0 None -1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597533 122192 0 None -1 2 Human 8.7 pIC50 = 8.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
11191817 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/acs.jmedchem.5b00741
CHEMBL3342955 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/acs.jmedchem.5b00741
11191817 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
11191817 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342955 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3342955 115027 2 None 3 2 Human 8.6 pIC50 = 8.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
122183756 122218 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597621 122218 0 None -1 2 Human 7.7 pIC50 = 7.7 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183681 122183 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 545 14 2 4 7.4 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4cccc(Cl)c4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
CHEMBL3597524 122183 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 545 14 2 4 7.4 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4cccc(Cl)c4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
127043236 140432 0 None -660 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 467 5 3 3 6.5 O=C(O)c1[nH]c2ccccc2c1C(=O)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3809164 140432 0 None -660 2 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 467 5 3 3 6.5 O=C(O)c1[nH]c2ccccc2c1C(=O)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
122183759 122222 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597625 122222 0 None -3 2 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 585 13 2 4 7.6 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
68695885 122182 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 511 14 2 4 6.7 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
CHEMBL3597523 122182 0 None -7 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 511 14 2 4 6.7 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
46830962 122231 21 None -14 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 601 14 2 4 7.6 Cc1c(F)cccc1CCCCOc1ccc(C#Cc2ccc(F)c3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597634 122231 21 None -14 3 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 601 14 2 4 7.6 Cc1c(F)cccc1CCCCOc1ccc(C#Cc2ccc(F)c3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
11853184 117922 3 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCn1cc(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403190 117922 3 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCn1cc(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
71654672 91882 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to controlAntagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to control
ChEMBL 510 19 2 5 7.0 CCCCCCCCCCCCOc1cccc(/C=C/C(=O)c2cc(C(=O)O)ccc2OCC(=O)O)c1 10.1016/j.ejmech.2013.01.041
CHEMBL2413379 91882 0 None - 1 Human 6.6 pIC50 = 6.6 Functional
Antagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to controlAntagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to control
ChEMBL 510 19 2 5 7.0 CCCCCCCCCCCCOc1cccc(/C=C/C(=O)c2cc(C(=O)O)ccc2OCC(=O)O)c1 10.1016/j.ejmech.2013.01.041
11853184 117922 3 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCn1cc(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1021/acs.jmedchem.5b00741
CHEMBL3403190 117922 3 None -2 2 Human 7.6 pIC50 = 7.6 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCn1cc(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1021/acs.jmedchem.5b00741
1836 2592 59 None -53703 18 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/acsmedchemlett.5b00482
3340 2592 59 None -53703 18 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/acsmedchemlett.5b00482
5281040 2592 59 None -53703 18 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/acsmedchemlett.5b00482
CHEMBL787 2592 59 None -53703 18 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/acsmedchemlett.5b00482
DB00471 2592 59 None -53703 18 Human 4.6 pIC50 = 4.6 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 10.1021/acsmedchemlett.5b00482
23124775 115029 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 560 15 3 6 5.6 O=C(O)CCCCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342957 115029 0 None -2 2 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 560 15 3 6 5.6 O=C(O)CCCCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
11261220 117918 0 None -5 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 539 13 2 7 5.6 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403186 117918 0 None -5 2 Human 8.5 pIC50 = 8.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 539 13 2 7 5.6 O=C(O)CCCN1CC(c2nnn[nH]2)Oc2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
46830677 122228 0 None -1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 623 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(C#Cc3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CCCC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597631 122228 0 None -1 3 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 623 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(C#Cc3ccc(OCCCCc4c(F)cc(F)c(F)c4F)cc3)c2n1CCCC(=O)O 10.1021/acs.jmedchem.5b00741
122183688 122190 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)c(F)cc(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597531 122190 0 None -1 2 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 597 14 2 4 7.6 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4c(F)c(F)cc(F)c4F)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
10438479 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acs.jmedchem.5b00741
6197 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3342944 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acs.jmedchem.5b00741
122183761 122224 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 613 15 2 4 8.4 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597627 122224 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 613 15 2 4 8.4 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
11249398 117784 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 519 14 2 6 5.2 O=C(O)CCCN1CC(C(=O)O)Oc2c(OCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401686 117784 0 None 1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 519 14 2 6 5.2 O=C(O)CCCN1CC(C(=O)O)Oc2c(OCc3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
3381 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10.1021/ml500298y
5311015 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10.1021/ml500298y
CHEMBL285954 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10.1021/ml500298y
122183762 122226 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cc(F)cc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597629 122226 0 None -1 2 Human 7.5 pIC50 = 7.5 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cc(F)cc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
118716774 115022 0 None -281 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 488 9 2 5 4.5 CC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342950 115022 0 None -281 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 488 9 2 5 4.5 CC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
127043053 140528 0 None -537 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 527 6 3 3 7.5 O=C(/C=C/c1c(C(=O)O)[nH]c2cccc(Cl)c12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3810290 140528 0 None -537 2 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 527 6 3 3 7.5 O=C(/C=C/c1c(C(=O)O)[nH]c2cccc(Cl)c12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
118729614 117920 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 541 14 2 6 6.0 O=C(O)CCCn1cc(C(=O)O)c(=O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403188 117920 0 None -1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 541 14 2 6 6.0 O=C(O)CCCn1cc(C(=O)O)c(=O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
118716776 114832 0 None -12 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 516 11 2 5 5.3 CCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3341770 114832 0 None -12 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 516 11 2 5 5.3 CCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
10438479 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acsmedchemlett.5b00482
6197 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acsmedchemlett.5b00482
CHEMBL3342944 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/acsmedchemlett.5b00482
10438479 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/ml500298y
6197 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/ml500298y
CHEMBL3342944 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 10.1021/ml500298y
122183684 122186 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 559 14 2 4 7.7 Cc1c(Cl)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)cn(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597527 122186 0 None -7 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 559 14 2 4 7.7 Cc1c(Cl)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)cn(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183685 122187 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 525 14 2 4 7.0 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4ccccc4)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
CHEMBL3597528 122187 0 None -1 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 525 14 2 4 7.0 Cc1c(CCCC(=O)O)c2cccc(/C=C/c3ccc(OCCCCc4ccccc4)cc3)c2n1CC(=O)O 10.1021/acs.jmedchem.5b00741
118729613 117916 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 518 13 3 6 4.8 O=C(O)CCCN1CC(CO)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3403184 117916 0 None 1 2 Human 6.4 pIC50 = 6.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 518 13 3 6 4.8 O=C(O)CCCN1CC(CO)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
118728613 117790 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 488 12 2 5 5.4 O=C(O)CCCN1CCOc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401692 117790 0 None -2 2 Human 5.4 pIC50 = 5.4 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 488 12 2 5 5.4 O=C(O)CCCN1CCOc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
2237 3162 79 None -3630 10 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acsmedchemlett.5b00482
3634 3162 79 None -3630 10 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acsmedchemlett.5b00482
4887 3162 79 None -3630 10 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acsmedchemlett.5b00482
CHEMBL21333 3162 79 None -3630 10 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acsmedchemlett.5b00482
DB01411 3162 79 None -3630 10 Human 4.4 pIC50 = 4.4 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acsmedchemlett.5b00482
90871050 115019 0 None -85 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 446 9 3 5 4.6 O=C(Nc1cccc2c1OC(C(=O)O)CN2)c1ccc(OCCCCc2ccccc2)cc1 10.1021/ml500298y
CHEMBL3342947 115019 0 None -85 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 446 9 3 5 4.6 O=C(Nc1cccc2c1OC(C(=O)O)CN2)c1ccc(OCCCCc2ccccc2)cc1 10.1021/ml500298y
127043248 140390 0 None -1819 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 523 7 3 4 6.9 COc1ccc2[nH]c(C(=O)O)c(/C=C/C(=O)Nc3cccc(/C=C/c4ccc5ccc(Cl)cc5n4)c3)c2c1 10.1021/acsmedchemlett.5b00482
CHEMBL3808613 140390 0 None -1819 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 523 7 3 4 6.9 COc1ccc2[nH]c(C(=O)O)c(/C=C/C(=O)Nc3cccc(/C=C/c4ccc5ccc(Cl)cc5n4)c3)c2c1 10.1021/acsmedchemlett.5b00482
127043244 140435 0 None -5888 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 511 6 3 3 7.0 O=C(/C=C/c1c(C(=O)O)[nH]c2ccc(F)cc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3809189 140435 0 None -5888 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 511 6 3 3 7.0 O=C(/C=C/c1c(C(=O)O)[nH]c2ccc(F)cc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
122183763 122227 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2c(F)ccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597630 122227 0 None -4 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 617 14 2 4 8.1 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2c(F)ccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
66739117 122194 0 None -9 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 573 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597535 122194 0 None -9 2 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 573 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
46834997 122221 0 None -3 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 599 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597624 122221 0 None -3 3 Human 8.3 pIC50 = 8.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 599 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
122183752 122213 0 None -17 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 11 2 4 6.8 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597617 122213 0 None -17 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 11 2 4 6.8 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
23124680 117785 0 None 12 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 515 13 2 5 5.8 O=C(O)CCCN1CC(C(=O)O)Oc2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401687 117785 0 None 12 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 515 13 2 5 5.8 O=C(O)CCCN1CC(C(=O)O)Oc2c(/C=C/c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
23124664 117789 0 None 12 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 671 15 3 8 5.3 O=C(O)CCCN1CC(C(=O)NS(=O)(=O)c2ccccc2)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
CHEMBL3401691 117789 0 None 12 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 671 15 3 8 5.3 O=C(O)CCCN1CC(C(=O)NS(=O)(=O)c2ccccc2)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1016/j.bmc.2015.03.011
127043237 140420 0 None -870 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 495 7 3 3 6.8 O=C(CCc1c(C(=O)O)[nH]c2ccccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3808985 140420 0 None -870 2 Human 4.3 pIC50 = 4.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 495 7 3 3 6.8 O=C(CCc1c(C(=O)O)[nH]c2ccccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
118716775 115023 0 None -34 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 502 10 2 5 4.9 CCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342951 115023 0 None -34 2 Human 5.3 pIC50 = 5.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 502 10 2 5 4.9 CCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
53394034 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/acsmedchemlett.5b00482
6196 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/acsmedchemlett.5b00482
CHEMBL3342945 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/acsmedchemlett.5b00482
53394034 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/ml500298y
6196 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/ml500298y
CHEMBL3342945 588 22 None 21 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 10.1021/ml500298y
122183757 122219 0 None -10 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597622 122219 0 None -10 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
11387037 115035 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1C[C@H](C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342963 115035 0 None -1 2 Human 7.3 pIC50 = 7.3 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 532 13 3 6 4.9 O=C(O)CCCN1C[C@H](C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
2855 4132 104 None -776 12 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acsmedchemlett.5b00482
3322 4132 104 None -776 12 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acsmedchemlett.5b00482
5717 4132 104 None -776 12 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acsmedchemlett.5b00482
CHEMBL603 4132 104 None -776 12 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acsmedchemlett.5b00482
DB00549 4132 104 None -776 12 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acsmedchemlett.5b00482
127043050 140439 0 None -6456 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 493 6 3 3 6.9 O=C(/C=C/c1c(C(=O)O)[nH]c2ccccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3809230 140439 0 None -6456 2 Human 4.2 pIC50 = 4.2 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 493 6 3 3 6.9 O=C(/C=C/c1c(C(=O)O)[nH]c2ccccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
11713438 122181 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
CHEMBL3597522 122181 0 None -3 2 Human 8.2 pIC50 = 8.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 527 15 2 5 6.5 O=C(O)CCCc1cn(CC(=O)O)c2c(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)cccc12 10.1021/acs.jmedchem.5b00741
122183760 122223 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 599 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597626 122223 0 None -2 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 599 14 2 4 8.0 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
23124623 115030 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 518 12 3 6 4.5 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342958 115030 0 None 19 2 Human 7.2 pIC50 = 7.2 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 518 12 3 6 4.5 O=C(O)CCCN1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
122183690 122193 0 None -6 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 14 2 4 7.5 Cc1c(F)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597534 122193 0 None -6 2 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 14 2 4 7.5 Cc1c(F)cccc1CCCCOc1ccc(/C=C/c2cccc3c(CCCC(=O)O)c(C)n(CC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
118729615 117921 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 542 15 2 7 6.0 O=C(O)CCCOc1nc2cccc(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)c2nc1C(=O)O 10.1016/j.bmc.2015.03.011
CHEMBL3403189 117921 0 None 6 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 542 15 2 7 6.0 O=C(O)CCCOc1nc2cccc(/C=C/c3ccc(OCCCCOc4ccccc4)cc3)c2nc1C(=O)O 10.1016/j.bmc.2015.03.011
71654671 91881 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to controlAntagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to control
ChEMBL 524 14 2 6 5.6 O=C(O)COc1ccc(C(=O)O)cc1C(=O)/C=C/c1ccc(OCCCCOc2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2013.01.041
CHEMBL2413378 91881 0 None - 1 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to controlAntagonist activity at human recombinant CysLT2 receptor expressed in human HEK293 cells assessed as reduction in LTD4-induced cytosolic free Ca2+ level after 30 mins by fluorescence assay relative to control
ChEMBL 524 14 2 6 5.6 O=C(O)COc1ccc(C(=O)O)cc1C(=O)/C=C/c1ccc(OCCCCOc2ccc(Cl)cc2)cc1 10.1016/j.ejmech.2013.01.041
127043247 140417 0 None -1995 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 529 6 3 3 7.2 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(F)cc(F)c12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3808968 140417 0 None -1995 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 529 6 3 3 7.2 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(F)cc(F)c12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
54677430 115018 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 510 8 2 7 5.1 CCN(CC)C(=O)/C=C(\C)c1ccc2oc(C(=O)c3ccc(C#N)cc3)c(NC(=O)/C(C#N)=C(/C)O)c2c1 10.1021/ml500298y
CHEMBL3342946 115018 0 None 1 2 Human 5.1 pIC50 = 5.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 510 8 2 7 5.1 CCN(CC)C(=O)/C=C(\C)c1ccc2oc(C(=O)c3ccc(C#N)cc3)c(NC(=O)/C(C#N)=C(/C)O)c2c1 10.1021/ml500298y
122183755 122217 0 None -7 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597620 122217 0 None -7 2 Human 7.1 pIC50 = 7.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 571 12 2 4 7.2 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
46835000 122230 0 None -7 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 583 14 2 4 7.5 Cc1c(F)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597633 122230 0 None -7 3 Human 8.1 pIC50 = 8.1 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 583 14 2 4 7.5 Cc1c(F)cccc1CCCCOc1ccc(C#Cc2cccc3c(CCCC(=O)O)c(C)n(CCCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
127043242 140450 0 None -3981 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 527 6 3 3 7.5 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(Cl)ccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
CHEMBL3809333 140450 0 None -3981 2 Human 4.1 pIC50 = 4.1 Functional
Antagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assayAntagonist activity against CysLT2 receptor (unknown origin) expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization pre-incubated for 10 mins before LTD4 addition by Fluo-4 AM dye based fluorimetric assay
ChEMBL 527 6 3 3 7.5 O=C(/C=C/c1c(C(=O)O)[nH]c2cc(Cl)ccc12)Nc1cccc(/C=C/c2ccc3ccc(Cl)cc3n2)c1 10.1021/acsmedchemlett.5b00482
23124563 115024 0 None -630 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 12 3 6 4.4 O=C(O)CCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342952 115024 0 None -630 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 546 12 3 6 4.4 O=C(O)CCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
23124629 115026 0 None -74 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 574 14 3 6 5.2 O=C(O)CCCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
CHEMBL3342954 115026 0 None -74 2 Human 6.1 pIC50 = 6.1 Functional
Antagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assayAntagonist activity at human CysLT2 receptor expressed in HEK293 cells assessed as inhibition of LTD4-inudced intracellular calcium influx preincubated for 30 mins before LTD4 addition by Fura2-AM assay
ChEMBL 574 14 3 6 5.2 O=C(O)CCCCC(=O)N1CC(C(=O)O)Oc2c(NC(=O)c3ccc(OCCCCc4ccccc4)cc3)cccc21 10.1021/ml500298y
122183754 122215 0 None -7 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 11 2 4 6.8 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
CHEMBL3597619 122215 0 None -7 2 Human 7.0 pIC50 = 7.0 Functional
Antagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assayAntagonist activity at human CysLT2 expressed in HEK293 cells assessed as inhibition of LTD4-induced calcium mobilization preincubated for 30 mins prior to LTD4 addition measured after 1 hr by Fura 2-AM dye-based fluorescence assay
ChEMBL 557 11 2 4 6.8 Cc1c(Cl)cccc1CCCCOc1ccc(C#Cc2cccc3c(CC(=O)O)c(C)n(CCC(=O)O)c23)cc1 10.1021/acs.jmedchem.5b00741
5861 2065 0 None - 1 Human 6.8 pA2 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 710 16 3 8 8.9 CCCc1c(OCCCC/C=C\C=C\[C@@H]([C@@H](c2cccc(c2)C(F)(F)F)O)Sc2ccc3c(c2)oc(cc3=O)C(=O)O)ccc(c1O)C(=O)C 25839425
6913104 2065 0 None - 1 Human 6.8 pA2 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 710 16 3 8 8.9 CCCc1c(OCCCC/C=C\C=C\[C@@H]([C@@H](c2cccc(c2)C(F)(F)F)O)Sc2ccc3c(c2)oc(cc3=O)C(=O)O)ccc(c1O)C(=O)C 25839425
CHEMBL1206833 2065 0 None - 1 Human 6.8 pA2 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 710 16 3 8 8.9 CCCc1c(OCCCC/C=C\C=C\[C@@H]([C@@H](c2cccc(c2)C(F)(F)F)O)Sc2ccc3c(c2)oc(cc3=O)C(=O)O)ccc(c1O)C(=O)C 25839425
2855 4132 104 None -776 12 Human 6.9 pA2 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 25839425
3322 4132 104 None -776 12 Human 6.9 pA2 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 25839425
5717 4132 104 None -776 12 Human 6.9 pA2 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 25839425
CHEMBL603 4132 104 None -776 12 Human 6.9 pA2 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 25839425
DB00549 4132 104 None -776 12 Human 6.9 pA2 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 25839425
3334 3147 9 None -48 2 Human 6.2 pA2 = 6.2 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC
Guide to Pharmacology 458 16 3 4 5.5 OC(=O)CCS[C@H](c1ccccc1CCCCCCCCc1ccccc1)[C@H](C(=O)O)O 25839425
60842 3147 9 None -48 2 Human 6.2 pA2 = 6.2 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC
Guide to Pharmacology 458 16 3 4 5.5 OC(=O)CCS[C@H](c1ccccc1CCCCCCCCc1ccccc1)[C@H](C(=O)O)O 25839425
CHEMBL22776 3147 9 None -48 2 Human 6.2 pA2 = 6.2 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in HUVEC
Guide to Pharmacology 458 16 3 4 5.5 OC(=O)CCS[C@H](c1ccccc1CCCCCCCCc1ccccc1)[C@H](C(=O)O)O 25839425
2237 3162 79 None -3630 10 Human 7.1 pA2 = 7.1 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVEC
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 25839425
3634 3162 79 None -3630 10 Human 7.1 pA2 = 7.1 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVEC
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 25839425
4887 3162 79 None -3630 10 Human 7.1 pA2 = 7.1 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVEC
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 25839425
CHEMBL21333 3162 79 None -3630 10 Human 7.1 pA2 = 7.1 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVEC
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 25839425
DB01411 3162 79 None -3630 10 Human 7.1 pA2 = 7.1 Functional
against LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVECagainst LTC<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HUVEC
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 25839425
53394034 588 22 None 21 2 Human 8.4 pA2 = 8.4 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVECagainst LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVEC
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
6196 588 22 None 21 2 Human 8.4 pA2 = 8.4 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVECagainst LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVEC
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
CHEMBL3342945 588 22 None 21 2 Human 8.4 pA2 = 8.4 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVECagainst LTC<sub>4</sub> and LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assays in HUVEC
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
3381 589 27 None 3 3 Rat 7.3 pA2 = 7.3 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparationagainst LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparation
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 7698171
5311015 589 27 None 3 3 Rat 7.3 pA2 = 7.3 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparationagainst LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparation
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 7698171
CHEMBL285954 589 27 None 3 3 Rat 7.3 pA2 = 7.3 Functional
against LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparationagainst LTC<sub>4</sub> and LTD<sub>4</sub> induced contraction in smooth muscle preparation
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 7698171
53394034 588 22 None 21 2 Human 8.3 pA2 = 8.3 Functional
against LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cellsagainst LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cells
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
6196 588 22 None 21 2 Human 8.3 pA2 = 8.3 Functional
against LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cellsagainst LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cells
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
CHEMBL3342945 588 22 None 21 2 Human 8.3 pA2 = 8.3 Functional
against LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cellsagainst LTD<sub>4</sub> Ca<sup>2+</sup> mobilisation assay in COS-7 cells
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21753081
3352 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
3352 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 21078884
5280879 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
5280879 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 21078884
5863 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
5863 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 21078884
CHEMBL509456 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
CHEMBL509456 2371 28 None -2041 4 Human 5.8 pEC50 = 5.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 21078884
3352 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
3352 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
5280879 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
5280879 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
5863 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
5863 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
CHEMBL509456 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
CHEMBL509456 2371 28 None -2041 4 Human 6.8 pEC50 = 6.8 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
3353 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
3353 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
3412 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
3412 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
6435286 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
6435286 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
CHEMBL1521056 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
CHEMBL1521056 2370 0 None -41 4 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
6194 2834 0 None 61 2 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 639 26 7 8 3.0 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)NC(=O)CCC(C(=O)O)NC 21078884
73755185 2834 0 None 61 2 Human 6.9 pEC50 = 6.9 Functional
UnclassifiedUnclassified
Guide to Pharmacology 639 26 7 8 3.0 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)NC(=O)CCC(C(=O)O)NC 21078884
3381 589 27 None -3 3 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
5311015 589 27 None -3 3 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
CHEMBL285954 589 27 None -3 3 Human 7.0 pEC50 = 7.0 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
3354 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
3354 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
5280493 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
5280493 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
CHEMBL451509 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
CHEMBL451509 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
DB08855 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
DB08855 2369 26 None -23 4 Human 7.1 pEC50 = 7.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
3381 589 27 None -3 3 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
5311015 589 27 None -3 3 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
CHEMBL285954 589 27 None -3 3 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
3354 2369 26 None -23 4 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21753081
5280493 2369 26 None -23 4 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21753081
CHEMBL451509 2369 26 None -23 4 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21753081
DB08855 2369 26 None -23 4 Human 7.2 pEC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21753081
3354 2369 26 None -23 4 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
5280493 2369 26 None -23 4 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
CHEMBL451509 2369 26 None -23 4 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
DB08855 2369 26 None -23 4 Human 7.3 pEC50 = 7.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 21078884
3353 2370 0 None -41 4 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
3412 2370 0 None -41 4 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
6435286 2370 0 None -41 4 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
CHEMBL1521056 2370 0 None -41 4 Human 7.4 pEC50 = 7.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
3353 2370 0 None -41 4 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
3412 2370 0 None -41 4 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
6435286 2370 0 None -41 4 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
CHEMBL1521056 2370 0 None -41 4 Human 7.5 pEC50 = 7.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21078884
6194 2834 0 None 61 2 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 639 26 7 8 3.0 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)NC(=O)CCC(C(=O)O)NC 21078884
73755185 2834 0 None 61 2 Human 8.1 pEC50 = 8.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 639 26 7 8 3.0 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)NC(=O)CCC(C(=O)O)NC 21078884
3353 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
3353 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
3353 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
3412 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
3412 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
3412 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
6435286 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
6435286 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
6435286 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
CHEMBL1521056 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
CHEMBL1521056 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
CHEMBL1521056 2370 0 None -41 4 Human 8.3 pEC50 = 8.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 21753081
3354 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10913337
3354 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
5280493 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10913337
5280493 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
CHEMBL451509 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10913337
CHEMBL451509 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
DB08855 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10913337
DB08855 2369 26 None -23 4 Human 8.4 pEC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
2855 4132 104 None -776 12 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
3322 4132 104 None -776 12 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
5717 4132 104 None -776 12 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
CHEMBL603 4132 104 None -776 12 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
DB00549 4132 104 None -776 12 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
2237 3162 79 None -3630 10 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
3634 3162 79 None -3630 10 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
4887 3162 79 None -3630 10 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
CHEMBL21333 3162 79 None -3630 10 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
DB01411 3162 79 None -3630 10 Human 8.3 pIC50 = 8.3 Functional
NoneNone
Drug Central 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 None
60490 207261 106 None 8 2 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 236 2 2 3 2.7 CC(c1cc2ccccc2s1)N(O)C(N)=O None
CHEMBL93 207261 106 None 8 2 Human 8.2 pIC50 = 8.2 Functional
NoneNone
Drug Central 236 2 2 3 2.7 CC(c1cc2ccccc2s1)N(O)C(N)=O None
10580 2931 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by antagonists.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by antagonists.
Guide to Pharmacology 584 13 3 6 5.7 OC(=O)CCCN1C[C@H](Oc2c1cccc2NC(=O)c1ccc(cc1)OCCCCc1cc(F)ccc1Cl)C(=O)O 31811124
145704683 2931 0 None - 1 Human 7.9 pIC50 = 7.9 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by antagonists.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by antagonists.
Guide to Pharmacology 584 13 3 6 5.7 OC(=O)CCCN1C[C@H](Oc2c1cccc2NC(=O)c1ccc(cc1)OCCCCc1cc(F)ccc1Cl)C(=O)O 31811124
10581 983 0 None -1819 2 Human 5.7 pIC50 = 5.7 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.
Guide to Pharmacology 587 17 2 7 5.4 O=C(CN1CC(Oc2c1cccc2CC(=O)c1ccc(cc1)OCCCCCc1ccccc1)C(=O)O)CCCC(=O)O 31811124
145996520 983 0 None -1819 2 Human 5.7 pIC50 = 5.7 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.
Guide to Pharmacology 587 17 2 7 5.4 O=C(CN1CC(Oc2c1cccc2CC(=O)c1ccc(cc1)OCCCCCc1ccccc1)C(=O)O)CCCC(=O)O 31811124
10582 991 0 None 194 2 Human 9.2 pIC50 = 9.2 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.
Guide to Pharmacology 573 17 2 6 6.2 OC(=O)CCCCN1CC(Oc2c1cccc2CC(=O)c1ccc(cc1)OCCCCCCc1ccccc1)C(=O)O 31811124
145996521 991 0 None 194 2 Human 9.2 pIC50 = 9.2 Functional
Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.Determined by measuring inhibition of LTD<sub>4</sub>-induced IP<sub>1</sub> production by the antagonist.
Guide to Pharmacology 573 17 2 6 6.2 OC(=O)CCCCN1CC(Oc2c1cccc2CC(=O)c1ccc(cc1)OCCCCCCc1ccccc1)C(=O)O 31811124
2855 4132 104 None -776 12 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10851239
3322 4132 104 None -776 12 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10851239
5717 4132 104 None -776 12 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10851239
CHEMBL603 4132 104 None -776 12 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10851239
DB00549 4132 104 None -776 12 Human 5.1 pIC50 = 5.1 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10851239
2855 4132 104 None -776 12 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 20423349
3322 4132 104 None -776 12 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 20423349
5717 4132 104 None -776 12 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 20423349
CHEMBL603 4132 104 None -776 12 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 20423349
DB00549 4132 104 None -776 12 Human 5.2 pIC50 = 5.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 20423349
3381 589 27 None -3 3 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 21903747
5311015 589 27 None -3 3 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 21903747
CHEMBL285954 589 27 None -3 3 Human 5.3 pIC50 = 5.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 21903747
3352 2371 28 None -2041 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
5280879 2371 28 None -2041 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
5863 2371 28 None -2041 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
CHEMBL509456 2371 28 None -2041 4 Human 5.7 pIC50 = 5.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10913337
3352 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
3352 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
5280879 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
5280879 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
5863 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
5863 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
CHEMBL509456 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 10851239
CHEMBL509456 2371 28 None -2041 4 Human 6.2 pIC50 = 6.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 11093801
3381 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10851239
3381 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
3381 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
5311015 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10851239
5311015 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
5311015 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
CHEMBL285954 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 10851239
CHEMBL285954 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
CHEMBL285954 589 27 None -3 3 Human 6.3 pIC50 = 6.3 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
3381 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
5311015 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
CHEMBL285954 589 27 None -3 3 Human 6.5 pIC50 = 6.5 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 11093801
3353 2370 0 None -41 4 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
3412 2370 0 None -41 4 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
6435286 2370 0 None -41 4 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
CHEMBL1521056 2370 0 None -41 4 Human 7.2 pIC50 = 7.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10913337
3381 589 27 None -3 3 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
5311015 589 27 None -3 3 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
CHEMBL285954 589 27 None -3 3 Human 7.7 pIC50 = 7.7 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 20423349
3353 2370 0 None -41 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
3412 2370 0 None -41 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
6435286 2370 0 None -41 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
CHEMBL1521056 2370 0 None -41 4 Human 8.2 pIC50 = 8.2 Functional
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 11093801
10438479 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
6197 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
CHEMBL3342944 1912 23 None - 1 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
3354 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
3354 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
5280493 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
5280493 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
CHEMBL451509 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
CHEMBL451509 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
DB08855 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 10851239
DB08855 2369 26 None -23 4 Human 8.4 pIC50 = 8.4 Functional
UnclassifiedUnclassified
Guide to Pharmacology 625 25 7 8 2.8 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)NCC(=O)O)NC(=O)CC[C@@H](C(=O)O)N 11093801
53394034 588 22 None 21 2 Human 6.9 pIC50 = 6.9 Functional
against 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblastsagainst 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblasts
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21903747
6196 588 22 None 21 2 Human 6.9 pIC50 = 6.9 Functional
against 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblastsagainst 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblasts
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21903747
CHEMBL3342945 588 22 None 21 2 Human 6.9 pIC50 = 6.9 Functional
against 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblastsagainst 30-300nM LTD<sub>4</sub> arrestin assay in C2C12 myofibroblasts
Guide to Pharmacology 589 16 3 6 6.0 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOc1ccccc1)C(=O)O 21903747
10438479 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in CHO cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in CHO cells
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
6197 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in CHO cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in CHO cells
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
CHEMBL3342944 1912 23 None - 1 Human 7.4 pIC50 = 7.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in CHO cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in CHO cells
Guide to Pharmacology 595 16 3 6 6.3 OC(=O)C1CCCC(C1)NC(=O)c1cc(ccc1OCCCc1ccc(cc1)OCCCCOC1CCCCC1)C(=O)O 20423349
2237 3162 79 None -3630 10 Human 5.4 pIC50 = 5.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10851239
3634 3162 79 None -3630 10 Human 5.4 pIC50 = 5.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10851239
4887 3162 79 None -3630 10 Human 5.4 pIC50 = 5.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10851239
CHEMBL21333 3162 79 None -3630 10 Human 5.4 pIC50 = 5.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10851239
DB01411 3162 79 None -3630 10 Human 5.4 pIC50 = 5.4 Functional
against [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cellsagainst [<sup>3</sup>H]LTD<sub>4</sub> in COS-7 cells
Guide to Pharmacology 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10851239
3381 589 27 None -3 3 Human 6.6 pKB = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 1331415
5311015 589 27 None -3 3 Human 6.6 pKB = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 1331415
CHEMBL285954 589 27 None -3 3 Human 6.6 pKB = 6.6 Functional
UnclassifiedUnclassified
Guide to Pharmacology 472 17 3 4 6.7 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)Sc1ccc(cc1)C(=O)O 1331415




Ligands (move mouse cursor over ligand name to see structure) Receptor Assay information Chemical information
Sel. page Similar-
ity
Common
name
GPCRdb
ID
#Vendors

Reference
ligand
Fold
selectivity
# Tested
GPCRs
Species

p-value
(-log)
Activity
Type
Activity
Relation
Activity
Value
Assay
Type
Assay
Description
Source

Mol
weight
Rot
Bonds
H don

H acc

LogP

Smiles

DOI

2237 3162 79 None - 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acs.jmedchem.5b00741
3634 3162 79 None - 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acs.jmedchem.5b00741
4887 3162 79 None - 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acs.jmedchem.5b00741
CHEMBL21333 3162 79 None - 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acs.jmedchem.5b00741
DB01411 3162 79 None - 3 Human 5.4 pIC50 = 5.4 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 481 9 2 7 4.6 O=C(c1ccc(cc1)OCCCCc1ccccc1)Nc1cccc2c1oc(cc2=O)c1[nH]nnn1 10.1021/acs.jmedchem.5b00741
54746913 175511 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CysLT2 (unknown origin)Inhibition of CysLT2 (unknown origin)
ChEMBL 412 5 3 6 1.5 O=C(O)CNC(=O)c1c(O)c2c(n(Cc3ccc(C(F)(F)F)cc3)c1=O)COC2 10.1021/acsmedchemlett.8b00274
CHEMBL4577928 175511 0 None - 0 Human 5.4 pIC50 = 5.4 Binding
Inhibition of CysLT2 (unknown origin)Inhibition of CysLT2 (unknown origin)
ChEMBL 412 5 3 6 1.5 O=C(O)CNC(=O)c1c(O)c2c(n(Cc3ccc(C(F)(F)F)cc3)c1=O)COC2 10.1021/acsmedchemlett.8b00274
2855 4132 104 None -776 6 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acs.jmedchem.5b00741
3322 4132 104 None -776 6 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acs.jmedchem.5b00741
5717 4132 104 None -776 6 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acs.jmedchem.5b00741
CHEMBL603 4132 104 None -776 6 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acs.jmedchem.5b00741
DB00549 4132 104 None -776 6 Human 5.1 pIC50 = 5.1 Binding
Antagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assayAntagonist activity at human CysLT2 expressed in HEK293T cells assessed as inhibition of LTC4-induced effect preincubated for 30 mins prior to LTC4 addition by Aequorin luminescence assay
ChEMBL 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C 10.1021/acs.jmedchem.5b00741
115219 1978 14 None -251188 3 Human 5.2 pKd = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 548 8 2 8 4.7 COc1cc(ccc1Cn1ncc2c1cc(cc2)NC(=O)OC1CCCC1)C(=O)NS(=O)(=O)c1ccccc1 1329767
3358 1978 14 None -251188 3 Human 5.2 pKd = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 548 8 2 8 4.7 COc1cc(ccc1Cn1ncc2c1cc(cc2)NC(=O)OC1CCCC1)C(=O)NS(=O)(=O)c1ccccc1 1329767
3414 1978 14 None -251188 3 Human 5.2 pKd = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 548 8 2 8 4.7 COc1cc(ccc1Cn1ncc2c1cc(cc2)NC(=O)OC1CCCC1)C(=O)NS(=O)(=O)c1ccccc1 1329767
CHEMBL22033 1978 14 None -251188 3 Human 5.2 pKd = 5.2 Binding
UnclassifiedUnclassified
Guide to Pharmacology 548 8 2 8 4.7 COc1cc(ccc1Cn1ncc2c1cc(cc2)NC(=O)OC1CCCC1)C(=O)NS(=O)(=O)c1ccccc1 1329767
3353 2370 0 None -21 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
3412 2370 0 None -21 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
6435286 2370 0 None -21 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
CHEMBL1521056 2370 0 None -21 2 Human 8.4 pKd = 8.4 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 10851239
2855 4132 104 3H-LTD4 -776 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
3322 4132 104 3H-LTD4 -776 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
5717 4132 104 3H-LTD4 -776 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
CHEMBL603 4132 104 3H-LTD4 -776 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
DB00549 4132 104 3H-LTD4 -776 6 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 575 8 2 7 5.7 COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C None
None 216221 0 3H-LTD4 -95 2 Human 6.0 pKi = 6 Binding
NoneNone
PDSP KiDatabase 514 11 1 5 6.5 CN(C)C(=O)CCSC(C1=CC=CC(=C1)C=CC2=NC3=C(C=CC(=C3)Cl)C=C2)SCCC(=O)O None
57340263 216220 0 3H-LTD4 1 2 Human 6.5 pKi = 6.5 Binding
NoneNone
PDSP KiDatabase 472 17 3 4 6.7 CCCCC/C=C\C/C=C/C=C/C=C/[C@H]([C@H](CCCC(=O)O)O)SC1=CC=C(C=C1)C(=O)O None
None 216208 0 3H-LTD4 -2187 4 Human 5.3 pKi = 5.3 Binding
NoneNone
PDSP KiDatabase 473 7 2 3 7.9 CC(C)(C1=CC=CC=C1CCC(C2=CC=CC(=C2)C=CC3=NC4=C(C=CC(=C4)Cl)C=C3)S)O None
3352 2371 28 None -125 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 9547367
5280879 2371 28 None -125 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 9547367
5863 2371 28 None -125 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 9547367
CHEMBL509456 2371 28 None -125 3 Human 6.5 pKi = 6.5 Binding
UnclassifiedUnclassified
Guide to Pharmacology 439 18 4 5 4.3 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SC[C@@H](C(=O)O)N 9547367
3353 2370 0 None -21 2 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 9547367
3412 2370 0 None -21 2 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 9547367
6435286 2370 0 None -21 2 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 9547367
CHEMBL1521056 2370 0 None -21 2 Human 7.7 pKi = 7.7 Binding
UnclassifiedUnclassified
Guide to Pharmacology 496 20 5 6 3.4 CCCCC/C=C\C/C=C\C=C\C=C\[C@H]([C@H](CCCC(=O)O)O)SCC(C(=O)NCC(=O)O)N 9547367
1836 2592 59 None -2 15 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
3340 2592 59 None -2 15 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
5281040 2592 59 None -2 15 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
CHEMBL787 2592 59 None -2 15 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None
DB00471 2592 59 None -2 15 Human 8.3 pKi None 8.3 Binding
NoneNone
Drug Central 585 12 2 4 8.9 OC(=O)CC1(CS[C@@H](c2cccc(c2)/C=C/c2ccc3c(n2)cc(cc3)Cl)CCc2ccccc2C(O)(C)C)CC1 None