Ligand source activities (1 row/activity)
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 3352 | 2371 | None | 24 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2041 | 4 | 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 | None | 24 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2041 | 4 | 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 | None | 24 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2041 | 4 | 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 | None | 24 | Human | Functional | pEC50 | = | 6.5 | 6.5 | -2041 | 4 | 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 | 100327 | None | 24 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -2 | 2 | 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 | 100327 | None | 24 | Human | Functional | pEC50 | = | 8.4 | 8.4 | -2 | 2 | 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 | None | 23 | Human | Functional | pEC50 | = | 8.1 | 8.1 | -23 | 4 | 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 | None | 23 | Human | Functional | pEC50 | = | 8.1 | 8.1 | -23 | 4 | 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 | None | 23 | Human | Functional | pEC50 | = | 8.1 | 8.1 | -23 | 4 | 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 | None | 23 | Human | Functional | pEC50 | = | 8.1 | 8.1 | -23 | 4 | 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 | 117983 | None | 0 | Human | Functional | pIC50 | = | 9.5 | 9.5 | 77 | 2 | 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 | 117983 | None | 0 | Human | Functional | pIC50 | = | 9.5 | 9.5 | 77 | 2 | 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 | 117851 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | 1 | 2 | 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 | 117851 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | 1 | 2 | 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 | 115095 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | 194 | 2 | 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 | 115095 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | 194 | 2 | 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 | 115100 | None | 4 | Human | Functional | pIC50 | = | 9.1 | 9.1 | 19 | 2 | 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 | 115100 | None | 4 | Human | Functional | pIC50 | = | 9.1 | 9.1 | 19 | 2 | 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 | 122280 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | -3 | 2 | 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 | 122280 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | -3 | 2 | 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 | 122278 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | -1 | 2 | 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 | 122278 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | -1 | 2 | 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 | 122255 | None | 0 | Human | Functional | pIC50 | = | 9 | 9.0 | 2 | 2 | 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 | 122255 | None | 0 | Human | Functional | pIC50 | = | 9 | 9.0 | 2 | 2 | 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 | 122257 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | -1 | 2 | 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 | 122257 | None | 0 | Human | Functional | pIC50 | = | 8.8 | 8.8 | -1 | 2 | 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 | 122291 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 3 | 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 | 122291 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 3 | 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 | 122295 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 3 | 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 | 122295 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -3 | 3 | 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 | 122251 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -4 | 2 | 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 | 122251 | None | 0 | Human | Functional | pIC50 | = | 7.9 | 7.9 | -4 | 2 | 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 | 122254 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 3 | 2 | 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 | 122254 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 3 | 2 | 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 | 122286 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | -19 | 2 | 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 | 122286 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | -19 | 2 | 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 | 117981 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 2 | 2 | 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 | 117981 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 2 | 2 | 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 | 115096 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 1 | 2 | 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 | 115096 | None | 0 | Human | Functional | pIC50 | = | 5.8 | 5.8 | 1 | 2 | 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 | 140612 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -2570 | 2 | 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 | 140612 | None | 0 | Human | Functional | pIC50 | = | 4.8 | 4.8 | -2570 | 2 | 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 | 115097 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 18 | 2 | 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 | 115097 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 18 | 2 | 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 | 117850 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 5 | 2 | 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 | 117850 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 5 | 2 | 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 | 117852 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | 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 | 117852 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | 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 | 115098 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | 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 | 115098 | None | 0 | Human | Functional | pIC50 | = | 7.8 | 7.8 | 1 | 2 | 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 | ||
Showing 1 to 50 of 405 entries
| Ligands (move mouse cursor over ligand name to see structure) | Receptor | Activity | Chemical information | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
Ligands (move mouse cursor over ligand name to see structure)
| Receptor
| Activity
| Chemical information
| |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Sel. page | Common name
| GPCRdb ID
| Reference ligand
| Vendors | Species
| Assay Type
| Activity Type
| Activity Relation
| Activity Value | p-value (-log) | Fold selectivity | Tested GPCRs | Assay Description
| Source
| Mol weight | Rot Bonds | H don | H acc | LogP | Smiles
| DOI
| |
| 2237 | 3162 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | ||
| 4887.0 | 3162 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | None | 53 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 3 | 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 | 175615 | None | 0 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 0 | 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 | 175615 | None | 0 | Human | Binding | pIC50 | = | 5.4 | 5.4 | - | 0 | 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 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | ||
| 5717.0 | 4132 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | None | 63 | Human | Binding | pIC50 | = | 5.1 | 5.1 | -776 | 6 | 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 | None | 12 | Human | Binding | pKd | = | 5.2 | 5.2 | -251188 | 3 | 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 | None | 12 | Human | Binding | pKd | = | 5.2 | 5.2 | -251188 | 3 | 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 | None | 12 | Human | Binding | pKd | = | 5.2 | 5.2 | -251188 | 3 | 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 | None | 12 | Human | Binding | pKd | = | 5.2 | 5.2 | -251188 | 3 | 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 | None | 0 | Human | Binding | pKd | = | 8.4 | 8.4 | -21 | 2 | 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 | None | 0 | Human | Binding | pKd | = | 8.4 | 8.4 | -21 | 2 | 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 | None | 0 | Human | Binding | pKd | = | 8.4 | 8.4 | -21 | 2 | 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 | None | 0 | Human | Binding | pKd | = | 8.4 | 8.4 | -21 | 2 | 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 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | 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 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | 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 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | NoneNone |
PDSP KiDatabase | 575 | 8 | 2 | 7 | 5.7 | COc1cc(ccc1Cc1cn(c2c1cc(cc2)NC(=O)OC1CCCC1)C)C(=O)NS(=O)(=O)c1ccccc1C | None | ||
| 5717.0 | 4132 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | 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 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | 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 | 3H-LTD4 | 63 | Human | Binding | pKi | = | 6 | 6.0 | -776 | 6 | 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 | 218708 | 3H-LTD4 | 0 | Human | Binding | pKi | = | 6 | 6.0 | -95 | 2 | 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 | 218707 | 3H-LTD4 | 0 | Human | Binding | pKi | = | 6.5 | 6.5 | 1 | 2 | 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 | 218695 | 3H-LTD4 | 0 | Human | Binding | pKi | = | 5.3 | 5.3 | -2187 | 4 | 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 | None | 24 | Human | Binding | pKi | = | 6.5 | 6.5 | -125 | 3 | 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 | None | 24 | Human | Binding | pKi | = | 6.5 | 6.5 | -125 | 3 | 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 | None | 24 | Human | Binding | pKi | = | 6.5 | 6.5 | -125 | 3 | 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 | None | 24 | Human | Binding | pKi | = | 6.5 | 6.5 | -125 | 3 | 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 | None | 0 | Human | Binding | pKi | = | 7.7 | 7.7 | -21 | 2 | 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 | None | 0 | Human | Binding | pKi | = | 7.7 | 7.7 | -21 | 2 | 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 | None | 0 | Human | Binding | pKi | = | 7.7 | 7.7 | -21 | 2 | 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 | None | 0 | Human | Binding | pKi | = | 7.7 | 7.7 | -21 | 2 | 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 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | ||
| 5281040.0 | 2592 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | None | 44 | Human | Binding | pKi | None | 8.3 | 8.3 | -2 | 15 | 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 | ||
Showing 1 to 45 of 45 entries