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
| |
| 44627488 | 14178 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | 2187 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 418 | 6 | 6 | 9 | -1.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1198696 | 14178 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | 2187 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 418 | 6 | 6 | 9 | -1.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL611791 | 14178 | None | 0 | Human | Functional | pEC50 | = | 9.0 | 9.0 | 2187 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 418 | 6 | 6 | 9 | -1.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | 10.1021/jm901432g | ||
| 16082712 | 89 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 85 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 420 | 6 | 6 | 10 | -1.2 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S | 10.1021/jm901432g | ||
| 6202 | 89 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 85 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 420 | 6 | 6 | 10 | -1.2 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S | 10.1021/jm901432g | ||
| CHEMBL216011 | 89 | None | 0 | Human | Functional | pEC50 | = | 8.7 | 8.7 | 85 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 420 | 6 | 6 | 10 | -1.2 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=S | 10.1021/jm901432g | ||
| 1748 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| 44585949 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| CHEMBL507060 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| 44627599 | 14179 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 472 | 9 | 5 | 11 | -0.2 | C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O | 10.1021/jm901432g | ||
| CHEMBL1198697 | 14179 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 472 | 9 | 5 | 11 | -0.2 | C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O | 10.1021/jm901432g | ||
| CHEMBL611792 | 14179 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 472 | 9 | 5 | 11 | -0.2 | C#CCCOP(=O)(O)OP(=O)(O)OC[C@H]1O[C@@H](n2ccc(=O)[nH]c2=S)[C@H](O)[C@@H]1O | 10.1021/jm901432g | ||
| 16220889 | 137039 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 582 | 9 | 9 | 16 | -3.4 | O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O | 10.1021/jm901432g | ||
| CHEMBL374384 | 137039 | None | 0 | Human | Functional | pEC50 | = | 8.0 | 8.0 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 582 | 9 | 9 | 16 | -3.4 | O=c1[nH]c(=S)ccn1[C@@H]1O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]2O[C@H](CO)[C@@H](O)[C@H](O)[C@H]2O)[C@@H](O)[C@H]1O | 10.1021/jm901432g | ||
| 1748 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| 44585949 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| CHEMBL507060 | 2658 | None | 1 | Human | Functional | pEC50 | = | 8.0 | 8.0 | 51 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| 46890713 | 14218 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 528 | 6 | 6 | 9 | -1.9 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm100287t | ||
| CHEMBL1085561 | 14218 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 528 | 6 | 6 | 9 | -1.9 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm100287t | ||
| CHEMBL1198914 | 14218 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 528 | 6 | 6 | 9 | -1.9 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm100287t | ||
| CHEMBL4851033 | 14218 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 528 | 6 | 6 | 9 | -1.9 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)CP(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm100287t | ||
| 45485237 | 199462 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 564 | 6 | 6 | 9 | -1.3 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm901432g | ||
| CHEMBL566925 | 199462 | None | 0 | Human | Functional | pEC50 | = | 6.9 | 6.9 | -1 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 564 | 6 | 6 | 9 | -1.3 | O=c1[nH]c(=O)n([C@@H]2O[C@H](COP(=O)(O)C(F)(F)P(=O)(O)O)[C@@H](O)[C@H]2O)cc1I | 10.1021/jm901432g | ||
| 44627802 | 14189 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 525 | 9 | 5 | 13 | -0.6 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1198725 | 14189 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 525 | 9 | 5 | 13 | -0.6 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL612119 | 14189 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 1 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 525 | 9 | 5 | 13 | -0.6 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3ccc([N+](=O)[O-])cc3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| 146015339 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| 1749 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| 6031 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| CHEMBL130266 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| DB03435 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm901432g | ||
| 146015339 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| 1749 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| 6031 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| CHEMBL130266 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| DB03435 | 3922 | None | 21 | Human | Functional | pEC50 | = | 6.8 | 6.8 | 1 | 7 | Agonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assayAgonist activity at human recombinant P2Y14 receptor expressed in HEK293 cells assessed as [3H]inositol phosphate production by scintillation proximity assay |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/jm100287t | ||
| 44627690 | 14286 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1162560 | 14286 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1199753 | 14286 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OCC(O)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| 44627692 | 14188 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1198717 | 14188 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL612065 | 14188 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 478 | 10 | 7 | 13 | -3.2 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)OC(CO)CO)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| 44627804 | 14357 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 4 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 514 | 8 | 5 | 11 | 0.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1162561 | 14357 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 4 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 514 | 8 | 5 | 11 | 0.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| CHEMBL1200114 | 14357 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | 4 | 2 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 514 | 8 | 5 | 11 | 0.1 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)Oc3cccc(Cl)c3)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm901432g | ||
| 16221095 | 143934 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis |
ChEMBL | 566 | 8 | 10 | 16 | -5.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@@H]3[C@@H](O)[C@H](O)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm061222w | ||
| CHEMBL390160 | 143934 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysisAgonist activity at human P2Y14 expressed in COS7 cells assessed as stimulation of PLC-mediated [3H]inositol hydrolysis |
ChEMBL | 566 | 8 | 10 | 16 | -5.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@@H]3[C@@H](O)[C@H](O)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1021/jm061222w | ||
| 46226448 | 202166 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells |
ChEMBL | 566 | 8 | 10 | 16 | -5.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1016/j.bmc.2009.05.024 | ||
| CHEMBL593346 | 202166 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human P2Y14 receptor expressed in human COS7 cellsAgonist activity at human P2Y14 receptor expressed in human COS7 cells |
ChEMBL | 566 | 8 | 10 | 16 | -5.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3[C@H](O)[C@@H](O)[C@H](O)[C@@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=O)[nH]1 | 10.1016/j.bmc.2009.05.024 | ||
| 44627806 | 14287 | None | 0 | Human | Functional | pEC50 | = | 5.7 | 5.7 | - | 1 | Agonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP productionAgonist activity at human P2Y14 receptor expressed in HEK293 cells coexpressing phospholipase C-activating Gi protein cells assessed as inhibition of forskolin induced [3H]cAMP production |
ChEMBL | 510 | 9 | 5 | 12 | -0.5 | COc1ccc(OP(=O)(O)OP(=O)(O)OC[C@H]2O[C@@H](n3ccc(=O)[nH]c3=O)[C@H](O)[C@@H]2O)cc1 | 10.1021/jm901432g | ||
Showing 1 to 50 of 561 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
| |
| 44422870 | 85611 | None | 4 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase CbetaAgonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta |
ChEMBL | 582 | 9 | 9 | 16 | -3.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | 10.1016/j.bmc.2015.03.042 | ||
| CHEMBL228111 | 85611 | None | 4 | Human | Binding | pEC50 | = | 5.0 | 5.0 | - | 0 | Agonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase CbetaAgonist activity at recombinant human P2Y14 receptor expressed in African green monkey COS7 cells co-transfected with Galphaqi assessed as stimulation of phospholipase Cbeta |
ChEMBL | 582 | 9 | 9 | 16 | -3.4 | O=c1ccn([C@@H]2O[C@H](COP(=O)(O)OP(=O)(O)O[C@H]3O[C@H](CO)[C@@H](O)[C@H](O)[C@H]3O)[C@@H](O)[C@H]2O)c(=S)[nH]1 | 10.1016/j.bmc.2015.03.042 | ||
| 146015339 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 1749 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 6031 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| CHEMBL130266 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| DB03435 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat C6 cellsAgonist activity at human P2Y14 expressed in rat C6 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 146015339 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 1749 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 6031 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| CHEMBL130266 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| DB03435 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.5 | 7.5 | - | 0 | Agonist activity at human P2Y14 expressed in rat CHO cellsAgonist activity at human P2Y14 expressed in rat CHO cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 146015339 | 3922 | None | 21 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14 |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 1749 | 3922 | None | 21 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14 |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 6031 | 3922 | None | 21 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14 |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| CHEMBL130266 | 3922 | None | 21 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14 |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| DB03435 | 3922 | None | 21 | Rat | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Antagonist activity at rat P2Y14Antagonist activity at rat P2Y14 |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 146015339 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 1749 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 6031 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| CHEMBL130266 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| DB03435 | 3922 | None | 21 | Human | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Agonist activity at human P2Y14 expressed in HEK293 cellsAgonist activity at human P2Y14 expressed in HEK293 cells |
ChEMBL | 404 | 6 | 6 | 10 | -2.6 | O[C@@H]1[C@@H](COP(=O)(OP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1021/acs.jmedchem.5b01972 | ||
| 42611190 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14 |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL5210307 | ||
| 5802 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14 |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL5210307 | ||
| CHEMBL1800685 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14Affinity Biochemical interaction (FLIPR assay) EUB0000274bCl P2RY14 |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL5210307 | ||
| 42611190 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | FLIPR assayFLIPR assay |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL4507292 | ||
| 5802 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | FLIPR assayFLIPR assay |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL4507292 | ||
| CHEMBL1800685 | 3156 | None | 14 | Human | Binding | pIC50 | = | 9.3 | 9.3 | -3 | 22 | FLIPR assayFLIPR assay |
ChEMBL | 475 | 4 | 2 | 2 | 7.4 | OC(=O)c1cc2cc(ccc2c(c1)c1ccc(cc1)C1CCNCC1)c1ccc(cc1)C(F)(F)F | 10.6019/CHEMBL4507292 | ||
| CHEMBL5083619 | 217364 | None | 0 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | N[C@@H]1C[C@H](CO)[C@@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 | 10.1021/acs.jmedchem.1c01964 | ||||
| CHEMBL5093569 | 217922 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | N[C@@H]1C[C@H](CO)C[C@H]1c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 | 10.1021/acs.jmedchem.1c01964 | ||||
| CHEMBL5081782 | 217257 | None | 0 | Human | Binding | pIC50 | = | 7 | 7.0 | - | 0 | Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | O=C(O)c1cc(-c2ccc([C@H]3C[C@H]4C[C@@H]3C(=O)N4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 | 10.1021/acs.jmedchem.1c01964 | ||||
| CHEMBL5079515 | 217109 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | N[C@H]1C[C@@H](C(=O)O)[C@H](c2ccc(-c3cc(C(=O)O)cc4cc(-c5ccc(C(F)(F)F)cc5)ccc34)cc2)C1 | 10.1021/acs.jmedchem.1c01964 | ||||
| CHEMBL5093465 | 217919 | None | 0 | Mouse | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | CC(=O)N1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 | 10.1021/acs.jmedchem.1c01964 | ||||
| CHEMBL5090079 | 217731 | None | 0 | Mouse | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to mouse P2Y14R expressed in HEK293 cells preincubated for 30 mins followed by addition of 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate incubated for 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | CS(=O)(=O)C1C[C@H]2C[C@@H]1C[C@@H]2c1ccc(-c2cc(C(=O)O)cc3cc(-c4ccc(C(F)(F)F)cc4)ccc23)cc1 | 10.1021/acs.jmedchem.1c01964 | ||||
| 156019395 | 178114 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay |
ChEMBL | 518 | 5 | 1 | 5 | 6.1 | O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 | 10.1021/acs.jmedchem.0c00745 | ||
| CHEMBL4646514 | 178114 | None | 0 | Human | Binding | pIC50 | = | 7.0 | 7.0 | - | 0 | Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay |
ChEMBL | 518 | 5 | 1 | 5 | 6.1 | O=C(O)c1cc(-c2ccc(C34CCN(CC3)CC4)cc2)cc(-n2cc(-c3ccc(C(F)(F)F)cc3)nn2)c1 | 10.1021/acs.jmedchem.0c00745 | ||
| 145978515 | 163783 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method |
ChEMBL | 499 | 8 | 3 | 7 | 4.0 | NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 | 10.1021/acs.jmedchem.8b00168 | ||
| CHEMBL4204811 | 163783 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Displacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric methodDisplacement of MRS4174 from human P2Y14R expressed in CHO cells preincubated for 30 mins followed by MRS4174 addition measured after 30 mins by flow cytometric method |
ChEMBL | 499 | 8 | 3 | 7 | 4.0 | NCCCNC(=O)c1ccc(-c2cc(C(=O)O)cc(-n3cc(-c4ccc(C(F)(F)F)cc4)nn3)c2)o1 | 10.1021/acs.jmedchem.8b00168 | ||
| 1748 | 2658 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1016/j.bmcl.2021.128137 | ||
| 44585949 | 2658 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1016/j.bmcl.2021.128137 | ||
| CHEMBL507060 | 2658 | None | 1 | Human | Binding | pIC50 | = | 8.0 | 8.0 | - | 0 | Binding affinity to human P2Y14 expressed in CHO cellsBinding affinity to human P2Y14 expressed in CHO cells |
ChEMBL | 402 | 6 | 6 | 9 | -2.5 | O[C@@H]1[C@@H](COP(=O)(CP(=O)(O)O)O)O[C@H]([C@@H]1O)n1ccc(=O)[nH]c1=O | 10.1016/j.bmcl.2021.128137 | ||
| 171466241 | 196813 | None | 0 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from mouse P2Y14R stably expressed in human HEK293 cells by flow cytometryDisplacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from mouse P2Y14R stably expressed in human HEK293 cells by flow cytometry |
ChEMBL | 503 | 4 | 2 | 2 | 8.1 | O=C(O)c1cc(-c2ccc(C3CCCNCCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 | 10.1021/acs.jmedchem.3c00664 | ||
| CHEMBL5432717 | 196813 | None | 0 | Mouse | Binding | pIC50 | = | 7.9 | 7.9 | - | 1 | Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from mouse P2Y14R stably expressed in human HEK293 cells by flow cytometryDisplacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from mouse P2Y14R stably expressed in human HEK293 cells by flow cytometry |
ChEMBL | 503 | 4 | 2 | 2 | 8.1 | O=C(O)c1cc(-c2ccc(C3CCCNCCC3)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 | 10.1021/acs.jmedchem.3c00664 | ||
| 156012972 | 177619 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay |
ChEMBL | 481 | 5 | 3 | 5 | 5.1 | O=C(O)c1[nH]c(-c2ccc(C3CCNCC3)cc2)cc1-c1cn(-c2ccc(C(F)(F)F)cc2)nn1 | 10.1021/acs.jmedchem.0c00745 | ||
| CHEMBL4639693 | 177619 | None | 0 | Human | Binding | pIC50 | = | 5.0 | 5.0 | - | 0 | Inhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assayInhibition of MRS4174 binding to human P2Y14R expressed in CHO cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins at pH 7.4 by flow cytomtery based competitive fluorescence assay |
ChEMBL | 481 | 5 | 3 | 5 | 5.1 | O=C(O)c1[nH]c(-c2ccc(C3CCNCC3)cc2)cc1-c1cn(-c2ccc(C(F)(F)F)cc2)nn1 | 10.1021/acs.jmedchem.0c00745 | ||
| CHEMBL5074788 | 216821 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Inhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysisInhibition of fluorescent antagonist binding to human P2Y14R expressed in CHO cells preincubated for 30 mins followed by 6-amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy 6-(4-(trifluoromethyl)phenyl)naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate addition and measured after 30 mins by BD FACSCalibur flow cytometry analysis |
ChEMBL | None | None | None | O=C(O)c1cc(-c2ccc([C@]3(O)C[C@H]4CC[C@@H]3CN4)cc2)c2ccc(-c3ccc(C(F)(F)F)cc3)cc2c1 | 10.1021/acs.jmedchem.1c01964 | ||||
| 135357071 | 171738 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis |
ChEMBL | 502 | 5 | 2 | 5 | 5.5 | O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)cc3)nn2)c1 | 10.1021/acs.jmedchem.6b00044 | ||
| CHEMBL4465763 | 171738 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | - | 0 | Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysisDisplacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)-butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from human P2Y14R expressed in CHO cells measured after 15 mins by flow cytometric analysis |
ChEMBL | 502 | 5 | 2 | 5 | 5.5 | O=C(O)c1cc(-c2ccc(C3CCNCC3)cc2)cc(-n2cc(-c3ccc(Br)cc3)nn2)c1 | 10.1021/acs.jmedchem.6b00044 | ||
| 126720252 | 164770 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | -2 | 13 | Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells by flow cytometryDisplacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells by flow cytometry |
ChEMBL | 697 | 15 | 2 | 6 | 9.2 | NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 | 10.1021/acs.jmedchem.3c00664 | ||
| CHEMBL4216870 | 164770 | None | 0 | Human | Binding | pIC50 | = | 6.9 | 6.9 | -2 | 13 | Displacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells by flow cytometryDisplacement of fluorescent tracer 4-(4-(1-(4-(1-(6-(3-carboxylato-4-(3-iminio-3H-xanthen-9-yl)benzamido)hexyl)-4,5-dihydro-1H-pyrrol-3-yl)butyl)piperidin-1-ium-4-yl)phenyl)-7-(4-(trifluoromethyl)phenyl)-2-naphthoate from human P2Y14R stably expressed in CHO cells by flow cytometry |
ChEMBL | 697 | 15 | 2 | 6 | 9.2 | NCCCCCCn1cc(CCCCN2CCC(c3ccc(-c4cc(C(=O)O)cc5cc(-c6ccc(C(F)(F)F)cc6)ccc45)cc3)CC2)nn1 | 10.1021/acs.jmedchem.3c00664 | ||
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