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
| |
| 10367574 | 13950 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.5 | 9.5 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 472 | 2 | 0 | 6 | 6.2 | Cc1cn2c(n1)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=Nc1cc(Cl)c(Cl)cc1-2 | 10.1021/jm00018a012 | ||
| CHEMBL119660 | 13950 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.5 | 9.5 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 472 | 2 | 0 | 6 | 6.2 | Cc1cn2c(n1)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=Nc1cc(Cl)c(Cl)cc1-2 | 10.1021/jm00018a012 | ||
| 172470461 | 197124 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 4 | 2 | 6 | 5.5 | Cc1nnc2n1-c1sc3c(c1[C@@H](c1ccccc1Cl)NC2)C[C@@H](C(=O)NCc1ccc(C(F)(F)F)cc1)C3 | 10.1021/acsmedchemlett.3c00194 | ||
| CHEMBL5439289 | 197124 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 4 | 2 | 6 | 5.5 | Cc1nnc2n1-c1sc3c(c1[C@@H](c1ccccc1Cl)NC2)C[C@@H](C(=O)NCc1ccc(C(F)(F)F)cc1)C3 | 10.1021/acsmedchemlett.3c00194 | ||
| 168814214 | 195676 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 553 | 3 | 1 | 6 | 5.5 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N[C@H]1CCc2ccccc2C1)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5408810 | 195676 | None | 0 | Human | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 553 | 3 | 1 | 6 | 5.5 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N[C@H]1CCc2ccccc2C1)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| 10028664 | 163829 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 493 | 3 | 0 | 7 | 5.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(C4CCCCC4)nn4c3N(CCCC4)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL420527 | 163829 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.4 | 9.4 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 493 | 3 | 0 | 7 | 5.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(C4CCCCC4)nn4c3N(CCCC4)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| 164607720 | 196875 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 493 | 4 | 2 | 6 | 4.6 | CCC12CC(NC(=O)[C@@H]3Cc4sc5c(c4C3)[C@H](c3ccccc3Cl)NCc3nnc(C)n3-5)(C1)C2 | 10.1021/acsmedchemlett.3c00194 | ||
| CHEMBL5433867 | 196875 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 493 | 4 | 2 | 6 | 4.6 | CCC12CC(NC(=O)[C@@H]3Cc4sc5c(c4C3)[C@H](c3ccccc3Cl)NCc3nnc(C)n3-5)(C1)C2 | 10.1021/acsmedchemlett.3c00194 | ||
| 168814178 | 195848 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N[C@H]1CCc2cccc(F)c21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5411872 | 195848 | None | 0 | Human | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N[C@H]1CCc2cccc(F)c21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| 10479006 | 13598 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 451 | 2 | 1 | 5 | 6.5 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3cc(Cl)c(Cl)cc3N=C(S)C2)cc1 | 10.1021/jm00018a011 | ||
| CHEMBL119412 | 13598 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 451 | 2 | 1 | 5 | 6.5 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3cc(Cl)c(Cl)cc3N=C(S)C2)cc1 | 10.1021/jm00018a011 | ||
| 10071745 | 110526 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 436 | 2 | 1 | 4 | 5.7 | Cc1nc2cnccc2n1-c1ccc(C2CC(=O)Nc3cc(Cl)c(Cl)cc3C2)cc1 | 10.1021/jm00018a011 | ||
| CHEMBL324709 | 110526 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 436 | 2 | 1 | 4 | 5.7 | Cc1nc2cnccc2n1-c1ccc(C2CC(=O)Nc3cc(Cl)c(Cl)cc3C2)cc1 | 10.1021/jm00018a011 | ||
| 10478956 | 115041 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 450 | 2 | 0 | 4 | 5.7 | Cc1nc2cnccc2n1-c1ccc(C2CC(=O)N(C)c3cc(Cl)c(Cl)cc3C2)cc1 | 10.1021/jm00018a011 | ||
| CHEMBL334275 | 115041 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 450 | 2 | 0 | 4 | 5.7 | Cc1nc2cnccc2n1-c1ccc(C2CC(=O)N(C)c3cc(Cl)c(Cl)cc3C2)cc1 | 10.1021/jm00018a011 | ||
| 10322057 | 13533 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 461 | 3 | 0 | 7 | 4.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccccc4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL119371 | 13533 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 461 | 3 | 0 | 7 | 4.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccccc4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL106908 | 5356 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.3 | 9.3 | - | 1 | In vitro inhibition of PAF-induced aggregation of rabbit washed platelets.In vitro inhibition of PAF-induced aggregation of rabbit washed platelets. |
ChEMBL | 586 | 9 | 1 | 9 | 6.3 | CCOC(=O)C1=C(c2ccc(-n3c(C)nc4cnccc43)cc2)N=C(C)/C(=C(/O)OCCOC)C1c1ccccc1Cl | 10.1021/jm00095a005 | ||
| 168814135 | 196363 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)NC1CCc2cc(F)ccc21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5422270 | 196363 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)NC1CCc2cc(F)ccc21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| 168814152 | 197154 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)NC1CCc2ccc(F)cc21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5439944 | 197154 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 557 | 3 | 1 | 6 | 5.8 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)NC1CCc2ccc(F)cc21)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| 10024618 | 168393 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 411 | 2 | 1 | 5 | 5.8 | Cc1cc2c(cc1C)N=C(c1ccc(-n3c(C)nc4cnccc43)cc1)CC(S)=N2 | 10.1021/jm00018a011 | ||
| CHEMBL434028 | 168393 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 411 | 2 | 1 | 5 | 5.8 | Cc1cc2c(cc1C)N=C(c1ccc(-n3c(C)nc4cnccc43)cc1)CC(S)=N2 | 10.1021/jm00018a011 | ||
| 10458486 | 110418 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 495 | 3 | 0 | 7 | 5.3 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccc(Cl)cc4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL324121 | 110418 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 495 | 3 | 0 | 7 | 5.3 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccc(Cl)cc4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| 135507267 | 111431 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 447 | 3 | 1 | 7 | 4.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccccc4)nn(C)c3NC(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL327034 | 111431 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 447 | 3 | 1 | 7 | 4.6 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(-c4ccccc4)nn(C)c3NC(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| 163298963 | 196511 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 483 | 6 | 1 | 6 | 4.8 | CCCN(CCC)C(=O)[C@@H]1Cc2sc3c(c2C1)[C@H](c1ccccc1Cl)NCc1nnc(C)n1-3 | 10.1021/acsmedchemlett.3c00194 | ||
| CHEMBL5425646 | 196511 | None | 0 | Human | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 483 | 6 | 1 | 6 | 4.8 | CCCN(CCC)C(=O)[C@@H]1Cc2sc3c(c2C1)[C@H](c1ccccc1Cl)NCc1nnc(C)n1-3 | 10.1021/acsmedchemlett.3c00194 | ||
| 10453303 | 113381 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 395 | 2 | 1 | 5 | 4.8 | Cc1cc2c(cc1C)NC(=O)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=N2 | 10.1021/jm00018a011 | ||
| CHEMBL331566 | 113381 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 395 | 2 | 1 | 5 | 4.8 | Cc1cc2c(cc1C)NC(=O)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=N2 | 10.1021/jm00018a011 | ||
| 10027595 | 13947 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 467 | 3 | 0 | 7 | 5.0 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(C4CCCCC4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL119659 | 13947 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.2 | 9.2 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 467 | 3 | 0 | 7 | 5.0 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(C4CCCCC4)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| 11754521 | 13606 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 471 | 6 | 0 | 8 | 4.1 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(COCC(C)C)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| CHEMBL119417 | 13606 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 471 | 6 | 0 | 8 | 4.1 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3c(COCC(C)C)nn(C)c3N(C)C(=O)C2)cc1 | 10.1021/jm00018a012 | ||
| 168814146 | 195220 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 547 | 3 | 0 | 6 | 6.3 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N(C)C1CCC(C)(C)CC1)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5399089 | 195220 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 547 | 3 | 0 | 6 | 6.3 | Cc1nnc2n1-c1sc3c(c1C(c1ccccc1Cl)=NC21CC1)C[C@H](C(=O)N(C)C1CCC(C)(C)CC1)C3 | 10.1021/acsmedchemlett.3c00324 | ||
| 168814148 | 196773 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 507 | 6 | 0 | 6 | 5.5 | CCCN(CCC)C(=O)[C@@H]1Cc2sc3c(c2C1)C(c1ccccc1Cl)=NC1(CC1)c1nnc(C)n1-3 | 10.1021/acsmedchemlett.3c00324 | ||
| CHEMBL5431916 | 196773 | None | 0 | Human | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR overexpressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 507 | 6 | 0 | 6 | 5.5 | CCCN(CCC)C(=O)[C@@H]1Cc2sc3c(c2C1)C(c1ccccc1Cl)=NC1(CC1)c1nnc(C)n1-3 | 10.1021/acsmedchemlett.3c00324 | ||
| 10003131 | 10104 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 435 | 2 | 1 | 5 | 5.5 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3cc(Cl)c(Cl)cc3NC(=O)C2)cc1 | 10.1021/jm00018a011 | ||
| CHEMBL115529 | 10104 | None | 0 | Guinea pig | Functional | pIC50 | = | 9.1 | 9.1 | - | 1 | Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets.Antagonistic activity was tested against Platelet-Activating Factor-induced aggregation of rabbit washed platelets. |
ChEMBL | 435 | 2 | 1 | 5 | 5.5 | Cc1nc2cnccc2n1-c1ccc(C2=Nc3cc(Cl)c(Cl)cc3NC(=O)C2)cc1 | 10.1021/jm00018a011 | ||
| 10068655 | 168056 | None | 0 | Guinea pig | Functional | pIC50 | = | 9 | 9.0 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 385 | 2 | 1 | 7 | 3.2 | Cc1nn(C)c2c1NC(=O)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=N2 | 10.1021/jm00018a012 | ||
| CHEMBL431664 | 168056 | None | 0 | Guinea pig | Functional | pIC50 | = | 9 | 9.0 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 385 | 2 | 1 | 7 | 3.2 | Cc1nn(C)c2c1NC(=O)CC(c1ccc(-n3c(C)nc4cnccc43)cc1)=N2 | 10.1021/jm00018a012 | ||
| 172449689 | 195838 | None | 0 | Human | Functional | pIC50 | = | 9.0 | 9.0 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 489 | 4 | 2 | 6 | 4.5 | Cc1nnc2n1-c1sc3c(c1[C@H](c1ccccc1Cl)NC2)C[C@@H](C(=O)NCc1ccccc1)C3 | 10.1021/acsmedchemlett.3c00194 | ||
| CHEMBL5411707 | 195838 | None | 0 | Human | Functional | pIC50 | = | 9.0 | 9.0 | - | 1 | Antagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assayAntagonist activity at human PAFR expressed in HEK293 cells assessed as inhibition of PAF C-16 ligand induced receptor activation preincubated for 90 mins followed by PAF ligand addition and measured after 60 mins by HTRF IP1 assay |
ChEMBL | 489 | 4 | 2 | 6 | 4.5 | Cc1nnc2n1-c1sc3c(c1[C@H](c1ccccc1Cl)NC2)C[C@@H](C(=O)NCc1ccccc1)C3 | 10.1021/acsmedchemlett.3c00194 | ||
| 10367575 | 61859 | None | 0 | Guinea pig | Functional | pIC50 | = | 8.9 | 8.9 | - | 1 | In vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit plateletsIn vitro antagonist activity against platelet activating factor (PAF) receptor, using washed rabbit platelets |
ChEMBL | 472 | 2 | 0 | 6 | 6.2 | Cc1cnc2n1-c1cc(Cl)c(Cl)cc1N=C(c1ccc(-n3c(C)nc4cnccc43)cc1)C2 | 10.1021/jm00018a012 | ||
Showing 1 to 50 of 1,907 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
| |
| 460131 | 97359 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 631 | 13 | 1 | 10 | 3.9 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)NC(C)CC(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL269132 | 97359 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.8 | 6.8 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 631 | 13 | 1 | 10 | 3.9 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)NC(C)CC(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 6324617 | 189672 | None | 13 | Guinea pig | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 424 | 0 | 3 | 10 | -1.4 | C[C@@H]1C(=O)O[C@H]2[C@H](O)[C@@]34[C@H]5C[C@@H](C(C)(C)C)[C@]36[C@@H](OC(=O)[C@@H]6O)O[C@@]4(C(=O)O5)[C@@]12O | 10.1021/jm00060a006 | ||
| CHEMBL514432 | 189672 | None | 13 | Guinea pig | Binding | pEC50 | = | 6.8 | 6.8 | - | 1 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 424 | 0 | 3 | 10 | -1.4 | C[C@@H]1C(=O)O[C@H]2[C@H](O)[C@@]34[C@H]5C[C@@H](C(C)(C)C)[C@]36[C@@H](OC(=O)[C@@H]6O)O[C@@]4(C(=O)O5)[C@@]12O | 10.1021/jm00060a006 | ||
| 3075901 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| CHEMBL6270 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.7 | 6.7 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| 3075901 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| CHEMBL6270 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.6 | 6.6 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| 131088 | 97281 | None | 4 | Guinea pig | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 588 | 10 | 0 | 10 | 3.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)C(C)(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL268596 | 97281 | None | 4 | Guinea pig | Binding | pEC50 | = | 6.5 | 6.5 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 588 | 10 | 0 | 10 | 3.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)C(C)(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 3075903 | 205245 | None | 6 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 546 | 10 | 0 | 10 | 2.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(C)=O)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL6217 | 205245 | None | 6 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 546 | 10 | 0 | 10 | 2.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(C)=O)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 131088 | 97281 | None | 4 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 588 | 10 | 0 | 10 | 3.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)C(C)(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL268596 | 97281 | None | 4 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 588 | 10 | 0 | 10 | 3.3 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)C(C)(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 3075899 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL6203 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.4 | 6.4 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 3075899 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL6203 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 7.3 | 7.3 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 3075899 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL6203 | 205218 | None | 3 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 642 | 11 | 0 | 10 | 4.2 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)c3ccccc3Cl)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 457910 | 97358 | None | 0 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 631 | 14 | 0 | 10 | 4.0 | CCCN(CCC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| CHEMBL269131 | 97358 | None | 0 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 631 | 14 | 0 | 10 | 4.0 | CCCN(CCC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| 10077575 | 95719 | None | 0 | Guinea pig | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 617 | 12 | 1 | 10 | 3.5 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)NC(C)C(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| CHEMBL258053 | 95719 | None | 0 | Guinea pig | Binding | pEC50 | = | 7.2 | 7.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 617 | 12 | 1 | 10 | 3.5 | COc1cc(C(=O)N2CCN(C(=O)c3cc(OC)c(OC)c(OC)c3)C(COC(=O)NC(C)C(C)C)C2)cc(OC)c1OC | 10.1021/jm00060a006 | ||
| 3013157 | 97389 | None | 2 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 603 | 13 | 1 | 10 | 3.2 | CCCCNC(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| CHEMBL269340 | 97389 | None | 2 | Guinea pig | Binding | pEC50 | = | 6.2 | 6.2 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 603 | 13 | 1 | 10 | 3.2 | CCCCNC(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| 3075901 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| CHEMBL6270 | 205347 | None | 3 | Guinea pig | Binding | pEC50 | = | 7.1 | 7.1 | - | 0 | Inhibition of [3H]PAF binding to rabbit platelet membraneInhibition of [3H]PAF binding to rabbit platelet membrane |
ChEMBL | 602 | 13 | 0 | 10 | 3.7 | CCC(CC)C(=O)OCC1CN(C(=O)c2cc(OC)c(OC)c(OC)c2)CCN1C(=O)c1cc(OC)c(OC)c(OC)c1 | 10.1021/jm00060a006 | ||
| 9954410 | 50209 | None | 1 | Human | Binding | pIC50 | = | 10.8 | 10.8 | - | 0 | Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes.Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes. |
ChEMBL | 430 | 10 | 1 | 6 | 3.5 | CCOC[C@H](CC(C)C)NS(=O)(=O)c1ccc(Cn2c(C)nc3cnccc32)cc1 | 10.1016/S0960-894X(01)81205-1 | ||
| CHEMBL157078 | 50209 | None | 1 | Human | Binding | pIC50 | = | 10.8 | 10.8 | - | 0 | Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes.Antagonistic activity for inhibition of [3H]PAF receptor binding to washed human platelet membranes. |
ChEMBL | 430 | 10 | 1 | 6 | 3.5 | CCOC[C@H](CC(C)C)NS(=O)(=O)c1ccc(Cn2c(C)nc3cnccc32)cc1 | 10.1016/S0960-894X(01)81205-1 | ||
| 14851874 | 98767 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 497 | 2 | 0 | 6 | 5.0 | Cc1nnc2n1-c1sc(C#CCN3C(=O)CCc4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| CHEMBL277701 | 98767 | None | 0 | Human | Binding | pIC50 | = | 9.7 | 9.7 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 497 | 2 | 0 | 6 | 5.0 | Cc1nnc2n1-c1sc(C#CCN3C(=O)CCc4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| 108156 | 2993 | None | 38 | Human | Binding | pIC50 | = | 9.6 | 9.6 | 1096 | 6 | Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrsDisplacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs |
ChEMBL | 523 | 25 | 0 | 7 | 5.6 | CCCCCCCCCCCCCCCCOC[C@@H](OC(=O)C)COP(=O)(OCC[N+](C)(C)C)[O-] | 10.1016/j.bmcl.2013.01.025 | ||
| 1831 | 2993 | None | 38 | Human | Binding | pIC50 | = | 9.6 | 9.6 | 1096 | 6 | Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrsDisplacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs |
ChEMBL | 523 | 25 | 0 | 7 | 5.6 | CCCCCCCCCCCCCCCCOC[C@@H](OC(=O)C)COP(=O)(OCC[N+](C)(C)C)[O-] | 10.1016/j.bmcl.2013.01.025 | ||
| 1833 | 2993 | None | 38 | Human | Binding | pIC50 | = | 9.6 | 9.6 | 1096 | 6 | Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrsDisplacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs |
ChEMBL | 523 | 25 | 0 | 7 | 5.6 | CCCCCCCCCCCCCCCCOC[C@@H](OC(=O)C)COP(=O)(OCC[N+](C)(C)C)[O-] | 10.1016/j.bmcl.2013.01.025 | ||
| CHEMBL1235246 | 2993 | None | 38 | Human | Binding | pIC50 | = | 9.6 | 9.6 | 1096 | 6 | Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrsDisplacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs |
ChEMBL | 523 | 25 | 0 | 7 | 5.6 | CCCCCCCCCCCCCCCCOC[C@@H](OC(=O)C)COP(=O)(OCC[N+](C)(C)C)[O-] | 10.1016/j.bmcl.2013.01.025 | ||
| DB02261 | 2993 | None | 38 | Human | Binding | pIC50 | = | 9.6 | 9.6 | 1096 | 6 | Displacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrsDisplacement of [3H]PAF from platelet activating factor receptor in human platelets after 3 hrs |
ChEMBL | 523 | 25 | 0 | 7 | 5.6 | CCCCCCCCCCCCCCCCOC[C@@H](OC(=O)C)COP(=O)(OCC[N+](C)(C)C)[O-] | 10.1016/j.bmcl.2013.01.025 | ||
| 14851876 | 73937 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 498 | 2 | 0 | 8 | 4.3 | Cc1nnc2n1-c1sc(C#CCn3c(=O)n(C)c4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| CHEMBL20195 | 73937 | None | 0 | Human | Binding | pIC50 | = | 9.5 | 9.5 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 498 | 2 | 0 | 8 | 4.3 | Cc1nnc2n1-c1sc(C#CCn3c(=O)n(C)c4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| 14851882 | 71698 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 526 | 2 | 0 | 9 | 3.7 | Cc1nnc2n1-c1sc(C#CCn3c(=O)n(C)c(=O)c4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| CHEMBL19640 | 71698 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 526 | 2 | 0 | 9 | 3.7 | Cc1nnc2n1-c1sc(C#CCn3c(=O)n(C)c(=O)c4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| 14851869 | 72034 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 499 | 2 | 0 | 7 | 4.4 | Cc1nnc2n1-c1sc(C#CCN3C(=O)COc4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| CHEMBL19747 | 72034 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 499 | 2 | 0 | 7 | 4.4 | Cc1nnc2n1-c1sc(C#CCN3C(=O)COc4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| 14851877 | 72861 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 523 | 2 | 1 | 6 | 5.6 | Cc1nnc2n1-c1sc(C#CCC34CCCc5cccc(c53)NC4=O)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| CHEMBL20019 | 72861 | None | 0 | Human | Binding | pIC50 | = | 9.2 | 9.2 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 523 | 2 | 1 | 6 | 5.6 | Cc1nnc2n1-c1sc(C#CCC34CCCc5cccc(c53)NC4=O)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
| 44297792 | 100948 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 1 | Compound was evaluated for inhibitory activity of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptorCompound was evaluated for inhibitory activity of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptor |
ChEMBL | 634 | 14 | 0 | 10 | 5.4 | CCCS(=O)(=O)c1cc(C2CC[C@@H](c3cc(OC)c(OC)c(OC)c3)O2)cc(OC)c1OCCS(=O)(=O)c1ccccc1 | 10.1016/S0960-894X(01)80446-7 | ||
| CHEMBL293773 | 100948 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 1 | Compound was evaluated for inhibitory activity of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptorCompound was evaluated for inhibitory activity of binding of [3H]-C18 PAF to human platelet membrane Platelet activating factor receptor |
ChEMBL | 634 | 14 | 0 | 10 | 5.4 | CCCS(=O)(=O)c1cc(C2CC[C@@H](c3cc(OC)c(OC)c(OC)c3)O2)cc(OC)c1OCCS(=O)(=O)c1ccccc1 | 10.1016/S0960-894X(01)80446-7 | ||
| 10002808 | 210792 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Inhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog bloodInhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog blood |
ChEMBL | 430 | 11 | 1 | 3 | 6.1 | CCCCc1c(/C=C/C(=O)N[C@@H](C)CCCc2cccnc2)cc(OC)c2ccccc12 | 10.1021/jm00172a029 | ||
| CHEMBL99294 | 210792 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | Inhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog bloodInhibition of [3H]PAF binding to platelet activating factor receptor citrate-treated dog blood |
ChEMBL | 430 | 11 | 1 | 3 | 6.1 | CCCCc1c(/C=C/C(=O)N[C@@H](C)CCCc2cccnc2)cc(OC)c2ccccc12 | 10.1021/jm00172a029 | ||
| 14851887 | 99305 | None | 0 | Human | Binding | pIC50 | = | 9 | 9.0 | - | 0 | PAF-antagonist activity determined in dog platelets by PAF-binding assayPAF-antagonist activity determined in dog platelets by PAF-binding assay |
ChEMBL | 560 | 3 | 0 | 8 | 5.8 | Cc1nnc2n1-c1sc(C#CCn3c(=O)n(-c4ccccc4)c4ccccc43)cc1C(c1ccccc1Cl)=NC2 | 10.1021/jm00107a048 | ||
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