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
| |
| 44263999 | 207549 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils |
ChEMBL | 558 | 15 | 5 | 6 | 3.3 | COc1ccc(NC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccccc2)C(=O)O)cc1 | 10.1021/jm950908d | ||
| CHEMBL7753 | 207549 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils |
ChEMBL | 558 | 15 | 5 | 6 | 3.3 | COc1ccc(NC(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(C)C)C(=O)NC(Cc2ccccc2)C(=O)O)cc1 | 10.1021/jm950908d | ||
| CHEMBL267388 | 213177 | None | 0 | Human | Functional | pEC50 | = | 9 | 9.0 | - | 1 | Agonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophilsAgonistic activity was determined by measuring the ability to induce superoxide production(as measured by reduction of cytochrome C) using human neutrophils |
ChEMBL | None | None | None | CSCC[C@H](NC(=O)Nc1ccc(Cl)cc1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](Cc1ccccc1)C(=O)O | 10.1021/jm950908d | ||||
| 1022 | 1669 | None | 42 | Human | Functional | pEC50 | = | 8 | 8.0 | 478 | 4 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | None | None | None | None | 10.1021/jm900592h | ||||
| 443295 | 1669 | None | 42 | Human | Functional | pEC50 | = | 8 | 8.0 | 478 | 4 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | None | None | None | None | 10.1021/jm900592h | ||||
| CHEMBL267179 | 1669 | None | 42 | Human | Functional | pEC50 | = | 8 | 8.0 | 478 | 4 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | None | None | None | None | 10.1021/jm900592h | ||||
| 145952664 | 162528 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method |
ChEMBL | 500 | 9 | 3 | 4 | 4.6 | COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(C)c(F)c3)CC2)cc1 | 10.1016/j.ejmech.2017.09.023 | ||
| CHEMBL4166385 | 162528 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method |
ChEMBL | 500 | 9 | 3 | 4 | 4.6 | COc1ccc(NC(=O)N[C@@H](Cc2ccc(C#N)cc2)C(=O)NCC2(c3ccc(C)c(F)c3)CC2)cc1 | 10.1016/j.ejmech.2017.09.023 | ||
| 71698968 | 90711 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 445 | 5 | 1 | 4 | 4.2 | Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391281 | 90711 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 445 | 5 | 1 | 4 | 4.2 | Cc1cc(Cc2cccc(Cl)c2)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 | 10.1016/j.ejmech.2013.03.066 | ||
| 44232677 | 198802 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | 1 | 2 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 408 | 7 | 1 | 7 | 2.7 | COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc([N+](=O)[O-])cc3)c2=O)c1 | 10.1021/jm900592h | ||
| CHEMBL562456 | 198802 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | 1 | 2 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 408 | 7 | 1 | 7 | 2.7 | COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc([N+](=O)[O-])cc3)c2=O)c1 | 10.1021/jm900592h | ||
| 71698530 | 90706 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 509 | 7 | 1 | 5 | 5.3 | COc1cccc(Cc2cc(C3CCCCC3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391257 | 90706 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 509 | 7 | 1 | 5 | 5.3 | COc1cccc(Cc2cc(C3CCCCC3)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1016/j.ejmech.2013.03.066 | ||
| 44233646 | 198879 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 2 | Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 393 | 7 | 1 | 6 | 2.8 | COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 | 10.1021/jm900592h | ||
| CHEMBL562910 | 198879 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 2 | Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 393 | 7 | 1 | 6 | 2.8 | COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 | 10.1021/jm900592h | ||
| 44233646 | 198879 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 2 | Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay |
ChEMBL | 393 | 7 | 1 | 6 | 2.8 | COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 | 10.1021/jm900592h | ||
| CHEMBL562910 | 198879 | None | 0 | Human | Functional | pEC50 | = | 6.0 | 6.0 | 1 | 2 | Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay |
ChEMBL | 393 | 7 | 1 | 6 | 2.8 | COc1ccc(NC(=O)Cn2nc(C)cc(Cc3cccc(OC)c3)c2=O)cc1 | 10.1021/jm900592h | ||
| 164916035 | 192459 | None | 3 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -16 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 446 | 5 | 2 | 3 | 4.2 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| CHEMBL5207056 | 192459 | None | 3 | Human | Functional | pEC50 | = | 6.0 | 6.0 | -16 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 446 | 5 | 2 | 3 | 4.2 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc32)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| 71698446 | 90743 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 427 | 5 | 1 | 5 | 3.6 | COc1ccc(-c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391452 | 90743 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 427 | 5 | 1 | 5 | 3.6 | COc1ccc(-c2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| 44232924 | 197779 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 455 | 7 | 1 | 5 | 3.9 | COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1021/jm900592h | ||
| CHEMBL551590 | 197779 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 in human neutrophiles assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 455 | 7 | 1 | 5 | 3.9 | COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1021/jm900592h | ||
| 44232924 | 197779 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay |
ChEMBL | 455 | 7 | 1 | 5 | 3.9 | COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1021/jm900592h | ||
| CHEMBL551590 | 197779 | None | 0 | Human | Functional | pEC50 | = | 5.0 | 5.0 | -1 | 2 | Agonist activity at FPR1 in human neutrophiles by chemotaxis assayAgonist activity at FPR1 in human neutrophiles by chemotaxis assay |
ChEMBL | 455 | 7 | 1 | 5 | 3.9 | COc1cccc(Cc2cc(C)nn(CCC(=O)Nc3ccc(Br)cc3)c2=O)c1 | 10.1021/jm900592h | ||
| 122487974 | 170517 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 497 | 9 | 1 | 5 | 5.3 | CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| CHEMBL4448213 | 170517 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 497 | 9 | 1 | 5 | 5.3 | CCCCC(C(=O)Nc1ccc(Br)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| 168279295 | 191155 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -91 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 442 | 5 | 2 | 3 | 4.4 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| CHEMBL5187135 | 191155 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -91 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 442 | 5 | 2 | 3 | 4.4 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCc3ccccc32)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| 71699142 | 90740 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 442 | 6 | 2 | 6 | 3.7 | COc1ccc(Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391449 | 90740 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -1 | 2 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 442 | 6 | 2 | 6 | 3.7 | COc1ccc(Nc2cc(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| 71698365 | 90738 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -7 | 2 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 484 | 7 | 2 | 7 | 3.9 | COc1ccc(Nc2c(C(C)=O)c(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391447 | 90738 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | -7 | 2 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 484 | 7 | 2 | 7 | 3.9 | COc1ccc(Nc2c(C(C)=O)c(C)nn(CC(=O)Nc3ccc(Br)cc3)c2=O)cc1 | 10.1016/j.ejmech.2013.03.066 | ||
| 71699061 | 90731 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 461 | 5 | 1 | 4 | 4.7 | Cc1cc(Cc2cccc3ccccc23)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 | 10.1016/j.ejmech.2013.03.066 | ||
| CHEMBL2391438 | 90731 | None | 0 | Human | Functional | pEC50 | = | 4.9 | 4.9 | - | 1 | Agonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilizationAgonist activity at FPR1 (unknown origin) transfected in human HL60 cells assessed as induction of Ca2+ mobilization |
ChEMBL | 461 | 5 | 1 | 4 | 4.7 | Cc1cc(Cc2cccc3ccccc23)c(=O)n(CC(=O)Nc2ccc(Br)cc2)n1 | 10.1016/j.ejmech.2013.03.066 | ||
| 146597625 | 191371 | None | 2 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -47 | 2 | Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay |
ChEMBL | 420 | 5 | 2 | 6 | 3.4 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccc(Cl)cc3)o2)c(F)c1 | 10.1021/acsmedchemlett.2c00079 | ||
| CHEMBL5190385 | 191371 | None | 2 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -47 | 2 | Agonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assayAgonist activity at human FPR1 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay |
ChEMBL | 420 | 5 | 2 | 6 | 3.4 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2Nc2nnc(-c3ccc(Cl)cc3)o2)c(F)c1 | 10.1021/acsmedchemlett.2c00079 | ||
| 168286767 | 191791 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -53 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 442 | 5 | 2 | 3 | 4.0 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| CHEMBL5196551 | 191791 | None | 0 | Human | Functional | pEC50 | = | 5.9 | 5.9 | -53 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 442 | 5 | 2 | 3 | 4.0 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccccc3C2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| 145949892 | 162915 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2 | 2 | Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method |
ChEMBL | 459 | 9 | 3 | 5 | 3.6 | O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 | 10.1016/j.ejmech.2017.09.023 | ||
| CHEMBL4172556 | 162915 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -2 | 2 | Agonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric methodAgonist activity at human FPR1 expressed in human HL60 cells assessed as induction of calcium mobilization measured every 5 secs for 240 secs by Fluo-4-AM dye based fluorometric method |
ChEMBL | 459 | 9 | 3 | 5 | 3.6 | O=C(Nc1ccc([N+](=O)[O-])cc1)N[C@H](Cc1cccnc1)C(=O)NCC1(c2ccccc2)CC1 | 10.1016/j.ejmech.2017.09.023 | ||
| 168279956 | 191192 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 460 | 5 | 2 | 3 | 4.2 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| CHEMBL5187563 | 191192 | None | 0 | Human | Functional | pEC50 | = | 5.8 | 5.8 | -4 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 460 | 5 | 2 | 3 | 4.2 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCc3ccc(F)cc3C2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| 168283359 | 190921 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -5 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 380 | 5 | 2 | 3 | 3.1 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| CHEMBL5183856 | 190921 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -5 | 2 | Agonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assayAgonist activity at human FPR1 transfected in human HL-60 cells assessed as increase in calcium mobilization measured every 5 seconds for 240 secs by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 380 | 5 | 2 | 3 | 3.1 | N#Cc1ccc(C[C@H](NC(=O)Nc2ccc(F)cc2)C(=O)N2CCCC2)cc1 | 10.1021/acs.jmedchem.1c02203 | ||
| 155519369 | 170481 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 441 | 7 | 1 | 6 | 4.0 | COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1OC | 10.1021/acs.jmedchem.8b01912 | ||
| CHEMBL4447830 | 170481 | None | 0 | Human | Functional | pEC50 | = | 6.8 | 6.8 | - | 1 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as intracellular calcium mobilization by Fluo-4-AM dye based fluorescence assay |
ChEMBL | 441 | 7 | 1 | 6 | 4.0 | COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1OC | 10.1021/acs.jmedchem.8b01912 | ||
| 44233647 | 197991 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -1 | 2 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 423 | 8 | 1 | 7 | 2.8 | COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 | 10.1021/jm900592h | ||
| CHEMBL554291 | 197991 | None | 0 | Human | Functional | pEC50 | = | 4.8 | 4.8 | -1 | 2 | Agonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assayAgonist activity at FPR1 expressed in human HL60 cells assessed as induction of intracellular calcium flux by FLIPR3 calcium assay |
ChEMBL | 423 | 8 | 1 | 7 | 2.8 | COc1cccc(Cc2cc(C)nn(CC(=O)Nc3ccc(OC)c(OC)c3)c2=O)c1 | 10.1021/jm900592h | ||
Showing 1 to 50 of 1,041 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
| |
| 126520336 | 194016 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assayAgonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay |
ChEMBL | 385 | 7 | 4 | 3 | 2.2 | CC(C)C[C@H](NC(=O)CNC(=O)Nc1ccc(Br)cc1)C(=O)O | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5276622 | 194016 | None | 0 | Human | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assayAgonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay |
ChEMBL | 385 | 7 | 4 | 3 | 2.2 | CC(C)C[C@H](NC(=O)CNC(=O)Nc1ccc(Br)cc1)C(=O)O | 10.1016/j.ejmech.2021.113167 | ||
| 11024 | 688 | None | 24 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 361 | 4 | 3 | 3 | 2.4 | COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 | 10.1016/j.ejmech.2021.113167 | ||
| 122583088 | 688 | None | 24 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 361 | 4 | 3 | 3 | 2.4 | COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL4784510 | 688 | None | 24 | Mouse | Binding | pEC50 | = | 9.2 | 9.2 | - | 0 | Agonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at mouse FPR1 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 361 | 4 | 3 | 3 | 2.4 | COc1cc(F)c(c(c1)F)[C@@H]1CNC(=O)[C@H]1NC(=O)Nc1ccccc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171351673 | 193646 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 463 | 6 | 2 | 3 | 4.5 | COc1cc(F)c([C@H]2CCN(CC3CC3)C(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5267736 | 193646 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 463 | 6 | 2 | 3 | 4.5 | COc1cc(F)c([C@H]2CCN(CC3CC3)C(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1016/j.ejmech.2021.113167 | ||
| 171352615 | 193980 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@@H]2CCN(Cc3ccccn3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5275766 | 193980 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@@H]2CCN(Cc3ccccn3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171355882 | 193998 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@H]2CCN(Cc3ccccn3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5276203 | 193998 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@H]2CCN(Cc3ccccn3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171357377 | 194090 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@H]2CCN(Cc3cccnc3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5278464 | 194090 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 448 | 6 | 2 | 4 | 3.9 | COc1ccc([C@H]2CCN(Cc3cccnc3)C(=O)[C@@H]2NC(=O)Nc2ccc(F)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 124093840 | 194425 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 373 | 4 | 3 | 3 | 3.1 | COc1ccc([C@H]2CCNC(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5285824 | 194425 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 373 | 4 | 3 | 3 | 3.1 | COc1ccc([C@H]2CCNC(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171347467 | 194446 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 473 | 7 | 2 | 3 | 5.3 | COc1cc(F)c([C@H]2CCN(CCC(F)F)C[C@@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5286200 | 194446 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 473 | 7 | 2 | 3 | 5.3 | COc1cc(F)c([C@H]2CCN(CCC(F)F)C[C@@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1016/j.ejmech.2021.113167 | ||
| 171358475 | 194598 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 437 | 5 | 2 | 5 | 4.3 | COc1ccc([C@H]2CCN(c3ccnnc3)C[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5290016 | 194598 | None | 0 | Human | Binding | pEC50 | = | 9 | 9.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assayAgonist activity at human FPR1 expressed in CHO cells assessed as increase in calcium flux incubated for 50 mins by FLIPR calcium 5 dye based fluorescence assay |
ChEMBL | 437 | 5 | 2 | 5 | 4.3 | COc1ccc([C@H]2CCN(c3ccnnc3)C[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171347985 | 194375 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assayAgonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay |
ChEMBL | 342 | 5 | 3 | 2 | 3.3 | CC(C)C(C(=O)O)C(C)NC(=O)Nc1ccc(Br)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5284816 | 194375 | None | 0 | Human | Binding | pEC50 | = | 8.8 | 8.8 | - | 0 | Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assayAgonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay |
ChEMBL | 342 | 5 | 3 | 2 | 3.3 | CC(C)C(C(=O)O)C(C)NC(=O)Nc1ccc(Br)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 156159233 | 194189 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 506 | 7 | 3 | 6 | 2.4 | CS(=O)(=O)NCC1(c2ccc(N3CCC[C@@H](NC(=O)Nc4cnc(Cl)cn4)C3=O)cc2)CCC1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5280720 | 194189 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 506 | 7 | 3 | 6 | 2.4 | CS(=O)(=O)NCC1(c2ccc(N3CCC[C@@H](NC(=O)Nc4cnc(Cl)cn4)C3=O)cc2)CCC1 | 10.1016/j.ejmech.2021.113167 | ||
| 122592369 | 183126 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 359 | 4 | 3 | 3 | 2.8 | COc1ccc([C@@H]2CNC(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1021/acs.jmedchem.9b02101 | ||
| CHEMBL4793814 | 183126 | None | 0 | Human | Binding | pEC50 | = | 7 | 7.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 359 | 4 | 3 | 3 | 2.8 | COc1ccc([C@@H]2CNC(=O)[C@@H]2NC(=O)Nc2ccc(Cl)cc2)cc1 | 10.1021/acs.jmedchem.9b02101 | ||
| 122582962 | 182818 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 391 | 5 | 3 | 4 | 2.4 | COc1ccc(NC(=O)N[C@@H]2C(=O)NC[C@H]2c2c(F)cc(OC)cc2F)cc1 | 10.1021/acs.jmedchem.9b02101 | ||
| CHEMBL4789579 | 182818 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 391 | 5 | 3 | 4 | 2.4 | COc1ccc(NC(=O)N[C@@H]2C(=O)NC[C@H]2c2c(F)cc(OC)cc2F)cc1 | 10.1021/acs.jmedchem.9b02101 | ||
| 122583080 | 182915 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 391 | 4 | 4 | 4 | 2.4 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(C)c(O)c2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| CHEMBL4790836 | 182915 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 391 | 4 | 4 | 4 | 2.4 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(C)c(O)c2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| 122487986 | 176078 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assayAgonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assay |
ChEMBL | 411 | 6 | 1 | 5 | 4.0 | COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL4588649 | 176078 | None | 0 | Human | Binding | pEC50 | = | 6 | 6.0 | - | 0 | Agonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assayAgonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assay |
ChEMBL | 411 | 6 | 1 | 5 | 4.0 | COc1cccc(Cc2cc(C)nn(C(C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1016/j.ejmech.2021.113167 | ||
| 122488043 | 174370 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 427 | 7 | 1 | 6 | 3.5 | COc1ccc(OC)c(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1021/acs.jmedchem.8b01912 | ||
| CHEMBL4549250 | 174370 | None | 0 | Human | Binding | pEC50 | = | 5 | 5.0 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 427 | 7 | 1 | 6 | 3.5 | COc1ccc(OC)c(Cc2cc(C)nn(CC(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1021/acs.jmedchem.8b01912 | ||
| 154971347 | 194508 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 460 | 4 | 2 | 3 | 5.0 | O=C(Nc1ccc(C(F)(F)F)cc1)N[C@@H]1CCCN(c2ccc(N3CCCCC3)cc2)C1=O | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5287909 | 194508 | None | 0 | Human | Binding | pEC50 | = | 8.0 | 8.0 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 460 | 4 | 2 | 3 | 5.0 | O=C(Nc1ccc(C(F)(F)F)cc1)N[C@@H]1CCCN(c2ccc(N3CCCCC3)cc2)C1=O | 10.1016/j.ejmech.2021.113167 | ||
| 122582941 | 181105 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 395 | 4 | 3 | 3 | 3.0 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| CHEMBL4758920 | 181105 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 395 | 4 | 3 | 3 | 3.0 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(Cl)cc2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| 129226959 | 194002 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 492 | 6 | 3 | 4 | 4.4 | COc1ccc(NC(=O)N[C@@H]2CCCN(c3ccc(-c4ccccc4C(N)=O)cc3)C2=O)cc1Cl | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5276320 | 194002 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assayAgonist activity at human FPR1 expressed in CHO cells assessed as cAMP level incubated for 1.5 hr by HTRF assay |
ChEMBL | 492 | 6 | 3 | 4 | 4.4 | COc1ccc(NC(=O)N[C@@H]2CCCN(c3ccc(-c4ccccc4C(N)=O)cc3)C2=O)cc1Cl | 10.1016/j.ejmech.2021.113167 | ||
| 122583133 | 181268 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 401 | 4 | 3 | 4 | 3.1 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(Cl)s2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| CHEMBL4760897 | 181268 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric methodAgonist activity at human FPR1 expressed in HEK 293 cells co-expressing Galpha15 measured every 1.5 sec for 80 sec by Fluo-4 NW staining based scanning fluorometric method |
ChEMBL | 401 | 4 | 3 | 4 | 3.1 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccc(Cl)s2)c(F)c1 | 10.1021/acs.jmedchem.9b02101 | ||
| 122487981 | 173851 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 397 | 6 | 1 | 5 | 3.4 | COc1ccccc1Cc1cc(C)nn(CC(=O)Nc2ccc(Cl)cc2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| CHEMBL4536766 | 173851 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 397 | 6 | 1 | 5 | 3.4 | COc1ccccc1Cc1cc(C)nn(CC(=O)Nc2ccc(Cl)cc2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| 155555898 | 174471 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 453 | 9 | 1 | 5 | 5.2 | CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| CHEMBL4551649 | 174471 | None | 0 | Human | Binding | pEC50 | = | 6.9 | 6.9 | - | 0 | Biased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assayBiased agonist activity at human FPR1 expressed in FlpIn-CHO cells assessed as stimulation of ERK1/2 phosphorylation measured after 7 mins by Alphascreen assay |
ChEMBL | 453 | 9 | 1 | 5 | 5.2 | CCCCC(C(=O)Nc1ccc(Cl)cc1)n1nc(C)cc(Cc2cccc(OC)c2)c1=O | 10.1021/acs.jmedchem.8b01912 | ||
| 171346443 | 194421 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Agonist activity at human FPR1 transfected in HL-60 cells assessed as increase in intracellular calcium flux incubated for 30 mins by Fluo-4 AM dye based fluorometer analysisAgonist activity at human FPR1 transfected in HL-60 cells assessed as increase in intracellular calcium flux incubated for 30 mins by Fluo-4 AM dye based fluorometer analysis |
ChEMBL | 399 | 4 | 2 | 4 | 2.6 | O=C(Cn1c(=O)[nH]cc(-c2ccccc2)c1=O)Nc1ccc(Br)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5285738 | 194421 | None | 0 | Human | Binding | pEC50 | = | 4.9 | 4.9 | - | 0 | Agonist activity at human FPR1 transfected in HL-60 cells assessed as increase in intracellular calcium flux incubated for 30 mins by Fluo-4 AM dye based fluorometer analysisAgonist activity at human FPR1 transfected in HL-60 cells assessed as increase in intracellular calcium flux incubated for 30 mins by Fluo-4 AM dye based fluorometer analysis |
ChEMBL | 399 | 4 | 2 | 4 | 2.6 | O=C(Cn1c(=O)[nH]cc(-c2ccccc2)c1=O)Nc1ccc(Br)cc1 | 10.1016/j.ejmech.2021.113167 | ||
| 171347365 | 194345 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assayAgonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assay |
ChEMBL | 411 | 6 | 1 | 5 | 4.0 | COc1cccc(Cc2cc(C)nn([C@@H](C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1016/j.ejmech.2021.113167 | ||
| CHEMBL5283998 | 194345 | None | 0 | Human | Binding | pEC50 | = | 5.9 | 5.9 | - | 0 | Agonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assayAgonist activity at human recombinant FPR1 stably transfected in Flp-In-CHO cells assessed as ERK1/2 phosphorylation incubated for 1 hr by Alphascreen fluorescence assay |
ChEMBL | 411 | 6 | 1 | 5 | 4.0 | COc1cccc(Cc2cc(C)nn([C@@H](C)C(=O)Nc3ccc(Cl)cc3)c2=O)c1 | 10.1016/j.ejmech.2021.113167 | ||
| 171347985 | 194375 | None | 0 | Human | Binding | pEC50 | = | 7.9 | 7.9 | - | 0 | Agonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assayAgonist activity at FPR1 (unknown origin) expressed in CHO/Galpha16 cells assessed as increase in calcium flux by FLIPR assay |
ChEMBL | 342 | 5 | 3 | 2 | 3.3 | CC(C)C(C(=O)O)C(C)NC(=O)Nc1ccc(Br)cc1 | 10.1016/j.ejmech.2021.113167 | ||
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