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Ligand source activities (1 row/activity)
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
1R-11 | 39 | None | 0 | Human | Binding | IC50 | = | 76.60 | 7.12 | - | 1 | Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-6 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay | ChEMBL | 382.2 | 12 | 3 | 7 | 2.42 | CCCCC[C@@H](O)c1c(/C=C/[C@@H](O)[C@@H](O)CCCC(=O)OC)nc(C)n1C | https://dx.doi.org/10.1016/j.ejmech.2018.10.049 | |
1R-11 | 39 | None | 0 | Human | Binding | IC50 | = | 5.60 | 8.25 | - | 1 | Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in TNFalpha secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay | ChEMBL | 382.2 | 12 | 3 | 7 | 2.42 | CCCCC[C@@H](O)c1c(/C=C/[C@@H](O)[C@@H](O)CCCC(=O)OC)nc(C)n1C | https://dx.doi.org/10.1016/j.ejmech.2018.10.049 | |
1R-11 | 39 | None | 0 | Human | Binding | IC50 | = | 5.10 | 8.29 | - | 1 | Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IL-12p70 secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay | ChEMBL | 382.2 | 12 | 3 | 7 | 2.42 | CCCCC[C@@H](O)c1c(/C=C/[C@@H](O)[C@@H](O)CCCC(=O)OC)nc(C)n1C | https://dx.doi.org/10.1016/j.ejmech.2018.10.049 | |
1R-11 | 39 | None | 0 | Human | Binding | IC50 | = | 4.40 | 8.36 | - | 1 | Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation by measuring reduction in IFNgamma secretion pretreated for 30 mins followed by LPS stimulation for 24 hrs by electrochemiluminescence assay | ChEMBL | 382.2 | 12 | 3 | 7 | 2.42 | CCCCC[C@@H](O)c1c(/C=C/[C@@H](O)[C@@H](O)CCCC(=O)OC)nc(C)n1C | https://dx.doi.org/10.1016/j.ejmech.2018.10.049 | |
1R-11 | 39 | None | 0 | Human | Binding | IC50 | = | 1.00 | 9.00 | - | 1 | Agonist activity at ALX/FPR2 in human THP1 cells harboring NF-kB-Luc assessed as inhibition of LPS-induced NFkB signalling activation pretreated for 30 mins followed by LPS stimulation for 24 hrs by luciferase reporter gene assay | ChEMBL | 382.2 | 12 | 3 | 7 | 2.42 | CCCCC[C@@H](O)c1c(/C=C/[C@@H](O)[C@@H](O)CCCC(=O)OC)nc(C)n1C | https://dx.doi.org/10.1016/j.ejmech.2018.10.049 | |
AG-26 | 310 | None | 3 | Human | Binding | EC50 | = | 990.00 | 6.00 | - | 3 | Agonist activity at human FPR2 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 | 304.1 | 5 | 2 | 2 | 3.71 | COc1ccc(CCNC(=O)Nc2ccc(Cl)cc2)cc1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
annexin I | 423 | None | 0 | Human | Binding | pKd | = | - | 6.50 | - | 2 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12368905 | |
BMS-986235 | 688 | None | 24 | Human | Binding | EC50 | = | 1250.00 | 5.90 | - | 4 | Agonist activity at human FPR2 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1016/j.ejmech.2021.113167 | |
BMS-986235 | 688 | None | 24 | Human | Binding | IC50 | = | 57.00 | 7.24 | - | 4 | Agonist activity at FPR2 in human HL-60 cells assessed as reduction in chemoattractant induced chemotaxis by luminescence cell viability assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
BMS-986235 | 688 | None | 24 | Human | Binding | EC50 | = | 130.00 | 6.89 | - | 4 | Agonist activity at human FPR2 expressed in CHO-K1 cells assessed as stimulation of beta-arrestin recruitment | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
BMS-986235 | 688 | None | 24 | Human | Binding | EC50 | = | 0.41 | 9.39 | - | 4 | Agonist activity at human FPR2 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 | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
BMS-986235 | 688 | None | 24 | Mouse | Binding | EC50 | = | 384.00 | 6.42 | - | 4 | Agonist activity at mouse FPR2 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1016/j.ejmech.2021.113167 | |
BMS-986235 | 688 | None | 24 | Mouse | Binding | EC50 | = | 0.50 | 9.30 | - | 4 | Agonist activity at mouse FPR2 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
BMS-986235 | 688 | None | 24 | Mouse | Binding | EC50 | = | 3.40 | 8.47 | - | 4 | Agonist activity at mouse FPR2 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 | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
CGEN-855A | 886 | None | 0 | Human | Binding | pKi | = | - | 7.27 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/19023040 | |
CHEMBL3588930 | 214264 | None | 0 | Human | Binding | IC50 | = | 50.00 | 7.30 | - | 1 | Allosteric antagonist activity against FPR2 (unknown origin) | ChEMBL | - | - | - | - | - | CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(N)=O)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1 | https://dx.doi.org/10.1016/j.bmc.2015.03.062 | |
CHEMBL3588930 | 214264 | None | 0 | Human | Binding | IC50 | = | 41.00 | 7.39 | - | 1 | Antagonist activity at FPR2 in human peripheral blood polymorphonuclear neutrophils assessed as inhibition of WKYMVM-peptide induced ROS production preincubated for 5 mins followed WKYMVM-peptide stimulation measured up to 20 mins by isoluminol-based chemiluminescence assay | ChEMBL | - | - | - | - | - | CCCCCCCCCCCCCCCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(=O)N[C@@H](CCCCN)C(=O)N(CCC(N)=O)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1)[C@@H](C)c1ccccc1 | https://dx.doi.org/10.1021/acs.jmedchem.7b00489 | |
CHEMBL377226 | 138466 | None | 0 | Human | Binding | EC50 | = | 10.00 | 8.00 | - | 4 | Agonist activity at human FPR2 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay | ChEMBL | 398.2 | 3 | 2 | 4 | 4.77 | Cn1c(C(C)(C)C)c(NC(=O)Nc2ccc(Cl)cc2)c(=O)n1-c1ccccc1 | https://dx.doi.org/10.1016/j.ejmech.2021.113167 | |
CHEMBL377226 | 138466 | None | 0 | Human | Binding | EC50 | = | 3100.00 | 5.51 | - | 4 | Agonist activity at human FPR2 expressed in CHO-K1 cells by beta-arrestin recruitment assay | ChEMBL | 398.2 | 3 | 2 | 4 | 4.77 | Cn1c(C(C)(C)C)c(NC(=O)Nc2ccc(Cl)cc2)c(=O)n1-c1ccccc1 | https://dx.doi.org/10.1016/j.ejmech.2021.113167 | |
CHEMBL377226 | 138466 | None | 0 | Mouse | Binding | EC50 | = | 50.00 | 7.30 | - | 4 | Agonist activity at mouse FPR2 expressed in CHO-A12 cells assessed as cAMP level incubated for 1.5 hr by HTRF assay | ChEMBL | 398.2 | 3 | 2 | 4 | 4.77 | Cn1c(C(C)(C)C)c(NC(=O)Nc2ccc(Cl)cc2)c(=O)n1-c1ccccc1 | https://dx.doi.org/10.1016/j.ejmech.2021.113167 |
Showing 1 to 20 of 236 entries
Ligands | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | Receptor | Activity | Chemical information | ||||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
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 | |
ACT-389949 | 273 | None | 0 | Human | Functional | pEC50 | = | - | 8.52 | - | 1 | FPR2/ALX internalization into monocytes. | Guide to Pharmacology | 428.1 | 6 | 1 | 8 | 3.95 | Cc1cccc(-c2oc(C)nc2C(=O)Nc2cnn(Cc3nc(C(C)(F)F)co3)n2)c1 | https://pubmed.ncbi.nlm.nih.gov/27730665 | |
AG-26 | 310 | None | 3 | Human | Functional | pEC50 | = | - | 6.30 | 2 | 3 | Unclassified | Guide to Pharmacology | 304.1 | 5 | 2 | 2 | 3.71 | COc1ccc(CCNC(=O)Nc2ccc(Cl)cc2)cc1 | https://pubmed.ncbi.nlm.nih.gov/19903830 | |
AG-26 | 310 | None | 3 | Human | Functional | EC50 | = | 400.00 | 6.40 | 2 | 3 | Agonist activity against human FPR2 expressed in human HL60 cells by Fluo-4AM dye based intracellular Ca2+ mobilization assay | ChEMBL | 304.1 | 5 | 2 | 2 | 3.71 | COc1ccc(CCNC(=O)Nc2ccc(Cl)cc2)cc1 | https://dx.doi.org/10.1016/j.bmc.2015.03.062 | |
AM-37 | 382 | None | 0 | Mouse | Functional | EC50 | = | 2100.00 | 5.68 | - | 2 | Agonist activity at FPR2 in BALB/c mouse assessed as stimulation of Ca2+ influx measured every 5 secs for 240 secs by FLIPR assay | ChEMBL | 525.3 | 9 | 4 | 4 | 5.32 | COc1ccc(NC(=O)N[C@H](Cc2c[nH]c3ccccc23)C(=O)NCC2(c3cccnc3)CCCCC2)cc1 | https://dx.doi.org/10.1016/j.bmc.2014.12.007 | |
amyloid β | 407 | None | 0 | Human | Functional | pEC50 | = | - | 7.00 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11316806 | |
amyloid β | 407 | None | 0 | Human | Functional | pEC50 | = | - | 7.00 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/11160457 | |
annexin I-(2-26) | 425 | None | 0 | Human | Functional | pEC50 | = | - | 5.91 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/10882119 | |
annexin I-(2-26) | 425 | None | 0 | Human | Functional | pEC50 | = | - | 5.91 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12560218 | |
annexin I-(2-26) | 425 | None | 0 | Human | Functional | pEC50 | = | - | 5.91 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/12368905 | |
annexin I-(2-26) | 425 | None | 0 | Human | Functional | pEC50 | = | - | 5.91 | -1 | 3 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/16278303 | |
aspirin-triggered resolvin D1 | 504 | None | 0 | Human | Functional | pEC50 | = | - | 11.10 | - | 1 | Unclassified | Guide to Pharmacology | 376.2 | 14 | 4 | 4 | 3.46 | CC/C=C\C[C@@H](O)/C=C/C=C\C=C\C=C\[C@@H](O)[C@@H](O)C/C=C\CCC(=O)O | https://pubmed.ncbi.nlm.nih.gov/22449948 | |
BMS-986235 | 688 | None | 24 | Human | Functional | pEC50 | = | - | 8.30 | -4 | 4 | Unclassified | Guide to Pharmacology | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://pubmed.ncbi.nlm.nih.gov/32407089 | |
BMS-986235 | 688 | None | 24 | Human | Functional | IC50 | = | 7.50 | 8.12 | -4 | 4 | Agonist activity at human FPR2 in human HL-60 cells assessed as inhibition of chemotaxis by measuring reduction in cell migration | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acsmedchemlett.2c00079 | |
BMS-986235 | 688 | None | 24 | Human | Functional | EC50 | = | 5.00 | 8.30 | -4 | 4 | Agonist activity at human FPR2 overexpressing CHO cells assessed as reduction in intracellular cAMP level incubated for 30 mins by HTRF assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acsmedchemlett.2c00079 | |
BMS-986235 | 688 | None | 24 | Human | Functional | EC50 | = | 5.00 | 8.30 | -4 | 4 | Agonist activity at human FPR2 expressed in CHO cells assessed as reduction cAMP accumulation incubated for 1 hr by TR-FRET assay | ChEMBL | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://dx.doi.org/10.1021/acs.jmedchem.9b02101 | |
BMS-986235 | 688 | None | 24 | Mouse | Functional | pEC50 | = | - | 9.30 | 4 | 4 | Unclassified | Guide to Pharmacology | 361.1 | 4 | 3 | 3 | 2.38 | COc1cc(F)c([C@@H]2CNC(=O)[C@H]2NC(=O)Nc2ccccc2)c(F)c1 | https://pubmed.ncbi.nlm.nih.gov/32407089 | |
CGEN-855A | 886 | None | 0 | Human | Functional | pIC50 | = | - | 6.72 | - | 1 | Unclassified | Guide to Pharmacology | - | - | - | - | - | - | https://pubmed.ncbi.nlm.nih.gov/19023040 | |
CHEMBL1288648 | 19050 | None | 8 | Human | Functional | EC50 | = | 3000.00 | 5.52 | - | 1 | Agonist activity against human FPR2 expressed in human HL60 cells by Fluo-4AM dye based intracellular Ca2+ mobilization assay | ChEMBL | 270.1 | 5 | 2 | 2 | 3.06 | COc1ccc(CCNC(=O)Nc2ccccc2)cc1 | https://dx.doi.org/10.1016/j.bmc.2015.03.062 | |
CHEMBL1289379 | 19139 | None | 7 | Human | Functional | EC50 | = | 900.00 | 6.05 | - | 1 | Agonist activity against human FPR2 expressed in human HL60 cells by Fluo-4AM dye based intracellular Ca2+ mobilization assay | ChEMBL | 288.1 | 5 | 2 | 2 | 3.20 | COc1ccc(CCNC(=O)Nc2ccc(F)cc2)cc1 | https://dx.doi.org/10.1016/j.bmc.2015.03.062 | |
CHEMBL1289381 | 19140 | None | 6 | Human | Functional | EC50 | = | 100.00 | 7.00 | - | 1 | Agonist activity against human FPR2 expressed in human HL60 cells by Fluo-4AM dye based intracellular Ca2+ mobilization assay | ChEMBL | 348.0 | 5 | 2 | 2 | 3.82 | COc1ccc(CCNC(=O)Nc2ccc(Br)cc2)cc1 | https://dx.doi.org/10.1016/j.bmc.2015.03.062 |
Showing 1 to 20 of 819 entries