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Ligand source activities (1 row/activity)

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	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

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Ligand source activities (1 row/activity)