GPCRdb

Finalizing display...

Ligand source activities (1 row/activity)

Affinity
Potency

Search:

	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

3570-0208 [PMID:19807662]	92	None	8	Human	Binding	pKi	=	-	7.00	-	1	Unclassified	Guide to Pharmacology	376.1	3	0	6	4.14	CCc1cc2c(=O)c(-c3nc4ccccc4n3C)c(C)oc2cc1OC(C)=O	https://pubmed.ncbi.nlm.nih.gov/19807662
BMS-986235	688	None	24	Human	Binding	EC50	=	2800.00	5.55	-	4	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 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	=	0.60	9.22	-	4	Agonist activity at mouse FPR1 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
CHEMBL162488	211269	None	0	Human	Binding	IC50	=	50.00	7.30	-	1	Binding affinity towards fMLF receptor using human neutrophils	ChEMBL	-	-	-	-	-	CC(C)C[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccccc1)NC(=O)Nc1ccccc1)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	https://dx.doi.org/10.1021/jm950908d
CHEMBL2021596	73998	None	0	Human	Binding	IC50	=	150.00	6.82	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	1199.9	15	4	11	4.54	C/C=C/CC(C)C(C)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2369724	212119	None	0	Human	Binding	IC50	=	1570.00	5.80	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@H]([C@H](C)CC)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2370883	212401	None	0	Human	Binding	IC50	=	5500.00	5.26	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)C1NC(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H](C(C)C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H]([C@@H](C)O)NC1=O	https://dx.doi.org/10.1021/jm010987v
CHEMBL2370885	212402	None	0	Human	Binding	IC50	=	6450.00	5.19	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)C1NC(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H](C(C)C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)CN(C)C(=O)[C@H](CC)NC1=O	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372456	212705	None	0	Human	Binding	IC50	=	3400.00	5.47	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CCC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](CCC)C(=O)N(C)[C@H](CC(C)C)C(=O)NC(C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372461	212706	None	0	Human	Binding	IC50	=	2300.00	5.64	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372466	212707	None	0	Human	Binding	IC50	=	7000.00	5.16	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	CC/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@@H]([C@@H](C)CC)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372473	212708	None	0	Human	Binding	IC50	=	6300.00	5.20	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	CC/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](CCCCN)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372474	212709	None	0	Human	Binding	IC50	=	2200.00	5.66	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](C)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372476	212710	None	0	Human	Binding	IC50	=	6330.00	5.20	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	CC[C@@H]1NC(=O)[C@H](CC2CCCCC2)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)[C@@H](C(C)C)NC(=O)[C@@H](CC(C)C)N(C)C(=O)CN(C)C1=O	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372477	212711	None	0	Human	Binding	IC50	=	2520.00	5.60	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N(C)[C@@H](C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372478	212712	None	0	Human	Binding	IC50	=	1800.00	5.75	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372485	212713	None	0	Human	Binding	IC50	=	9200.00	5.04	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H](CC)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@H](C(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@H](C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372486	212714	None	0	Human	Binding	IC50	=	560.00	6.25	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N(C)CC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@](O)(C(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372487	212715	None	0	Human	Binding	IC50	=	750.00	6.12	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)N(C)CC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@](O)(C(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v
CHEMBL2372488	212716	None	0	Human	Binding	IC50	=	300.00	6.52	-	1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	ChEMBL	-	-	-	-	-	C/C=C/C[C@@H](C)[C@@H](O)[C@H]1C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@H](CC(C)C)C(=O)N[C@@H](C)C(=O)N[C@](O)(C(C)C)C(=O)N(C)[C@@H](CC(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N(C)[C@@H](C(C)C)C(=O)N1C	https://dx.doi.org/10.1021/jm010987v

Showing 1 to 20 of 173 entries

Search:

	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

3570-0208 [PMID:19807662]	92	None	8	Human	Functional	IC50	=	1400.00	5.85	-	1	Antagonist activity against human FPR1 expressed in human HL-60 cells assessed as inhibition of fMLF-induced calcium mobilization preincubated for 30 mins followed by fMLF addition and measured every 5s for 240s by Fluo4AM dye based scanning fluorimetric analysis	ChEMBL	376.1	3	0	6	4.14	CCc1cc2c(=O)c(-c3nc4ccccc4n3C)c(C)oc2cc1OC(C)=O	https://dx.doi.org/10.1016/j.ejmech.2023.115854
3570-0208 [PMID:19807662]	92	None	8	Human	Functional	Ki	=	100.00	7.00	-	1	Antagonist activity at FPR1	ChEMBL	376.1	3	0	6	4.14	CCc1cc2c(=O)c(-c3nc4ccccc4n3C)c(C)oc2cc1OC(C)=O	https://dx.doi.org/10.1016/j.bmcl.2011.03.049
A77636	208	None	8	Human	Functional	IC50	=	21729.90	4.66	-7244	27	GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1	ChEMBL	329.2	2	3	4	3.25	NC[C@@H]1O[C@H](C23CC4CC(CC(C4)C2)C3)Cc2c1ccc(O)c2O	https://dx.doi.org/10.6019/CHEMBL5442687
AG-09/1	307	None	0	Human	Functional	pEC50	=	-	5.60	-	1	Unclassified	Guide to Pharmacology	358.1	6	2	6	3.21	COc1ccc2[nH]c(SCC(=O)Nc3ccc([N+](=O)[O-])cc3)nc2c1	https://pubmed.ncbi.nlm.nih.gov/19903830
AG-11/03	308	None	0	Human	Functional	pEC50	=	-	5.60	-	1	Unclassified	Guide to Pharmacology	359.1	6	2	5	4.02	COc1ccc2[nH]c(SCC(=O)Nc3ccc(SC)cc3)nc2c1	https://pubmed.ncbi.nlm.nih.gov/22127612
AG-14	309	None	0	Human	Functional	pEC50	=	-	7.40	-	1	Unclassified	Guide to Pharmacology	404.1	7	1	6	3.77	COc1cc(/C=N/NC(=O)c2ccc3c(c2)OCO3)ccc1OCc1ccccc1	https://pubmed.ncbi.nlm.nih.gov/17229869
annexin I	423	None	0	Mouse	Functional	pEC50	=	-	6.60	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17948261
annexin I	423	None	0	Mouse	Functional	pEC50	=	-	6.60	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11395373
annexin I-(2-26)	425	None	0	Human	Functional	pEC50	=	-	5.95	-1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10882119
annexin I-(2-26)	425	None	0	Human	Functional	pEC50	=	-	5.95	-1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12560218
aprepitant	448	None	58	Human	Functional	IC50	=	11590.10	4.94	-48977	8	GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1	ChEMBL	534.1	6	2	5	4.95	C[C@@H](O[C@H]1OCCN(Cc2nc(=O)[nH][nH]2)[C@H]1c1ccc(F)cc1)c1cc(C(F)(F)F)cc(C(F)(F)F)c1	https://dx.doi.org/10.6019/CHEMBL5442687
BENZYLPENICILLIN	100446	None	26	Human	Functional	Ki	=	7800.00	5.11	-	2	PubChem BioAssay. Dose Response Assay for Formylpeptide Receptor (FPR) Ligands and Dose Response Counter-Screen Assay for Formylpeptide-Like-1 (FPRL1) Ligands. (Class of assay: confirmatory)	ChEMBL	334.1	4	2	4	0.86	CC1(C)S[C@@H]2[C@H](NC(=O)Cc3ccccc3)C(=O)N2[C@H]1C(=O)O	-
BMS-986235	688	None	24	Human	Functional	pEC50	=	-	6.40	-177	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	EC50	=	400.00	6.40	-177	4	Agonist activity at human FPR1 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	=	400.00	6.40	-177	4	Agonist activity at human FPR1 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	=	-	6.30	-12	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	Mouse	Functional	EC50	=	500.00	6.30	-12	4	Agonist activity at mouse FPR1 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
BVT173187	751	None	0	Human	Functional	pIC50	=	-	7.00	-	1	Unclassified	Guide to Pharmacology	329.0	2	2	2	4.91	Cc1ccc(Cl)c(NC(=O)c2cc(Cl)cc(Cl)c2O)c1	https://pubmed.ncbi.nlm.nih.gov/22410002
CHEMBL103769	4750	None	24	Human	Functional	IC50	=	3572.79	5.45	-123	29	GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.6019/CHEMBL5442687
CHEMBL103769	4750	None	24	Human	Functional	IC50	=	3392.28	5.47	-123	29	GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR1	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.6019/CHEMBL5442687

Showing 1 to 20 of 509 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)