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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

2-hydroxyoctanoic acid	67	None	51	Human	Binding	Ki	=	100000.00	4.00	-	2	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	160.1	6	2	2	1.40	CCCCCCC(O)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxy capric acid	99	None	58	Human	Binding	Ki	=	3310.00	5.48	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	188.1	8	2	2	2.18	CCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxy capric acid	99	None	58	Human	Binding	EC50	=	4050.00	5.39	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	188.1	8	2	2	2.18	CCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxylauric acid	100	None	48	Human	Binding	Ki	=	110.00	6.96	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxylauric acid	100	None	48	Human	Binding	EC50	=	3250.00	5.49	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Binding	Ki	=	0.63	9.20	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Binding	EC50	=	11000.00	4.96	-	1	Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.0c01378
6-n-octylaminouracil	164	None	39	Human	Binding	EC50	=	1750.00	5.76	-	1	Agonist activity at recombinant human GPR84 expressed in HEK293 cells assessed as beta-arrestin 2 recruitment measured after 20 mins by luciferase reporter gene assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Binding	EC50	=	114.00	6.94	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cells assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-nonylpyridine-2,4-diol	165	None	0	Human	Binding	EC50	=	501.00	6.30	-	1	Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as induction of beta-arrestin recruitment by luminescence assay	ChEMBL	237.2	8	2	2	3.37	CCCCCCCCCc1cc(O)cc(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.0c01378
6-nonylpyridine-2,4-diol	165	None	0	Human	Binding	Ki	=	1.56	8.81	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	237.2	8	2	2	3.37	CCCCCCCCCc1cc(O)cc(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-nonylpyridine-2,4-diol	165	None	0	Human	Binding	EC50	=	5000.00	5.30	-	1	Agonist activity at human GPR84 expressed in CHO cells assessed as induction of beta-arrestin recruitment by chemiluminescence PathHunter assay	ChEMBL	237.2	8	2	2	3.37	CCCCCCCCCc1cc(O)cc(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.0c01378
CHEMBL1232858	16449	None	37	Human	Binding	Ki	=	472.00	6.33	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	244.2	12	2	2	3.74	CCCCCCCCCCC[C@@H](O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL1232858	16449	None	37	Human	Binding	EC50	=	452.00	6.34	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	244.2	12	2	2	3.74	CCCCCCCCCCC[C@@H](O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL124310	16722	None	1	Human	Binding	Ki	=	91.00	7.04	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	197.1	5	3	5	1.49	CCCCCNc1cc(O)nc(O)n1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL125436	17037	None	0	Human	Binding	Ki	=	0.73	9.14	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	267.2	10	3	5	3.44	CCCCCCCCCCNc1cc(O)nc(O)n1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL2004471	72940	None	46	Human	Binding	Ki	=	318.00	6.50	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	244.2	12	2	2	3.74	CCCCCCCCCCCCC(O)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL2004471	72940	None	46	Human	Binding	EC50	=	4360.00	5.36	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as beta-arrestin 2 recruitment measured after 90 mins by beta-galactosidase based PathHunter assay	ChEMBL	244.2	12	2	2	3.74	CCCCCCCCCCCCC(O)C(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL246297	93565	None	2	Human	Binding	IC50	=	14000.00	4.85	-	1	Displacement of [3H]PSB-1584 from recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 measured after 6 hrs by scintillation counting method	ChEMBL	274.1	2	0	2	4.26	Cn1cc(Cc2cn(C)c3ccccc23)c2ccccc21	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
CHEMBL246298	93566	None	3	Human	Binding	EC50	=	1200.00	5.92	-	1	Agonist activity at human GPR84 expressed in CHO cells assessed as beta-arrestin recruitment after 90 mins by beta-galactosidase complementation assay	ChEMBL	306.1	4	2	2	4.26	COc1ccc2[nH]cc(Cc3c[nH]c4ccc(OC)cc34)c2c1	https://dx.doi.org/10.1021/acs.jmedchem.6b01593

Showing 1 to 20 of 136 entries

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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

2-hydroxy capric acid	65	None	0	Human	Functional	pEC50	=	-	4.50	-	1	Unclassified	Guide to Pharmacology	188.1	8	2	2	2.18	CCCCCCCCC(O)C(=O)O	https://pubmed.ncbi.nlm.nih.gov/23449982
2-hydroxylauric acid	66	None	35	Human	Functional	pEC50	=	-	5.00	-1	2	Unclassified	Guide to Pharmacology	216.2	10	2	2	2.96	CCCCCCCCCCC(O)C(=O)O	https://pubmed.ncbi.nlm.nih.gov/23449982
2-hydroxylauric acid	66	None	35	Human	Functional	EC50	=	12882.50	4.89	-1	2	Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCCC(O)C(=O)O	https://dx.doi.org/10.1039/C7MD00130D
3-hydroxy capric acid	99	None	58	Human	Functional	pEC50	=	-	3.60	-	1	Unclassified	Guide to Pharmacology	188.1	8	2	2	2.18	CCCCCCCC(O)CC(=O)O	https://pubmed.ncbi.nlm.nih.gov/23449982
3-hydroxy capric acid	99	None	58	Human	Functional	EC50	=	31800.00	4.50	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay	ChEMBL	188.1	8	2	2	2.18	CCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxylauric acid	100	None	48	Human	Functional	pEC50	=	-	4.90	-	1	Unclassified	Guide to Pharmacology	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://pubmed.ncbi.nlm.nih.gov/23449982
3-hydroxylauric acid	100	None	48	Human	Functional	EC50	=	5248.07	5.28	-	1	Agonist activity at N-terminal FLAG-tagged/C-terminal eYFP-fused human GPR84 expressed in CHO cell membranes assessed as induction of [35S]GTPgammaS binding after 1 hr by liquid scintillation counting method	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1039/C7MD00130D
3-hydroxylauric acid	100	None	48	Human	Functional	EC50	=	1310.00	5.88	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cell membranes co-expressing beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation preincubated for 5 mins followed by forskolin stimulation and measured after 15 mins by radioactive assay	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
3-hydroxylauric acid	100	None	48	Human	Functional	EC50	=	13000.00	4.89	-	1	Agonist activity at human Gialpha-coupled GPR84 expressed in baculovirus infected sf9 insect cells assessed as induction of [35S]GTPgammaS incubated for 1 hr by liquid scintillation counting method	ChEMBL	216.2	10	2	2	2.96	CCCCCCCCCC(O)CC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.0c01378
6-n-octylaminouracil	164	None	39	Human	Functional	pEC50	=	-	7.00	-	1	Unclassified	Guide to Pharmacology	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://pubmed.ncbi.nlm.nih.gov/23449982
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	110.00	6.96	-	1	Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as beta-arrestin recruitment treated for 90 mins by luminescence based assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.3c00951
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	17.00	7.77	-	1	Agonist activity at human GPR84 expressed in recombinant CHO cells harboring beta-galactosidase fragment assessed as inhibition of forskolin induced cAMP production incubated for 15 mins by radioactive [3H]cAMP based assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.3c00951
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	19.00	7.72	-	1	Agonist activity at human GPR84 expressed in CHO-K1 cells assessed as reduction in forskolin-stimulated cAMP production incubated for 30 mins by luminescence assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.0c01378
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	1250.00	5.90	-	1	Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as increase in intracellular calcium mobilization by Fluo-4 AM dye based fluorescence assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	341.00	6.47	-	1	Agonist activity at recombinant human GPR84 stably expressed in HEK293 cells co-expressing Galpha16 assessed as inhibition of forskolin-induced cAMP accumulation preincubated for 30 mins followed by forskolin addition and measured after 30 mins by HTRF assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	105.00	6.98	-	1	Agonist activity at recombinant human GPR84 expressed in HEK293 cells co-expressing Gqi5 assessed as increase in myo-[3H]inositol phosphate accumulation measured after 2 hrs by topcount scintillation counting method	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	512.00	6.29	-	1	Agonist activity at human Gi1alpha-coupled GPR84 expressed in baculovirus infected Sf9 insect cells assessed as stimulation of [35S]GTPgammaS binding measured after 1 hr by liquid scintillation counting method	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	16.70	7.78	-	1	Agonist activity at recombinant human GPR84 expressed in CHO cells co-expressing beta-galactosidase/beta-arrestin2 assessed as inhibition of forskolin-stimulated [3H]cAMP accumulation measured after 15 mins by radioactive assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.9b01339
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	512.00	6.29	-	1	Agonist activity at human GPR84 by [35S]GTPgammaS binding assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acs.jmedchem.6b01593
6-n-octylaminouracil	164	None	39	Human	Functional	EC50	=	512.00	6.29	-	1	Agonist activity at human GPR84 fused with bovine Galphai1 protein expressed in baculovirus infected sf9 cell membrane incubated for 1 hr by [35S]GTPgammaS binding assay	ChEMBL	239.2	8	3	3	1.84	CCCCCCCCNc1cc(=O)[nH]c(=O)[nH]1	https://dx.doi.org/10.1021/acsmedchemlett.6b00025

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Ligand source activities (1 row/activity)