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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

α-NETA	368	None	2	Human	Binding	IC50	=	380.00	6.42	-	3	Antagonist activity at human CMKLR1	ChEMBL	242.2	4	0	1	3.12	C[N+](C)(C)CCC(=O)c1cccc2ccccc12	https://dx.doi.org/10.1021/acs.jmedchem.3c01011
CHEMBL3956726	150885	None	0	Human	Binding	IC50	=	7220.00	5.14	-	1	Antagonist activity at human CMKLR1	ChEMBL	486.2	4	1	2	6.36	Cc1cccc(C)c1N1C[C@](C(=O)Nc2cc(C(F)(F)F)cc(C(F)(F)F)c2)(C(C)C)CC1=O	https://dx.doi.org/10.1021/acs.jmedchem.3c01011
CHEMBL4448632	170544	None	6	Human	Binding	IC50	=	380.00	6.42	-	2	Inhibition of chemR23 expressed in human CAL1 cells assessed as reduction in chemerin-induced chemotaxis incubated for 4 hrs by cell counting based CellTiter-Glo assay	ChEMBL	495.2	9	2	7	5.40	CCCCN(c1nc2cc(C(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4746987	180101	None	0	Human	Binding	IC50	=	235.00	6.63	-	1	Inhibition of chemR23 expressed in human CAL1 cells assessed as reduction in chemerin-induced chemotaxis incubated for 4 hrs by cell counting based CellTiter-Glo assay	ChEMBL	532.2	9	2	7	6.56	CCCCN(c1nc2c(C(=O)O)cccc2o1)[C@H](C)c1ccc(-c2cc(Cl)ccc2-c2nc(=O)o[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2020.115622
CHEMBL4783675	182363	None	6	Human	Binding	IC50	=	63.00	7.20	-	1	Inhibition of chemR23 expressed in human CAL1 cells assessed as reduction in chemerin-induced chemotaxis incubated for 4 hrs by cell counting based CellTiter-Glo assay	ChEMBL	510.2	8	2	7	5.82	Cc1ccc(-c2nc(=O)o[nH]2)c(-c2ccc([C@@H](C)N(CC3CC3)c3nc4c(C(=O)O)cccc4o3)cc2)c1	https://dx.doi.org/10.1016/j.bmc.2020.115622
CHEMBL5396770	195106	None	0	Human	Binding	IC50	=	5754.40	5.24	-	1	Antagonist activity at human CMKLR1	ChEMBL	428.2	8	1	4	6.44	CC(C)n1nc(-c2ccccc2)c2ccc(COc3ccc([C@@H](C)CC(=O)O)cc3)cc21	https://dx.doi.org/10.1021/acs.jmedchem.3c01011
chemerin	908	None	0	Human	Binding	pKd	=	-	8.31	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/18165312
chemerin C-terminal peptide	909	None	15	Human	Binding	pKd	=	-	7.88	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/18165312
chemerin C-terminal peptide	909	None	15	Human	Binding	pKd	=	-	7.88	-	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/14701797
resolvin E1	3319	None	18	Human	Binding	EC50	=	1.00	9.00	-	1	Antagonist activity at human CMKLR1	ChEMBL	350.2	13	4	4	2.90	CC[C@@H](O)/C=C/C=C\C[C@@H](O)/C=C/C=C/C=C\[C@@H](O)CCCC(=O)O	https://dx.doi.org/10.1021/acs.jmedchem.3c01011
resolvin E1	3319	None	18	Human	Binding	pKd	=	-	7.95	-	1	Unclassified	Guide to Pharmacology	350.2	13	4	4	2.90	CC[C@@H](O)/C=C/C=C\C[C@@H](O)/C=C/C=C/C=C\[C@@H](O)CCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/15753205
resolvin E1	3319	None	18	Human	Binding	pKd	=	-	7.95	-	1	Unclassified	Guide to Pharmacology	350.2	13	4	4	2.90	CC[C@@H](O)/C=C/C=C\C[C@@H](O)/C=C/C=C/C=C\[C@@H](O)CCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/20887750
resolvin E1	3319	None	18	Human	Binding	pKd	=	-	7.95	-	1	Unclassified	Guide to Pharmacology	350.2	13	4	4	2.90	CC[C@@H](O)/C=C/C=C\C[C@@H](O)/C=C/C=C/C=C\[C@@H](O)CCCC(=O)O	https://pubmed.ncbi.nlm.nih.gov/17339491
tethered chemerin 9	3787	None	0	Human	Binding	pIC50	~	-	8.26	-	1	Binding affinity in a radioligand displacement assay using membranes prepared from chemerinR-expressing CHO-K1 cells and ¹²⁵I-YHSFFFPGQFAFS as tracer.	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/14530373
tethered chemerin 9	3787	None	0	Human	Binding	pIC50	~	-	8.26	-	1	Binding affinity in a radioligand displacement assay using membranes prepared from chemerinR-expressing CHO-K1 cells and ¹²⁵I-YHSFFFPGQFAFS as tracer.	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/24659779

Showing 1 to 15 of 15 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

α-NETA	368	None	2	Human	Functional	pIC50	=	-	6.43	83	3	Antagonism of chemerin-stimulated β-arrestin 2 recruitment to CMKLR1 in a cellular assay.	Guide to Pharmacology	242.2	4	0	1	3.12	C[N+](C)(C)CCC(=O)c1cccc2ccccc12	https://pubmed.ncbi.nlm.nih.gov/25437209
CHEMBL4442745	170134	None	0	Human	Functional	IC50	=	8400.00	5.08	-	1	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	452.2	8	1	6	6.22	CCCCN(c1nc2ccccc2o1)C(C)(C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4446260	170383	None	0	Human	Functional	IC50	=	3300.00	5.48	2	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	424.2	8	1	6	5.48	CCCCN(Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1)c1nc2ccccc2o1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4446260	170383	None	0	Human	Functional	EC50	=	5200.00	5.28	2	2	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	424.2	8	1	6	5.48	CCCCN(Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1)c1nc2ccccc2o1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4447627	170467	None	0	Human	Functional	IC50	=	1200.00	5.92	2	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	492.1	8	1	6	6.79	CCCCN(Cc1ccc(-c2ccccc2-c2nnn[nH]2)cc1)c1nc2cc(Cl)cc(Cl)c2o1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4448308	170525	None	0	Human	Functional	IC50	=	120.00	6.92	-	1	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	509.3	10	2	7	5.33	CCCCN(c1nc2cc(CC(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4448308	170525	None	0	Human	Functional	EC50	=	2300.00	5.64	-	1	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	509.3	10	2	7	5.33	CCCCN(c1nc2cc(CC(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4448632	170544	None	6	Human	Functional	IC50	=	38.00	7.42	-1	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	495.2	9	2	7	5.40	CCCCN(c1nc2cc(C(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4448632	170544	None	6	Human	Functional	EC50	=	280.00	6.55	-1	2	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	495.2	9	2	7	5.40	CCCCN(c1nc2cc(C(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4448632	170544	None	6	Mouse	Functional	IC50	=	150.00	6.82	1	2	Inhibition of chemR23 expressed in mouse BA/F3 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	495.2	9	2	7	5.40	CCCCN(c1nc2cc(C(=O)NC)ccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4457246	171178	None	0	Human	Functional	IC50	=	7600.00	5.12	1	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)[C@@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4458521	171248	None	0	Human	Functional	IC50	=	2800.00	5.55	-	1	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	459.2	7	1	7	5.28	c1ccc(CN(Cc2ccc(-c3ccccc3-c3nnn[nH]3)cc2)c2nc3ccccc3o2)nc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4463797	171595	None	0	Human	Functional	IC50	=	250.00	6.60	10	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)C(C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4463797	171595	None	0	Human	Functional	EC50	=	2700.00	5.57	10	2	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)C(C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4467290	171849	None	0	Human	Functional	IC50	=	110.00	6.96	-2	3	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4467290	171849	None	0	Human	Functional	EC50	=	1200.00	5.92	-2	3	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4467290	171849	None	0	Human	Functional	IC50	=	110.00	6.96	-2	3	Inhibition of chemR23 in human CAL1 cells assessed as inhibition of chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by human chemerin addition by FDSS6000 analysis	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2020.115622
CHEMBL4467290	171849	None	0	Mouse	Functional	IC50	=	150.00	6.82	2	3	Inhibition of chemR23 expressed in mouse BA/F3 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	438.2	8	1	6	6.04	CCCCN(c1nc2ccccc2o1)[C@H](C)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4472121	172171	None	0	Human	Functional	IC50	=	940.00	6.03	4	2	Inhibition of chemR23 in human CAL1 cells assessed as reduction in chemerin-induced intracellular calcium ion concentration preincubated for 45 mins followed by chemerin addition	ChEMBL	452.2	9	1	6	6.43	CCCCN(c1nc2ccccc2o1)C(CC)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091
CHEMBL4472121	172171	None	0	Human	Functional	EC50	=	4500.00	5.35	4	2	Agonist activity at chemR23 expressed in human CAL1 cells assessed as increase in intracellular calcium ion concentration	ChEMBL	452.2	9	1	6	6.43	CCCCN(c1nc2ccccc2o1)C(CC)c1ccc(-c2ccccc2-c2nnn[nH]2)cc1	https://dx.doi.org/10.1016/j.bmc.2019.115091

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Ligand source activities (1 row/activity)