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

ACT-660602	275	None	12	Human	Binding	IC50	=	204.00	6.69	-	2	Inhibition of CXCR3 receptor internalization in human venous whole blood incubated for 30 mins by flow cytometer analysis	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-777991	276	None	10	Human	Binding	IC50	=	56.00	7.25	-	4	Antagonist activity at CXCR3 in human whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytometric analysis	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	Kd	=	4.60	8.34	-	4	Binding affinity to human CXCR3 expressed in CHO-K1 cell membrane assessed as dissociation constant using tritium-labeled ligand by FLIPR assay	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	IC50	=	5.30	8.28	-	4	Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	IC50	=	3.20	8.49	-	4	Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	IC50	=	3.30	8.48	-	4	Antagonist activity at human CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL9 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	IC50	=	10.90	7.96	-	4	Antagonist activity at human CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary human T cells assessed as inhibition of CXCLI1 mediated cell migration incubated for 45 mins by Boyden chamber assay	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	IC50	=	56.30	7.25	-	4	Antagonist activity at CXCR3 (unknown origin) in human T cells in venous blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytometric analysis	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Human	Binding	pKd	=	-	8.34	-	4	Binding affinity determined in an association assay using [³H]ACT-777991	Guide to Pharmacology	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://pubmed.ncbi.nlm.nih.gov/36883854
ACT-777991	276	None	10	Dog	Binding	IC50	=	4.00	8.40	-	4	Antagonist activity at dog CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Dog	Binding	IC50	=	2.80	8.55	-	4	Antagonist activity at dog CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Rat	Binding	IC50	=	291.00	6.54	-	4	Antagonist activity at CXCR3 in Wistar rat whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytometric analysis	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Rat	Binding	IC50	=	2.20	8.66	-	4	Antagonist activity at rat CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Mouse	Binding	IC50	=	161.00	6.79	-	4	Antagonist activity at CXCR3 in DBA/1 mouse whole blood assessed as receptor internalization incubated for 30 mins in presence of CXCL10 by flow cytometric analysis	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Mouse	Binding	IC50	=	4.40	8.36	-	4	Antagonist activity at mouse CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL11 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Mouse	Binding	IC50	=	1.50	8.82	-	4	Antagonist activity at mouse CXCR3 expressed in CHO-K1 cells assessed as reduction in CXCL10 induced calcium flux by FLIPR method	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
ACT-777991	276	None	10	Mouse	Binding	IC50	=	10.50	7.98	-	4	Antagonist activity at mouse CXCR3-mediated chemotaxis expressed in CD3/CD28-activated primary mouse T cells assessed as inhibition of CXCLI1 mediated cell migration incubated for 45 mins by Boyden chamber assay	ChEMBL	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://dx.doi.org/10.1021/acs.jmedchem.3c00074
AMG487	393	None	25	Human	Binding	pIC50	=	-	8.10	-	1	Antagonism of ¹²⁵I-IP10 binding to CXCR3 in a radioligand competition binding assay	Guide to Pharmacology	603.2	10	0	8	5.81	CCOc1ccc(-n2c(C(C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1	https://pubmed.ncbi.nlm.nih.gov/17448658
AMG487	393	None	25	Human	Binding	IC50	=	251.19	6.60	-	1	Inhibition of human wild type CXCR3	ChEMBL	603.2	10	0	8	5.81	CCOc1ccc(-n2c(C(C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)cc3)nc3ncccc3c2=O)cc1	https://dx.doi.org/10.1021/acs.jmedchem.6b01309
CCL11	827	None	0	Human	Binding	pKi	=	-	7.20	-446	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9660793

Showing 1 to 20 of 1,640 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

ACT-660602	275	None	12	Human	Functional	pIC50	=	-	8.57	-7	2	Antagonist potency determined by FLIPR calcium mobilization assay, in CHO-K1 cells expressing recombinant CXCR3 receptors with CXCL10 as agonist	Guide to Pharmacology	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://pubmed.ncbi.nlm.nih.gov/35947786
ACT-660602	275	None	12	Human	Functional	IC50	=	3.40	8.47	-7	2	Antagonist activity at CXCR3 (unknown origin) in presence of CXCL11 by calcium FLIPR assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-660602	275	None	12	Human	Functional	IC50	=	2.70	8.57	-7	2	Antagonist activity at CXCR3 (unknown origin) in presence of CXCL10 by calcium FLIPR assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-660602	275	None	12	Human	Functional	IC50	=	3.80	8.42	-7	2	Antagonist activity at CXCR3 (unknown origin) in presence of CXCL9 by calcium FLIPR assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-660602	275	None	12	Human	Functional	IC50	=	222.00	6.65	-7	2	Antagonist activity at recombinant human CXCR3 in human U2SO cells assessed as reduction in CXCL10-induced beta-arrestin recruitment by TANGO assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-660602	275	None	12	Human	Functional	IC50	=	2.70	8.57	-7	2	Antagonist activity at recombinant human CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-660602	275	None	12	Mouse	Functional	IC50	=	1.79	8.75	7	2	Antagonist activity at recombinant mouse CXCR3 expressed in human CHO-K1 cells co-expressing Galpha15 incubated for 10 mins by Fluo-4AM dye based FLIPR assay	ChEMBL	534.1	4	0	9	3.58	Cc1nc(C)n(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2C)n1	https://dx.doi.org/10.1021/acs.jmedchem.2c00675
ACT-777991	276	None	10	Human	Functional	pIC50	=	-	8.48	-2	4	Antagonism of CXCL9-mediated CXCR3 activation in a calcium signaling assay	Guide to Pharmacology	550.1	6	1	10	2.64	Cc1ncn(CC(=O)N2CCN(c3sc(C(F)(F)F)nc3-c3cnc(C(F)(F)F)nc3)C[C@H]2CCO)n1	https://pubmed.ncbi.nlm.nih.gov/36883854
CHEMBL10097	4336	None	0	Human	Functional	IC50	=	830.00	6.08	-	1	Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge	ChEMBL	396.2	4	1	3	3.93	O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Cl)cc3)CC2)C(=O)N1	https://dx.doi.org/10.1016/j.bmcl.2008.07.115
CHEMBL10309	4653	None	0	Human	Functional	IC50	=	1330.00	5.88	13	2	Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge	ChEMBL	440.1	4	1	3	4.04	O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1	https://dx.doi.org/10.1016/j.bmcl.2008.07.115
CHEMBL10309	4653	None	0	Human	Functional	IC50	=	610.00	6.21	13	2	Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge	ChEMBL	440.1	4	1	3	4.04	O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1	https://dx.doi.org/10.1016/j.bmcl.2008.07.115
CHEMBL10309	4653	None	0	Human	Functional	IC50	=	780.00	6.11	13	2	Antagonist activity at human CXCR3 expressed in CHO cells assessed as inhibition of ITAC-stimulated [35S]GTPgammaS binding pretreated 30 mins before ITAC challenge	ChEMBL	440.1	4	1	3	4.04	O=C1CCC(c2ccccc2)(C2CCN(Cc3ccc(Br)cc3)CC2)C(=O)N1	https://dx.doi.org/10.1016/j.bmcl.2008.07.115
CHEMBL1075640	5480	None	0	Human	Functional	IC50	=	75.00	7.12	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	604.2	9	0	6	6.67	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077809	5649	None	0	Human	Functional	IC50	=	450.00	6.35	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	576.2	9	0	8	5.18	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cn3cnc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077810	5651	None	0	Human	Functional	IC50	=	500.00	6.30	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	587.2	9	0	7	5.93	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(C(F)(F)F)cn3)nc3ccccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077817	5658	None	0	Human	Functional	IC50	=	17.00	7.77	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	654.2	9	0	6	7.55	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3cc(C(F)(F)F)cc(C(F)(F)F)c3)nc3ccccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077818	5659	None	0	Human	Functional	IC50	=	220.00	6.66	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	620.2	10	0	7	6.55	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(OC(F)(F)F)c(F)c3)nc3ccccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077819	5660	None	21	Human	Functional	IC50	=	20.00	7.70	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	605.2	9	0	7	6.07	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077820	5661	None	0	Human	Functional	IC50	=	23.00	7.64	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	605.2	9	0	7	6.07	CCOc1ccc(-n2c([C@@H](C)N(Cc3cccnc3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3cnccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032
CHEMBL1077823	5664	None	0	Human	Functional	IC50	=	59.00	7.23	-	1	Antagonist activity against human CXCR3 expressed in human PBMC assessed as inhibition of cell migration in response to ITAC in plasma	ChEMBL	609.2	9	0	8	5.97	CCOc1ccc(-n2c([C@@H](C)N(Cc3cc(C)no3)C(=O)Cc3ccc(F)c(C(F)(F)F)c3)nc3ncccc3c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.07.032

Showing 1 to 20 of 762 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)