GPCRdb

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Ligand source activities (1 row/activity)

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Potency

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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

BI-44370	114530	None	8	Human	Binding	Ki	=	0.30	9.52	-	1	Antagonist activity against human CGRP receptor	ChEMBL	633.4	6	2	7	3.94	Cc1cc(C[C@@H](OC(=O)N2CCC(N3CCc4ccccc4NC3=O)CC2)C(=O)N2CCC(N3CCOCC3)CC2)cc(C)c1O	https://dx.doi.org/10.1021/jm500364u
CHEMBL1088906	7728	None	0	Human	Binding	Ki	=	6000.00	5.22	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	480.2	3	1	8	2.40	CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)oc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089207	7769	None	0	Human	Binding	Ki	=	185.00	6.73	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	491.2	3	1	8	2.20	CN1C(=O)NC(=O)C12Cc1cc3ncc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089433	7795	None	0	Human	Binding	Ki	=	0.12	9.92	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	487.2	2	2	5	4.24	CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089496	7816	None	0	Human	Binding	Ki	=	720.00	6.14	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	500.2	4	2	7	1.98	CN1C(=O)NC(=O)[C@]12Cc1cc(F)c(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089497	7817	None	0	Human	Binding	Ki	=	6600.00	5.18	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	479.2	3	2	7	2.13	CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089497	7817	None	0	Human	Binding	Ki	=	320.00	6.50	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	479.2	3	2	7	2.13	CN1C(=O)NC(=O)[C@@]12Cc1cc3nc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)[nH]c3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089772	7849	None	0	Human	Binding	Ki	=	1.30	8.89	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	481.2	3	2	5	3.26	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090515	7971	None	0	Human	Binding	Ki	=	0.41	9.39	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	502.2	2	1	7	2.76	CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090841	8035	None	0	Human	Binding	Ki	=	1.50	8.82	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	453.2	2	2	5	2.70	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090846	8036	None	0	Human	Binding	Ki	=	8.90	8.05	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	426.2	2	1	4	2.73	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090847	8037	None	0	Human	Binding	Ki	=	1.40	8.85	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	446.2	2	1	4	4.10	O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090848	8038	None	0	Human	Binding	Ki	=	0.30	9.52	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	468.2	2	2	7	1.37	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1091903	8173	None	0	Human	Binding	Ki	=	17.00	7.77	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	490.2	3	1	7	2.80	CN1C(=O)NC(=O)[C@]12Cc1cc3ccc(Cn4c(=O)n(-c5ccccn5)c5ccccc54)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092208	8210	None	0	Human	Binding	Ki	=	0.07	10.14	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	501.2	3	2	5	4.63	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092837	8329	None	0	Human	Binding	Ki	=	0.55	9.26	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	473.2	2	2	5	4.06	O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092838	8330	None	0	Human	Binding	Ki	=	0.52	9.28	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	467.2	2	2	5	2.87	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092882	8340	None	0	Human	Binding	Ki	=	0.02	10.64	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	488.2	2	2	7	2.73	O=C1Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092883	8341	None	0	Human	Binding	Ki	=	3.00	8.52	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	482.2	2	1	7	1.40	CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)NC(=O)N3C)c3cccc1c32	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1093189	8383	None	0	Human	Binding	Ki	=	55.00	7.26	-	1	Displacement of [125I]human CLR from human CGRP expressed in HEK293 cells coexpressing human RAMP1	ChEMBL	500.2	4	2	7	1.98	CN1C(=O)NC(=O)[C@]12Cc1ccc(NC(=O)Cn3c(=O)n(-c4ccccn4)c4ccccc43)c(F)c1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086

Showing 1 to 20 of 739 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

CHEMBL1089433	7795	None	0	Human	Functional	IC50	=	1.30	8.89	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	487.2	2	2	5	4.24	CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089433	7795	None	0	Human	Functional	IC50	=	0.52	9.28	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	487.2	2	2	5	4.24	CC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089772	7849	None	0	Human	Functional	IC50	=	44.00	7.36	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	481.2	3	2	5	3.26	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1089772	7849	None	0	Human	Functional	IC50	=	7.20	8.14	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	481.2	3	2	5	3.26	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)NC(=O)N1C)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090515	7971	None	0	Human	Functional	IC50	=	95.00	7.02	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	502.2	2	1	7	2.76	CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090515	7971	None	0	Human	Functional	IC50	=	1.20	8.92	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	502.2	2	1	7	2.76	CN1C(=O)Cn2c(=O)n(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc1c32	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090841	8035	None	0	Human	Functional	IC50	=	43.00	7.37	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	453.2	2	2	5	2.70	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090841	8035	None	0	Human	Functional	IC50	=	7.30	8.14	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	453.2	2	2	5	2.70	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090846	8036	None	0	Human	Functional	IC50	=	850.00	6.07	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	426.2	2	1	4	2.73	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090846	8036	None	0	Human	Functional	IC50	=	50.00	7.30	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	426.2	2	1	4	2.73	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4C(=O)CCc5ccccc54)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090847	8037	None	0	Human	Functional	IC50	=	81.00	7.09	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	446.2	2	1	4	4.10	O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090847	8037	None	0	Human	Functional	IC50	=	4.70	8.33	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	446.2	2	1	4	4.10	O=C1CCc2ccccc2N1Cc1ccc2cc3c(cc2n1)C[C@@]1(C3)C(=O)Nc2ncccc21	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090848	8038	None	0	Human	Functional	IC50	=	14.00	7.85	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	468.2	2	2	7	1.37	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1090848	8038	None	0	Human	Functional	IC50	=	1.70	8.77	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	468.2	2	2	7	1.37	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(Cn4c(=O)n5c6c(cccc64)NC(=O)C5)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092208	8210	None	0	Human	Functional	IC50	=	1.50	8.82	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	501.2	3	2	5	4.63	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092208	8210	None	0	Human	Functional	IC50	=	0.68	9.17	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	501.2	3	2	5	4.63	CCC12CC(=O)Nc3cccc(c31)N(Cc1ccc3cc4c(cc3n1)C[C@@]1(C4)C(=O)Nc3ncccc31)C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092837	8329	None	0	Human	Functional	IC50	=	4.10	8.39	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	473.2	2	2	5	4.06	O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092837	8329	None	0	Human	Functional	IC50	=	0.86	9.07	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	473.2	2	2	5	4.06	O=C1CC2CN(Cc3ccc4cc5c(cc4n3)C[C@@]3(C5)C(=O)Nc4ncccc43)c3cccc(c32)N1	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092838	8330	None	0	Human	Functional	IC50	=	6.50	8.19	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production in the presence of 50% human serum	ChEMBL	467.2	2	2	5	2.87	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086
CHEMBL1092838	8330	None	0	Human	Functional	IC50	=	2.20	8.66	-	1	Antagonist activity at human CLR expressed in human HEK293 cells coexpressing human RAMP1 assessed as Inhibition of CGRP-induced cAMP production	ChEMBL	467.2	2	2	5	2.87	CN1C(=O)NC(=O)[C@@]12Cc1cc3ccc(CN4CC5(C)CC(=O)Nc6cccc4c65)nc3cc1C2	https://dx.doi.org/10.1016/j.bmcl.2010.02.086

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Ligand source activities (1 row/activity)