GPCRdb

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

Ava3	525	None	0	Human	Binding	pKi	=	-	9.40	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17486669
Ava5	526	None	0	Human	Binding	pKi	=	-	8.90	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17486669
CHEMBL1729021	59876	None	0	Human	Binding	IC50	=	270.00	6.57	-	2	Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ChEMBL	356.1	4	0	5	4.30	COc1ccc(Oc2c(Cl)cnn(-c3cc(C)cc(C)c3)c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2012.12.030
CHEMBL1736481	60069	None	0	Human	Binding	IC50	=	1700.00	5.77	-	2	Antagonist activity against human NPBWR1 expressed in HEK293 cells co-expressing Gqi3 assessed as inhibition of agonist-induced response by FLIPR assay	ChEMBL	356.1	5	0	5	4.05	COc1ccc(Oc2c(Cl)cnn(Cc3ccc(C)cc3)c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2012.12.030
CHEMBL1938418	69877	None	0	Mouse	Binding	IC50	=	0.18	9.74	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	588.3	7	1	7	6.31	COc1ccc(C2(N[C@@H]3CC[C@H](C(=O)N4CCN(c5nc6ccc(F)cc6o5)CC4)[C@@H](c4ccsc4)C3)CCC2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940354	70157	None	0	Human	Binding	IC50	=	324.00	6.49	-	2	Displacement of [125]-hNPW23 from human NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	538.2	7	1	6	5.76	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(Cl)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940354	70157	None	0	Mouse	Binding	IC50	=	25.00	7.60	-	2	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	538.2	7	1	6	5.76	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(Cl)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940355	70158	None	0	Mouse	Binding	IC50	=	3715.00	5.43	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	537.2	7	1	5	6.36	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(Cl)cc4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940359	70161	None	0	Mouse	Binding	IC50	=	74.00	7.13	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	538.2	7	1	6	5.76	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4cccc(Cl)n4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940360	70163	None	0	Mouse	Binding	IC50	=	18.00	7.75	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	518.3	7	1	6	5.41	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(C)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940362	70165	None	0	Mouse	Binding	IC50	=	1140.00	5.94	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	534.3	8	1	7	5.11	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(OC)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940363	70166	None	0	Mouse	Binding	IC50	=	194.00	6.71	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	529.3	7	1	7	4.97	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(C#N)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940364	70167	None	0	Mouse	Binding	IC50	=	14.00	7.85	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	510.2	7	1	7	5.17	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4nccs4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940365	70168	None	0	Mouse	Binding	IC50	=	42.00	7.38	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	588.1	7	1	7	5.93	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4ncc(Br)s4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940366	70169	None	0	Mouse	Binding	IC50	=	4.50	8.35	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	579.2	7	1	8	5.58	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4nnc(C(F)(F)F)s4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940367	70170	None	0	Mouse	Binding	IC50	=	2.80	8.55	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	560.2	7	1	7	6.32	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4nc5ccccc5s4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940368	70171	None	0	Mouse	Binding	IC50	=	8.30	8.08	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	544.3	7	1	7	5.85	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4nc5ccccc5o4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940369	70172	None	0	Mouse	Binding	IC50	=	4.50	8.35	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	543.3	7	2	6	5.58	COc1ccc([C@@H](C)N[C@@H]2CC[C@H](C(=O)N3CCN(c4nc5ccccc5[nH]4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940370	70173	None	0	Mouse	Binding	IC50	=	1525.00	5.82	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	524.2	7	1	6	5.20	COc1ccc(CN[C@@H]2CC[C@H](C(=O)N3CCN(c4ccc(Cl)cn4)CC3)[C@@H](c3ccsc3)C2)cc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126
CHEMBL1940371	70174	None	0	Mouse	Binding	IC50	=	217.00	6.66	-	1	Displacement of [125]-hNPW23 from mouse NPBWR1 expressed in CHO-K1 cells membrane by scintillation proximity assay	ChEMBL	508.2	6	1	5	5.75	C[C@@H](N[C@@H]1CC[C@H](C(=O)N2CCN(c3ccc(Cl)cn3)CC2)[C@@H](c2ccsc2)C1)c1ccccc1	https://dx.doi.org/10.1016/j.bmcl.2011.11.126

Showing 1 to 20 of 118 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

CHEMBL1164334	10462	None	13	Human	Functional	IC50	=	1200.00	5.92	-	1	Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ChEMBL	262.1	1	1	1	4.25	FC(F)(F)c1ccc2[nH]c(-c3ccccc3)nc2c1	https://dx.doi.org/10.1016/j.bmcl.2020.127510
CHEMBL1164403	10463	None	46	Human	Functional	IC50	=	10000.00	5.00	-	1	Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ChEMBL	239.1	2	1	3	3.14	O=[N+]([O-])c1ccc2[nH]c(-c3ccccc3)nc2c1	https://dx.doi.org/10.1016/j.bmcl.2020.127510
CHEMBL1311692	21031	None	15	Human	Functional	IC50	=	7020.00	5.15	1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	432.1	6	0	6	2.05	COc1cc(OC)c(S(=O)(=O)N2CCCCC2)cc1S(=O)(=O)N1CCCCC1	-
CHEMBL1312413	21135	None	1	Human	Functional	IC50	=	5577.00	5.25	3	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	353.1	3	2	5	4.22	CCc1ccc(C2CC(c3ccccc3Cl)Nc3nc(N)nn32)cc1	-
CHEMBL1319565	21834	None	5	Human	Functional	IC50	=	10262.00	4.99	1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	421.3	9	1	5	4.04	CCN(CC)CCNC(=O)CCc1c(C)nc2c(c(C)nn2-c2ccc(C)cc2)c1C	-
CHEMBL1332346	23337	None	0	Human	Functional	IC50	=	16295.00	4.79	-1	3	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	579.3	7	0	5	4.94	COC(=O)[C@@]1(Cc2ccc(F)cc2)[C@H]2c3cc(C(=O)N(C)C)n(Cc4ccccc4)c3C[C@H]2CN1C(=O)c1ccccc1	-
CHEMBL1335685	23771	None	0	Human	Functional	IC50	=	10642.00	4.97	1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	461.2	7	1	6	4.30	COCCNC1=N[C@@H](c2cccc(C(F)(F)F)c2)C(C(=O)OC)=C(C)N1Cc1ccccc1	-
CHEMBL1335692	23776	None	4	Human	Functional	IC50	=	34598.00	4.46	-1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	391.2	6	2	3	3.34	CC(C)Cc1cc(C(=O)N2CCCC(CO)(Cc3ccc(F)cc3F)C2)[nH]n1	-
CHEMBL1336601	23879	None	11	Human	Functional	IC50	=	19005.00	4.72	1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	413.1	8	1	5	4.05	COc1ccnc(Oc2ccc(F)cc2)c1C(=O)N=CNOCc1ccc(F)cc1	-
CHEMBL1339046	24153	None	1	Human	Functional	IC50	=	23855.00	4.62	-	1	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	395.2	4	0	4	3.88	CCN1CCN(C(=O)c2ccc3c(c2)N(Cc2ccc(C)cc2)CCS3)CC1	-
CHEMBL1344766	24815	None	6	Human	Functional	IC50	=	28272.00	4.55	-1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	385.2	4	1	6	3.33	OC1(c2ccc(F)cc2)CC2CCC(C1)N2Cc1nnnn1C1CCCCC1	-
CHEMBL1350024	25432	None	5	Human	Functional	IC50	=	6453.00	5.19	2	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	539.1	7	1	5	5.24	O=C(NCCCN1CCOCC1)c1ccc2c(c1)N(Cc1c(F)cccc1Cl)C(=O)c1ccccc1S2	-
CHEMBL1351920	25653	None	14	Human	Functional	IC50	=	29406.00	4.53	-	1	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	280.1	2	0	4	3.32	Cc1cc(=O)oc2cc(OC(=O)c3ccccc3)ccc12	-
CHEMBL1353612	25888	None	4	Human	Functional	IC50	=	22456.00	4.65	-1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	379.2	8	1	6	4.14	CCn1c(CNc2ccc(Cl)cc2)nnc1SCCN1CCCCC1	-
CHEMBL1358809	26328	None	5	Human	Functional	IC50	=	13894.00	4.86	1	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	425.0	5	5	5	1.57	N=C(N)NS(=O)(=O)c1ccc(NC(=S)NC(=O)Cc2ccc(Cl)cc2)cc1	-
CHEMBL1359426	26412	None	6	Human	Functional	IC50	=	5862.00	5.23	2	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	460.1	7	2	6	4.30	COc1cc(/C=C(\C#N)C(=O)Nc2ccc(C(=O)O)cc2)ccc1OC(=O)c1cccc(F)c1	-
CHEMBL1370401	27735	None	9	Human	Functional	IC50	=	12540.00	4.90	-	1	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	393.2	3	1	3	4.43	Cc1ccc(C2C3=C(NCCN=C3c3ccccc3)C(=O)N2c2ccccc2)cc1	-
CHEMBL1381596	29157	None	12	Human	Functional	IC50	=	3600.00	5.44	3	2	Antagonist activity at human NPBWR1 expressed in HEK293T cells co-expressing Galphaqi3 assessed as calcium release after 15 mins by FLIPR assay assay	ChEMBL	346.1	4	0	5	3.83	COc1ccc(Oc2c(Cl)cnn(-c3ccc(F)cc3)c2=O)cc1	https://dx.doi.org/10.1016/j.bmcl.2012.09.074
CHEMBL1382150	29210	None	3	Human	Functional	IC50	=	5295.00	5.28	5	2	PUBCHEM_BIOASSAY: Fluorescence-based dose response cell-based high throughput screening assay to identify antagonists of the G-protein coupled receptor 7 (GPR7). (Class of assay: confirmatory) [Related pubchem assays: 1952 (Screening assay (GPR7 antagonists).), 1880 (Summary AID.)]	ChEMBL	485.2	7	1	7	3.30	Cc1ccc(-n2c(SCC(N)=O)nnc2-c2ccc(S(=O)(=O)N3CCCCC3)cc2)c(C)c1	-
CHEMBL1407741	31989	None	39	Human	Functional	IC50	=	2687.00	5.57	-	1	Antagonist activity at human NPBWR1 assessed as inhibition of agonist-induced cAMP accumulation by cAMP assay	ChEMBL	273.0	2	1	3	3.79	O=[N+]([O-])c1ccc2[nH]c(-c3ccc(Cl)cc3)nc2c1	https://dx.doi.org/10.1016/j.bmcl.2020.127510

Showing 1 to 20 of 327 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)