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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

CHEMBL3403768	118057	None	0	Human	Binding	EC50	=	195.00	6.71	-	1	Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay	ChEMBL	369.2	10	2	3	4.46	CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL3403768	118057	None	0	Human	Binding	Ki	=	612.00	6.21	-	1	Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay	ChEMBL	369.2	10	2	3	4.46	CCCC(C)COc1ccc([C@H](CO)NC(=O)[C@@H](C)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL3403780	118066	None	0	Human	Binding	EC50	=	304.00	6.52	-	2	Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay	ChEMBL	368.2	10	2	3	4.42	CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL3403780	118066	None	0	Human	Binding	Ki	=	219.00	6.66	-	2	Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay	ChEMBL	368.2	10	2	3	4.42	CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL3403780	118066	None	0	Mouse	Binding	EC50	=	940.00	6.03	-	2	Agonist activity at GPR88 in mouse striatal membranes assessed as increase in [35S]-GTP-gammaS binding	ChEMBL	368.2	10	2	3	4.42	CCCC(C)COc1ccc([C@H](CN)NC(=O)[C@@H](C)c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmc.2016.11.058
CHEMBL5285428	194406	None	3	Human	Binding	EC50	=	1738.00	5.76	-	1	Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay	ChEMBL	455.3	10	1	3	6.21	CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL5285428	194406	None	3	Human	Binding	Ki	=	487.00	6.31	-	1	Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay	ChEMBL	455.3	10	1	3	6.21	CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
CHEMBL5499810	197511	None	0	Human	Binding	EC50	=	10000.00	5.00	-	1	Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@H]3C[C@@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.2c01983
CHEMBL5500144	197560	None	0	Human	Binding	EC50	=	9841.00	5.01	-	1	Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay	ChEMBL	491.3	10	1	5	5.17	CO[C@H](C)[C@H](N)CN(C(=O)[C@H]1C[C@@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.2c01983
compound 2 [PMID: 24793972]	1064	None	6	Human	Binding	Ki	=	277.00	6.56	-	2	Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay	ChEMBL	455.3	10	1	3	6.21	CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
compound 2 [PMID: 24793972]	1064	None	6	Human	Binding	EC50	=	74.00	7.13	-	2	Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay	ChEMBL	455.3	10	1	3	6.21	CCCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)CC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
RTI-122	3411	None	1	Human	Binding	EC50	=	11.50	7.94	-	2	Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay	ChEMBL	491.3	10	1	5	5.17	CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.2c01983
RTI-122	3411	None	1	Mouse	Binding	EC50	=	155.00	6.81	-	2	Displacement of [35S]GTPgammaS from mouse striatal membrane GPR88 incubated for 60 mins by radioligand binding assay	ChEMBL	491.3	10	1	5	5.17	CO[C@H](C)[C@H](N)CN(C(=O)[C@@H]1C[C@H]1c1ccc(F)cn1)c1ccc(-c2ccc(OC(C)C)cc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.2c01983
RTI-13951-33	3412	None	10	Human	Binding	EC50	=	64.70	7.19	-3	3	Displacement of [35S]GTPgammaS from PPLS-HA tagged human GPR88 overexpressed in CHO cells membrane incubated for 60 mins radioligand binding assay	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1021/acs.jmedchem.2c01983
RTI-13951-33	3412	None	10	Human	Binding	Ki	=	224.00	6.65	-3	3	Displacement of [3H]RTI-33 from GPR88 (unknown origin) by competition binding assay	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
RTI-13951-33	3412	None	10	Human	Binding	EC50	=	45.00	7.35	-3	3	Agonist activity at GPR88 (unknown origin) transfected in HEK293 cells assessed as cAMP level by GloSensor cAMP assay	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
RTI-13951-33	3412	None	10	Human	Binding	Kd	=	85.00	7.07	-3	3	Binding affinity to PPLS-HA tagged human GPR88 expressed in CHO cell membrane by filtration method	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120
RTI-13951-33	3412	None	10	Mouse	Binding	Kd	=	41.00	7.39	3	3	Binding affinity to GPR88 in mouse striatal membrane by filtration method	ChEMBL	459.3	10	1	5	4.39	COCc1ccc(-c2ccc(N(C[C@@H](N)[C@@H](C)OC)C(=O)[C@@H]3C[C@H]3c3ccccn3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2022.129120

Showing 1 to 18 of 18 entries

	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

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Ligand source activities (1 row/activity)