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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

β³-tetrapeptide	621	None	0	Human	Binding	pKd	=	-	7.55	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12595949
β³-tetrapeptide	621	None	0	Mouse	Binding	pKd	=	-	7.35	-1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12595949
1-(benzo[d]thiazol-2-yl)-N-(3-ethoxy-4-methoxyphenyl)piperidin-4-amine	220110	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-1	3	-	PDSP KiDatabase	383.2	6	1	6	4.78	CCOc1cc(NC2CCN(c3nc4ccccc4s3)CC2)ccc1OC	-
1-(benzo[d]thiazol-2-ylmethyl)-N-(3-ethoxy-4-methoxyphenyl)piperidin-4-amine	220111	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-1	3	-	PDSP KiDatabase	397.2	7	1	6	4.78	CCOc1cc(NC2CCN(Cc3nc4ccccc4s3)CC2)ccc1OC	-
2-(4-((4-(benzo[d]oxazol-2-ylamino)piperidin-1-yl)methyl)-2-ethoxy-5-fluorophenoxy)ethanol	220122	UNDEFINED	0	Human	Binding	pKi	=	10000.00	5.00	-1	3	-	PDSP KiDatabase	429.2	9	2	7	3.81	CCOc1cc(CN2CCC(Nc3nc4ccccc4o3)CC2)c(F)cc1OCCO	-
[D-Tyr⁸]CYN 154806	1506	None	0	Human	Binding	pKi	=	-	5.90	-398	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12616335
[L-Tyr⁸]CYN 154806	2375	None	0	Human	Binding	pKi	None	-	6.35	-79	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12616335
astemizole	505	UNDEFINED	55	Human	Binding	pKi	=	10000.00	5.00	-5754	48	-	PDSP KiDatabase	458.2	8	1	5	5.35	COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	-
BIM 23052	642	None	0	Human	Binding	pKi	=	-	8.40	-4	9	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9650799
BIM 23068	648	None	0	Human	Binding	pKi	=	-	8.00	-6	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7988476
BIM 23268	218833	UNDEFINED	0	Human	Binding	pKi	=	16.30	7.79	-57	9	-	PDSP KiDatabase	1077.5	14	12	13	0.55	CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O	-
BIM 23268	218833	125I-SOMATOSTATIN	0	Human	Binding	pKi	=	174.00	6.76	-57	9	-	PDSP KiDatabase	1077.5	14	12	13	0.55	CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O	-
BIM 23268	218833	125I-Tyr11-somatostatin-14	0	Human	Binding	pKi	=	16.30	7.79	-57	9	-	PDSP KiDatabase	1077.5	14	12	13	0.55	CC(O)C1NC(=O)C(CCCCN)NC(=O)C(Cc2c[nH]c3ccccc23)NC(=O)C(Cc2ccccc2)NC(=O)C(Cc2ccccc2)NC(=O)C(N)CSSCC(C(N)=O)NC(=O)C(Cc2ccccc2)NC1=O	-
BIM 23295	652	None	0	Human	Binding	pKi	=	-	8.50	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9600011
BN-81,644	697	None	5	Human	Binding	Ki	=	7100.00	5.15	-11220	4	Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype	ChEMBL	426.3	8	3	2	7.02	CCCCC1(CCCC)N[C@@H](c2ncc(-c3ccccc3)[nH]2)Cc2c1[nH]c1ccccc21	https://dx.doi.org/10.1021/jm0108449
CGP 23996	891	None	0	Human	Binding	pKi	=	-	8.70	-2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9650799
CGP 23996	891	None	0	Human	Binding	pKi	=	-	8.70	-2	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10598788
CHEMBL103769	4750	None	24	Human	Binding	Ki	=	6.00	8.22	4	29	Inhibition of [125 I -Tyr]SRIF-14 binding to membranes isolated from CHO-K1 cells expressing cloned human SRIF receptor (sst-4) subtype	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.1021/jm0108449
CHEMBL103769	4750	None	24	Human	Binding	Ki	=	6.00	8.22	4	29	Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in BHK cell membranes after 30 to 90 mins by gamma counting method	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.1039/C8MD00388B
CHEMBL103769	4750	None	24	Human	Binding	Ki	=	148.00	6.83	4	29	Displacement of [125I]-Tyr-SRIF from recombinant human SST4 receptor expressed in CHOK1 cell membranes after 90 mins by gamma counting method	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.1039/C8MD00388B

Showing 1 to 20 of 811 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

analog 32 [PMID:18543899]	410	None	0	Human	Functional	pIC50	=	-	6.34	-380	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/18543899
BIM 23052	642	None	0	Rat	Functional	pIC50	=	-	8.10	-19	9	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9166718
BIM 23454	654	None	0	Human	Functional	pIC50	None	-	6.50	-10	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11897676
BIM 23627	655	None	0	Human	Functional	pIC50	=	-	6.40	-63	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11897676
cefapirin	220190	None	0	Human	Functional	pIC50	=	5.17	8.29	-1	14	None	Drug Central	423.1	7	2	8	0.47	CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)CSc3ccncc3)[C@H]2SC1	-
cefonicid	220188	None	0	Human	Functional	pIC50	=	4.24	8.37	-	1	None	Drug Central	542.0	9	4	12	-0.92	O=C(O)C1=C(CSc2nnnn2CS(=O)(=O)O)CS[C@@H]2[C@H](NC(=O)[C@H](O)c3ccccc3)C(=O)N12	-
CEPHALOTHIN	205166	None	47	Human	Functional	pIC50	=	4.40	8.36	7244	2	None	Drug Central	396.0	6	2	7	0.59	CC(=O)OCC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)Cc3cccs3)[C@H]2SC1	-
CEPHRADINE	53808	None	48	Human	Functional	pIC50	=	4.30	8.37	6309	2	None	Drug Central	349.1	4	3	5	0.35	CC1=C(C(=O)O)N2C(=O)[C@@H](NC(=O)[C@H](N)C3=CCC=CC3)[C@H]2SC1	-
CHEMBL103769	4750	None	24	Human	Functional	EC50	=	27.91	7.55	89	29	Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay	ChEMBL	554.0	11	3	4	5.37	S=C(NCCCc1c[nH]cn1)NCCCN(Cc1ccc(Cl)c(Cl)c1)c1ccc(Br)cn1	https://dx.doi.org/10.1039/C8MD00388B
CHEMBL3421842	118883	None	0	Human	Functional	EC50	=	0.40	9.40	-	2	Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ChEMBL	309.2	3	2	3	2.36	Cc1cc2ccccc2c(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)n1	https://dx.doi.org/10.1021/ml500538a
CHEMBL3421843	118884	None	3	Human	Functional	EC50	=	0.40	9.40	-	2	Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ChEMBL	298.2	3	2	4	1.39	Cn1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc21	https://dx.doi.org/10.1021/ml500538a
CHEMBL3421844	118885	None	0	Human	Functional	EC50	=	1.20	8.92	-	1	Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ChEMBL	303.1	3	2	4	1.78	CC(C)(NC(=O)[C@@H]1[C@H]2CNC[C@H]21)c1noc2c(F)cccc12	https://dx.doi.org/10.1021/ml500538a
CHEMBL3421845	118886	None	0	Human	Functional	EC50	=	4.30	8.37	-	2	Agonist activity at human somatostatin 4 receptor expressed in H4 cells assessed as inhibition of forskolin-induced intracellular cAMP accumulation incubated for 60 mins by time-resolved fluorescence assay	ChEMBL	310.2	3	2	4	1.75	Cc1nc(C(C)(C)NC(=O)[C@@H]2[C@H]3CNC[C@H]32)c2ccccc2n1	https://dx.doi.org/10.1021/ml500538a
CHEMBL4462793	171523	None	0	Human	Functional	EC50	=	6.80	8.17	-	3	Agonist activity at recombinant human SST4 receptor expressed in CHOK1 cell membranes assessed as inhibition of forskolin-stimulated cAMP accumulation measured after 2.5 to 20 hrs by TR-FRET assay	ChEMBL	478.1	9	2	4	5.80	Clc1ccc(Cc2nnc(CCc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)cc1Cl	https://dx.doi.org/10.1039/C8MD00388B
CHEMBL5171935	190151	None	0	Human	Functional	EC50	=	3.30	8.48	-	2	Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ChEMBL	474.2	9	2	6	3.70	CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4ccccc34)n2CCCc2c[nH]cn2)c1	https://dx.doi.org/10.1039/D1MD00044F
CHEMBL5172730	190192	None	0	Human	Functional	EC50	=	401.90	6.40	-	1	Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ChEMBL	306.2	6	2	4	2.71	c1ccc2c(Cc3nncn3CCCc3c[nH]cn3)c[nH]c2c1	https://dx.doi.org/10.1039/D1MD00044F
CHEMBL5172814	190201	None	0	Human	Functional	EC50	=	2.50	8.60	-	2	Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ChEMBL	492.2	9	2	6	3.84	CS(=O)(=O)c1cccc(Cc2nnc(Cc3c[nH]c4cc(F)ccc34)n2CCCc2c[nH]cn2)c1	https://dx.doi.org/10.1039/D1MD00044F
CHEMBL5173784	190267	None	0	Human	Functional	EC50	=	2.20	8.66	-	2	Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ChEMBL	482.1	8	2	4	5.74	Fc1ccc2c(Cc3nnc(Cc4cc(Cl)cc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1	https://dx.doi.org/10.1039/D1MD00044F
CHEMBL5174433	190311	None	0	Human	Functional	EC50	=	3.98	8.40	-16	5	Agonist activity at human SST4	ChEMBL	430.2	3	2	5	4.29	Cc1ccc(F)c2[nH]c(-c3cncc(-c4cc(F)cc(C#N)c4)c3N3CC[C@H](N)C3)nc12	https://dx.doi.org/10.1016/j.bmcl.2022.128807
CHEMBL5174969	190342	None	0	Human	Functional	EC50	=	0.80	9.10	-	2	Agonist activity at recombinant human SST4 receptor expressed in CHO-K1 cells assessed as inhibition of forskolin-stimulated cAMP production measured after 2.5 to 20 hrs in presence of 3-isobutyl-1-methylxanthine by TR-FRET LANCE assay	ChEMBL	448.2	8	2	4	5.09	Fc1ccc2c(Cc3nnc(Cc4cccc(Cl)c4)n3CCCc3c[nH]cn3)c[nH]c2c1	https://dx.doi.org/10.1039/D1MD00044F

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Ligand source activities (1 row/activity)