GPCRdb

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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

	[(CH₂NH)^4,5]secretin	924	None	0	Human	Binding	pKi	=	-	5.30	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/1702423
	[Arg¹⁶]chicken secretin	468	None	0	Rat	Binding	pIC50	=	-	7.70	-	7	Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
	CHEMBL1256314	211124	None	0	Human	Binding	Ki	=	11.00	7.96	-	1	Displacement of [125I]-secretin-27 from secretin receptor expressed in CHO cells by gamma-spectrometer analysis	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N[C@H](C(N)=O)C(C)C	https://dx.doi.org/10.1016/j.bmcl.2010.08.062
	SECRETIN	213407	None	12	Human	Binding	Ki	=	3.50	8.46	-	1	Displacement of [125I]-secretin-27 from secretin receptor expressed in CHO cells by gamma-spectrometer analysis	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@H](C(N)=O)C(C)C	https://dx.doi.org/10.1016/j.bmcl.2010.08.062
	secretin	3572	None	0	Rat	Binding	pKi	=	-	8.50	3162	7	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/1646711
	secretin	3572	None	0	Rat	Binding	pIC50	=	-	9.00	3162	7	Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714
	secretin	3573	None	0	Rat	Binding	pKi	=	-	8.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10383421
	secretin	3573	None	0	Rat	Binding	pKi	=	-	8.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9694908
	VIP	3995	None	15	Rat	Binding	pIC50	=	-	6.20	-	8	Inhibition of [125I]Tyr25 secretin binding in membranes from CHO cells expressing recombinant receptor	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9437714

Showing 1 to 9 of 9 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

	CHEMBL1256314	211124	None	0	Human	Functional	EC50	=	0.10	10.00	-	1	Agonist activity at secretin receptor expressed in CHO cells assessed as increase of cAMP level	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)[C@H](CO)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@@H]1CSSC[C@H](NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc2cnc[nH]2)[C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N1)C(=O)N[C@H](C(N)=O)C(C)C	https://dx.doi.org/10.1016/j.bmcl.2010.08.062
	CHEMBL5396976	195117	None	0	Human	Functional	EC50	=	78.10	7.11	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	563.3	7	2	8	7.16	O=C(O)c1cn(C2CCCCC2)c2nc(Oc3cccc4ccccc34)nc(Nc3ccc(N4CCOCC4)cc3)c12	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5404963	195503	None	0	Human	Functional	EC50	=	91.10	7.04	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	534.3	6	2	8	6.98	OC1CCN(c2ccc(Nc3nc(Oc4cccc5ccccc45)nc4c3ncn4C3CCCCC3)cc2)CC1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5408063	195651	None	0	Human	Functional	EC50	=	80.60	7.09	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	527.2	7	1	7	8.81	c1ccc(Oc2ccc(Nc3nc(Oc4cccc5ccccc45)nc4c3ncn4C3CCCCC3)cc2)cc1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5418444	196191	None	0	Human	Functional	EC50	=	80.20	7.10	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	536.3	6	2	9	6.56	Oc1ccc2c(Oc3nc(Nc4ccc(N5CCOCC5)cc4)c4ncn(C5CCCCC5)c4n3)cccc2c1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5423791	196427	None	0	Human	Functional	EC50	=	80.20	7.10	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	536.3	6	2	9	6.56	Oc1cc(N2CCOCC2)ccc1Nc1nc(Oc2cccc3ccccc23)nc2c1ncn2C1CCCCC1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5429270	196665	None	0	Human	Functional	EC50	=	84.40	7.07	-	1	Positive allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	536.3	6	2	9	5.83	O[C@@H]1CCC[C@H](n2cnc3c(Nc4ccc(N5CCOCC5)cc4)nc(Oc4cccc5ccccc45)nc32)C1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5432045	196778	None	0	Human	Functional	EC50	=	87.50	7.06	-	1	Negative allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as decrease in SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	511.2	6	1	6	8.69	c1ccc(-c2ccc(Nc3nc(Oc4cccc5ccccc45)nc4c3ncn4C3CCCCC3)cc2)cc1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	CHEMBL5434238	196888	None	0	Human	Functional	EC50	=	79.10	7.10	-	1	Negative allosteric modulation of SCTR (unknown origin) overexpressed in CHO cells assessed as decrease in SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins by Lance cAMP assay	ChEMBL	561.3	6	1	6	9.84	c1ccc2c(Oc3nc(Nc4ccc(-c5cccc6ccccc56)cc4)c4ncn(C5CCCCC5)c4n3)cccc2c1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	purmorphamine	3236	None	58	Human	Functional	EC50	=	68.08	7.17	12	3	Positive allosteric modulation of SCTR (unknown origin) expressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 1 uM incubated for 20 mins in presence of 1 uM SCT by Lance cAMP assay (Rvb = 7.77 +/- 0.116 No_unit)	ChEMBL	520.3	6	1	8	6.86	c1ccc2c(Oc3nc(Nc4ccc(N5CCOCC5)cc4)c4ncn(C5CCCCC5)c4n3)cccc2c1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	purmorphamine	3236	None	58	Human	Functional	EC50	=	40.55	7.39	12	3	Positive allosteric modulation of SCTR (unknown origin) expressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 10 uM incubated for 20 mins in presence of 1 uM SCT by Lance cAMP assay (Rvb = 7.77 +/- 0.116 No_unit)	ChEMBL	520.3	6	1	8	6.86	c1ccc2c(Oc3nc(Nc4ccc(N5CCOCC5)cc4)c4ncn(C5CCCCC5)c4n3)cccc2c1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	purmorphamine	3236	None	58	Human	Functional	EC50	=	85.51	7.07	12	3	Positive allosteric modulation of SCTR (unknown origin) expressed in CHO cells assessed as potentiation of SCT-induced cAMP production by measuring secretin EC50 at 100 uM incubated for 20 mins in presence of 1 uM SCT by Lance cAMP assay (Rvb = 7.77 +/- 0.116 No_unit)	ChEMBL	520.3	6	1	8	6.86	c1ccc2c(Oc3nc(Nc4ccc(N5CCOCC5)cc4)c4ncn(C5CCCCC5)c4n3)cccc2c1	https://dx.doi.org/10.1016/j.ejmech.2022.114642
	secretin	3572	None	0	Human	Functional	pEC50	=	-	9.70	5	7	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7612008
	SECRETIN	213407	None	12	Human	Functional	EC50	=	0.08	10.10	-	1	Agonist activity at secretin receptor expressed in CHO cells assessed as increase of cAMP level	ChEMBL	-	-	-	-	-	CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@H](C(N)=O)C(C)C	https://dx.doi.org/10.1016/j.bmcl.2010.08.062
	SECRETIN	213407	None	12	Human	Functional	pEC50	=	9.70	8.01	-	1	None	Drug Central	-	-	-	-	-	CC(C)C[C@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](C)NC(=O)CNC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)Cc1cnc[nH]1)[C@@H](C)O)[C@@H](C)O)C(=O)N[C@H](C(N)=O)C(C)C	-
	secretin-(5-27) (pig)	3575	None	0	Rat	Functional	pIC50	None	-	5.00	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/1646711
	VIP	3995	None	15	Human	Functional	pIC50	=	-	5.40	-3090	8	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/1646711

Showing 1 to 17 of 17 entries