GPCRdb

Ligand source activities (1 row/activity)

Affinity
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

5-(N,N-hexamethylene)-amiloride	147	3H-CCK8	37	Rat	Binding	pKi	=	10000.00	5.00	-162	20	-	PDSP KiDatabase	311.1	2	3	5	0.51	NC(N)=NC(=O)c1nc(Cl)c(N2CCCCCC2)nc1N	-
A-71623	207	None	26	Rat	Binding	Ki	=	250.00	6.60	-831	3	Binding affinity towards Cholecystokinin type B receptor in rat cortex synaptosomes using [125I]BH-CCK-8 as radioligand	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm990252e
ABT-594	219818	3H-Devazepide	0	Human	Binding	pKi	=	1000.00	6.00	-2	37	-	PDSP KiDatabase	198.1	3	1	3	1.48	Clc1ccc(OCC2CCN2)cn1	-
AG-041R	306	None	0	Human	Binding	pKi	None	-	8.30	-	1	Unclassified	Guide to Pharmacology	544.3	11	3	5	5.09	CCOC(CN1C(=O)[C@](CC(=O)Nc2ccc(C)cc2)(NC(=O)Nc2ccc(C)cc2)c2ccccc21)OCC	https://pubmed.ncbi.nlm.nih.gov/11738246
AMILORIDE	209968	3H-CCK8	39	Rat	Binding	pKi	=	10000.00	5.00	-7	22	-	PDSP KiDatabase	229.0	1	5	6	-1.08	N=C(N)NC(=O)c1nc(Cl)c(N)nc1N	-
ANETHOLTRITHION	63103	None	64	Human	Binding	AC50	=	5300.10	5.28	-	10	Binding affinity towards human CCKBR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	240.0	2	0	4	4.21	COc1ccc(-c2cc(=S)ss2)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
apomorphine	445	None	20	Human	Binding	AC50	=	23400.20	4.63	-	29	Binding affinity towards human CCKBR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	267.1	0	2	3	2.85	CN1CCc2cccc3c2[C@H]1Cc1ccc(O)c(O)c1-3	https://dx.doi.org/10.1038/s41467-023-40064-9
ARL-15849	472	None	0	Rat	Binding	pKi	None	-	6.60	-7943	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/9476993
ASENAPINE	107587	3H-CCK8	16	Rat	Binding	pKi	=	1000.00	6.00	-5888	54	-	PDSP KiDatabase	285.1	0	0	2	4.26	CN1CC2c3ccccc3Oc3ccc(Cl)cc3C2C1	-
ATOMOXETINE	205585	UNDEFINED	33	Mouse	Binding	pKi	=	1000.00	6.00	-1	37	-	PDSP KiDatabase	255.2	6	1	2	3.73	CNCC[C@@H](Oc1ccccc1C)c1ccccc1	-
AZLOCILLIN	46456	None	38	Human	Binding	AC50	=	12999.90	4.89	-	1	Binding affinity towards human CCKBR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	461.1	5	4	6	0.09	CC1(C)S[C@@H]2[C@H](NC(=O)[C@H](NC(=O)N3CCNC3=O)c3ccccc3)C(=O)N2[C@H]1C(=O)O	https://dx.doi.org/10.1038/s41467-023-40064-9
BBL-454	590	None	0	Rat	Binding	pKi	None	-	8.60	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/14698161
BC-254	591	None	0	Rat	Binding	pKi	None	-	7.40	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/1614411
BCTC	218979	3H-CCK8	0	Rat	Binding	pKi	=	10000.00	5.00	-10471285	17	-	PDSP KiDatabase	372.2	2	1	3	4.39	CC(C)(C)c1ccc(NC(=O)N2CCN(c3ncccc3Cl)CC2)cc1	-
BENZAMIL	79975	3H-CCK8	30	Rat	Binding	pKi	=	10000.00	5.00	-15	17	-	PDSP KiDatabase	319.1	3	4	5	0.54	N/C(=N\C(=O)c1nc(Cl)c(N)nc1N)NCc1ccccc1	-
CANDESARTAN CILEXETIL	4402	None	68	Human	Binding	AC50	=	31029.90	4.51	-	29	Binding affinity towards human CCKBR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	610.3	10	1	11	6.32	CCOc1nc2cccc(C(=O)OC(C)OC(=O)OC3CCCCC3)c2n1Cc1ccc(-c2ccccc2-c2nn[nH]n2)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
CCK-33	815	125I-CCK	0	Rat	Binding	pKi	=	1.65	8.78	-3	4	-	PDSP KiDatabase	-	-	-	-	-	-	-
CCK-8	822	None	42	Human	Binding	pKi	=	9.55	8.02	-1	6	Tested for the inhibition of [3H]pCCK-8 binding to Cholecystokinin type B receptor in guinea pig brain	Drug Central	-	-	-	-	-	-	-
CCK-8	822	None	42	Human	Binding	Ki	=	0.64	9.19	-1	6	Inhibition of [3H]pCCK-8 binding to Guinea pig cortex membrane Cholecystokinin type B receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm9603072
CCK-8	822	None	42	Human	Binding	IC50	=	0.35	9.46	-1	6	In vitro for binding affinity against human cholecystokinin type B receptor.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm970265x

Showing 1 to 20 of 2,888 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

A-71378	206	None	0	Human	Functional	pIC50	=	-	6.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8914862
BC-264	592	None	0	Rat	Functional	pIC50	None	-	9.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/14698161
CCK-33	815	None	0	Human	Functional	pIC50	None	-	8.80	-	4	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8349705
CCK-4	819	None	0	Human	Functional	pIC50	=	-	7.50	158	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8349705
CCK-58	821	None	0	Mouse	Functional	pIC50	=	-	9.50	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12370550
CCK-8	822	None	42	Human	Functional	EC50	=	26.92	7.57	-1	6	Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm050921q
CCK-8	822	None	42	Human	Functional	pIC50	None	-	9.95	-1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7681836
CCK-8	822	None	42	Human	Functional	pIC50	None	-	9.95	-1	6	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8349705
CCK-8	822	None	42	Human	Functional	EC50	=	27.00	7.57	-1	6	Antagonist activity at CCK2 receptor expressed in HEK293 cells assessed as accumulation of [3H]inositol phosphates by PI assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm050921q
CCK-8	822	None	42	Human	Functional	EC50	=	0.50	9.30	-1	6	Agonist activity at human CCK2R expressed in human 1321N1 cells assessed as IP1 accumulation after 1 hr by HTRF assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/acs.jmedchem.8b01558
CCK-8	822	None	42	Rat	Functional	EC50	=	0.63	9.20	-6	6	Effective concentration for the stimulation of Inositol Phosphate accumulation in CHO cells expressing wild-type Cholecystokinin type B receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm9603072
CCK-8	822	None	42	Rat	Functional	EC50	=	0.63	9.20	-6	6	Affinity against Cholecystokinin type B receptor expressed in CHO cells on rat brain.	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm0000416
CE-326597	876	None	4	Human	Functional	EC50	=	977.24	6.01	-2	3	Partial agonist activity at wild-type human CCK2R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis	ChEMBL	594.3	8	1	5	6.53	CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21	https://dx.doi.org/10.1021/acs.jmedchem.5b01110
CE-326597	876	None	4	Human	Functional	EC50	=	1000.00	6.00	-2	3	Partial agonist activity at wild-type human CCK2R expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis	ChEMBL	594.3	8	1	5	6.53	CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21	https://dx.doi.org/10.1021/acs.jmedchem.5b01110
CE-326597	876	None	4	Human	Functional	EC50	=	281.84	6.55	-2	3	Agonist activity at human CCK2R V6.51I, Y6.52F mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis	ChEMBL	594.3	8	1	5	6.53	CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21	https://dx.doi.org/10.1021/acs.jmedchem.5b01110
CE-326597	876	None	4	Human	Functional	EC50	=	58.88	7.23	-2	3	Agonist activity at human CCK2R H7.39L mutant expressed in CHO cells assessed as intracellular calcium response by fluorescence analysis	ChEMBL	594.3	8	1	5	6.53	CC(C)N(Cc1ccccc1)C(=O)CN1C(=O)[C@@H](Cc2c[nH]c3ccccc23)c2nnc(-c3ccccc3)n2-c2ccccc21	https://dx.doi.org/10.1021/acs.jmedchem.5b01110
CHEMBL100538	4264	None	0	Rat	Functional	EC50	=	1.50	8.82	-	2	Affinity against Cholecystokinin type B receptor expressed in CHO cells on rat brain.	ChEMBL	692.3	20	7	7	1.25	CCCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O)N(C)C(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCC(=O)O	https://dx.doi.org/10.1021/jm0000416
CHEMBL1076229	5491	None	0	Human	Functional	ED50	=	3.10	8.51	-	1	Agonist activity at human CCK2 receptor expressed in COS7 cells assessed as stimulation of [3H]inositol phosphate formation	ChEMBL	1259.5	33	13	12	5.41	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCNC(=O)CCNC(=S)Nc1ccc(O)c(NC(=O)CNC(=O)CSC(c2ccccc2)(c2ccccc2)c2ccccc2)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.ejmech.2009.09.043
CHEMBL1076230	5492	None	0	Human	Functional	ED50	=	84.54	7.07	-	1	Agonist activity at human CCK2 receptor expressed in COS7 cells assessed as stimulation of [3H]inositol phosphate formation	ChEMBL	1118.4	27	11	10	7.00	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=S)Nc1ccc(O)c(NC(=O)CNC(=O)CSC(c2ccccc2)(c2ccccc2)c2ccccc2)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(=O)O	https://dx.doi.org/10.1016/j.ejmech.2009.09.043
CHEMBL1076232	5493	None	0	Human	Functional	ED50	=	5.01	8.30	-	1	Agonist activity at human CCK2 receptor expressed in COS7 cells assessed as stimulation of [3H]inositol phosphate formation	ChEMBL	1343.6	39	13	12	7.75	CCCC[C@H](NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)CCCCCNC(=O)CCCCCNC(=S)Nc1ccc(O)c(NC(=O)CNC(=O)CSC(c2ccccc2)(c2ccccc2)c2ccccc2)c1)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O	https://dx.doi.org/10.1016/j.ejmech.2009.09.043

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Ligand source activities (1 row/activity)