GPCRdb

Finalizing display...

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

[Bpa¹,Ile¹³]motilin (human)	709	None	0	Human	Binding	pKi	None	-	7.90	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11461914
[D-Bpa⁵,Ile¹³]motilin (human)	3625	None	0	Human	Binding	pKi	None	-	6.40	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/15677347
[L-Bpa⁵,Ile¹³]motilin (human)	3628	None	0	Human	Binding	pKi	None	-	7.30	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/15677347
ACETOPHENAZINE	7074	None	25	Human	Binding	AC50	=	26999.80	4.57	-	16	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	411.2	7	1	6	3.49	CC(=O)c1ccc2c(c1)N(CCCN1CCN(CCO)CC1)c1ccccc1S2	https://dx.doi.org/10.1038/s41467-023-40064-9
amiodarone	398	None	47	Human	Binding	AC50	=	16000.00	4.80	-	40	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	645.0	11	0	4	6.94	CCCCc1oc2ccccc2c1C(=O)c1cc(I)c(OCCN(CC)CC)c(I)c1	https://dx.doi.org/10.1038/s41467-023-40064-9
AMPRENAVIR	10211	None	50	Human	Binding	AC50	=	7300.00	5.14	-	3	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	505.2	11	3	7	2.40	CC(C)CN(C[C@@H](O)[C@H](Cc1ccccc1)NC(=O)O[C@H]1CCOC1)S(=O)(=O)c1ccc(N)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
aripiprazole	470	None	70	Human	Binding	AC50	=	8338.70	5.08	-	60	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	447.1	7	1	4	4.86	O=C1CCc2ccc(OCCCCN3CCN(c4cccc(Cl)c4Cl)CC3)cc2N1	https://dx.doi.org/10.1038/s41467-023-40064-9
astemizole	505	None	55	Human	Binding	AC50	=	630.00	6.20	-	48	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	458.2	8	1	5	5.35	COc1ccc(CCN2CCC(Nc3nc4ccccc4n3Cc3ccc(F)cc3)CC2)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
ATAZANAVIR	10423	None	49	Human	Binding	AC50	=	6400.00	5.19	-	4	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	704.4	14	5	9	4.21	COC(=O)N[C@H](C(=O)N[C@@H](Cc1ccccc1)[C@@H](O)CN(Cc1ccc(-c2ccccn2)cc1)NC(=O)[C@@H](NC(=O)OC)C(C)(C)C)C(C)(C)C	https://dx.doi.org/10.1038/s41467-023-40064-9
AZELNIDIPINE	18563	None	62	Human	Binding	AC50	=	16000.00	4.80	-	6	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	582.2	9	2	9	4.69	CC1=C(C(=O)OC(C)C)C(c2cccc([N+](=O)[O-])c2)C(C(=O)OC2CN(C(c3ccccc3)c3ccccc3)C2)=C(N)N1	https://dx.doi.org/10.1038/s41467-023-40064-9
BAZEDOXIFENE	178724	None	43	Human	Binding	AC50	=	16000.00	4.80	-	19	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	470.3	7	2	5	6.33	Cc1c(-c2ccc(O)cc2)n(Cc2ccc(OCCN3CCCCCC3)cc2)c2ccc(O)cc12	https://dx.doi.org/10.1038/s41467-023-40064-9
BENIDIPINE	77126	None	16	Human	Binding	AC50	=	3500.00	5.46	-	11	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	505.2	7	1	8	4.21	COC(=O)C1=C(C)NC(C)=C(C(=O)OC2CCCN(Cc3ccccc3)C2)C1c1cccc([N+](=O)[O-])c1	https://dx.doi.org/10.1038/s41467-023-40064-9
benperidol	596	None	33	Human	Binding	AC50	=	25999.80	4.58	-	24	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	381.2	6	1	4	3.77	O=C(CCCN1CCC(n2c(=O)[nH]c3ccccc32)CC1)c1ccc(F)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
BENZETHONIUM	11852	None	18	Human	Binding	AC50	=	2700.00	5.57	-	35	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	412.3	11	0	2	6.07	CC(C)(C)CC(C)(C)c1ccc(OCCOCC[N+](C)(C)Cc2ccccc2)cc1	https://dx.doi.org/10.1038/s41467-023-40064-9
BEPRIDIL	4301	None	35	Human	Binding	AC50	=	20245.60	4.69	-	22	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	366.3	10	0	3	4.83	CC(C)COCC(CN(Cc1ccccc1)c1ccccc1)N1CCCC1	https://dx.doi.org/10.1038/s41467-023-40064-9
BOPINDOLOL	121354	None	36	Human	Binding	AC50	=	23000.10	4.64	-	12	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	380.2	7	2	4	4.47	Cc1cc2c(OCC(CNC(C)(C)C)OC(=O)c3ccccc3)cccc2[nH]1	https://dx.doi.org/10.1038/s41467-023-40064-9
CANDESARTAN CILEXETIL	4402	None	68	Human	Binding	AC50	=	21999.90	4.66	-	29	Binding affinity towards human MLNR 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
cannabidiol	788	None	26	Human	Binding	AC50	=	20493.90	4.69	-	23	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	314.2	6	2	2	5.85	C=C(C)[C@@H]1CCC(C)=C[C@H]1c1c(O)cc(CCCCC)cc1O	https://dx.doi.org/10.1038/s41467-023-40064-9
CAROVERINE	59901	None	35	Human	Binding	AC50	=	16800.00	4.78	-	13	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	365.2	8	0	5	3.34	CCN(CC)CCn1c(=O)c(Cc2ccc(OC)cc2)nc2ccccc21	https://dx.doi.org/10.1038/s41467-023-40064-9
carvedilol	803	None	59	Human	Binding	AC50	=	7606.10	5.12	-	35	Binding affinity towards human MLNR in an in vitro assay with cellular components measured by scintillation proximity assay	ChEMBL	406.2	10	3	5	3.74	COc1ccccc1OCCNCC(O)COc1cccc2[nH]c3ccccc3c12	https://dx.doi.org/10.1038/s41467-023-40064-9

Showing 1 to 20 of 255 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

3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A	201376	None	0	Rabbit	Functional	EC50	=	260.00	6.58	-	1	Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction	ChEMBL	763.5	8	6	14	2.36	CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@]1(C)O	https://dx.doi.org/10.1021/jm901107f
3 9-DIHYDRO-N-DESMETHYL-N-ISOPROPYLERYTHROMYCIN A	201376	None	0	Rabbit	Functional	EC50	=	260.00	6.58	-	1	Agonist activity at motilin receptor in rabbit smooth muscle assessed as maximal possible tissue contraction	ChEMBL	763.5	8	6	14	2.36	CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@]1(C)O	https://dx.doi.org/10.1016/j.bmcl.2011.04.078
[Leu¹³]motilin (human)	2299	None	0	Human	Functional	pIC50	None	-	9.00	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10381885
[nLeu¹³,Glu¹⁴]motilin (human)	2829	None	0	Human	Functional	pIC50	None	-	9.50	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10381885
[Phe³,Leu¹³]motilin (human)	3105	None	0	Human	Functional	pIC50	None	-	8.90	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10381885
alemcinal	341	None	0	Human	Functional	pIC50	=	-	7.20	-	1	Unclassified	Guide to Pharmacology	697.5	8	2	11	5.20	CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)C[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)CC)[C@H]2O)[C@@]2(C)CC(C)=C(O2)[C@H](C)[C@@H](O)[C@H]1C	https://pubmed.ncbi.nlm.nih.gov/15764739
azithromycin	561	None	43	Human	Functional	pEC50	=	-	5.50	60	3	Unclassified	Guide to Pharmacology	748.5	7	5	14	1.90	CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)CN(C)[C@H](C)[C@@H](O)[C@]1(C)O	https://pubmed.ncbi.nlm.nih.gov/23190027
azithromycin	561	None	43	Human	Functional	pEC50	=	5.50	8.26	60	3	None	Drug Central	748.5	7	5	14	1.90	CC[C@H]1OC(=O)[C@H](C)[C@@H](O[C@H]2C[C@@](C)(OC)[C@@H](O)[C@H](C)O2)[C@H](C)[C@@H](O[C@@H]2O[C@H](C)C[C@H](N(C)C)[C@H]2O)[C@](C)(O)C[C@@H](C)CN(C)[C@H](C)[C@@H](O)[C@]1(C)O	-
camicinal	785	None	28	Human	Functional	pEC50	=	-	7.90	-	1	Unclassified	Guide to Pharmacology	424.3	6	2	4	3.27	C[C@H]1CN(Cc2ccc(CC(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)CCN1	https://pubmed.ncbi.nlm.nih.gov/19374732
camicinal	785	None	28	Human	Functional	pEC50	=	-	7.90	-	1	Unclassified	Guide to Pharmacology	424.3	6	2	4	3.27	C[C@H]1CN(Cc2ccc(CC(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)CCN1	https://pubmed.ncbi.nlm.nih.gov/25341626
camicinal	785	None	28	Human	Functional	EC50	=	970.00	6.01	-	1	Agonist activity at human GPR38 expressed in COS-7 cells	ChEMBL	424.3	6	2	4	3.27	C[C@H]1CN(Cc2ccc(CC(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)CCN1	https://dx.doi.org/10.1016/j.bmcl.2022.128554
camicinal	785	None	28	Human	Functional	EC50	=	12.59	7.90	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay	ChEMBL	424.3	6	2	4	3.27	C[C@H]1CN(Cc2ccc(CC(=O)N3CCC(Nc4cccc(F)c4)CC3)cc2)CCN1	https://dx.doi.org/10.1021/jm801332q
CHEMBL1077735	5636	None	0	Human	Functional	EC50	=	501.19	6.30	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	387.2	4	1	6	1.58	O=S(=O)(Cc1ccc2c(c1)CCNCC2)c1ccc(N2CCOCC2)nc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1077736	5637	None	0	Human	Functional	EC50	=	125.89	6.90	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	357.2	6	1	3	3.69	CCCCc1ccc(S(=O)(=O)Cc2ccc3c(c2)CCNCC3)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1077991	5693	None	0	Human	Functional	EC50	=	25.12	7.60	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	413.1	4	1	3	4.29	O=S(=O)(Cc1ccc2c(c1)CCNCC2)c1ccc(-c2ccc(F)c(F)c2)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1078104	5709	None	0	Human	Functional	EC50	=	794.33	6.10	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	416.1	5	2	4	3.46	O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(Cl)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1078207	5713	None	0	Human	Functional	EC50	=	10.00	8.00	158	5	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	458.2	6	2	4	4.48	O=S(=O)(Nc1ccc2c(c1)CCN(Cc1cc[nH]n1)CC2)c1ccc(-c2ccccc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1078208	5714	None	0	Human	Functional	EC50	=	3.98	8.40	39	5	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	440.2	7	2	5	3.60	CC(C)Oc1ccc(S(=O)(=O)Nc2ccc3c(c2)CCN(Cc2cc[nH]n2)CC3)cc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1078267	5721	None	0	Human	Functional	EC50	=	7.94	8.10	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	412.1	4	1	4	4.06	O=S(=O)(Cc1ccc2c(c1)CCNCC2)c1ccc(-c2ccc(Cl)cc2)nc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027
CHEMBL1078268	5722	None	0	Human	Functional	EC50	=	5.01	8.30	-	1	Agonist activity at human recombinant motilin receptor expressed in CHO cells by FLIPR assay	ChEMBL	396.1	4	1	4	3.55	O=S(=O)(Cc1ccc2c(c1)CCNCC2)c1ccc(-c2ccc(F)cc2)nc1	https://dx.doi.org/10.1016/j.bmcl.2009.09.027

Showing 1 to 20 of 337 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)