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

[Phe³]OT	3106	None	0	Human	Binding	pKi	None	-	8.80	50	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7774575
[Phe³]OT	3106	None	0	Human	Binding	pKi	None	-	8.80	50	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8955347
[Thr⁴,Gly⁷]OT	3815	None	0	Human	Binding	pKi	=	-	8.30	44	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7475979
[Thr⁴,Gly⁷]OT	3815	None	0	Human	Binding	pKi	=	-	8.30	44	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8955347
[Thr⁴,Gly⁷]OT	3815	None	0	Human	Binding	pKi	=	-	8.30	44	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/2827511
[Thr⁴,Gly⁷]OT	3815	None	0	Human	Binding	pKi	=	-	8.30	44	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/23723434
arginine vasotocin	466	None	0	Human	Binding	pKi	=	-	9.40	7	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7774575
arginine vasotocin	466	None	0	Human	Binding	pKi	=	-	9.40	7	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/8955347
atosiban	518	None	30	Human	Binding	pKi	None	-	6.80	-46	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/10519430
atosiban	518	None	30	Human	Binding	pKi	None	-	6.80	-46	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12660315
atosiban	518	None	30	Human	Binding	pKi	None	-	6.80	-46	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/14722330
atosiban	518	None	30	Human	Binding	pKi	None	-	6.80	-46	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/15880385
atosiban	518	None	30	Human	Binding	pKi	None	-	6.80	-46	5	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/7475979
Atosiban	218972	3H-Oxytocin	0	Human	Binding	pKi	=	27.00	7.57	-4	5	-	PDSP KiDatabase	993.4	18	11	15	-3.04	CCOc1ccc(CC2NC(=O)CCSSCC(C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(C(C)O)NC(=O)C(C(C)CC)NC2=O)cc1	-
Atosiban	218972	None	0	Human	Binding	pKi	=	7.96	8.10	-4	5	Binding affinity to human oxytocin receptor	Drug Central	993.4	18	11	15	-3.04	CCOc1ccc(CC2NC(=O)CCSSCC(C(=O)N3CCCC3C(=O)NC(CCCN)C(=O)NCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(C(C)O)NC(=O)C(C(C)CC)NC2=O)cc1	-
atosiban	518	None	30	Human	Binding	Ki	=	397.00	6.40	-46	5	Binding affinity to oxytocin receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2008.11.064
atosiban	518	None	30	Human	Binding	Ki	=	32.00	7.50	-46	5	Binding affinity to recombinant oxytocin receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2007.11.008
atosiban	518	None	30	Human	Binding	Ki	=	11.00	7.96	-46	5	Binding affinity to human oxytocin receptor	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2007.11.008
atosiban	518	None	30	Human	Binding	Ki	=	39.81	7.40	-46	5	Displacement of [3H]oxytocin from human OTR	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm060073e
atosiban	518	None	30	Human	Binding	Ki	=	27.00	7.57	-46	5	Displacement of [125I]OVTA antagonist from human oxytocin receptor expressed in HEK293-EBNA cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm050645f

Showing 1 to 20 of 1,472 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

[Mpa¹,D-Tyr(Et)²,D-Tic⁷,Aib⁹]OT	2608	None	0	Human	Functional	pIC50	None	-	7.10	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17316912
[Mpa¹,D-Tyr(Et)²,D-Tic⁷,D-Tic⁹]OT	2610	None	0	Human	Functional	pIC50	None	-	7.60	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17316912
[Mpa¹,D-Tyr(Et)²,D-Tic⁷]OT	2609	None	0	Human	Functional	pIC50	None	-	7.30	-	1	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/17316912
atosiban	518	None	30	Human	Functional	IC50	=	372.00	6.43	-12	5	Antagonist activity at human OTR expressed in HEK293 cell membranes assessed as inhibition of OT-induced IP1 accumulation measured after 1 hr by fluorescence assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.ejmech.2017.05.013
atosiban	518	None	30	Human	Functional	IC50	=	59.00	7.23	-12	5	Inhibitory activity against human Oxytocin induced intracellular Calcium mobilization in human Oxytocin receptor transfected HEK293-EBNA cells	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1021/jm050645f
atosiban	518	None	30	Rat	Functional	Kd	=	5.13	8.29	1	5	Antagonist activity in rat uterus by uterotonic assay	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.ejmech.2006.12.016
atosiban	518	None	30	Rat	Functional	IC50	=	12.00	7.92	1	5	Antagonism of OT-induced response at OT receptor in rat uterine strips	ChEMBL	-	-	-	-	-	-	https://dx.doi.org/10.1016/j.bmcl.2005.10.107
carbetocin	797	None	33	Human	Functional	EC50	=	10.00	8.00	1	5	Agonist activity at human OTR receptor expressed in HEK293FT cells incubated for 30 mins by beta-arrestin recruitment assay	ChEMBL	-	-	-	-	-	CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.8b00697
carbetocin	797	None	33	Human	Functional	EC50	=	41.00	7.39	1	5	Agonist activity at human OTR receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay	ChEMBL	-	-	-	-	-	CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.8b00697
carbetocin	797	None	33	Human	Functional	pEC50	=	-	8.00	1	5	Agonist activity at hOT receptor receptor expressed in HEK293FT cells by beta-arrestin recruitment assay.	Guide to Pharmacology	-	-	-	-	-	CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O	https://pubmed.ncbi.nlm.nih.gov/30199637
carbetocin	797	None	33	Mouse	Functional	pEC50	=	-	7.21	-10	5	Agonist activity at MmOT receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay.	Guide to Pharmacology	-	-	-	-	-	CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O	https://pubmed.ncbi.nlm.nih.gov/30199637
carbetocin	797	None	33	Mouse	Functional	EC50	=	62.00	7.21	-10	5	Agonist activity at mouse OTR receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay	ChEMBL	-	-	-	-	-	CC[C@H](C)[C@@H]1NC(=O)[C@H](Cc2ccc(OC)cc2)NC(=O)CCCSC[C@@H](C(=O)N2CCC[C@H]2C(=O)N[C@@H](CC(C)C)C(=O)NCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCC(N)=O)NC1=O	https://dx.doi.org/10.1021/acs.jmedchem.8b00697
CHEMBL1077300	5605	None	0	Human	Functional	Ki	=	13.90	7.86	-	1	Antagonist activity at human oxytocin receptor expressed in CHO cells by beta lactamase assay	ChEMBL	359.2	5	0	4	3.25	CCN(C(=O)N1CC(Oc2cccc(F)c2C)C1)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.01.143
CHEMBL1088765	7694	None	0	Human	Functional	Ki	=	85.00	7.07	-	1	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	336.2	5	0	5	3.25	CCN(C(=O)c1cnn(-c2ccccc2)c1C)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1088766	7695	None	0	Human	Functional	Ki	=	98.00	7.01	-	1	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	366.2	7	0	6	2.88	COCCN(C(=O)c1cnn(-c2ccccc2)c1C)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1088767	7696	None	0	Human	Functional	Ki	=	91.00	7.04	-	1	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	366.2	6	0	6	3.26	CCN(C(=O)c1cnn(-c2ccc(OC)cc2)c1C)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1089025	7741	None	0	Human	Functional	Ki	=	129.00	6.89	-	2	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	348.2	5	0	5	3.52	CCN(C(=O)c1cnc(-c2ccccc2C)cn1)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1089026	7742	None	0	Human	Functional	Ki	=	150.00	6.82	-	1	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	362.2	5	0	5	3.91	COc1ccc(N(C(=O)c2cnc(-c3ccccc3C)cn2)C(C)C)cn1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1089272	7773	None	0	Human	Functional	Ki	=	48.00	7.32	-	1	Antagonist activity at human cloned OT receptor by cell based beta-lactamase reporter gene assay	ChEMBL	336.1	6	0	4	3.67	CCN(C(=O)COc1ccc2ccccc2c1)c1ccc(OC)nc1	https://dx.doi.org/10.1016/j.bmcl.2010.02.018
CHEMBL1089391	7788	None	0	Human	Functional	Ki	=	19.70	7.71	-	1	Antagonist activity at human oxytocin receptor expressed in CHO cells by beta lactamase assay	ChEMBL	369.2	5	0	7	2.69	COc1ccc(-n2c(C)nnc2N2CC(Oc3cccc(F)c3C)C2)cn1	https://dx.doi.org/10.1016/j.bmcl.2010.01.143

Showing 1 to 20 of 463 entries

Join us

Cite us

Main reference

Ligand source activities (1 row/activity)