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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

CHEMBL182554	65228	None	0	Human	Binding	IC50	=	10000.00	5.00	-	2	Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand	ChEMBL	502.3	10	3	5	5.74	COc1cc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)ccc1C(=O)NCCCN1CCCCC1	https://dx.doi.org/10.1016/j.bmcl.2004.07.077
CHEMBL184292	66192	None	0	Human	Binding	IC50	=	6310.00	5.20	-	2	Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand	ChEMBL	458.2	8	3	4	5.34	CCN1CCCC1CNC(=O)c1ccc(NC(=O)Nc2ccc(Oc3ccccc3)cc2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.07.077
CHEMBL184438	66227	None	0	Human	Binding	IC50	=	10000.00	5.00	-	2	Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand	ChEMBL	501.3	10	4	5	5.69	COc1cc(NC(=O)Nc2cccc(Nc3ccccc3)c2)ccc1C(=O)NCCCN1CCCCC1	https://dx.doi.org/10.1016/j.bmcl.2004.07.077
CHEMBL186894	67017	None	0	Human	Binding	IC50	=	2880.00	5.54	-	2	Binding affinity against human Melanin-concentrating hormone receptor 2 stably transfected CHO cells was determined using [125I]MCH as radioligand	ChEMBL	549.3	10	3	5	5.67	O=C(Nc1ccc(Oc2ccccc2)cc1)Nc1ccc(C(=O)NCCN2CCN(Cc3ccccc3)CC2)cc1	https://dx.doi.org/10.1016/j.bmcl.2004.07.077
CHEMBL1934130	69576	None	0	Human	Binding	Ki	=	13.00	7.89	-	2	Displacement of [3H]N-(1'-((9-ethyl-9H-carbazol-3-yl)methyl)-2,3-dihydrospiro[indene-1,4'-piperidine]-3-yl)acetamide from human MCHR2 expressed in HEK293 cells after 2 hrs	ChEMBL	466.2	3	2	4	4.84	CC(=O)N[C@@H]1CC2(CCN(Cc3ccc4c(c3)c3ccccc3n4C(N)=O)CC2)c2ccccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL194408	70332	None	0	Human	Binding	IC50	=	4.50	8.35	-	2	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	460.1	8	1	5	4.87	Cc1cc(N(C)CCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL194837	70585	None	0	Human	Binding	IC50	=	8.70	8.06	-	11	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	447.1	8	1	5	4.81	Cc1cc(OCCN(C)C)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL195635	71220	None	0	Human	Binding	IC50	=	6.30	8.20	-	2	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	528.2	7	1	6	5.52	Cc1cc(N2CCC(N3CCCC3)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL196196	71485	None	0	Human	Binding	IC50	=	8.40	8.08	-	3	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	458.2	8	2	5	5.07	Cc1cc(NCCN(C)C)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL196581	71748	None	0	Human	Binding	IC50	=	7.10	8.15	-	3	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	476.2	10	2	6	4.82	Cc1cc(NCCCN(C)C)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL196667	71783	None	0	Human	Binding	IC50	=	3.70	8.43	-	3	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	444.1	5	2	5	4.28	Cc1cc(N2CCNCC2)nc2ccc(NC(=O)COc3ccc(Cl)cc3Cl)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL197026	71886	None	0	Human	Binding	IC50	=	4.70	8.33	-	2	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	474.2	6	2	6	4.39	Cc1cc(N2CCC(N)CC2)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL197050	71895	None	0	Human	Binding	IC50	=	6.40	8.19	-	2	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	445.2	7	2	5	4.52	Cc1cc(N(C)CCO)nc2ccc(NC(=O)/C=C/c3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL217480	82470	None	0	Human	Binding	IC50	=	960.00	6.02	-	2	Displacement of 125I-[Phe13,Tyr19]-MCH from human MCH-R2	ChEMBL	453.2	7	2	3	6.82	CCCc1cc(NC2CCC2)c2cc(NC(=O)/C=C/c3ccc(C(F)(F)F)cc3)ccc2n1	https://dx.doi.org/10.1016/j.bmcl.2006.08.008
CHEMBL373084	135936	None	0	Human	Binding	IC50	=	6.80	8.17	-	3	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	446.1	8	2	5	4.52	CNCCN(C)c1cc(C)c2cc(NC(=O)COc3ccc(Cl)cc3Cl)ccc2n1	https://dx.doi.org/10.1021/jm050103y
CHEMBL427540	166471	None	0	Human	Binding	IC50	=	6.80	8.17	-	2	Displacement of 15 pM [125I]-MCH from human MCH2R expressed in CHO-K1 in whole-cell binding assay	ChEMBL	472.2	6	2	6	4.01	Cc1cc(N2CC3CC2CN3)nc2ccc(NC(=O)COc3ccc(OC(F)(F)F)cc3)cc12	https://dx.doi.org/10.1021/jm050103y
CHEMBL540930	195697	None	0	Human	Binding	IC50	=	4600.00	5.34	-	2	Displacement of [125I]MCH from human MCHR2 expressed in CHO cells	ChEMBL	600.2	8	2	4	6.49	O=C(CC1CCN(Cc2ccn(-c3ccc(C(F)(F)F)cc3)c2)CC1)NC(c1ccc(F)cc1)c1c[nH]c(=O)c(Cl)c1	https://dx.doi.org/10.1016/j.bmcl.2009.05.067
CHEMBL557629	198218	None	0	Human	Binding	Ki	=	1.60	8.80	-46	3	Displacement of [35S] 4-(1-(3,4-difluorophenyl)-2-(ethyl(3-(6-fluoro-3H-spiro[isobenzofuran-1,4'-piperidine]-1'-yl)propyl)amino)-2-oxoethyl)-3-oxopiperazine-1-sulfonic acid from human MCH2R	ChEMBL	2419.1	58	33	31	-3.45	CSCC[C@H](NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H](N)CC(=O)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(=N)N)C(=O)N[C@H]1CSSC[C@@H](C(=O)N[C@@H](Cc2c[nH]c3ccccc23)C(=O)N[C@@H](CCC(N)=O)CN[C@@H](Cc2ccc(O)cc2)C(=O)O)NC(=O)[C@@H]2CCCN2C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](Cc2ccccc2)NC(=O)[C@H](C(C)C)NC(=O)[C@H](CCCNC(=N)N)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCSC)NC1=O	https://dx.doi.org/10.1016/j.bmcl.2009.03.102

Showing 1 to 18 of 18 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

[Ava^9,10,Ava^14,15]-Ac-hMCH_6-16-NH2	528	None	0	Human	Functional	pIC50	None	-	7.30	1	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12009900
[Phe¹³,Tyr¹⁹]MCH	3103	None	0	Human	Functional	pIC50	None	-	8.80	-1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11459838
[Phe¹³,Tyr¹⁹]MCH	3103	None	0	Human	Functional	pIC50	None	-	8.80	-1	3	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/11404457
Ac-hMCH-(6-16)-NH2	258	None	0	Human	Functional	pIC50	None	-	8.60	-15	2	Unclassified	Guide to Pharmacology	-	-	-	-	-	-	https://pubmed.ncbi.nlm.nih.gov/12009900
ATC0065	510	None	0	Human	Functional	pIC50	None	-	5.85	-	2	Unclassified	Guide to Pharmacology	551.2	8	2	6	5.91	CN(C)c1nc(N[C@H]2CC[C@@H](NCCc3ccc(Br)cc3OC(F)(F)F)CC2)nc2ccccc12	https://pubmed.ncbi.nlm.nih.gov/15677346
CHEMBL1934102	69548	None	4	Human	Functional	IC50	=	1000.00	6.00	19	2	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	392.2	3	0	2	6.38	CCn1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934103	69549	None	0	Human	Functional	IC50	=	10000.00	5.00	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	406.2	4	0	2	6.42	CCn1c2ccccc2c2cc(CCN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934104	69550	None	0	Human	Functional	IC50	=	15000.00	4.82	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	420.3	5	0	2	6.81	CCn1c2ccccc2c2cc(CCCN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934105	69551	None	0	Human	Functional	IC50	=	60000.00	4.22	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	406.2	2	0	2	6.01	CCn1c2ccccc2c2cc(C(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934106	69552	None	0	Human	Functional	IC50	=	60000.00	4.22	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	421.2	2	1	2	6.41	CCn1c2ccccc2c2cc(NC(=O)N3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934107	69553	None	0	Human	Functional	IC50	=	100.00	7.00	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	364.2	2	1	1	5.88	C1=CC2(CCN(Cc3ccc4[nH]c5ccccc5c4c3)CC2)c2ccccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934108	69554	None	0	Human	Functional	IC50	=	70.00	7.16	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	406.2	2	0	3	6.01	CC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934109	69555	None	0	Human	Functional	IC50	=	4.00	8.40	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	435.2	2	0	3	5.88	CN(C)C(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934110	69556	None	0	Human	Functional	IC50	=	300.00	6.52	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	422.2	2	0	4	5.97	COC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934111	69557	None	0	Human	Functional	IC50	=	200.00	6.70	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	442.2	3	0	4	5.16	CS(=O)(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934112	69558	None	0	Human	Functional	IC50	=	4.00	8.40	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	407.2	2	1	3	5.28	NC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934113	69559	None	0	Human	Functional	IC50	=	100.00	7.00	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	420.2	3	0	3	6.41	CCC(=O)n1c2ccccc2c2cc(CN3CCC4(C=Cc5ccccc54)CC3)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934114	69560	None	0	Human	Functional	IC50	=	30.00	7.52	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	410.2	3	1	3	5.26	CCn1c2ccccc2c2cc(CN3CCC4(CC3)c3ccccc3CC4O)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934115	69561	None	0	Human	Functional	IC50	=	200.00	6.70	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	410.2	3	1	3	5.79	CCn1c2ccccc2c2cc(CN3CCC4(CC3)CC(O)c3ccccc34)ccc21	https://dx.doi.org/10.1016/j.bmcl.2011.10.125
CHEMBL1934116	69562	None	0	Human	Functional	IC50	=	10.00	8.00	-	1	Antagonist activity at human MCHR2 receptor expressed in CHO cells assessed as inhibition of MCH-stimulated Ca2+ flux preincubated for 10 mins prior to MCH-stimulation by FLIPR assay	ChEMBL	382.2	2	2	2	4.77	O[C@@H]1Cc2ccccc2C12CCN(Cc1ccc3[nH]c4ccccc4c3c1)CC2	https://dx.doi.org/10.1016/j.bmcl.2011.10.125

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Ligand source activities (1 row/activity)