RY764 [Ligand Id: 1337] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL364346
  • MC2 receptor/Melanocortin receptor 2 in Human [ChEMBL: CHEMBL1965] [GtoPdb: 283] [UniProtKB: Q01718]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
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  • MC4 receptor/Melanocortin receptor 4 in Human [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
  • MC4 receptor/Melanocortin receptor 4 in Mouse [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450]
  • MC4 receptor/Melanocortin receptor 4 in Rat [ChEMBL: CHEMBL2700] [GtoPdb: 285] [UniProtKB: P70596]
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  • MC5 receptor/Melanocortin receptor 5 in Human [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MC2 receptor/Melanocortin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1965] [GtoPdb: 283] [UniProtKB: Q01718]
ChEMBL Inhibition concentration (binding affinity) against human melanocortin receptor 2 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 5 pIC50 >10000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
ChEMBL Inhibition concentration (binding affinity) against human melanocortin receptor 3 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 6.03 pIC50 942 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
ChEMBL Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 5.1 pIC50 8000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Inhibition concentration (binding affinity) against dog melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 5.15 pIC50 7000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Inhibition concentration (binding affinity) against human melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 8.1 pIC50 8 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
GtoPdb - - 8.1 pIC50 - - - Bioorg Med Chem Lett (2005) 15: 3501-5 [PMID:15982875]
ChEMBL Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells) F 4.96 pEC50 11000 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Concentration of compound at 50% maximum cAMP accumulation in human melanocortin receptor (hMC4R) F 4.96 pEC50 11000 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Concentration of compound at 50% maximum cAMP accumulation in dog melanocortin receptor (dMC4R) F 4.96 pEC50 11000 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Effective concentration (binding affinity) exhibited against human melanocortin receptor 4 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells) F 7.96 pEC50 11 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
MC4 receptor/Melanocortin receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450]
ChEMBL Inhibition concentration (binding affinity) against mouse melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Concentration of compound at 50% maximum cAMP accumulation in mouse melanocortin receptor (mMC4R) F 5.22 pEC50 6000 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
MC4 receptor/Melanocortin receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2700] [GtoPdb: 285] [UniProtKB: P70596]
ChEMBL Inhibition concentration (binding affinity) against rat melanocortin receptor 4 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Concentration of compound at 50% maximum cAMP accumulation in rat melanocortin receptor (rMC4R) F 5.3 pEC50 5000 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
MC5 receptor/Melanocortin receptor 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4608] [GtoPdb: 286] [UniProtKB: P33032]
ChEMBL Inhibition concentration (binding affinity) against human melanocortin receptor 5 by displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells B 6.02 pIC50 945 nM IC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]
ChEMBL Effective concentration (binding affinity) exhibited against human melanocortin receptor 5 by radio labeled ligand assay (Displacement of [125I]NDP-alpha-MSH from the human receptors expressed in CHO cells) F 6.07 pEC50 850 nM EC50 Bioorg Med Chem Lett (2005) 15: 3501-3505 [PMID:15982875]

ChEMBL data shown on this page come from version 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]