SHU9119 [Ligand Id: 1325] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3422426
  • MC1 receptor in Human [GtoPdb: 282] [UniProtKB: Q01726]
  • MC1 receptor/Melanocortin receptor 1 in Mouse [ChEMBL: CHEMBL4077] [GtoPdb: 282] [UniProtKB: Q01727]
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  • MC3 receptor/Melanocortin receptor 3 in Human [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
  • MC3 receptor/Melanocortin receptor 3 in Mouse [ChEMBL: CHEMBL4774] [GtoPdb: 284] [UniProtKB: P33033]
  • MC3 receptor in Rat [GtoPdb: 284] [UniProtKB: P32244]
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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]
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  • MC5 receptor in Human [GtoPdb: 286] [UniProtKB: P33032]
  • MC5 receptor/Melanocortin receptor 5 in Mouse [ChEMBL: CHEMBL4489] [GtoPdb: 286] [UniProtKB: P41149]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
MC1 receptor in Human [GtoPdb: 282] [UniProtKB: Q01726]
GtoPdb - - 9.2 pKd - - - Neuropeptides (1999) 33: 191-6 [PMID:10657491];
J Med Chem (1995) 38: 3454-61 [PMID:7658432]
MC1 receptor/Melanocortin receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4077] [GtoPdb: 282] [UniProtKB: Q01727]
ChEMBL Agonist activity at mouse melanocortin-1 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay B 9.17 pEC50 0.67 nM EC50 ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
ChEMBL Agonist activity at mouse MC1R expressed in HEK293 cells by cAMP functional bioassay F 9.19 pEC50 0.64 nM EC50 J Med Chem (2015) 58: 4638-4647 [PMID:25898270]
MC3 receptor/Melanocortin receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4644] [GtoPdb: 284] [UniProtKB: P41968]
GtoPdb - - 9.1 pKi - - - Eur J Pharmacol (2002) 440: 141-57 [PMID:12007532];
Neuropeptides (1999) 33: 191-6 [PMID:10657491];
J Med Chem (1995) 38: 3454-61 [PMID:7658432]
ChEMBL Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins B 9.89 pKi 0.13 nM Ki J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC3R expressed in HEK293 cell membranes incubated for 120 mins B 9.89 pKi 0.13 nM Ki J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay F 7.08 pIC50 83.18 nM IC50 J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Antagonist activity at human MC3R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay F 7.08 pIC50 83 nM IC50 J Med Chem (2021) 64: 357-369 [PMID:33190475]
MC3 receptor/Melanocortin receptor 3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4774] [GtoPdb: 284] [UniProtKB: P33033]
ChEMBL Competitive antagonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis B 8.7 pKd 2 nM Kd ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
ChEMBL Displacement of MTII from mouse MC3R expressed in HEK293 cells B 9.5 pKd 0.32 nM Kd J Med Chem (2015) 58: 4638-4647 [PMID:25898270]
ChEMBL Agonist activity at mouse melanocortin-3 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay B 8.52 pEC50 3 nM EC50 ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
MC3 receptor in Rat [GtoPdb: 284] [UniProtKB: P32244]
GtoPdb - - 9.1 pKi 0.88 nM Ki Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100]
MC4 receptor/Melanocortin receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL259] [GtoPdb: 285] [UniProtKB: P32245]
GtoPdb - - 9.6 pKi - - - Neuropeptides (1999) 33: 191-6 [PMID:10657491];
Eur J Pharmacol (1999) 378: 249-258 [PMID:10493100]
ChEMBL Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins B 10.54 pKi 0.03 nM Ki J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Displacement of [125I]-[NIe,DPhe7]-alpha-MSH from human MC4R expressed in HEK293 cell membranes incubated for 120 mins B 10.55 pKi 0.03 nM Ki J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay F 7.42 pIC50 38.02 nM IC50 J Med Chem (2021) 64: 357-369 [PMID:33190475]
ChEMBL Antagonist activity at human MC4R expressed in HEK293 cells expressing the GScAMP22F cAMP reporter assessed as reduction in alpha-MSH-induced cAMP accumulation by cAMP split-luciferase reporter gene assay F 7.42 pIC50 38 nM IC50 J Med Chem (2021) 64: 357-369 [PMID:33190475]
MC4 receptor/Melanocortin receptor 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3719] [GtoPdb: 285] [UniProtKB: P56450]
ChEMBL Competitive antagonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells assessed as inhibition of MTII-induced response after 6 hrs by Schild analysis B 9.7 pKd 0.2 nM Kd ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
ChEMBL Displacement of MTII from mouse MC4R expressed in HEK293 cells B 10.4 pKd 0.04 nM Kd J Med Chem (2015) 58: 4638-4647 [PMID:25898270]
ChEMBL Agonist activity at mouse melanocortin-4 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay B 4 pEC50 >100000 nM EC50 ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
MC5 receptor in Human [GtoPdb: 286] [UniProtKB: P33032]
GtoPdb - - 9 pKd - - - Neuropeptides (1999) 33: 191-6 [PMID:10657491]
MC5 receptor/Melanocortin receptor 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4489] [GtoPdb: 286] [UniProtKB: P41149]
ChEMBL Agonist activity at mouse melanocortin-5 receptor transfected in HEK293 cells after 6 hrs by beta-galactosidase reporter gene assay B 8.62 pEC50 2.4 nM EC50 ACS Med Chem Lett (2015) 6: 123-127 [PMID:25699138]
ChEMBL Agonist activity at mouse MC5R expressed in HEK293 cells by cAMP functional bioassay F 8.64 pEC50 2.31 nM EC50 J Med Chem (2015) 58: 4638-4647 [PMID:25898270]

ChEMBL data shown on this page come from version 32:

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]