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 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]