SHU9119 [Ligand Id: 1325] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3422426 |
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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 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]
