UNC1215 [Ligand Id: 8232] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2426364
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  • Lethal(3)malignant brain tumor-like protein 1 in Human [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468]
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  • L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7]
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  • Lethal(3)malignant brain tumor-like protein 4 in Human [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19]
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  • lysine demethylase 5A/Lysine-specific demethylase 5A in Human [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375]
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  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • Scm-like with four mbt domains 1, isoform CRA_b in Human [ChEMBL: CHEMBL1764944] [UniProtKB: Q9UHJ3]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Chromobox protein homolog 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1764946] [UniProtKB: O95931]
ChEMBL Inhibition of CBX7 (8 to 62) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.52 pIC50 >30000 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of CBX7 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
E3 ubiquitin-protein ligase UHRF1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424510] [UniProtKB: Q96T88]
ChEMBL Inhibition of UHRF1 tandem tudor domain (121 to 286) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H3K9Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.52 pIC50 >30000 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of UHRF1 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
Lethal(3)malignant brain tumor-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287622] [UniProtKB: Q9Y468]
ChEMBL Binding affinity to L3MBTL1 (unknown origin) by isothermal titration calorimetric assay B 5.03 pKd 9400 nM Kd J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
ChEMBL Inhibition of His-tagged L3MBTL1 (unknown origin) using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 5.05 pIC50 8900 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of L3MBTL1 (unknown origin) after 30 mins by AlphaScreen assay B 5.64 pIC50 2300 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
L3MBTL histone methyl-lysine binding protein 3/Lethal(3)malignant brain tumor-like protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287623] [GtoPdb: 2830] [UniProtKB: Q96JM7]
GtoPdb - - 6.92 pKd 120 nM Kd Nat Chem Biol (2013) 9: 184-91 [PMID:23292653]
ChEMBL Binding affinity to L3MBTL3 (unknown origin) by isothermal titration calorimetric assay B 6.92 pKd 120 nM Kd J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
ChEMBL Inhibition of L3MBTL3 (unknown origin) assessed as dissociation constant by isothermal titration calorimetry B 6.92 pKd 120 nM Kd J Med Chem (2019) 62: 8996-9007 [PMID:31260300]
ChEMBL Inhibition of L3MBTL3 (unknown origin) after 30 mins by AlphaScreen assay B 7.19 pIC50 64 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
ChEMBL Inhibition of L3MBTL3 (unknown origin) using H4K20me2 as substrate after 30 mins by LNCE-TR-FRET assay B 7.31 pIC50 49 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
ChEMBL Inhibition of His-tagged L3MBTL3 (unknown origin) using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 7.62 pIC50 24 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
Lethal(3)malignant brain tumor-like protein 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287624] [UniProtKB: Q8NA19]
ChEMBL Inhibition of L3MBTL4 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
lysine demethylase 5A/Lysine-specific demethylase 5A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424504] [GtoPdb: 2680] [UniProtKB: P29375]
ChEMBL Inhibition of GST-tagged Jarid1A (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.52 pIC50 >30000 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of JARID1A (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
MBT domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1287625] [UniProtKB: Q05BQ5]
ChEMBL Inhibition of MBTD1 (130 to 566) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me1 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.11 pIC50 78000 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of MBTD1 (unknown origin) after 30 mins by AlphaScreen assay B 5.05 pIC50 9000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Antagonist activity at muscarinic M1 receptor (unknown origin) expressed in HEK293T cells assessed as inhibition of UNC1679 calcium mobilization F 5.46 pIC50 3500 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
PHD finger protein 23 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424508] [UniProtKB: Q9BUL5]
ChEMBL Inhibition of GST-tagged PHF23 (unknown origin) using H3K4Me3 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.52 pIC50 >30000 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of PHF23 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
Scm-like with four mbt domains 1, isoform CRA_b in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1764944] [UniProtKB: Q9UHJ3]
ChEMBL Inhibition of SFMBT1 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]
Tumor suppressor p53-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424509] [UniProtKB: Q12888]
ChEMBL Inhibition of 53BP1 (1485 to 1611) (unknown origin) expressed in Escherichia coli BL21 Rosetta DE3 using H4K20Me2 as substrate incubated for 30 mins at room temperature followed by incubation under dark condition for 30 mins by AlphaScreen assay B 4.86 pIC50 13700 nM IC50 Medchemcomm (2013) 4: 1501-1507 [PMID:24466405]
ChEMBL Inhibition of 53BP1 (unknown origin) after 30 mins by AlphaScreen assay B 5 pIC50 >10000 nM IC50 J Med Chem (2013) 56: 7358-7371 [PMID:24040942]

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]