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

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ChEMBL ligand: CHEMBL2426364
  • α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • κ receptor/Kappa-type opioid receptor in Human [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
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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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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor/Muscarinic acetylcholine receptor M5 in Human [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
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  • Scm-like with four MBT domains protein 1 in Human [ChEMBL: CHEMBL1764944] [UniProtKB: Q9UHJ3]
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  • DAT/Sodium-dependent dopamine transporter in Human [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b ADRA2C B 6.07 pKi 860 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of alpha2C receptor (unknown origin) by radioligand binding assay B 6.07 pKi 860 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 chromo domain containing CBX7 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.52 pIC50 >30000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 tudor domain containing UHRF1 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.52 pIC50 >30000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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]
κ receptor/Kappa-type opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL237] [GtoPdb: 318] [UniProtKB: P41145]
ChEMBL Inhibition of KOR (unknown origin) by radioligand binding assay B 5.4 pKi 4000 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 Binding affinity to L3MBTL1 (unknown origin) by ITC assay B 5.03 pKd 9400 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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]
ChEMBL Selectivity interaction (AlphaScreen assay) EUB0000214b L3MBTL B 5.7 pIC50 2000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MBT domain containing L3MBTL1 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 5.7 pIC50 2000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 Selectivity interaction (ITC) EUB0000214b L3MBTL3 B 6.92 pKd 120 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to His-tagged wild type L3MBTL3 (unknown origin) assessed as dissociation constant by ITC analysis B 6.92 pKd 120 nM Kd Eur J Med Chem (2023) 256: 115444-115444 [PMID:37178483]
ChEMBL Binding affinity to L3MBTL3 (unknown origin) by ITC assay B 6.92 pKd 120 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
ChEMBL Affinity Phenotypic Cellular interaction (Foci formation of GFP-3MBT in HEK293 cells) EUB0000214b L3MBTL3 F 6.3 pIC50 500 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of GFP-3MBT tagged L3MBTL3 (unknown origin) expressed in HEK293 cells assessed as disruption of foci formation by immunofluorescence assay B 6.3 pIC50 500 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 GFP-3MBT tagged L3MBTL3 (unknown origin) expressed in HEK293 cells assessed as reduction in recovery of fluorescence intensity measured up to 60 secs by FRAP assay B 7.3 pIC50 50 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 Affinity Biochemical interaction (AlphaScreen assay) EUB0000214b L3MBTL3 B 7.4 pIC50 40 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of L3MBTL3 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 7.4 pIC50 40 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 Selectivity interaction (AlphaScreen assay) EUB0000214b L3MBTL4 B 4.96 pIC50 11000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MBT domain containing L3MBTL4 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.96 pIC50 11000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 PHD finger domain containing JARID1A (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.52 pIC50 >30000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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]
ChEMBL Selectivity interaction (AlphaScreen assay) EUB0000214b MBTD1 B 5.22 pIC50 6000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MBT domain containing MBTD1 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 5.22 pIC50 6000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
Mortality factor 4-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630863] [UniProtKB: Q9UBU8]
ChEMBL Binding affinity to MRG15 (unknown origin) by ITC assay B 4.54 pKd 28900 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
ChEMBL Antagonist activity at human M1 receptor assessed as reduction in acetylcholine-induced response by Schild analysis F 5.65 pKd 2238.72 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM1 B 7.01 pKi 97 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of M1 receptor (unknown origin) by radioligand binding assay B 7.01 pKi 97 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
ChEMBL Inhibition of M1 receptor (unknown origin) by Ca2+ mobilization assay F 5.44 pIC50 3600 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Antagonist activity at human M2 receptor assessed as reduction in acetylcholine-induced response by Schild analysis F 7.61 pKd 24.55 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM2 B 7.14 pKi 72 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of M2 receptor (unknown origin) by radioligand binding assay B 7.14 pKi 72 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM3 B 6.05 pKi 890 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of M3 receptor (unknown origin) by radioligand binding assay B 6.05 pKi 890 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM4 B 6.4 pKi 400 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of M4 receptor (unknown origin) by radioligand binding assay B 6.4 pKi 400 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912]
ChEMBL Selectivity interaction (NIMH Psychoactive Drug Screening Program Selectivity Panel (radioligand binding assay)) EUB0000214b CHRM5 B 5.37 pKi 4300 nM Ki Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of M5 receptor (unknown origin) by radioligand binding assay B 5.37 pKi 4300 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
PHD finger protein 20 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6067596] [UniProtKB: Q9BVI0]
ChEMBL Binding affinity to PHF20 (unknown origin) by ITC assay B 5.25 pKd 5600 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
PHD finger protein 20-like protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6066242] [UniProtKB: A8MW92]
ChEMBL Binding affinity to tudor domain containing PHF20L1 (unknown origin) by ITC assay B 4.89 pKd >13000 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 PHD finger domain containing PHF23 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.52 pIC50 >30000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1764944] [UniProtKB: Q9UHJ3]
ChEMBL Selectivity interaction (AlphaScreen assay) EUB0000214b SFMBT1 B 4.52 pIC50 >30000 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MBT domain containing SFMBT (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 4.52 pIC50 >30000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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]
DAT/Sodium-dependent dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959]
ChEMBL Inhibition of DAT (unknown origin) by radioligand binding assay B 5 pKi >10000 nM Ki Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
TP53-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2424509] [UniProtKB: Q12888]
ChEMBL Binding affinity to 53BP1 (unknown origin) by ITC assay B 4.51 pKd >31000 nM Kd Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]
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 Inhibition of tudor domain containing 53BP1 (unknown origin) using H4K20me2 peptide by Alpha-Screen methylated histone peptide competition assay B 5.4 pIC50 4000 nM IC50 Nat Chem Biol (2013) 9: 184-191 [PMID:23292653]

ChEMBL data shown on this page come from version 36:

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]