UNC1215 [Ligand Id: 8232] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2426364 |
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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 |
| 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] |
| ChEMBL | Selectivity interaction (AlphaScreen assay) EUB0000214b L3MBTL | B | 5.7 | pIC50 | 2000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | 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 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 | 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 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 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] |
| ChEMBL | Selectivity interaction (AlphaScreen assay) EUB0000214b MBTD1 | B | 5.22 | pIC50 | 6000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| 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 | 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 | 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 |
| 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 |
| 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 |
| 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 |
| 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 | Selectivity interaction (AlphaScreen assay) EUB0000214b SFMBT1 | B | 4.52 | pIC50 | >30000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 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]
