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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 |
| 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]