UNC0642 [Ligand Id: 7017] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2441082 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | Binding affinity to adrenergic alpha1D receptor (unknown origin) by radioligand binding assay | B | 5.35 | pKi | 4500 | nM | Ki | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| ChEMBL | Binding affinity to adrenergic alpha2C receptor (unknown origin) by radioligand binding assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| DNA methyltransferase 1/DNA (cytosine-5)-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1993] [GtoPdb: 2605] [UniProtKB: P26358] | ||||||||
| ChEMBL | Inhibition of human DNMT1 using polydeoxyinosine polydeoxycytosine DNA as substrate after 15 mins in presence of SAM by TR-FRET assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| H3 receptor/Histamine H3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL264] [GtoPdb: 264] [UniProtKB: Q9Y5N1] | ||||||||
| ChEMBL | Binding affinity to histamine H3 receptor (unknown origin) by radioligand binding assay | B | 7.35 | pKi | 45 | nM | Ki | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| euchromatic histone lysine methyltransferase 2/Histone-lysine N-methyltransferase, H3 lysine-9 specific 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6032] [GtoPdb: 2652] [UniProtKB: Q96KQ7] | ||||||||
| ChEMBL | Non-competitive inhibition of lysine methyltransferase G9a (unknown origin) using SAM as substrate by Michaelis-Menten kinetic assay | B | 8.43 | pKi | 3.7 | nM | Ki | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase G9a in human U2OS cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase G9a in human PC3 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase G9a in human MDA-MB-231 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay | B | 6.96 | pIC50 | 110 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase G9a in human PANC1 cells assessed as reduction of H3K9me2 cellular level by immunofluorescence in-cell Western assay | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| GtoPdb | - | - | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-42 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase G9a (unknown origin) using [3H]-SAM as substrate after 0.25 hrs by scintillation proximity assay | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| ChEMBL | Inhibition of G9a (unknown origin) | B | 8.6 | pIC50 | <2.5 | nM | IC50 | Bioorg Med Chem (2016) 24: 6102-6108 [PMID:27720557] |
| ChEMBL | Inhibition of human G9a using biotinylated-H3K9 peptide as substrate after 1 hr in presence of SAM by TR-FRET assay | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2018) 61: 6518-6545 [PMID:29953809] |
| euchromatic histone lysine methyltransferase 1/Histone-lysine N-methyltransferase, H3 lysine-9 specific 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6031] [GtoPdb: 2651] [UniProtKB: Q9H9B1] | ||||||||
| GtoPdb | - | - | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-42 [PMID:24102134] |
| ChEMBL | Inhibition of lysine methyltransferase GLP (unknown origin) using [3H]-SAM as substrate after 0.25 hrs by scintillation proximity assay | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
| μ receptor/Mu opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL233] [GtoPdb: 319] [UniProtKB: P35372] | ||||||||
| ChEMBL | Binding affinity to mu opioid receptor (unknown origin) by radioligand binding assay | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2013) 56: 8931-8942 [PMID:24102134] |
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]
