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] |
| ChEMBL | Selectivity interaction (Enzyme panel (GPCRS, ion channels, and transporters)) EUB0000194b ADRA1D | B | 5.35 | pKi | 4500 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Enzyme panel (GPCRS, ion channels, and transporters)) EUB0000194b ADRA2C | B | 5 | pKi | >10000 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Selectivity interaction (Enzyme panel (GPCRS, ion channels, and transporters)) EUB0000194b HRH3 | B | 7.35 | pKi | 45 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| coactivator associated arginine methyltransferase 1/Histone-arginine methyltransferase CARM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5406] [GtoPdb: 1255] [UniProtKB: Q86X55] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b CARM1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| enhancer of zeste 2 polycomb repressive complex 2 subunit/Histone-lysine N-methyltransferase EZH2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2189110] [GtoPdb: 2654] [UniProtKB: Q15910] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b EZH2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | Binding affinity to human G9a (913 to 1193 residues) assessed as dissociation constant by isothermal titration calorimetry method | B | 6.64 | pKd | 230 | nM | Kd | J Med Chem (2022) 65: 10506-10522 [PMID:35763668] |
| 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 human G9a (913 to 1193 residues) using H3 peptide as substrate measured upto 45 mins in presence of SAM cofactor | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2022) 65: 10506-10522 [PMID:35763668] |
| 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 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 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 | Affinity Phenotypic Cellular interaction (Immunofluorescence in-cell Western (reduction of H3K9me2 in MDA MB231 cells)) EUB0000194b EHMT2/G9a | B | 6.97 | pIC50 | 106 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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] |
| ChEMBL | Inhibition of human recombinant G9a (785 to 1210 residues) using Histone H3 and SAM as substrate incubated for 2 hrs by chemiluminescence analysis | B | 7.92 | pIC50 | 11.97 | nM | IC50 | ACS Med Chem Lett (2023) 14: 1531-1536 [PMID:37974951] |
| GtoPdb | - | - | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-42 [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 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 | Affinity Biochemical interaction (Enzymatic activity assay) EUB0000194b EHMT2/G9a | B | 8.6 | pIC50 | <2.5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of G9a (unknown origin) | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2023) 66: 4059-4085 [PMID:36882960] |
| ChEMBL | Inhibition of G9a (unknown origin) using H3(1-20)-cys as substrate by HPLC analysis | B | 8.6 | pIC50 | <2.5 | nM | IC50 | Eur J Med Chem (2023) 246: 115028-115028 [PMID:36528996] |
| ChEMBL | Inhibition of G9a (unknown origin) incorporation of tritium-labeled methyl group to biotinylated peptide substrates by Scintillation proximity assay | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2023) 66: 8086-8102 [PMID:37268593] |
| ChEMBL | Inhibition of G9a (unknown origin) | B | 8.6 | pIC50 | <2.5 | nM | IC50 | ACS Med Chem Lett (2023) 14: 1531-1536 [PMID:37974951] |
| 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] |
| ChEMBL | Inhibition of G9a (unknown origin) by AlphaLISA assay | B | 9.29 | pIC50 | 0.51 | nM | IC50 | J Med Chem (2023) 66: 8086-8102 [PMID:37268593] |
| 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] | ||||||||
| ChEMBL | Binding affinity to human GLP (982 to 1266 residues) assessed as dissociation constant by isothermal titration calorimetry method | B | 7.21 | pKd | 62 | nM | Kd | J Med Chem (2022) 65: 10506-10522 [PMID:35763668] |
| ChEMBL | Inhibition of human GLP (982 to 1266 residues) using H3 peptide as substrate measured upto 45 mins in presence of SAM cofactor | B | 6.74 | pIC50 | 180 | nM | IC50 | J Med Chem (2022) 65: 10506-10522 [PMID:35763668] |
| ChEMBL | Affinity Phenotypic Cellular interaction (Immunofluorescence in-cell Western (reduction of H3K9me2 in MDA MB231 cells)) EUB0000194b EHMT1/GLP | B | 6.97 | pIC50 | 106 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of GLP (unknown origin) | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem (2022) 53: 116524-116524 [PMID:34847495] |
| GtoPdb | - | - | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2013) 56: 8931-42 [PMID:24102134] |
| ChEMBL | Inhibition of GLP (unknown origin) using H3(1-20)-cys as substrate by HPLC analysis | B | 8.6 | pIC50 | <2.5 | nM | IC50 | Eur J Med Chem (2023) 246: 115028-115028 [PMID:36528996] |
| 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] |
| ChEMBL | Inhibition of GLP (unknown origin) incorporation of tritium-labeled methyl group to biotinylated peptide substrates by Scintillation proximity assay | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2023) 66: 8086-8102 [PMID:37268593] |
| ChEMBL | Affinity Biochemical interaction (Enzymatic activity assay) EUB0000194b EHMT1/GLP | B | 8.6 | pIC50 | <2.5 | nM | IC50 | Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3 |
| ChEMBL | Inhibition of GLP (unknown origin) | B | 8.6 | pIC50 | <2.5 | nM | IC50 | J Med Chem (2023) 66: 4059-4085 [PMID:36882960] |
| lysine methyltransferase 2A/Histone-lysine N-methyltransferase MLL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293299] [GtoPdb: 2688] [UniProtKB: Q03164] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b MLL | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| SET domain containing 7, histone lysine methyltransferase/Histone-lysine N-methyltransferase SETD7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5523] [GtoPdb: 2703] [UniProtKB: Q8WTS6] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SETD7 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| SET domain bifurcated histone lysine methyltransferase 1/Histone-lysine N-methyltransferase SETDB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321646] [GtoPdb: 2705] [UniProtKB: Q15047] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SETDB1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| SUV39H2 histone lysine methyltransferase/Histone-lysine N-methyltransferase SUV39H2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795177] [GtoPdb: 2716] [UniProtKB: Q9H5I1] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SUV39H2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| lysine methyltransferase 5B/Histone-lysine N-methyltransferase SUV420H1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321645] [GtoPdb: 2717] [UniProtKB: Q4FZB7] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SUV420H1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| lysine methyltransferase 5C/Histone-lysine N-methyltransferase SUV420H2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321644] [GtoPdb: 2718] [UniProtKB: Q86Y97] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SUV420H2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| 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 | Selectivity interaction (Enzyme panel (GPCRS, ion channels, and transporters)) EUB0000194b OPRM1 | B | 5 | pKi | >10000 | nM | Ki | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| lysine methyltransferase 5A/N-lysine methyltransferase SETD8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795176] [GtoPdb: 2704] [UniProtKB: Q9NQR1] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b SETD8 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| protein arginine methyltransferase 1 /Protein-arginine N-methyltransferase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5524] [GtoPdb: 1252] [UniProtKB: Q99873] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b PRMT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| protein arginine methyltransferase 3/Protein arginine N-methyltransferase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5891] [GtoPdb: 1254] [UniProtKB: O60678] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b PRMT3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| protein arginine methyltransferase 5 /Protein arginine N-methyltransferase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795116] [GtoPdb: 1256] [UniProtKB: O14744] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b PRMT5 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
| protein arginine methyltransferase 8/Protein arginine N-methyltransferase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108648] [GtoPdb: 1259] [UniProtKB: Q9NR22] | ||||||||
| ChEMBL | Selectivity interaction (HMT panel) EUB0000194b PRMT8 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomics Library wave 3 |
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]
