C646 [Ligand Id: 7004] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL1797936 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CREB binding protein/CREB-binding protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5747] [GtoPdb: 2734] [UniProtKB: Q92793] | ||||||||
| ChEMBL | Inhibition of CBP (unknown origin) using biotinylated H4 (1 to 25)-GSGSK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| lysine acetyltransferase 2A/Histone acetyltransferase GCN5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5501] [GtoPdb: 2736] [UniProtKB: Q92830] | ||||||||
| ChEMBL | Inhibition of GST tagged human GCN5 (323 to end residues) expressed in Sf9 cells using biotinylated H3 (1 to 21)-GGK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 4.32 | pIC50 | 47400 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| lysine acetyltransferase 5/Histone acetyltransferase KAT5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5750] [GtoPdb: 2664] [UniProtKB: Q92993] | ||||||||
| ChEMBL | Inhibition of GST tagged human TIP60 expressed in Sf9 cells using biotinylated H4 (1 to 25)-GSGSK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 4.43 | pIC50 | 37200 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| ChEMBL | Inhibition of recombinant human full length KAT5 using histone H2A peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis | B | 4.74 | pIC50 | 18300 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| lysine acetyltransferase 6A/Histone acetyltransferase KAT6A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3774298] [GtoPdb: 2665] [UniProtKB: Q92794] | ||||||||
| ChEMBL | Inhibition of recombinant human KAT6A (488 to 778 residues) using histone H3 peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis | B | 4.82 | pIC50 | 15000 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| lysine acetyltransferase 6B/Histone acetyltransferase KAT6B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3774300] [GtoPdb: 2666] [UniProtKB: Q8WYB5] | ||||||||
| ChEMBL | Inhibition of MYST4 (unknown origin) using biotinylated H4 (1 to 25)-GSGSK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 4.68 | pIC50 | 21000 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| ChEMBL | Inhibition of recombinant human KAT6B (657 to 1069 residues) using histone H4 peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis | B | 5.25 | pIC50 | 5600 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| lysine acetyltransferase 7/Histone acetyltransferase KAT7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3774299] [GtoPdb: 2667] [UniProtKB: O95251] | ||||||||
| ChEMBL | Inhibition of recombinant human full length KAT7 using histone H3 peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| ChEMBL | Inhibition of MYST2 (unknown origin) using biotinylated H4 (1 to 25)-GSGSK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 5.11 | pIC50 | 7810 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] | ||||||||
| ChEMBL | Competitive inhibition of p300 HAT | B | 6.4 | pKi | 400 | nM | Ki | Bioorg Med Chem (2011) 19: 3605-3615 [PMID:21316248] |
| ChEMBL | Competitive inhibition of p300 (unknown origin) using acetyl CoA as substrate | B | 6.4 | pKi | 400 | nM | Ki | Medchemcomm (2012) 3: 135-161 |
| ChEMBL | Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2016) 59: 1249-1270 [PMID:26701186] |
| ChEMBL | Competitive inhibition of p300 HAT domain (unknown origin) using varying concentrations of acetyl-CoA and constant concentration of H4-15 as substrates preincubated for 10 mins followed by substrate addition and measured after 10 mins | B | 6.4 | pKi | 400 | nM | Ki | Eur J Med Chem (2021) 209: 112915-112915 [PMID:33139110] |
| ChEMBL | Inhibition of recombinant human KAT3B HAT domain (1287 to 1673 residues) expressed in Escherichia coli using histone H3 peptide and [Acetyl-3H]-acetyl-coA as substrates incubated for 1 hrs by scintillation counter analysis | B | 6.4 | pKi | 400 | nM | Ki | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| GtoPdb | - | - | 6.4 | pKi | 400 | nM | Ki | Chem Biol (2010) 17: 471-82 [PMID:20534345] |
| ChEMBL | Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of DTT and BSA | B | 4.29 | pIC50 | 51000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290] |
| ChEMBL | Inhibition of EP300 (unknown origin) by AlphaLISA immunodetection assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | Bioorg Med Chem Lett (2021) 51: 128358-128358 [PMID:34534674] |
| ChEMBL | Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of DTT | B | 4.89 | pIC50 | 13000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290] |
| ChEMBL | Inhibition of FLAG-tagged p300 (1195 to 1673 residues) (unknown origin) expressed in competent Escherichia coli BL21-CodonPlus(DE3)-RIL cells using histone H4 substrate incubated for 10 mins by scintillation counting method in presence of [14C]acetyl-CoA | B | 5.05 | pIC50 | 9000 | nM | IC50 | J Med Chem (2016) 59: 1249-1270 [PMID:26701186] |
| ChEMBL | Inhibition of recombinant P300 catalytic domain (1284 to 1673 residues) (unknown origin) using FITC- histone H4 peptide (1 to 19 residues) as substrate by electrophoretic mobility shift assay | B | 5.17 | pIC50 | 6800 | nM | IC50 | ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290] |
| ChEMBL | Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis in presence of BSA | B | 5.7 | pIC50 | 2000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290] |
| ChEMBL | Inhibition of synthetic VMA-tagged p300 (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 cells using H4-15 peptide substrate incubated for 10 mins by radiometric filter binding assay in presence of [14C]acetyl-CoA | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2016) 59: 1249-1270 [PMID:26701186] |
| ChEMBL | Inhibition of VMA intein chitin binding domain-fused P300 (unknown origin) (1287 to 1652 residues) expressed in Escherichia coli BL21(RIL)-DE3 cells using [12C]-acetyl-CoA/[14C]-acetyl-CoA as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by phosphor imaging analysis | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2020) 63: 1337-1360 [PMID:31910017] |
| ChEMBL | Inhibition of p300 HAT domain (unknown origin) using histone H4-15 peptide and acetyl-coA as substrates preincubated for 10 mins followed by substrate addition and measured after 10 mins | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2022) 237: 114407-114407 [PMID:35512565] |
| ChEMBL | Inhibition of KAT3B HAT domain (1287 to 1652 residues) (unknown origin) expressed in Escherichia coli BL21(RIL)-DE3 using histone H4-15 peptide and 14C-acetyl-coA as substrates preincubated for 10 mins followed by substrate addition and measured after 10 mins by radioactive assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| ChEMBL | Inhibition of recombinant P300 (1195 to 1662 residues) (unknown origin) using FITC-histone H4 as substrate incubated for 10 mins by microfluidic electrophoresis | B | 6 | pIC50 | 1000 | nM | IC50 | ACS Med Chem Lett (2016) 7: 151-155 [PMID:26985290] |
| ChEMBL | Inhibition of p300 (unknown origin) | B | 6.4 | pIC50 | 400 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of p300 (unknown origin) using biotinylated histone H3 (1 to 21 residues) as substrate measured after 90 mins in presence of Acetyl CoA by AlphaLISA assay | B | 6.64 | pIC50 | 230 | nM | IC50 | Eur J Med Chem (2019) 180: 171-190 [PMID:31306905] |
| ChEMBL | Inhibition of recombinant human KAT3B (1287 to 1673 residues) using histone H3 peptide and [3H]-acetyl-coA as substrates incubated for 1 hrs by liquid scintillation counter analysis | B | 6.72 | pIC50 | 191 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| lysine acetyltransferase 2B/Histone acetyltransferase PCAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5500] [GtoPdb: 2737] [UniProtKB: Q92831] | ||||||||
| ChEMBL | Inhibition of GST tagged human PCAF (431 to end residues) expressed in Sf9 cells using biotinylated H3 (1 to 21)-GGK peptide as substrate incubated for 1 hr by AlphaLISA assay | B | 4.41 | pIC50 | 38900 | nM | IC50 | Bioorg Med Chem Lett (2022) 66: 128726-128726 [PMID:35413416] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of human recombinant KDAC2 | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| histone deacetylase 3/Histone deacetylase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1829] [GtoPdb: 2617] [UniProtKB: O15379] | ||||||||
| ChEMBL | Inhibition of human recombinant KDAC3 | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of human recombinant KDAC6 | B | 5.15 | pIC50 | 7000 | nM | IC50 | J Med Chem (2023) 66: 6591-6616 [PMID:37155735] |
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]
