santacruzamate A [Ligand Id: 7916] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3086767 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| histone deacetylase 1/Histone deacetylase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL325] [GtoPdb: 2658] [UniProtKB: Q13547] | ||||||||
| ChEMBL | Inhibition of recombinant full length C-terminal FLAG-tagged/C-terminal His-tagged human HDAC1 using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 10/Histone deacetylase 10 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5103] [GtoPdb: 2614] [UniProtKB: Q969S8] | ||||||||
| ChEMBL | Inhibition of recombinant N-terminal FLAG-tagged human HDAC10 (2 to 631 residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 11/Histone deacetylase 11 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3310] [GtoPdb: 2615] [UniProtKB: Q96DB2] | ||||||||
| ChEMBL | Inhibition of full length recombinant human HDAC11 expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 2/Histone deacetylase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1937] [GtoPdb: 2616] [UniProtKB: Q92769] | ||||||||
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC2 expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| ChEMBL | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system using fluorogenic peptide RHKK(Ac) as substrate by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| ChEMBL | Inhibition of full length recombinant human HDAC2 expressed in baculovirus expression system using fluorogenic peptide RHKK(Ac) as substrate by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| GtoPdb | - | - | 9.92 | pIC50 | 0.12 | nM | IC50 | J Nat Prod (2013) 76: 2026-33 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay | B | 9.92 | pIC50 | 0.12 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC2 after 30 mins by fluorescence assay | B | 9.95 | pIC50 | 0.11 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| histone deacetylase 3/Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111363] [GtoPdb: 2617] [UniProtKB: O15379, Q9Y618] | ||||||||
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC3/GST-tagged human Ncor2 (395 to 489 residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 4/Histone deacetylase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3524] [GtoPdb: 2659] [UniProtKB: P56524] | ||||||||
| ChEMBL | Inhibition of recombinant C-terminal His-tagged/N-terminal GST-tagged human HDAC4 (627 to 1084 residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| GtoPdb | - | - | 6 | pIC50 | >1000 | nM | IC50 | J Nat Prod (2013) 76: 2026-33 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC4 after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC4 after 30 mins by fluorescence assay | B | 6 | pIC50 | >1000 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| histone deacetylase 5/Histone deacetylase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2563] [GtoPdb: 2660] [UniProtKB: Q9UQL6] | ||||||||
| ChEMBL | Inhibition of recombinant C-terminal His-tagged human HDAC5 catalytic domain (656 to 1122 residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 6/Histone deacetylase 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1865] [GtoPdb: 2618] [UniProtKB: Q9UBN7] | ||||||||
| ChEMBL | Inhibition of recombinant full length N-terminal GST-tagged human HDAC6 expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| GtoPdb | - | - | 6.36 | pIC50 | 434 | nM | IC50 | J Nat Prod (2013) 76: 2026-33 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | B | 6.36 | pIC50 | 433.5 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| ChEMBL | Inhibition of human recombinant HDAC6 after 30 mins by fluorescence assay | B | 6.36 | pIC50 | 433 | nM | IC50 | J Nat Prod (2013) 76: 2026-2033 [PMID:24164245] |
| histone deacetylase 7/Histone deacetylase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2716] [GtoPdb: 2661] [UniProtKB: Q8WUI4] | ||||||||
| ChEMBL | Inhibition of recombinant N-terminal GST-tagged human HDAC7 (518 to end residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 8/Histone deacetylase 8 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3192] [GtoPdb: 2619] [UniProtKB: Q9BY41] | ||||||||
| ChEMBL | Inhibition of recombinant full length C-terminal His-tagged human HDAC8 expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
| histone deacetylase 9/Histone deacetylase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4145] [GtoPdb: 2620] [UniProtKB: Q9UKV0] | ||||||||
| ChEMBL | Inhibition of recombinant C-terminal His-tagged human HDAC9 (604 to 1066 residues) expressed in baculovirus expression system using fluorogenic substrate by fluorescence assay | B | 5.3 | pIC50 | 5000 | nM | IC50 | Bioorg Med Chem (2016) 24: 5183-5196 [PMID:27614919] |
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]
