UMI-77 [Ligand Id: 8105] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1331211 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415] | ||||||||
| ChEMBL | Displacement of Flu-BID/FAM-BID from His-tagged BCL2 (1 to 202) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay | B | 4.62 | pKi | 23830 | nM | Ki | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
| ChEMBL | Inhibition of Bcl2 (unknown origin) using 5-FAM-Bid-BH3 as substrate incubated for 30 mins followed by substrate addition and measured after 20 mins by fluorescence polarization assay | B | 4.96 | pKi | 11000 | nM | Ki | Bioorg Med Chem (2021) 29: 115850-115850 [PMID:33229135] |
| ChEMBL | Inhibition of 5-FAM-tagged Bid-BH3 peptide binding to Bcl2 (unknown origin) by fluorescence polarization assay | B | 5.54 | pKi | 2900 | nM | Ki | Bioorg Med Chem (2019) 27: 2771-2783 [PMID:31079964] |
| Bcl-2-like 2/Apoptosis regulator Bcl-W in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843] | ||||||||
| ChEMBL | Displacement of Flu-BID/FAM-BID from His-tagged BCLW (1 to 155) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay | B | 5.09 | pKi | 8190 | nM | Ki | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
| Bcl-2-like 1/Apoptosis regulator Bcl-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817] | ||||||||
| ChEMBL | Displacement of Flu-BID/FAM-BID from His-tagged BCLX-L (1 to 209) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay | B | 4.48 | pKi | 32990 | nM | Ki | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
| Bcl-2-related protein A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6044] [UniProtKB: Q16548] | ||||||||
| ChEMBL | Displacement of Flu-BID/FAM-BID from His-tagged A1-BFL-1 (1 to 151) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay | B | 5.27 | pKi | 5330 | nM | Ki | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
| Histone acetyltransferase GCN5 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4669] [UniProtKB: Q03330] | ||||||||
| ChEMBL | Inhibition of yeast histone acetyltransferase Gcn5-Ada2-Ada3 complex using tetramer and [3H]-acetyl-CoA assessed as acetate incorporation after 30 mins by liquid scintillation counting | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2015) 58: 2091-2113 [PMID:25634295] |
| E1A binding protein p300/Histone acetyltransferase p300 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472] | ||||||||
| ChEMBL | Inhibition of recombinant histone acetyltransferase p300 (unknown origin) using dH3-H4 tetramer and [3H]-acetyl-CoA assessed as acetate incorporation after 30 mins by liquid scintillation counting | B | 6.48 | pIC50 | 330 | nM | IC50 | J Med Chem (2015) 58: 2091-2113 [PMID:25634295] |
| Histone acetyltransferase RTT109 in Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3414417] [UniProtKB: Q07794] | ||||||||
| ChEMBL | Inhibition of Vps75-stimulated recombinant Saccharomyces cerevisiae histone acetyltransferase Rtt109 using [3H]-acetyl-CoA assessed as acetate incorporation after 30 mins by liquid scintillation counting | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2015) 58: 2091-2113 [PMID:25634295] |
| MCL1 apoptosis regulator, BCL2 family member/Induced myeloid leukemia cell differentiation protein Mcl-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4361] [GtoPdb: 2847] [UniProtKB: Q07820] | ||||||||
| ChEMBL | Inhibition of fluorescein-labeled Bid BH3 peptide (79 to 99 residues) binding to His-tagged MCL1 (171 to 327 residues) (unknown origin) expressed in Escherichia coli Bl21(DE3) cells incubated for 3 hrs by fluorescence polarization assay | B | 5.73 | pKi | 1870 | nM | Ki | Medchemcomm (2016) 7: 778-787 |
| ChEMBL | Displacement of Flu-BID/FAM-BID from His-tagged MCL1 (171 to 327) (unknown origin) expressed in Escherichia coli BL21(DE3) after 3 hrs by fluorescence polarization assay | B | 6.31 | pKi | 490 | nM | Ki | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
| ChEMBL | Inhibition of MCL1 (unknown origin) by fluorescence polarization assay | B | 6.31 | pKi | 490 | nM | Ki | Eur J Med Chem (2018) 146: 471-482 [PMID:29407973] |
| ChEMBL | Inhibition of human MCl-1 by fluorescence polarization assay | B | 6.31 | pKi | 490 | nM | Ki | Eur J Med Chem (2019) 177: 63-75 [PMID:31129454] |
| ChEMBL | Inhibition of Mcl-1 (unknown origin) using 5-FAM-Bid-BH3 as substrate incubated for 30 mins followed by substrate addition and measured after 20 mins by fluorescence polarization assay | B | 6.68 | pKi | 210 | nM | Ki | Bioorg Med Chem (2021) 29: 115850-115850 [PMID:33229135] |
| ChEMBL | Inhibition of 5-FAM-tagged Bid-BH3 peptide binding to Mcl1 (unknown origin) by fluorescence polarization assay | B | 6.74 | pKi | 180 | nM | Ki | Bioorg Med Chem (2019) 27: 2771-2783 [PMID:31079964] |
| ChEMBL | Binding affinity to His-tagged MCL1 (171 to 327) (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of MCL1-N-terminal biotin-labeled BIM BH3 peptide interaction after 30 mins by surface plasmon resonance analysis | B | 5.62 | pIC50 | 2400 | nM | IC50 | J Med Chem (2014) 57: 4111-4133 [PMID:24749893] |
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]
