UMI-77 [Ligand Id: 8105] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1331211
  • BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415]
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  • Bcl-2-like 2/Apoptosis regulator Bcl-W in Human [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843]
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  • Bcl-2-like 1/Apoptosis regulator Bcl-X in Human [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817]
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  • Histone acetyltransferase GCN5 in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL4669] [UniProtKB: Q03330]
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  • E1A binding protein p300/Histone acetyltransferase p300 in Human [ChEMBL: CHEMBL3784] [GtoPdb: 2735] [UniProtKB: Q09472]
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  • Histone acetyltransferase RTT109 in Saccharomyces cerevisiae (strain ATCC 204508 / S288c) (Baker's yeast) [ChEMBL: CHEMBL3414417] [UniProtKB: Q07794]
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  • MCL1 apoptosis regulator, BCL2 family member/Induced myeloid leukemia cell differentiation protein Mcl-1 in Human [ChEMBL: CHEMBL4361] [GtoPdb: 2847] [UniProtKB: Q07820]
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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]
ChEMBL Inhibition of Bfl-1 (unknown origin) assessed as inhibition constant B 5.5 pKi 3170 nM Ki Bioorg Med Chem Lett (2024) 101: 129658-129658 [PMID:38373466]
ChEMBL Inhibition of recombinant Bfl-1 (1-152) (unknown origin) by TR-FRET assay B 5.08 pIC50 8410 nM IC50 Bioorg Med Chem Lett (2024) 101: 129658-129658 [PMID:38373466]
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 Mcl-1 (unknown origin) assessed as inhibition constant B 5.72 pKi 1910 nM Ki Bioorg Med Chem Lett (2024) 101: 129658-129658 [PMID:38373466]
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 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 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 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 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]