navitoclax [Ligand Id: 8319] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL443684 (Navitoclax, A-855071.0, ABT-263)
  • BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415]
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  • Bcl-2-like 1/Apoptosis regulator Bcl-X in Human [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817]
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  • Bcl2-antagonist of cell death (BAD) in Human [ChEMBL: CHEMBL3817] [UniProtKB: Q92934]
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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]
GtoPdb - - 9 pKi <1 nM Ki J. Med. Chem. (2008) 51: 6902-15 [PMID:18841882]
ChEMBL Displacement of fluorescein labeled Bax peptide from Bcl2 by fluorescence polarization assay B 9 pKi <1 nM Ki J. Med. Chem. (2008) 51: 6902-6915 [PMID:18841882]
ChEMBL Binding affinity to Bcl-2 (unknown origin) by fluorescence polarization assay B 9 pKi <1 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 2105-2114 [PMID:26988306]
ChEMBL Binding affinity to BCL2 (unknown origin) by fluorescence polarization assay B 9 pKi <1 nM Ki MedChemComm (2016) 7: 778-787
ChEMBL Inhibition of Bcl-2 (unknown origin) by fluorescence polarization assay B 9 pKi <1 nM Ki Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL Inhibition of Bcl2 (unknown origin) B 10.36 pKi 0.04 nM Ki J Med Chem (2018) 61: 2636-2651 [PMID:28926247]
ChEMBL Inhibition of human BCL-2 overexpressed in mouse FDC-P1 cells assessed as cell viability after 24 hrs by Cell Titer Glo assay B 7.82 pIC50 <15 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3026-3033 [PMID:24881567]
ChEMBL Displacement of Bax-derived peptide from Bcl-2 (unknown origin) by fluorescence polarization assay B 7.99 pIC50 10.3 nM IC50 Bioorg Med Chem (2018) 26: 443-454 [PMID:29229225]
Bcl-2-like 1/Apoptosis regulator Bcl-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817]
ChEMBL Binding affinity to Bcl-xl B 7.44 pKi 36 nM Ki J. Med. Chem. (2010) 53: 6779-6810 [PMID:20925433]
GtoPdb - - 9 pKi <1 nM Ki J. Med. Chem. (2008) 51: 6902-15 [PMID:18841882]
ChEMBL Binding affinity to Bcl-xL by competitive fluorescence polarization assay B 9 pKi <1 nM Ki J. Med. Chem. (2010) 53: 2577-2588 [PMID:20192224]
ChEMBL Binding affinity to Bcl-XL (unknown origin) by fluorescence polarization assay B 9 pKi <1 nM Ki Bioorg. Med. Chem. Lett. (2016) 26: 2105-2114 [PMID:26988306]
ChEMBL Inhibition of Bcl-xL (unknown origin) by fluorescence polarization assay B 9 pKi <1 nM Ki Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL Binding affinity to Bcl-XL (unknown origin) by fluorescence polarization assay B 9.3 pKi <0.5 nM Ki MedChemComm (2016) 7: 778-787
ChEMBL Inhibition of Bcl-xL (unknown origin) B 10.26 pKi 0.06 nM Ki J Med Chem (2018) 61: 2636-2651 [PMID:28926247]
ChEMBL Inhibition of human BCL-xL overexpressed in mouse FDC-P1 cells assessed as cell viability after 24 hrs by Cell Titer Glo assay B 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (2014) 24: 3026-3033 [PMID:24881567]
ChEMBL Displacement of FITC-Bid from GST-tagged human Bcl-xL expressed in Escherichia coli after 2 hrs by TR-FRET assay B 8.48 pIC50 3.3 nM IC50 J. Med. Chem. (2013) 56: 9635-9645 [PMID:24215352]
Bcl2-antagonist of cell death (BAD) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3817] [UniProtKB: Q92934]
ChEMBL Displacement of fluorescein labeled BAD peptide from Bcl-XL by fluorescence polarization assay B 9 pKi <1 nM Ki J. Med. Chem. (2008) 51: 6902-6915 [PMID:18841882]
ChEMBL Binding affinity to BH3 binding groove of BclXL B 9.3 pKi <0.5 nM Ki J. Med. Chem. (2008) 51: 3661-3680 [PMID:18457385]
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) by fluorescence polarization assay B 6.26 pKi 550 nM Ki Eur J Med Chem (2018) 146: 471-482 [PMID:29407973]
ChEMBL Displacement of FITC-Bid from GST-tagged human Mcl-1 expressed in Escherichia coli after 2 hrs by TR-FRET assay B 4.52 pIC50 >30000 nM IC50 J. Med. Chem. (2013) 56: 9635-9645 [PMID:24215352]
ChEMBL Binding affinity to MCL1 (unknown origin) by fluorescence polarization assay B 6.3 pIC50 500 nM IC50 MedChemComm (2016) 7: 778-787

ChEMBL data shown on this page come from version 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]