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ChEMBL ligand: CHEMBL443684 (A-855071.0, ABT-263, Navitoclax) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415] | ||||||||
ChEMBL | Binding affinity to human full-length N-terminal His6-tagged prephosphorylated Bcl2 (2 to 206 residues) expressed in Escherichia coli S12 extract by isothermal titration calorimetry | B | 5.74 | pKd | 1803 | nM | Kd | J Med Chem (2020) 63: 13733-13744 [PMID:33197310] |
ChEMBL | Binding affinity to human full-length N-terminal His6-tagged Bcl2 (2 to 206 residues) expressed in Escherichia coli S12 extract by isothermal titration calorimetry | B | 7.69 | pKd | 20.6 | nM | Kd | J Med Chem (2020) 63: 13733-13744 [PMID:33197310] |
ChEMBL | Displacement of biotin-tagged MRPEPATIAQELRRIGDEFNA from C-terminal His-tagged human BCL-2 (1` to 211 residues) expressed in Escherichia coli measured after 2 hrs by AlphaScreen assay | B | 9.19 | pKd | 0.65 | nM | Kd | J Med Chem (2021) 64: 14230-14246 [PMID:34533954] |
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 Flu-Bax peptide binding to Bcl2 (unknown origin) by time-resolved fluorescence resonance energy transfer assay | B | 9 | pKi | <1 | nM | Ki | Eur J Med Chem (2019) 177: 63-75 [PMID:31129454] |
ChEMBL | Binding affinity to Bcl-2 (unknown origin) assessed as inhibition constant by competitive fluorescence polarization assay | B | 9 | pKi | <=1 | nM | Ki | Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811] |
ChEMBL | Inhibition of BCL2 (unknown origin) by TR-FRET assay | B | 9.3 | pKi | <0.5 | nM | Ki | J Med Chem (2020) 63: 11420-11435 [PMID:32539387] |
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 Bcl2 (unknown origin) | B | 10.36 | pKi | 0.04 | nM | Ki | J Med Chem (2019) 62: 10005-10025 [PMID:31188592] |
ChEMBL | Inhibition of BCL-2 (unknown origin) by fluorescence polarization assay | B | 11 | pKi | <0.01 | nM | Ki | Eur J Med Chem (2019) 167: 76-95 [PMID:30769242] |
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] |
ChEMBL | Inhibition of recombinant human C-terminal 6xHis-tagged Bcl-2 (M1 to F212 residues) expressed in Escherichia coli using HyLite Fluor 647-labeled BIM peptide as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126682-126682 [PMID:31606346] |
Bcl-2-like 2/Apoptosis regulator Bcl-W in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4677] [GtoPdb: 2846] [UniProtKB: Q92843] | ||||||||
ChEMBL | Inhibition of BCL-W (unknown origin) by fluorescence polarization assay | B | 6.61 | pKi | 245 | nM | Ki | Eur J Med Chem (2019) 167: 76-95 [PMID:30769242] |
ChEMBL | Binding affinity to Bcl-w (unknown origin) assessed as inhibition constant by competitive fluorescence polarization assay | B | 9 | pKi | <=1 | nM | Ki | Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811] |
ChEMBL | Inhibition of recombinant human N-terminal 6xHis-tagged Bcl-w (M1 to R171) expressed in Escherichia coli using HyLite Fluor 647-labeled Bim peptide as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 7.15 | pIC50 | 70 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126682-126682 [PMID:31606346] |
Bcl-2-like 1/Apoptosis regulator Bcl-X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817] | ||||||||
ChEMBL | Displacement of biotin-tagged LWAAQRYGRELRRMSDEFEGSFKGL from human BCL-XL expressed in Escherichia coli measured after 2 hrs by AlphaScreen assay | B | 8.68 | pKd | 2.07 | nM | Kd | J Med Chem (2021) 64: 14230-14246 [PMID:34533954] |
ChEMBL | Inhibition of BCL-XL (unknown origin) by fluorescence polarization assay | B | 7.32 | pKi | 48 | nM | Ki | Eur J Med Chem (2019) 167: 76-95 [PMID:30769242] |
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 | 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 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 | Binding affinity to His-tagged Bcl-xL (unknown origin) assessed as inhibition constant by competitive fluorescence polarization assay | B | 9 | pKi | <=1 | nM | Ki | Eur J Med Chem (2020) 201: 112446-112446 [PMID:32563811] |
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 Flu-Bax peptide binding to Bcl-xL (unknown origin) by time-resolved fluorescence resonance energy transfer assay | B | 9.3 | pKi | <0.5 | nM | Ki | Eur J Med Chem (2019) 177: 63-75 [PMID:31129454] |
ChEMBL | Inhibition of F-Bak binding to GST-tagged BCL-XL (unknown origin) measured after 1 hr by TR-FRET assay | B | 10 | pKi | <0.1 | nM | Ki | ACS Med Chem Lett (2021) 12: 1011-1016 [PMID:34141086] |
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 | Inhibition of recombinant human N-terminal GST-tagged Bcl-xl (1 to 209 residues) expressed in Escherichia coli using HyLite Fluor 647-labeled BIM peptide as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 8.1 | pIC50 | <8 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126682-126682 [PMID:31606346] |
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] |
Aspartyl/asparaginyl beta-hydroxylase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4680030] [UniProtKB: Q12797] | ||||||||
ChEMBL | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with high 200 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | B | 5.88 | pIC50 | 1330 | nM | IC50 | Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066] |
ChEMBL | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using high 10 uM hFX-CP as substrate mixture with 10 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | B | 5.92 | pIC50 | 1210 | nM | IC50 | Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066] |
ChEMBL | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and 2 uM FAS incubated for 35 mins by MS analysis | B | 5.99 | pIC50 | 1030 | nM | IC50 | Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066] |
ChEMBL | Inhibition of N-His6-tagged human AspH (315-755) expressed in Escherichia coli BL21 (DE3) using 1 uM hFX-CP as substrate mixture with 3 uM 2OG, 100 uM L-ascorbic acid and high 20 uM FAS incubated for 35 mins by MS analysis | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem (2020) 28: 115675-115675 [PMID:33069066] |
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 | Inhibition of F-Bak binding to GST-tagged MCL1 (unknown origin) measured after 1 hr by TR-FRET assay | B | 6.65 | pKi | >224 | nM | Ki | ACS Med Chem Lett (2021) 12: 1011-1016 [PMID:34141086] |
ChEMBL | Inhibition of Flu-Bax peptide binding to MCl-1 (unknown origin) by time-resolved fluorescence resonance energy transfer assay | B | 9 | pKi | <1 | nM | Ki | Eur J Med Chem (2019) 177: 63-75 [PMID:31129454] |
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 | Inhibition of recombinant human C-terminal 6xHis-tagged Mcl-1 (E171 ti G327) expressed in Escherichia coli using biotin-labeled BIM peptide as substrate incubated for 120 to 180 mins by TR-FRET assay | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 126682-126682 [PMID:31606346] |
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 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]