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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 | 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) 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 | 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 | 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 (2019) 62: 10005-10025 [PMID:31188592] |
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 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 | 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 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 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]