sabutoclax [Ligand Id: 7920] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL1094250
  • BCL2 apoptosis regulator/Apoptosis regulator Bcl-2 in Human [ChEMBL: CHEMBL4860] [GtoPdb: 2844] [UniProtKB: P10415]
There should be some charts here, you may need to enable JavaScript!
  • Bcl-2-like 1/Apoptosis regulator Bcl-X in Human [ChEMBL: CHEMBL4625] [GtoPdb: 2845] [UniProtKB: Q07817]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • MCL1 apoptosis regulator, BCL2 family member/Induced myeloid leukemia cell differentiation protein Mcl-1 in Human [ChEMBL: CHEMBL4361] [GtoPdb: 2847] [UniProtKB: Q07820]
There should be some charts here, you may need to enable JavaScript!
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 FITC-labeled Bak BH3 peptide from Bcl-2 after 30 mins by fluorescence polarization assay B 5.94 pIC50 1140 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Bcl-2 after 30 mins by fluorescence polarization assay B 6.49 pIC50 320 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
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 by isothermal titration calorimetric assay B 5.62 pKd 2400 nM Kd J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Binding affinity to Bcl-XL by isothermal titration calorimetric assay B 7 pKd 100 nM Kd J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Bcl-XL after 30 mins by fluorescence polarization assay B 6.17 pIC50 680 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Bcl-XL after 30 mins by fluorescence polarization assay B 6.51 pIC50 310 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
Bcl-2-related protein A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6044] [UniProtKB: Q16548]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Bfl-1 after 30 mins by fluorescence polarization assay B 6.21 pIC50 620 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Bfl-1 after 30 mins by fluorescence polarization assay B 6.23 pIC50 590 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
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 Displacement of FITC-labeled Bak BH3 peptide from Mcl-1 after 30 mins by fluorescence polarization assay B 6.7 pIC50 200 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]
ChEMBL Displacement of FITC-labeled Bak BH3 peptide from Mcl-1 after 30 mins by fluorescence polarization assay B 6.74 pIC50 180 nM IC50 J Med Chem (2010) 53: 4166-4176 [PMID:20443627]

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]