LCL161 [Ligand Id: 7912] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2431768 (Lcl 161, Lcl-161, Lcl161, LCL161)
  • baculoviral IAP repeat containing 2/Baculoviral IAP repeat-containing protein 2 in Human [ChEMBL: CHEMBL5462] [GtoPdb: 2791] [UniProtKB: Q13490]
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  • baculoviral IAP repeat containing 3/Baculoviral IAP repeat-containing protein 3 in Human [ChEMBL: CHEMBL5335] [GtoPdb: 2792] [UniProtKB: Q13489]
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  • X-linked inhibitor of apoptosis/Inhibitor of apoptosis protein 3 in Human [ChEMBL: CHEMBL4198] [GtoPdb: 2790] [UniProtKB: P98170]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
baculoviral IAP repeat containing 2/Baculoviral IAP repeat-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5462] [GtoPdb: 2791] [UniProtKB: Q13490]
ChEMBL Binding affinity to cIAP1-BIR3 domain (unknown origin) B 7.98 pKd 10.4 nM Kd J Med Chem (2019) 62: 5750-5772 [PMID:30676015]
ChEMBL Inhibition of His-thrombin-TEV-tagged cIAP1 BIR2 domain (174 to 256) (unknown origin) after 1 hr by TR-FRET assay B 5.57 pIC50 2720 nM IC50 J. Med. Chem. (2013) 56: 7772-7787 [PMID:24083782]
ChEMBL Inhibition of cIAP1 BIR2 domain (unknown origin) B 5.67 pIC50 2140 nM IC50 J. Med. Chem. (2013) 56: 7788-7803 [PMID:24093940]
ChEMBL Inhibition of cIAP1 BIR3 domain (unknown origin) B 7.21 pIC50 61 nM IC50 J. Med. Chem. (2013) 56: 7788-7803 [PMID:24093940]
ChEMBL Inhibition of His-thrombin-TEV-tagged cIAP1 BIR3 domain (260 to 352) (unknown origin) after 1 hr by TR-FRET assay B 7.24 pIC50 58 nM IC50 J. Med. Chem. (2013) 56: 7772-7787 [PMID:24083782]
GtoPdb Assay uses recombinantly expressed BIR3 domain of cIAP1 - 7.24 pIC50 58 nM IC50 J Med Chem (2013) 56: 7772-87 [PMID:24083782]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.68 pIC50 21 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.68 pIC50 21 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.73 pIC50 18.6 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP1-BIR3 (258 to 363 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.73 pIC50 18.6 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs B 9.4 pIC50 0.4 nM IC50 J Med Chem (2018) 61: 7314-7329 [PMID:30091600]
ChEMBL Induction of cIAP1 degradation in human MDA-MB-231 cells after 2 hrs B 9.4 pEC50 0.4 nM EC50 J Med Chem (2017) 60: 4611-4625 [PMID:28492317]
baculoviral IAP repeat containing 3/Baculoviral IAP repeat-containing protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5335] [GtoPdb: 2792] [UniProtKB: Q13489]
ChEMBL Binding affinity to cIAP2-BIR3 domain (unknown origin) B 7.89 pKd 12.9 nM Kd J Med Chem (2019) 62: 5750-5772 [PMID:30676015]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.72 pIC50 19 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.72 pIC50 19 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.96 pIC50 11 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal 6x-His-tagged recombinant human cIAP2-BIR3 (244 to 349 residues) expressed in Escherichia coli incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.96 pIC50 11 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
X-linked inhibitor of apoptosis/Inhibitor of apoptosis protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4198] [GtoPdb: 2790] [UniProtKB: P98170]
ChEMBL Binding affinity to XIAP-BIR3 domain (241 to 356 residues) (unknown origin) by fluorescence polarization-based competition assay B 7.28 pKd 52.7 nM Kd J Med Chem (2019) 62: 5750-5772 [PMID:30676015]
ChEMBL Inhibition of His-tagged XIAP BIR2 domain (124 to 240) (unknown origin) after 1 hr by TR-FRET assay B 5.98 pIC50 1050 nM IC50 J. Med. Chem. (2013) 56: 7772-7787 [PMID:24083782]
ChEMBL Inhibition of XIAP BIR2 domain (unknown origin) B 5.98 pIC50 1040 nM IC50 J. Med. Chem. (2013) 56: 7788-7803 [PMID:24093940]
ChEMBL Displacement of biotinylated AVPF from N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 8 hrs by DELFIA B 7.28 pIC50 53 nM IC50 J Med Chem (2019) 62: 5616-5627 [PMID:31095386]
ChEMBL Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.3 pIC50 50 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs without 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.3 pIC50 50 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Displacement of biotinylated AVPF from N-terminal His tagged recombinant human XIAP-BIR3 domain (253 to 347 residues) expressed in Escherichia coli BL21(DE3) cells incubated for 2 hrs by DELFIA B 7.32 pIC50 48 nM IC50 J Med Chem (2019) 62: 5616-5627 [PMID:31095386]
ChEMBL Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.4 pIC50 40 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of N-terminal His-tagged human XIAP-BIR3 (253 to 347 residues) expressed in Escherichia coli BL21-Gold(DE3) pLysS incubated for 2 hrs after 6 hrs pre-incubation with enzyme by biotinylated AVPI peptide based DELFIA B 7.4 pIC50 40 nM IC50 J Med Chem (2019) 62: 9188-9200 [PMID:31550155]
ChEMBL Inhibition of full length FLAG-tagged XIAP (unknown origin) interaction with full length untagged caspase-9 expressed in HEK293 cells after 2 hrs by immunoprecipitation assay B 7.46 pIC50 35 nM IC50 J Med Chem (2018) 61: 7314-7329 [PMID:30091600]
GtoPdb Assay uses recombinantly expressed BIR3 domain of XIAP - 7.52 pIC50 30 nM IC50 J Med Chem (2013) 56: 7772-87 [PMID:24083782]
ChEMBL Inhibition of His-tagged XIAP BIR3 domain (241 to 356) (unknown origin) after 1 hr by TR-FRET assay B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2013) 56: 7772-7787 [PMID:24083782]
ChEMBL Inhibition of XIAP BIR3 domain (unknown origin) B 7.52 pIC50 30 nM IC50 J. Med. Chem. (2013) 56: 7788-7803 [PMID:24093940]
ChEMBL Inhibition of GST-tagged full length XIAP (unknown origin) assessed as caspase 3/7 reactivation in S-100 cell extract after 4 hrs by fluorescence assay B 6.55 pEC50 283 nM EC50 J. Med. Chem. (2013) 56: 7772-7787 [PMID:24083782]
ChEMBL Inhibition of full length FLAG-tagged XIAP (unknown origin) interaction with full length untagged caspase-9 expressed in HEK293 cells after 2 hrs by immunoprecipitation assay B 7.46 pEC50 35 nM EC50 J Med Chem (2017) 60: 4611-4625 [PMID:28492317]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]