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ChEMBL ligand: CHEMBL2431768 (Lcl 161, Lcl-161, Lcl161, LCL161, Nvp-lcl 161) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 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 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 | 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 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 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]