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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 | Antagonist activity at N-terminal His-tagged cIAP1-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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 | Antagonist activity at N-terminal His-tagged cIAP1-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay | B | 7.8 | pIC50 | 16 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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 | Antagonist activity at N-terminal His-tagged cIAP2-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
ChEMBL | Antagonist activity at N-terminal His-tagged cIAP2-BIR3 domain (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay | B | 7.78 | pIC50 | 16.7 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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] |
baculoviral IAP repeat containing 7/Baculoviral IAP repeat-containing protein 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075127] [GtoPdb: 2794] [UniProtKB: Q96CA5] | ||||||||
ChEMBL | Antagonist activity at N-terminal His-tagged wild type ML-IAP BIR domain (63 to 179 residues)(unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
ChEMBL | Antagonist activity at N-terminal His-tagged wild type ML-IAP BIR domain (63 to 179 residues) (unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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 | Antagonist activity at N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues)(unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate preincubated for 2 hrs with protein followed by substrate addition measured after 2 hrs by DELFIA assay | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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 | Antagonist activity at N-terminal His-tagged XIAP-BIR3 domain (253 to 347 residues)(unknown origin) expressed in Escherichia coli BL21 using AVPIAQKSEK-biotinylated peptide as substrate incubated for 2 hrs by DELFIA assay | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2021) 64: 16147-16158 [PMID:34705456] |
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 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]