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ChEMBL ligand: CHEMBL2063869 (Gdc-0152) |
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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 | 7.77 | pKd | 17 | nM | Kd | J Med Chem (2019) 62: 5750-5772 [PMID:30676015] |
ChEMBL | Displacement of AVPFAK(5-FAM)K (Hid-FAM) from cIAP1 BIR2 domain after 30 mins by fluorescence polarization-based competition assay | B | 4.84 | pKi | 14500 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
ChEMBL | Displacement of 5-FAM-conjugated AVP-diPhe-FAM from cIAP1 BIR3 domain after 30 mins by fluorescence polarization-based competition assay | B | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
GtoPdb | BIR3 domain of hcIAP1 (BIRC2) | - | 7.77 | pKi | 17 | nM | Ki | J Med Chem (2012) 55: 4101-13 [PMID:22413863] |
ChEMBL | Displacement of AVPIAQKSEK-biotin from cIAP1 BIR3 (unknown origin) after 1 hr by DELFIA | B | 7.98 | pIC50 | 10.4 | nM | IC50 | J Med Chem (2018) 61: 6350-6363 [PMID:29940121] |
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 | 7.37 | pKd | 43 | nM | Kd | J Med Chem (2019) 62: 5750-5772 [PMID:30676015] |
ChEMBL | Displacement of AVPFAK(5-FAM)K (Hid-FAM) from cIAP2 BIR2 domain after 30 mins by fluorescence polarization-based competition assay | B | 5.02 | pKi | 9600 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
ChEMBL | Displacement of 5-FAM-conjugated AVP-diPhe-FAM from cIAP2 BIR3 domain after 30 mins by fluorescence polarization-based competition assay | B | 7.37 | pKi | 43 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
GtoPdb | BIR3 domain of hcIPA2 (BIRC3) | - | 7.37 | pKi | 43 | nM | Ki | J Med Chem (2012) 55: 4101-13 [PMID:22413863] |
ChEMBL | Displacement of AVPIAQKSEK-biotin from cIAP2 BIR3 (unknown origin) after 1 hr by DELFIA | B | 7.89 | pIC50 | 12.9 | nM | IC50 | J Med Chem (2018) 61: 6350-6363 [PMID:29940121] |
baculoviral IAP repeat containing 7/Baculoviral IAP repeat-containing protein 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075127] [GtoPdb: 2794] [UniProtKB: Q96CA5] | ||||||||
ChEMBL | Binding affinity to ML-IAP-BIR domain (unknown origin) | B | 7.85 | pKd | 14 | nM | Kd | J Med Chem (2019) 62: 5750-5772 [PMID:30676015] |
ChEMBL | Binding affinity to ML-IAP BIR domain after 30 mins by fluorescence polarization-based competition assay | B | 7.3 | pKi | <50 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
GtoPdb | BIR domain of hML-IAP (BIRC7) | - | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2012) 55: 4101-13 [PMID:22413863] |
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-BIR2 domain (unknown origin) by fluorescence polarization-based competition assay | B | 6.95 | pKd | 112 | nM | Kd | J Med Chem (2019) 62: 5750-5772 [PMID:30676015] |
ChEMBL | Binding affinity to N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold by isothermal titration calorimetric analysis | B | 7.06 | pKd | 88 | nM | Kd | J Med Chem (2018) 61: 6350-6363 [PMID:29940121] |
ChEMBL | Binding affinity to XIAP-BIR3 domain (241 to 356 residues) (unknown origin) by fluorescence polarization-based competition assay | B | 7.55 | pKd | 28 | nM | Kd | J Med Chem (2019) 62: 5750-5772 [PMID:30676015] |
ChEMBL | Competitive inhibition of XIAP-BIR2 domain (unknown origin) by fluorescence polarization assay | B | 4.53 | pKi | 29800 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4253-4257 [PMID:23743278] |
ChEMBL | Competitive inhibition of XIAP-BIR3 domain (unknown origin) by fluorescence polarization assay | B | 6.59 | pKi | 260 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4253-4257 [PMID:23743278] |
ChEMBL | Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR2 domain after 30 mins by fluorescence polarization-based competition assay | B | 6.95 | pKi | 112 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
GtoPdb | BIR3 domain of hXIAP | - | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2012) 55: 4101-13 [PMID:22413863] |
ChEMBL | Displacement of 5-FAM-conjugated AVP-diPhe-FAM from XIAP BIR3 domain after 30 mins by fluorescence polarization-based competition assay | B | 7.55 | pKi | 28 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
ChEMBL | Displacement of AVPIAQKSEK-biotin from N-terminal His-tagged human recombinant XIAP BIR3 (253 to 347 residues) expressed in Escherichia coli BL21(DE3) Gold after 1 hr by DELFIA | B | 7.28 | pIC50 | 52.7 | nM | IC50 | J Med Chem (2018) 61: 6350-6363 [PMID:29940121] |
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 | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2019) 62: 5616-5627 [PMID:31095386] |
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 | 7.68 | pIC50 | 21 | nM | IC50 | J Med Chem (2019) 62: 5616-5627 [PMID:31095386] |
Max-like protein X in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2062357] [UniProtKB: Q9UH92] | ||||||||
ChEMBL | Displacement of 5-FAM-conjugated AVP-diPhe-FAM from MLXBIR3SG after 30 mins by fluorescence polarization-based competition assay | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2012) 55: 4101-4113 [PMID:22413863] |
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]