GDC-0152 [Ligand Id: 7733] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2063869 (Gdc-0152)
  • 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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  • baculoviral IAP repeat containing 7/Baculoviral IAP repeat-containing protein 7 in Human [ChEMBL: CHEMBL1075127] [GtoPdb: 2794] [UniProtKB: Q96CA5]
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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 7.77 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 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]