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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 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]