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ChEMBL ligand: CHEMBL4173974 (Astx 660, Astx-660, Astx660, ASTX-660, ASTX660, Tolinapant) |
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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 | Inhibition of CIAP1 (unknown origin) | B | 7.92 | pIC50 | 12 | nM | IC50 | Eur J Med Chem (2019) 167: 76-95 [PMID:30769242] |
ChEMBL | Induction of intracellular cIAP1 degradation in human MDA-MB-231 cells after 2 hrs | B | 9.66 | pIC50 | 0.22 | nM | IC50 | J Med Chem (2018) 61: 7314-7329 [PMID:30091600] |
GtoPdb | Measuring inhibition of intracellular degradation of cIAP1 in MDA-MB-231 cells | - | 9.66 | pIC50 | 0.22 | nM | IC50 | J Med Chem (2018) 61: 7314-7329 [PMID:30091600] |
Genome polyprotein in Zika virus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523954] [UniProtKB: A0A024AXB9] | ||||||||
ChEMBL | Inhibition of Zika virus NS2B-NS3 protease | B | 6.1 | pKi | 800 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 126965-126965 [PMID:31980339] |
Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
ChEMBL | Inhibition of human ERG expressed in CHOK1 cells incubated for 600 secs at -80 mV holding potential by automated patch clamp assay | B | 4.16 | pIC50 | 69000 | nM | IC50 | J Med Chem (2018) 61: 7314-7329 [PMID:30091600] |
X-linked inhibitor of apoptosis/Inhibitor of apoptosis protein 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4198] [GtoPdb: 2790] [UniProtKB: P98170] | ||||||||
ChEMBL | Inhibition of XIAP (unknown origin) | B | 7.4 | pIC50 | <40 | nM | IC50 | Eur J Med Chem (2019) 167: 76-95 [PMID:30769242] |
GtoPdb | Determined in a cellular XIAP-caspase 9 immunoprecipitation assay | - | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2018) 61: 7314-7329 [PMID:30091600] |
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 | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2018) 61: 7314-7329 [PMID:30091600] |
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]