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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] |
ChEMBL | Inhibition of cIAP1 (unknown origin) | B | 9.66 | pIC50 | 0.22 | nM | IC50 | J Med Chem (2023) 66: 3173-3194 [PMID:36821822] |
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 | Inhibition of XIAP (unknown origin) | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2023) 66: 3173-3194 [PMID:36821822] |
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]