ML216 [Ligand Id: 13026] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL2426168
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  • BLM RecQ like helicase/Bloom syndrome protein in Human [ChEMBL: CHEMBL1293237] [GtoPdb: 3260] [UniProtKB: P54132]
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  • WRN RecQ like helicase/Werner syndrome ATP-dependent helicase in Human [ChEMBL: CHEMBL2146312] [GtoPdb: 3259] [UniProtKB: Q14191]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
ATP-dependent DNA helicase Q1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293236] [UniProtKB: P46063]
ChEMBL Inhibition of RECQ1 (unknown origin) by gel-based DNA unwinding assay B 4.3 pIC50 >50000 nM IC50 Bioorg Med Chem Lett (2013) 23: 5660-5666 [PMID:24012121]
BLM RecQ like helicase/Bloom syndrome protein in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293237] [GtoPdb: 3260] [UniProtKB: P54132]
ChEMBL Inhibition of BLM helicase (unknown origin) assessed as branch migration activity B 4.3 pIC50 50000 nM IC50 Bioorg Med Chem Lett (2014) 24: 3006-3013 [PMID:24856061]
ChEMBL Inhibition of 5'-biotin labeled duplex forked-DNA binding to BLM (unknown origin) assessed as increase in unbound DNA levels after 1 hr by ELISA B 4.46 pIC50 34820 nM IC50 J Med Chem (2019) 62: 3147-3162 [PMID:30827110]
ChEMBL Inhibition of BLM helicase (unknown origin) binding to DNA B 5.52 pIC50 3000 nM IC50 Bioorg Med Chem Lett (2014) 24: 3006-3013 [PMID:24856061]
ChEMBL Inhibition of His-tagged BLM (unknown origin) expressed in Escherichia coli BL21 (DE3) assessed as reduction in BLM helicase unwinding activity using 5'-biotin labeled forked-DNA as substrate after 1 hr by PAGE analysis B 5.67 pIC50 2150 nM IC50 J Med Chem (2019) 62: 3147-3162 [PMID:30827110]
GtoPdb Inhibition of BLM-mediated DNA unwinding - 5.74 pIC50 1800 nM IC50 Bioorg Med Chem Lett (2013) 23: 5660-6 [PMID:24012121]
ChEMBL Inhibition of BLM (unknown origin) by gel-based DNA unwinding assay B 5.74 pIC50 1800 nM IC50 Bioorg Med Chem Lett (2013) 23: 5660-5666 [PMID:24012121]
WRN RecQ like helicase/Werner syndrome ATP-dependent helicase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2146312] [GtoPdb: 3259] [UniProtKB: Q14191]
ChEMBL Inhibition of WRN helicase (unknown origin) B 5.3 pIC50 5000 nM IC50 Bioorg Med Chem Lett (2014) 24: 3006-3013 [PMID:24856061]
ChEMBL Inhibition of WRN (unknown origin) by gel-based DNA unwinding assay B 5.57 pIC50 2700 nM IC50 Bioorg Med Chem Lett (2013) 23: 5660-5666 [PMID:24012121]
GtoPdb Inhibition of WRN-mediated DNA unwinding - 5.57 pIC50 2700 nM IC50 Bioorg Med Chem Lett (2013) 23: 5660-6 [PMID:24012121]

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]