Synonyms: BGC 945 | BGC-945 | N-[4-[2-Propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-d-glutamic acid 1 [3] | ONX 0801
Compound class:
Synthetic organic
Comment: ONX-0801 (originally named BGC 945) is a first-in-class small molecule inhibitor of thymidylate synthase (TS), that has been designed to accumulate differentially in cancer cells overexpressing the α-folate receptor [3] (FOLR1; P15328). Functionally, it resembles the TS inhibitors plevitrexed and raltitrexed. ONX-0801 is an oncology drug lead for epithelial tumours such as ovarian [1], lung and endometrial cancers, and mesothelioma tumours.
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Campbell IG, Jones TA, Foulkes WD, Trowsdale J. (1991)
Folate-binding protein is a marker for ovarian cancer. Cancer Res, 51 (19): 5329-38. [PMID:1717147] |
2. Gibbs DD, Theti DS, Wood N, Green M, Raynaud F, Valenti M, Forster MD, Mitchell F, Bavetsias V, Henderson E et al.. (2005)
BGC 945, a novel tumor-selective thymidylate synthase inhibitor targeted to alpha-folate receptor-overexpressing tumors. Cancer Res, 65 (24): 11721-8. [PMID:16357184] |
3. Tochowicz A, Dalziel S, Eidam O, O'Connell 3rd JD, Griner S, Finer-Moore JS, Stroud RM. (2013)
Development and binding mode assessment of N-[4-[2-propyn-1-yl[(6S)-4,6,7,8-tetrahydro-2-(hydroxymethyl)-4-oxo-3H-cyclopenta[g]quinazolin-6-yl]amino]benzoyl]-l-γ-glutamyl-D-glutamic acid (BGC 945), a novel thymidylate synthase inhibitor that targets tumor cells. J Med Chem, 56 (13): 5446-55. [PMID:23710599] |