Synonyms: CCS-1477 | CCS1477
Compound class:
Synthetic organic
Comment: Inobrodib (CCS1477) is an orally active, potent, and selective inhibitor of the bromodomains of the E1A binding protein p300 and CREB binding protein (CBP) histone acetyltransferases (HATs) [1-2,5].
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. He ZX, Wei BF, Zhang X, Gong YP, Ma LY, Zhao W. (2021)
Current development of CBP/p300 inhibitors in the last decade. Eur J Med Chem, 209: 112861. [PMID:33045661] |
2. Liu R, Yang H, Chen Z, Zhou K, Shi Q, Li J, Huang Y, Huang X, Li Y. (2022)
Design, synthesis and biological evaluation of (R)-5-methylpyrrolidin-2-ones as p300 bromodomain inhibitors with Anti-Tumor activities in multiple tumor lines. Bioorg Chem, 124: 105803. [PMID:35439627] |
3. Nicosia L, Spencer GJ, Brooks N, Amaral FMR, Basma NJ, Chadwick JA, Revell B, Wingelhofer B, Maiques-Diaz A, Sinclair O et al.. (2023)
Therapeutic targeting of EP300/CBP by bromodomain inhibition in hematologic malignancies. Cancer Cell, 41 (12): 2136-2153.e13. [PMID:37995682] |
4. Rasool RU, Natesan R, Asangani IA. (2021)
Toppling the HAT to Treat Lethal Prostate Cancer. Cancer Discov, 11 (5): 1011-1013. [PMID:33947717] |
5. Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand SN, Pal A, Figueiredo I, Riisnaes R, Gurel B et al.. (2021)
Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov, 11 (5): 1118-1137. [PMID:33431496] |
6. Xiang Q, Wang C, Wu T, Zhang C, Hu Q, Luo G, Hu J, Zhuang X, Zou L, Shen H et al.. (2022)
Design, Synthesis, and Biological Evaluation of 1-(Indolizin-3-yl)ethan-1-ones as CBP Bromodomain Inhibitors for the Treatment of Prostate Cancer. J Med Chem, 65 (1): 785-810. [PMID:34962793] |