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Compound class: Synthetic organic
Comment: JQ1 is a selective and potent inhibitor of BET family bromodomains . This is a compound from the Structural Genomics Consortium's (SGC) Epigenetics Probes Collection.
Ligand Activity Visualisation Charts
These 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.✖
1. Casey SC, Tong L, Li Y, Do R, Walz S, Fitzgerald KN, Gouw AM, Baylot V, Gütgemann I, Eilers M et al.. (2016)
MYC regulates the antitumor immune response through CD47 and PD-L1.
Science, 352 (6282): 227-31. [PMID:26966191]
2. Filippakopoulos P, Qi J, Picaud S, Shen Y, Smith WB, Fedorov O, Morse EM, Keates T, Hickman TT, Felletar I et al.. (2010)
Selective inhibition of BET bromodomains.
Nature, 468 (7327): 1067-73. [PMID:20871596]
3. Matzuk MM, McKeown MR, Filippakopoulos P, Li Q, Ma L, Agno JE, Lemieux ME, Picaud S, Yu RN, Qi J et al.. (2012)
Small-molecule inhibition of BRDT for male contraception.
Cell, 150 (4): 673-84. [PMID:22901802]