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. Author manuscript; available in PMC: 2015 Dec 16.
Published in final edited form as: Chem Biol. 2011 May 27;18(5):642–654. doi: 10.1016/j.chembiol.2011.03.007

Table 1. Structures (A) and Biological Validation (B) of Photoreactive Small-Molecule Probes used in the Study.

graphic file with name emss-66204-t0007.jpg
graphic file with name emss-66204-t0008.jpg
Compound R JMJD2E PHD2
FDH coupled assay NMR-based binding assay MS-based hydroxylation assay
IC50a K D a IC50a
DR014 graphic file with name emss-66204-t0009.jpg 3870 μM No binding @ 250 μM No inhibition @ 300 μM
DR031 graphic file with name emss-66204-t0010.jpg 625 μM No binding @ 250 μM No inhibition @ 300 μM
DR025 graphic file with name emss-66204-t0011.jpg 58.5 μM 17.7 μM 41.8 μM
DR024
(Scaffold) 		OH No inhibition @ 300 μM No binding @ 250 μM No inhibition @ 300 μM
DR016
(Competitor) 		graphic file with name emss-66204-t0012.jpg 40.7 μM 0.7 μM 20.8 μM
a

See also Figure S1A-C.