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. Author manuscript; available in PMC: 2019 May 1.
Published in final edited form as: Drug Discov Today. 2018 Jun 21;23(11):1910–1918. doi: 10.1016/j.drudis.2018.06.017

Table 1. MIF inhibitors with a phenol functionality as the key structural element that presumably binds to the active site residue Asn-97 of MIF.

Class Compound Structure Activity, μM Reference(s)
chromen-4-one Orita-13 graphic file with name emss-80985-i001.jpg Ki = 0.04 [39] (TA), Ki = 17 [49] (TA), Ki = 13-22 [40] (TA)
isoxazoline ISO-1 graphic file with name emss-80985-i002.jpg IC50 = 7 [41] (TA), IC50 = 24 [40] (TA);
Max. 40% inhibition [42] (BA)
Alam-4b graphic file with name emss-80985-i003.jpg IC50 = 7.3 [46] (TA)
ISO-66 graphic file with name emss-80985-i004.jpg IC50 = 1.5 [47] (TA)
1,2,3-triazole Jorgensen-3g graphic file with name emss-80985-i005.jpg IC50 = 0.75 [48] (TA);
IC50 = 0.9 [48] (BA)
Jorgensen-3h graphic file with name emss-80985-i006.jpg IC50 = 1 [48] (BA)
Dziedzic-3bb
(Cisneros-3i)		 graphic file with name emss-80985-i007.jpg Dziedzic-3bb: Ki = 0.057 [49] (TA)
Cisneros-3i: Ki = 0.057 [50] (TA); Kd = 0.071 [50] (BA)
Cisneros-3j graphic file with name emss-80985-i008.jpg Ki = 0.034 [50] (TA); Kd = 0.063 [50] (BA)

TA, tautomerase assay; BA, binding assay MIF-CD74