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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 2. Covalent MIF inhibitors and MIF inhibitors with other structures.

Class Compound Structure Activity, μM Reference(s)
phenyl-pyrimidine 4-IPP graphic file with name emss-80985-i009.jpg IC50 = 0.2-0.5 [51] (TA)
isothiocyanate BITC graphic file with name emss-80985-i010.jpg IC50 = 0.79 [53] (TA)
benzoxazinone NVS-2 graphic file with name emss-80985-i011.jpg IC50 = 0.020 [55] (TA); Ki = 0.027 [50] (TA); Kd = 0.055 [50] (BA)
benzoxazol-2-one MIF098 (Alissa-5) graphic file with name emss-80985-i012.jpg IC50 = 0.01 [56] (TA)
pyrimidazole K664-1 graphic file with name emss-80985-i013.jpg IC50 = 0.11 [59] (TA); Ki = 45 [40] (TA), Ki = 0.16 [58] (TA)
chromene T-614 graphic file with name emss-80985-i014.jpg IC50 = 6.81 [58] (TA)
Kok-10 graphic file with name emss-80985-i015.jpg IC50 = 18 [60] (TA)
Kok-17 graphic file with name emss-80985-i016.jpg IC50 = 6.2 [60] (TA)
isoxazoline CPSI-2705 graphic file with name emss-80985-i017.jpg 2-10-fold more potent than ISO-1 [35] (TA)
CPSI-1306 graphic file with name emss-80985-i018.jpg 100-fold more potent than ISO-1 [35] (TA)
isocoumarin SCD-19 graphic file with name emss-80985-i019.jpg 100% inhibition at concentration of 100 μM [37] (TA)

TA, tautomerase assay; BA, binding assay MIF-CD74k