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. Author manuscript; available in PMC: 2019 Apr 17.
Published in final edited form as: Chem Rev. 2018 Sep 7;119(2):1323–1455. doi: 10.1021/acs.chemrev.8b00201

Table 11.

Activity of MetAP inhibitors.

Compound Inhibition (nM) Ref.
MetAPi-1 Ki = 15, Co-hMetAP2; Ki = 4400, Mn-hMetAP2 727
MetAPi-2 Ki = 18, Co-hMetAP2 727
MetAPi-3 Ki = 0.5, Co-hMetAP2 728
MetAPi-4 Ki = 2, Co-hMetAP2 728
MetAPi-5 IC50 = 9100, Mn-hMetAP2 729
MetAPi-6 IC50 = 19, Mn-hMetAP2 730
MetAPi-7 IC50 = 1100, Mn-hMetAP2 731
MetAPi-8 IC50 = 11, Mn-hMetAP2 731
MetAPi-9 IC50 = 230, Mn-hMetAP2 732
MetAPi-10 IC50 = 38, Mn-hMetAP2 732
MetAPi-11 IC50 = 700, Mn-hMetAP2 732
MetAPi-12 IC50 = 800, Co-hMetAP2 733
MetAPi-13 IC50 = 110, Co-EcMetAP 734
MetAPi-14 IC50 = 78, Co-EcMetAP 735
MetAPi-15 IC50 = 184, Ni-EcMetAP; IC50 = 137, Co-EcMetAP 736
MetAPi-16 IC50 = 240, Mn-EcMetAP; IC50 = 116000, Fe-EcMetAP 737,738
MetAPi-17 IC50 = 790, Fe-EcMetAP 738
MetAPi-18 IC50 = 950, Fe-EcMetAP 739
MetAPi-19 IC50 = 13000, Fe-EcMetAP 740
MetAPi-20 IC50 = 12900, Fe-EcMetAP 740
MetAPi-21 IC50 = 5000, Co-EcMetAP 741
MetAPi-22 IC50 = 110, Co-EcMetAP 742
MetAPi-23 IC50 = 67, Co-EcMetAP 737
A311263 IC50 = 30, Mn-hMetAP2 724
A320282 IC50 =180, Mn-hMetAP2 724
A357300 IC50 = 110, Mn-hMetAP2 724
LAF389 IC50 = 800, Co-hMetAP2 721
Nitroxoline IC50 = 55, Mn-hMetAP2; IC50 = 60, Co-BpMetAP 743,744
TNP-470 IC50 =1.3, Co-hMetAP2 717