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Potency data for probe TP-004 and control TPn-004


In vitro potency


Target name Target information Species Assay description TP-004 TPn-004 Publication of assay conditions
METAP2, KAT6A Homo sapiens Biochemical activity-MetAP2 using Co IC50 = 31 nM PMID: 22086725
METAP2, KAT6A Homo sapiens Biochemical activity-MetAP2 using Mn IC50 = 7 nM PMID: 30069049
EDNRA, METAP2 Membranes prepared from CHO cells stably transfected with human EDNRA and EDNRB Homo sapiens Inhibition of [125I]-endothelin-1 binding to EDNRA IC50 > 10 µM PMID: 10082200


In cell potency


Target name Target information Species Assay description TP-004 TPn-004 Publication of assay conditions
METAP2 HUVEC cells (Lonza) Homo sapiens Cellular assay: Cell activity Western Blot Nmet14-3-3gamma HUVEC: Measurement of the accumulation of N-Met 14-3-3gamma which is a client protein of MetAP2 EC50 = 15 nM PMID: 27155900