Compound name
TP-004
Protein family
Aminopeptidase
Target name
METAP2
Affinity biochemical (nM)
7
CG-Set
Protease set
Recommended Concentration
1 µM
Compound EUbOPEN ID
EUB0000303b
SMILES
Cc1nc(N2CC[C@H](O)C2)ncc1-c1cc(C(F)(F)F)cc2[nH]ncc12
InChIKey
BNTAEJNPQLMGDJ-NSHDSACASA-N
NCBI gene ID
10988
UniProt ID
P50579
Synonyms
METAP2, MNPEP, P67EIF2
Mode of action
Inhibitor
Negative control
TPn-004
Affinity biochemical definition
IC50
Affinity biochemical assay type
Biochemical activity assay (addition of Mn)
Affinity Biochemical Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-004
https://doi.org/10.1016/j.bmcl.2016.04.073
Affinity biochemical relation
=
Selectivity platform
Ricerca panel
Selectivity platform number of targets
100
Selectivity remarks
Highly selective in panel of GPCRs, ion channels, transporters, enzymes and proteases, at 10 µM: METAP2/1 >1000-fold; Selectivity against other proteases: < 1000 -fold; Clean in KinomeScan (DiscoverX) against 468 targets at 1 µM, closest targets as % of contr.: LATS2 (26%), EPHB6 (36%), WNK2 (41%), GRK2 (42%), RPS6KA3 (48%), SGK1 (49%); Clean in screen against 45 GPCR targets (PDSP screen) at 10 µM, closest targets: Ki(SLC6A3) = 1679 nM, Ki(GABAA/BZP) = 4538 nM
Selectivity Source Knowledge
https://www.sgc-ffm.uni-frankfurt.de/#!specificprobeoverview/TP-004
Selectivity Number of Off-targets
0