Target Validation Information
TTD ID T82739
Target Name Plasma kallikrein (KLKB1)
Type of Target
Successful
Drug Potency against Target (3,4-dichlorophenyl)(1H-pyrazol-1-yl)methanone Drug Info IC50 = 5700 nM [2]
(3-nitro-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info IC50 = 6100 nM [2]
(3-nitro-1H-pyrazol-1-yl)(phenyl)methanone Drug Info IC50 = 18800 nM [2]
(4-bromo-1H-pyrazol-1-yl)(p-tolyl)methanone Drug Info IC50 = 6200 nM [2]
1-benzoyl-N-phenyl-1H-pyrazole-3-carboxamide Drug Info IC50 = 12300 nM [2]
D-Pro-Phe-Arg chloromethyl ketone Drug Info IC50 = 31 nM [3]
ZK-810388 Drug Info Ki = 37 nM [1]
ZK-814048 Drug Info Ki = 1000 nM [1]
References
REF 1 Thiophene-anthranilamides as highly potent and orally available factor Xa inhibitors. J Med Chem. 2007 Jun 28;50(13):2967-80.
REF 2 N-benzoylpyrazoles are novel small-molecule inhibitors of human neutrophil elastase. J Med Chem. 2007 Oct 4;50(20):4928-38.
REF 3 Novel 3-carboxamide-coumarins as potent and selective FXIIa inhibitors. J Med Chem. 2008 Jun 12;51(11):3077-80.

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