Target Validation Information
Target ID T04820
Target Name Cyclin-dependent protein kinase Pfmrk
Target Type
Research
Drug Potency against Target 5-Nitro-1H-indole-2,3-dione Drug Info IC50 = 5900 nM [527246]
WR-289009 Drug Info IC50 = 8200 nM [529988]
3-[3-(2-Hydroxy-ethoxy)-phenyl]-1H-quinolin-2-one Drug Info IC50 = 18000 nM [527246]
WR-089120 Drug Info IC50 = 10000 nM [529988]
WR-289016 Drug Info IC50 = 1300 nM [529988]
WR-289010 Drug Info IC50 = 9000 nM [529988]
WR-289012 Drug Info IC50 = 19000 nM [529988]
WR-080539 Drug Info IC50 = 17000 nM [529988]
KENPAULLONE Drug Info IC50 = 15000 nM [527246]
N'-(2-fluorobenzoyl)-2-naphthohydrazide Drug Info IC50 = 400 nM
2,5-dichloro-N-p-tolylthiophene-3-sulfonamide Drug Info IC50 = 600 nM
N-(2-aminoethyl)isoquinoline-5-sulfonamide Drug Info IC50 = 700 nM [528918]
2-chloro-N-(o-tolylcarbamoyl)benzamide Drug Info IC50 = 200 nM
WR-190706 Drug Info IC50 = 12000 nM [529988]
2,5-dichloro-N-phenylthiophene-3-sulfonamide Drug Info IC50 = 14900 nM
WR-203581 Drug Info IC50 = 18000 nM [529988]
APIGENIN Drug Info IC50 = 7000 nM [527246]
(E)-1-(4-Nitro-phenyl)-3-pyridin-2-yl-propenone Drug Info IC50 = 18000 nM [527246]
5-chloro-4-nitrothiophene-2-sulfonamide Drug Info IC50 = 17400 nM
References
Ref 527246J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 527246J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 527246J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
Ref 528918Bioorg Med Chem Lett. 2007 Sep 1;17(17):4961-6. Epub 2007 Jun 12.Evaluation of broad spectrum protein kinase inhibitors to probe the architecture of the malarial cyclin dependent protein kinase Pfmrk.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 529988Bioorg Med Chem Lett. 2009 Apr 1;19(7):1982-5. Epub 2009 Feb 13.Selective inhibition of Pfmrk, a Plasmodium falciparum CDK, by antimalarial 1,3-diaryl-2-propenones.
Ref 527246J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.
Ref 527246J Med Chem. 2004 Oct 21;47(22):5418-26.A three-dimensional in silico pharmacophore model for inhibition of Plasmodium falciparum cyclin-dependent kinases and discovery of different classes of novel Pfmrk specific inhibitors.

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