Table 13SAR Analysis on the Northern Ring: Amines and Sulfonamides
Entry No. | CID SID Broad ID | * | Potency (μM) Mean ± S.E.M. (n=replicates) | Fold Selectivity | ||||
---|---|---|---|---|---|---|---|---|
STK33 | PKA | |||||||
R1 | n | IC50 | n | IC50 | ||||
1 | 262953 125081987 BRD-K68252161 | S | H | 3 | > 10 | 2 | > 10 | NA |
Solubility (PBS): <78 μM, Purity: 98% | ||||||||
2 | 53347978 125081986 BRD-K31697157 | S | 3 | > 10 | 2 | > 10 | NA | |
Solubility (PBS): <0.5 μM, Purity: 78% | ||||||||
3 | 867021 125299432 BRD-K39555138 | S | 2 | > 10 | - | ND | NA | |
Solubility (PBS): <0.5 μM, Purity: 90% | ||||||||
4 | 53377446 125299423 BRD-K68237450 | S | 2 | 1.6 ± 0.4 | - | ND10 | NA | |
Solubility (PBS): <0.5 μM, Purity: 96% | ||||||||
5 | 53377416 125299422 BRD-K83627917 | S | 2 | > 10 | ND | NA | ||
Solubility (PBS): <0.5 μM, Purity: 96% | ||||||||
6 | 3578433 125299443 BRD-K16816344 | S | 2 | > 10 | - | ND | NA | |
Solubility (PBS): <0.5 μM, Purity: 82% | ||||||||
7 | 53377447 125299425 BRD-K07038789 | S | 2 | > 10 | 2 | ND | NA | |
Solubility (PBS): <0.5 μM, Purity: 94% | ||||||||
8 | 53377443 125299421 BRD-K81609743 | S | 2 | > 10 | ND | NA | ||
Solubility (PBS): 20.9 μM, Purity: 100% | ||||||||
9 | 7161416 125299433 BRD-K96715376 | S | 2 | 7.3 ± 3.4 | ND | NA | ||
Solubility (PBS): 1.4 μM, Purity: 100% | ||||||||
10 | 53377451 125299420 BRD-K36530332 | S | 2 | > 10 | ND | NA | ||
Solubility (PBS): 93.2 μM, Purity: 93% |
NA=Not applicable;
- *
P=purchased; S=synthesized
- PubChem SubstanceRelated PubChem Substances
- A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.[ACS Med Chem Lett. 2012]A Potent and Selective Quinoxalinone-Based STK33 Inhibitor Does Not Show Synthetic Lethality in KRAS-Dependent Cells.Weïwer M, Spoonamore J, Wei J, Guichard B, Ross NT, Masson K, Silkworth W, Dandapani S, Palmer M, Scherer CA, et al. ACS Med Chem Lett. 2012 Dec 13; 3(12):1034-1038. Epub 2012 Oct 22.
- STK33 kinase activity is nonessential in KRAS-dependent cancer cells.[Cancer Res. 2011]STK33 kinase activity is nonessential in KRAS-dependent cancer cells.Babij C, Zhang Y, Kurzeja RJ, Munzli A, Shehabeldin A, Fernando M, Quon K, Kassner PD, Ruefli-Brasse AA, Watson VJ, et al. Cancer Res. 2011 Sep 1; 71(17):5818-26. Epub 2011 Jul 8.
- Targeting of KRAS mutant tumors by HSP90 inhibitors involves degradation of STK33.[J Exp Med. 2012]Targeting of KRAS mutant tumors by HSP90 inhibitors involves degradation of STK33.Azoitei N, Hoffmann CM, Ellegast JM, Ball CR, Obermayer K, Gößele U, Koch B, Faber K, Genze F, Schrader M, et al. J Exp Med. 2012 Apr 9; 209(4):697-711. Epub 2012 Mar 26.
- Review KRAS mutations in lung cancer.[Clin Lung Cancer. 2013]Review KRAS mutations in lung cancer.Karachaliou N, Mayo C, Costa C, Magrí I, Gimenez-Capitan A, Molina-Vila MA, Rosell R. Clin Lung Cancer. 2013 May; 14(3):205-14. Epub 2012 Nov 1.
- Review Gene methylation in gastric cancer.[Clin Chim Acta. 2013]Review Gene methylation in gastric cancer.Qu Y, Dang S, Hou P. Clin Chim Acta. 2013 Sep 23; 424:53-65. Epub 2013 May 10.
- Table 13, SAR Analysis on the Northern Ring: Amines and Sulfonamides - Probe Rep...Table 13, SAR Analysis on the Northern Ring: Amines and Sulfonamides - Probe Reports from the NIH Molecular Libraries Program
Your browsing activity is empty.
Activity recording is turned off.
See more...