Reaction Details
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Serine/threonine-protein kinase WNK1 [1-491]
Ligand
BDBM203827
Substrate
n/a
Meas. Tech.
In vitro OSR1 Phosphorylation Assay (OSR1)
pH
7.3000±n/a
Temperature
277.1500±n/a K
IC50
41±0.0 nM
Comments
extracted
Citation
Yamada, K; Park, HM; Rigel, DF; DiPetrillo, K; Whalen, EJ; Anisowicz, A; Beil, M; Berstler, J; Brocklehurst, CE; Burdick, DA; Caplan, SL; Capparelli, MP; Chen, G; Chen, W; Dale, B; Deng, L; Fu, F; Hamamatsu, N; Harasaki, K; Herr, T; Hoffmann, P; Hu, QY; Huang, WJ; Idamakanti, N; Imase, H; Iwaki, Y; Jain, M; Jeyaseelan, J; Kato, M; Kaushik, VK; Kohls, D; Kunjathoor, V; LaSala, D; Lee, J; Liu, J; Luo, Y; Ma, F; Mo, R; Mowbray, S; Mogi, M; Ossola, F; Pandey, P; Patel, SJ; Raghavan, S; Salem, B; Shanado, YH; Trakshel, GM; Turner, G; Wakai, H; Wang, C; Weldon, S; Wielicki, JB; Xie, X; Xu, L; Yagi, YI; Yasoshima, K; Yin, J; Yowe, D; Zhang, JH; Zheng, G; Monovich, L Small-molecule WNK inhibition regulates cardiovascular and renal function. Nat Chem Biol 12:896-898 (2016) [PubMed] Article More Info.:
Target
Name:
Serine/threonine-protein kinase WNK1 [1-491]
Synonyms:
With-No-Lysine kinase 1 (WNK1) | WNK1_HUMAN | WNK1 | HSN2 | KDP | KIAA0344 | PRKWNK1 | With-No-Lysine (K) Kinase 1 (WNK1)
Type:
n/a
Mol. Mass.:
53757.75
Organism:
Human
Description:
Q9H4A3 (1-491aa). Carna Biosciences, cat no. 05-179
Residue:
491
Sequence:
MSGGAAEKQSSTPGSLFLSPPAPAPKNGSSSDSSVGEKLGAAAADAVTGRTEEYRRRRHTMDKDSRGAAATTTTTEHRFFRRSVICDSNATALELPGLPLSLPQPSIPAAVPQSAPPEPHREETVTATATSQVAQQPPAAAAPGEQAVAGPAPSTVPSSTSKDRPVSQPSLVGSKEEPPPARSGSGGGSAKEPQEERSQQQDDIEELETKAVGMSNDGRFLKFDIEIGRGSFKTVYKGLDTETTVEVAWCELQDRKLTKSERQRFKEEAEMLKGLQHPNIVRFYDSWESTVKGKKCIVLVTELMTSGTLKTYLKRFKVMKIKVLRSWCRQILKGLQFLHTRTPPIIHRDLKCDNIFITGPTGSVKIGDLGLATLKRASFAKSVIGTPEFMAPEMYEEKYDESVDVYAFGMCMLEMATSEYPYSECQNAAQIYRRVTSGVKPASFDKVAIPEVKEIIEGCIRQNKDERYSIKDLLNHAFFQEETGVRVELAE
Inhibitor
Name:
BDBM203827
Synonyms:
WNK463 (2) | WNK463 | N-(tert-butyl)-1-(1-(5-(5-(trifluoromethyl)-1,3,4-oxadiazol- 2-yl)pyridin-2-yl)piperidin-4-yl)-1H-imidazole-5-carboxamide
Type:
Small organic molecule
Emp. Form.:
n/a
Mol. Mass.:
n/a
SMILES:
CC(C)(C)NC(=O)c1cncn1C1CCN(CC1)c1ccc(cc1)-c1nnc(o1)C(F)(F)F
