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Target
Potassium voltage-gated channel subfamily D member 3
Ligand
BDBM50591317
Substrate
n/a
Meas. Tech.
ChEMBL_2199960 (CHEMBL5112476)
IC50
28000±n/a nM
Citation
 Lowe, MA; Cardenas, A; Valentin, JP; Zhu, Z; Abendroth, J; Castro, JL; Class, R; Delaunois, A; Fleurance, R; Gerets, H; Gryshkova, V; King, L; Lorimer, DD; MacCoss, M; Rowley, JH; Rosseels, ML; Royer, L; Taylor, RD; Wong, M; Zaccheo, O; Chavan, VP; Ghule, GA; Tapkir, BK; Burrows, JN; Duffey, M; Rottmann, M; Wittlin, S; Angulo-Barturen, I; Jiménez-Díaz, MB; Striepen, J; Fairhurst, KJ; Yeo, T; Fidock, DA; Cowman, AF; Favuzza, P; Crespo-Fernandez, B; Gamo, FJ; Goldberg, DE; Soldati-Favre, D; Laleu, B; de Haro, T Discovery and Characterization of Potent, Efficacious, Orally Available Antimalarial Plasmepsin X Inhibitors and Preclinical Safety Assessment of  J Med Chem 65:14121-14143 (2022) [PubMed] 
Target
Name:
Potassium voltage-gated channel subfamily D member 3
Synonyms:
KCND3 | KCND3_HUMAN | Kv channel-interacting protein 2/Potassium voltage-gated channel subfamily D member 3 | Potassium voltage-gated channel subfamily D member 3 | Voltage-gated potassium channel | Voltage-gated potassium channel subunit Kv4.3
Type:
PROTEIN
Mol. Mass.:
73464.62
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1478652
Residue:
655
Sequence:
MAAGVAAWLPFARAAAIGWMPVANCPMPLAPADKNKRQDELIVLNVSGRRFQTWRTTLERYPDTLLGSTEKEFFFNEDTKEYFFDRDPEVFRCVLNFYRTGKLHYPRYECISAYDDELAFYGILPEIIGDCCYEEYKDRKRENAERLMDDNDSENNQESMPSLSFRQTMWRAFENPHTSTLALVFYYVTGFFIAVSVITNVVETVPCGTVPGSKELPCGERYSVAFFCLDTACVMIFTVEYLLRLFAAPSRYRFIRSVMSIIDVVAIMPYYIGLVMTNNEDVSGAFVTLRVFRVFRIFKFSRHSQGLRILGYTLKSCASELGFLLFSLTMAIIIFATVMFYAEKGSSASKFTSIPASFWYTIVTMTTLGYGDMVPKTIAGKIFGSICSLSGVLVIALPVPVIVSNFSRIYHQNQRADKRRAQKKARLARIRVAKTGSSNAYLHSKRNGLLNEALELTGTPEEEHMGKTTSLIESQHHHLLHCLEKTTGLSYLVDDPLLSVRTSTIKNHEFIDEQMFEQNCMESSMQNYPSTRSPSLSSHPGLTTTCCSRRSKKTTHLPNSNLPATRLRSMQELSTIHIQGSEQPSLTTSRSSLNLKADDGLRPNCKTSQITTAIISIPTPPALTPEGESRPPPASPGPNTNIPSIASNVVKVSAL
  
Inhibitor
Name:
BDBM50591317
Synonyms:
CHEMBL5191783
Type:
Small organic molecule
Emp. Form.:
C25H30ClN5O2
Mol. Mass.:
467.991
SMILES:
C[C@H]1C[C@H](CCO1)N1C(=O)C[C@](C)(NC1=N)c1cccc(Nc2ccc(nc2)C2CC2)c1Cl |r|
Structure:
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