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Target
Potassium voltage-gated channel subfamily A member 5
Ligand
BDBM50385940
Substrate
n/a
Meas. Tech.
ChEMBL_824434 (CHEMBL2044873)
IC50
227±n/a nM
Citation
 Finlay, HJ; Lloyd, J; Vaccaro, W; Kover, A; Yan, L; Bhave, G; Prol, J; Huynh, T; Bhandaru, R; Caringal, Y; DiMarco, J; Gan, J; Harper, T; Huang, C; Conder, ML; Sun, H; Levesque, P; Blanar, M; Atwal, K; Wexler, R Discovery of ((S)-5-(methoxymethyl)-7-(1-methyl-1H-indol-2-yl)-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(3-methylisoxazol-5-yl)pyrrolidin-1-yl)methanone as a potent and selective I(Kur) inhibitor. J Med Chem 55:3036-48 (2012) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily A member 5
Synonyms:
HK2 | HPCN1 | KCNA5 | KCNA5_HUMAN | Potassium voltage-gated channel subfamily A member 5 | Voltage-gated potassium channel | Voltage-gated potassium channel subunit Kv1.5
Type:
Enzyme
Mol. Mass.:
67222.47
Organism:
Homo sapiens (Human)
Description:
P22460
Residue:
613
Sequence:
MEIALVPLENGGAMTVRGGDEARAGCGQATGGELQCPPTAGLSDGPKEPAPKGRGAQRDADSGVRPLPPLPDPGVRPLPPLPEELPRPRRPPPEDEEEEGDPGLGTVEDQALGTASLHHQRVHINISGLRFETQLGTLAQFPNTLLGDPAKRLRYFDPLRNEYFFDRNRPSFDGILYYYQSGGRLRRPVNVSLDVFADEIRFYQLGDEAMERFREDEGFIKEEEKPLPRNEFQRQVWLIFEYPESSGSARAIAIVSVLVILISIITFCLETLPEFRDERELLRHPPAPHQPPAPAPGANGSGVMAPPSGPTVAPLLPRTLADPFFIVETTCVIWFTFELLVRFFACPSKAGFSRNIMNIIDVVAIFPYFITLGTELAEQQPGGGGGGQNGQQAMSLAILRVIRLVRVFRIFKLSRHSKGLQILGKTLQASMRELGLLIFFLFIGVILFSSAVYFAEADNQGTHFSSIPDAFWWAVVTMTTVGYGDMRPITVGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETDHEEPAVLKEEQGTQSQGPGLDRGVQRKVSGSRGSFCKAGGTLENADSARRGSCPLEKCNVKAKSNVDLRRSLYALCLDTSRETDL
  
Inhibitor
Name:
BDBM50385940
Synonyms:
CHEMBL2042159
Type:
Small organic molecule
Emp. Form.:
C25H25Cl2N5O2
Mol. Mass.:
498.404
SMILES:
Cc1cc(on1)[C@@H]1CCCN1C(=O)C1[C@@H](c2ccc(Cl)c(Cl)c2)n2nc(cc2N=C1C)C1CC1 |r,c:32|
Structure:
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