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Target
Potassium voltage-gated channel subfamily A member 5
Ligand
BDBM50254778
Substrate
n/a
Meas. Tech.
ChEMBL_608671 (CHEMBL1067155)
IC50
200±n/a nM
Citation
Lloyd, J; Finlay, HJ; Vacarro, W; Hyunh, T; Kover, A; Bhandaru, R; Yan, L; Atwal, K; Conder, ML; Jenkins-West, T; Shi, H; Huang, C; Li, D; Sun, H; Levesque, P Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers. Bioorg Med Chem Lett 20:1436-9 (2010) [PubMed] Article
More Info.:
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:
BDBM50254778
Synonyms:
(7-(3,4-dichlorophenyl)-5-methyl-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)((S)-2-(methoxymethyl)pyrrolidin-1-yl)methanone | CHEMBL520586
Type:
Small organic molecule
Emp. Form.:
C20H22Cl2N4O2
Mol. Mass.:
421.32
SMILES:
COC[C@@H]1CCCN1C(=O)C1C(c2ccc(Cl)c(Cl)c2)n2nccc2N=C1C |r,c:28|