Target
Potassium voltage-gated channel subfamily A member 3
Ligand
BDBM50115504
Substrate
n/a
Meas. Tech.
ChEMBL_1513934 (CHEMBL3611616)
IC50
0.054±n/a nM
Citation
 Murray, JKQian, YXLiu, BElliott, RAral, JPark, CZhang, XStenkilsson, MSalyers, KRose, MLi, HYu, SAndrews, KLColombero, AWerner, JGaida, KSickmier, EAMiu, PItano, AMcGivern, JGegg, CVSullivan, JKMiranda, LP Pharmaceutical Optimization of Peptide Toxins for Ion Channel Targets: Potent, Selective, and Long-Lived Antagonists of Kv1.3. J Med Chem 58:6784-802 (2015) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily A member 3
Synonyms:
HGK5 | HLK3 | HPCN3 | HuKIII | KCNA3 | KCNA3_HUMAN | Potassium voltage-gated channel subfamily A member 3 | Voltage-gated potassium channel | Voltage-gated potassium channel subunit Kv1.3
Type:
PROTEIN
Mol. Mass.:
63835.47
Organism:
Human
Description:
ChEMBL_1513935
Residue:
575
Sequence:
MDERLSLLRSPPPPSARHRAHPPQRPASSGGAHTLVNHGYAEPAAGRELPPDMTVVPGDHLLEPEVADGGGAPPQGGCGGGGCDRYEPLPPSLPAAGEQDCCGERVVINISGLRFETQLKTLCQFPETLLGDPKRRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRIRRPVNVPIDIFSEEIRFYQLGEEAMEKFREDEGFLREEERPLPRRDFQRQVWLLFEYPESSGPARGIAIVSVLVILISIVIFCLETLPEFRDEKDYPASTSQDSFEAAGNSTSGSRAGASSFSDPFFVVETLCIIWFSFELLVRFFACPSKATFSRNIMNLIDIVAIIPYFITLGTELAERQGNGQQAMSLAILRVIRLVRVFRIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEADDPTSGFSSIPDAFWWAVVTMTTVGYGDMHPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETEGEEQSQYMHVGSCQHLSSSAEELRKARSNSTLSKSEYMVIEEGGMNHSAFPQTPFKTGNSTATCTTNNNPNSCVNIKKIFTDV
  
Inhibitor
Name:
BDBM50115504
Synonyms:
CHEMBL3609223
Type:
Small organic molecule
Emp. Form.:
C167H271N53O47S7
Mol. Mass.:
3997.721
SMILES:
[H][C@@]12CCCN1C(=O)[C@@]([H])(NC(=O)[C@@]([H])(NC(=O)[C@H](CC(O)=O)NC(=O)[C@@]([H])(NC(=O)[C@H](CSSC[C@H](NC(=O)[C@@]([H])(NC(=O)CNC(=O)[C@]1([H])CSSC[C@]3([H])NC(=O)[C@H](C)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](C)NC(=O)[C@@]([H])(NC(=O)[C@]([H])(CSSC[C@]([H])(NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](Cc4ccc(O)cc4)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCSC)NC(=O)[C@H](CO)NC(=O)[C@H](Cc4cnc[nH]4)NC(=O)[C@H](CCCCN)NC3=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@]([H])([C@@H](C)O)C(=O)N1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CCCCN)NC2=O)[C@@H](C)O)[C@@H](C)O)C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CCCNC(N)=N)[C@@H](C)CC)[C@@H](C)O)[C@@H](C)CC |r|
Structure:
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