Target
Potassium voltage-gated channel subfamily A member 1
Ligand
BDBM50115595
Substrate
n/a
Meas. Tech.
ChEMBL_1513932 (CHEMBL3611614)
IC50
0.004±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 1
Synonyms:
KCNA1 | KCNA1_HUMAN | Potassium (voltage dependent) | Potassium voltage-gated channel subfamily A member 1 | Voltage-gated potassium channel | Voltage-gated potassium channel subfamily A member 1/beta-1 | Voltage-gated potassium channel subunit Kv1.1
Type:
Enzyme Catalytic Domain
Mol. Mass.:
56451.30
Organism:
Homo sapiens (Human)
Description:
Potassium (voltage dependent) 0 0::Q09470
Residue:
495
Sequence:
MTVMSGENVDEASAAPGHPQDGSYPRQADHDDHECCERVVINISGLRFETQLKTLAQFPNTLLGNPKKRMRYFDPLRNEYFFDRNRPSFDAILYYYQSGGRLRRPVNVPLDMFSEEIKFYELGEEAMEKFREDEGFIKEEERPLPEKEYQRQVWLLFEYPESSGPARVIAIVSVMVILISIVIFCLETLPELKDDKDFTGTVHRIDNTTVIYNSNIFTDPFFIVETLCIIWFSFELVVRFFACPSKTDFFKNIMNFIDIVAIIPYFITLGTEIAEQEGNQKGEQATSLAILRVIRLVRVFRIFKLSRHSKGLQILGQTLKASMRELGLLIFFLFIGVILFSSAVYFAEAEEAESHFSSIPDAFWWAVVSMTTVGYGDMYPVTIGGKIVGSLCAIAGVLTIALPVPVIVSNFNYFYHRETEGEEQAQLLHVSSPNLASDSDLSRRSSSTMSKSEYMEIEEDMNNSIAHYRQVNIRTANCTTANQNCVNKSKLLTDV
  
Inhibitor
Name:
BDBM50115595
Synonyms:
CHEMBL3609238
Type:
Small organic molecule
Emp. Form.:
C168H272N54O47S7
Mol. Mass.:
4024.746
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](C)NC(=O)CNC(=O)[C@]1([H])CSSC[C@]3([H])NC(=O)[C@H](CCC(N)=O)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(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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