Target
Potassium voltage-gated channel subfamily A member 1
Ligand
BDBM50115634
Substrate
n/a
Meas. Tech.
ChEMBL_1513932 (CHEMBL3611614)
IC50
0.005±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:
BDBM50115634
Synonyms:
CHEMBL3609071
Type:
Small organic molecule
Emp. Form.:
C181H287N55O46S7
Mol. Mass.:
4194.011
SMILES:
[H][C@@]12CCCN1C(=O)[C@@]([H])(NC(=O)[C@@]([H])(NC(=O)[C@H](Cc1cccc3ccccc13)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](CCC(N)=O)NC(=O)[C@H](Cc4ccccc4)NC(=O)[C@H](CCCCN)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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