Target
Potassium channel subfamily K member 2
Ligand
BDBM181128
Substrate
n/a
Meas. Tech.
TREK1 Assay
pH
7.3±n/a
Temperature
295.15±n/a K
EC50
24800±n/a nM
Comments
extracted
Citation
 Viswanath, ANJung, SYHwang, EMPark, KDLim, SMMin, SJCho, YSPae, AN Identification of the first in silico-designed TREK1 antagonists that block channel currents dose dependently. Chem Biol Drug Des 88:807-819 (2016) [PubMed]  Article 
Target
Name:
Potassium channel subfamily K member 2
Synonyms:
KCNK2 | KCNK2_HUMAN | Outward rectifying potassium channel protein TREK-1 | TREK | TREK-1 K(+) channel subunit | TREK1 | Twik-RElated Potassium (K+) channel 1 (TREK1) | Two pore domain potassium channel TREK-1 | Two pore potassium channel TPKC1
Type:
Protein
Mol. Mass.:
47099.16
Organism:
Homo sapiens (Human)
Description:
O95069
Residue:
426
Sequence:
MLPSASRERPGYRAGVAAPDLLDPKSAAQNSKPRLSFSTKPTVLASRVESDTTINVMKWKTVSTIFLVVVLYLIIGATVFKALEQPHEISQRTTIVIQKQTFISQHSCVNSTELDELIQQIVAAINAGIIPLGNTSNQISHWDLGSSFFFAGTVITTIGFGNISPRTEGGKIFCIIYALLGIPLFGFLLAGVGDQLGTIFGKGIAKVEDTFIKWNVSQTKIRIISTIIFILFGCVLFVALPAIIFKHIEGWSALDAIYFVVITLTTIGFGDYVAGGSDIEYLDFYKPVVWFWILVGLAYFAAVLSMIGDWLRVISKKTKEEVGEFRAHAAEWTANVTAEFKETRRRLSVEIYDKFQRATSIKRKLSAELAGNHNQELTPCRRTLSVNHLTSERDVLPPLLKTESIYLNGLTPHCAGEEIAVIENIK
  
Inhibitor
Name:
BDBM181128
Synonyms:
US9138393, Diltiazem
Type:
Small organic molecule
Emp. Form.:
C22H26N2O4S
Mol. Mass.:
414.518
SMILES:
COc1ccc(cc1)[C@@H]1Sc2ccccc2N(C(C)N(C)C)C(=O)[C@@H]1OC(C)=O |r|
Structure:
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