Target
Potassium channel subfamily K member 2
Ligand
BDBM78433
Substrate
n/a
Meas. Tech.
TREK1 Assay
pH
7.3±n/a
Temperature
295.15±n/a K
EC50
4700±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:
BDBM78433
Synonyms:
2-[4-[3-[2-(trifluoromethyl)-10-phenothiazinyl]propyl]-1-piperazinyl]ethanol;hydrochloride | 2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazin-1-yl]ethanol;hydrochloride | 2-[4-[3-[2-(trifluoromethyl)phenothiazin-10-yl]propyl]piperazino]ethanol;hydrochloride | FLUPHENAZINE | FLUPHENAZINE HYDROCHLORIDE | MLS001076508 | SMR000058411 | cid_3372 | cid_6602611 | med.21724, Compound 17
Type:
Small organic molecule
Emp. Form.:
C22H26F3N3OS
Mol. Mass.:
437.522
SMILES:
OCCN1CCN(CCCN2c3ccccc3Sc3ccc(cc23)C(F)(F)F)CC1
Structure:
Search PDB for entries with ligand similarity: