Target
Potassium channel subfamily K member 2
Ligand
BDBM22871
Substrate
n/a
Meas. Tech.
TREK1 Assay
pH
7.3±n/a
Temperature
295.15±n/a K
EC50
19700±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:
BDBM22871
Synonyms:
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3,5,7,9,12,14-heptaene | 2-chloro-11-(4-methylpiperazin-1-yl)dibenzo[b,f][1,4]oxazepine | 8-chloro-6-(4-methylpiperazino)benzo[b][1,4]benzoxazepine;succinic acid | CHEMBL831 | CL71,563 | Cloxazepine | Loxapine
Type:
Small organic molecule
Emp. Form.:
C18H18ClN3O
Mol. Mass.:
327.808
SMILES:
CN1CCN(CC1)C1=Nc2ccccc2Oc2ccc(Cl)cc12 |t:8|
Structure:
Search PDB for entries with ligand similarity: