Target
Potassium voltage-gated channel subfamily KQT member 2/3
Ligand
BDBM50339279
Substrate
n/a
Meas. Tech.
ChEMBL_736251 (CHEMBL1693395)
EC50
1250±n/a nM
Citation
 Qi, JZhang, FMi, YFu, YXu, WZhang, DWu, YDu, XJia, QWang, KZhang, H Design, synthesis and biological activity of pyrazolo[1,5-a]pyrimidin-7(4H)-ones as novel Kv7/KCNQ potassium channel activators. Eur J Med Chem 46:934-43 (2011) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily KQT member 2/3
Synonyms:
Voltage-gated potassium channel subunit Kv7.2/Kv7.3 | Voltage-gated potassium channel, KQT; KCNQ2(Kv7.2)/KCNQ3(Kv7.3)
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 91707
Components:
This complex has 3 components.
Component 1
Name:
Potassium voltage-gated channel subfamily KQT member 2
Synonyms:
KCNQ (Kv7) potassium channel | KCNQ2 | KCNQ2_HUMAN | KQT-like 2 | Neuroblastoma-specific potassium channel subunit alpha KvLQT2 | Potassium voltage-gated channel subfamily KQT member 2 | Voltage-gated potassium channel subunit Kv7.2
Type:
PROTEIN
Mol. Mass.:
95883.20
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1457496
Residue:
872
Sequence:
MVQKSRNGGVYPGPSGEKKLKVGFVGLDPGAPDSTRDGALLIAGSEAPKRGSILSKPRAGGAGAGKPPKRNAFYRKLQNFLYNVLERPRGWAFIYHAYVFLLVFSCLVLSVFSTIKEYEKSSEGALYILEIVTIVVFGVEYFVRIWAAGCCCRYRGWRGRLKFARKPFCVIDIMVLIASIAVLAAGSQGNVFATSALRSLRFLQILRMIRMDRRGGTWKLLGSVVYAHSKELVTAWYIGFLCLILASFLVYLAEKGENDHFDTYADALWWGLITLTTIGYGDKYPQTWNGRLLAATFTLIGVSFFALPAGILGSGFALKVQEQHRQKHFEKRRNPAAGLIQSAWRFYATNLSRTDLHSTWQYYERTVTVPMYSSQTQTYGASRLIPPLNQLELLRNLKSKSGLAFRKDPPPEPSPSKGSPCRGPLCGCCPGRSSQKVSLKDRVFSSPRGVAAKGKGSPQAQTVRRSPSADQSLEDSPSKVPKSWSFGDRSRARQAFRIKGAASRQNSEEASLPGEDIVDDKSCPCEFVTEDLTPGLKVSIRAVCVMRFLVSKRKFKESLRPYDVMDVIEQYSAGHLDMLSRIKSLQSRVDQIVGRGPAITDKDRTKGPAEAELPEDPSMMGRLGKVEKQVLSMEKKLDFLVNIYMQRMGIPPTETEAYFGAKEPEPAPPYHSPEDSREHVDRHGCIVKIVRSSSSTGQKNFSAPPAAPPVQCPPSTSWQPQSHPRQGHGTSPVGDHGSLVRIPPPPAHERSLSAYGGGNRASMEFLRQEDTPGCRPPEGNLRDSDTSISIPSVDHEELERSFSGFSISQSKENLDALNSCYAAVAPCAKVRPYIAEGESDTDSDLCTPCGPPPRSATGEGPFGDVGWAGPRK
  
Component 2
Name:
Potassium voltage-gated channel subfamily KQT member 3
Synonyms:
KCNQ (Kv7) potassium channel | KCNQ3 | KCNQ3_HUMAN | Voltage-gated potassium channel subunit Kv7.3
Type:
PROTEIN
Mol. Mass.:
96759.41
Organism:
Homo sapiens (Human)
Description:
ChEMBL_938652
Residue:
872
Sequence:
MGLKARRAAGAAGGGGDGGGGGGGAANPAGGDAAAAGDEERKVGLAPGDVEQVTLALGAGADKDGTLLLEGGGRDEGQRRTPQGIGLLAKTPLSRPVKRNNAKYRRIQTLIYDALERPRGWALLYHALVFLIVLGCLILAVLTTFKEYETVSGDWLLLLETFAIFIFGAEFALRIWAAGCCCRYKGWRGRLKFARKPLCMLDIFVLIASVPVVAVGNQGNVLATSLRSLRFLQILRMLRMDRRGGTWKLLGSAICAHSKELITAWYIGFLTLILSSFLVYLVEKDVPEVDAQGEEMKEEFETYADALWWGLITLATIGYGDKTPKTWEGRLIAATFSLIGVSFFALPAGILGSGLALKVQEQHRQKHFEKRRKPAAELIQAAWRYYATNPNRIDLVATWRFYESVVSFPFFRKEQLEAASSQKLGLLDRVRLSNPRGSNTKGKLFTPLNVDAIEESPSKEPKPVGLNNKERFRTAFRMKAYAFWQSSEDAGTGDPMAEDRGYGNDFPIEDMIPTLKAAIRAVRILQFRLYKKKFKETLRPYDVKDVIEQYSAGHLDMLSRIKYLQTRIDMIFTPGPPSTPKHKKSQKGSAFTFPSQQSPRNEPYVARPSTSEIEDQSMMGKFVKVERQVQDMGKKLDFLVDMHMQHMERLQVQVTEYYPTKGTSSPAEAEKKEDNRYSDLKTIICNYSETGPPEPPYSFHQVTIDKVSPYGFFAHDPVNLPRGGPSSGKVQATPPSSATTYVERPTVLPILTLLDSRVSCHSQADLQGPYSDRISPRQRRSITRDSDTPLSLMSVNHEELERSPSGFSISQDRDDYVFGPNGGSSWMREKRYLAEGETDTDTDPFTPSGSMPLSSTGDGISDSVWTPSNKPI
  
Inhibitor
Name:
BDBM50339279
Synonyms:
5-(Chloromethyl)-3-(naphthalen-1-yl)-2-(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-7(4H)-one | CHEMBL1689652
Type:
Small organic molecule
Emp. Form.:
C18H11ClF3N3O
Mol. Mass.:
377.748
SMILES:
FC(F)(F)c1[nH]n2c(nc(CCl)cc2=O)c1-c1cccc2ccccc12 |(-2.75,-35.11,;-3.52,-36.45,;-5.06,-36.46,;-4.3,-35.1,;-2.74,-37.78,;-3.35,-39.19,;-2.2,-40.22,;-.88,-39.44,;.46,-40.22,;.46,-41.77,;1.8,-42.54,;3.14,-41.77,;-.88,-42.53,;-2.21,-41.77,;-3.55,-42.54,;-1.2,-37.94,;-.37,-36.63,;-1.09,-35.27,;-.27,-33.97,;1.29,-34.03,;2,-35.4,;3.53,-35.47,;4.24,-36.83,;3.42,-38.13,;1.88,-38.06,;1.17,-36.7,)|
Structure:
Search PDB for entries with ligand similarity: