Target
Potassium voltage-gated channel subfamily KQT member 2/3
Ligand
BDBM50526877
Substrate
n/a
Meas. Tech.
ChEMBL_1901601 (CHEMBL4403823)
EC50
210±n/a nM
Citation
 Ostacolo, CMiceli, FDi Sarno, VNappi, PIraci, NSoldovieri, MVCiaglia, TAmbrosino, PVestuto, VLauritano, AMusella, SPepe, GBasilicata, MGManfra, MPerinelli, DRNovellino, EBertamino, AGomez-Monterrey, IMCampiglia, PTaglialatela, M Synthesis and Pharmacological Characterization of Conformationally Restricted Retigabine Analogues as Novel Neuronal Kv7 Channel Activators. J Med Chem 63:163-185 (2020) [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:
BDBM50526877
Synonyms:
CHEMBL4545892
Type:
Small organic molecule
Emp. Form.:
C23H25F3N2O
Mol. Mass.:
402.4526
SMILES:
CCCCCCC(=O)Nc1ccc2n(Cc3ccc(cc3)C(F)(F)F)ccc2c1
Structure:
Search PDB for entries with ligand similarity: