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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50243844
Substrate
n/a
Meas. Tech.
ChEMBL_538846 (CHEMBL1033089)
IC50
88±n/a nM
Citation
 Yang, ZQ; Barrow, JC; Shipe, WD; Schlegel, KA; Shu, Y; Yang, FV; Lindsley, CW; Rittle, KE; Bock, MG; Hartman, GD; Uebele, VN; Nuss, CE; Fox, SV; Kraus, RL; Doran, SM; Connolly, TM; Tang, C; Ballard, JE; Kuo, Y; Adarayan, ED; Prueksaritanont, T; Zrada, MM; Marino, MJ; Graufelds, VK; DiLella, AG; Reynolds, IJ; Vargas, HM; Bunting, PB; Woltmann, RF; Magee, MM; Koblan, KS; Renger, JJ Discovery of 1,4-substituted piperidines as potent and selective inhibitors of T-type calcium channels. J Med Chem 51:6471-7 (2008) [PubMed]  Article 
Target
Name:
Potassium voltage-gated channel subfamily H member 2
Synonyms:
1,3-beta-glucan synthase component GLS2 | Cytochrome P450 3A4 | ERG | ERG1 | Eag-related protein 1 | Ether a-go-go related gene potassium channel (hERG) | Ether-a-go-go-related gene (HERG) | Ether-a-go-go-related gene potassium channel (hERG) | Ether-a-go-go-related gene potassium channel 1 | Ether-a-go-go-related gene potassium channel 1 (HERG) | Ether-a-go-go-related gene potassium channel 1 (hERG1) | Ether-a-go-go-related protein (hERG) | Ether-a-go-go-related protein 1 | Ether-a-go-go-related protein 1 (HERG) | H-ERG | HERG | KCNH2 | KCNH2_HUMAN | Potassium voltage-gated channel subfamily H member 2 (hERG) | Transcriptional regulator ERG | Voltage-gated potassium channel subunit Kv11.1 | eag homolog | hERG Potassium Channel 1 | putative potassium channel subunit
Type:
Multi-pass membrane protein
Mol. Mass.:
126672.65
Organism:
Homo sapiens (Human)
Description:
Q12809
Residue:
1159
Sequence:
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVMQRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDGAVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSVRSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSPPRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPPRHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIAPKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIYTAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANEEVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLDRYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSSGLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVSAIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGFPECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALYFISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLEVLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTEQPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSSPRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTPSLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSAVTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPGQLGALTSQPLHRHGSDPGS
  
Inhibitor
Name:
BDBM50243844
Synonyms:
1-(3-Chloro-phenyl)-3-[1-(3,3-dimethyl-butyl)-4-phenyl-piperidin-4-ylmethyl]-urea | 1-(3-chlorophenyl)-3-((1-(3,3-dimethylbutyl)-4-phenylpiperidin-4-yl)methyl)urea | CHEMBL488294
Type:
Small organic molecule
Emp. Form.:
C25H34ClN3O
Mol. Mass.:
428.01
SMILES:
CC(C)(C)CCN1CCC(CNC(=O)Nc2cccc(Cl)c2)(CC1)c1ccccc1
Structure:
Search PDB for entries with ligand similarity: