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Target
Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM29977
Substrate
BDBM24064
Meas. Tech.
hERG Radioligand Binding Assay
pH
7.4±n/a
Temperature
295.15±n/a K
IC50
9000±n/a nM
Citation
 Kobayashi, K; Uchiyama, M; Ito, H; Takahashi, H; Yoshizumi, T; Sakoh, H; Nagatomi, Y; Asai, M; Miyazoe, H; Tsujita, T; Hirayama, M; Ozaki, S; Tani, T; Ishii, Y; Ohta, H; Okamoto, O Discovery of novel arylpyrazole series as potent and selective opioid receptor-like 1 (ORL1) antagonists. Bioorg Med Chem Lett 19:3627-31 (2009) [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:
BDBM29977
Synonyms:
arylpyrazole, 22
Type:
Small organic molecule
Emp. Form.:
C21H24ClN5
Mol. Mass.:
381.902
SMILES:
Cc1c(CNC2CCCC2)nn(c1-c1cncc(C)c1)-c1ncccc1Cl
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
BDBM24064
Synonyms:
L-706,000 | L-706000 | MK-499 | N-[(4R)-1'-[(2R)-6-cyano-1,2,3,4-tetrahydronaphthalen-2-yl]-3,4-dihydrospiro[1-benzopyran-2,4'-piperidine]-4-ol]methanesulfonamide | [35S]-MK499
Type:
radiolabeled ligand
Emp. Form.:
C25H29N3O4S
Mol. Mass.:
467.58
SMILES:
CS(=O)(=O)Nc1ccc2OC3(CCN(CC3)[C@@H]3CCc4cc(ccc4C3)C#N)C[C@@H](O)c2c1 |r|
Structure:
Search PDB for entries with ligand similarity: