Reaction Details
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Potassium voltage-gated channel subfamily H member 2
Ligand
BDBM50173461
Substrate
n/a
Meas. Tech.
ChEMBL_321319 (CHEMBL882589)
IC50
2250±n/a nM
Citation
Kym, PR; Iyengar, R; Souers, AJ; Lynch, JK; Judd, AS; Gao, J; Freeman, J; Mulhern, M; Zhao, G; Vasudevan, A; Wodka, D; Blackburn, C; Brown, J; Che, JL; Cullis, C; Lai, SJ; LaMarche, MJ; Marsilje, T; Roses, J; Sells, T; Geddes, B; Govek, E; Patane, M; Fry, D; Dayton, BD; Brodjian, S; Falls, D; Brune, M; Bush, E; Shapiro, R; Knourek-Segel, V; Fey, T; McDowell, C; Reinhart, GA; Preusser, LC; Marsh, K; Hernandez, L; Sham, HL; Collins, CA Discovery and characterization of aminopiperidinecoumarin melanin concentrating hormone receptor 1 antagonists. J Med Chem 48:5888-91 (2005) [PubMed] Article More Info.:
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:
BDBM50173461
Synonyms:
4-(1-Benzo[1,3]dioxol-5-ylmethyl-piperidin-4-ylamino)-6-chloro-chromen-2-one | CHEMBL194564
Type:
Small organic molecule
Emp. Form.:
C22H21ClN2O4
Mol. Mass.:
412.866
SMILES:
Clc1ccc2oc(=O)cc(NC3CCN(Cc4ccc5OCOc5c4)CC3)c2c1
Structure:
